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LemonBalm.nxml | Lemon Balm | 2024-02-10 | Lemon balm is an oily extract of the leaves of Melissa officinalis, a flowering perennial shrub native to the east Mediterranean and west Asian regions that is now cultivated widely. Lemon balm was used in traditional medicine for nervousness, anxiety, insomnia, and menstrual irregularities. Lemon balm extracts are gen... | Lemon balm is an extract made from the fresh or dried leaves of Melissa officialis, a moderate sized, flowering shrub native to the eastern Mediterranean area and western Asia but now cultivated in many areas of the world. Lemon balm extracts contain aromatic, lemony smelling oils, chief of which are citronellal and ge... | Lemon balm extract has not been linked to serum enzyme elevations during therapy, although there have been few prospective studies in humans that have reported on laboratory test results during treatment. In small trials, lemon balm extracts have appeared to be well tolerated with only a few minor adverse non-specific ... | null | null | Lemon Balm – Generic | Herbal and Dietary Supplements | null |
Trazodone.nxml | Trazodone | 2020-02-26 | Trazodone is a serotoninergic modulating antidepressant that is used in therapy of depression, aggressive behavior and panic disorder. Trazodone therapy can be associated with transient, usually asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute l... | Trazodone (traz' oh done) is a triazolopyridine derivative whose mechanism of action is believed to be inhibition of serotonin reuptake and modulation of serotonin receptor activity, which results in increased levels and activity of serotonin. Trazodone was approved for use in major depressive disorder in the United St... | Liver test abnormalities occur in a proportion of patients on trazodone, but elevations are usually modest and usually do not require dose modification or discontinuation. At least a dozen instances of acute, clinically apparent episodes of liver injury with marked liver enzyme elevations with or without jaundice have ... | The mechanism by which trazodone causes liver injury is not known. Trazodone is extensively metabolized by the liver, mainly via the cytochrome P450 system (CYP3A4), and hepatotoxicity may be mediated by toxic intermediates of its metabolism. Trazodone is susceptible to multiple drug-drug interactions. | The serum aminotransferase elevations that occur on trazodone therapy are usually self-limited and do not require dose modification or discontinuation of therapy. Rare instances of acute liver failure and chronic hepatitis have been attributed to trazodone therapy. Persons with intolerance to trazodone may have similar... | Trazodone – Generic, Desyrel® | Antidepressant Agents | null |
Atovaquone.nxml | Atovaquone | 2017-02-02 | Atovaquone is a naphthoquinone used for the prevention and treatment of Pneumocystis jevorici (formerly carinii) pneumonia and, in combination with proguanil, prevention and treatment of P. falciparum malaria. Atovaquone therapy is associated with low rates of serum enzyme elevations and has been linked to only rare ca... | Atovaquone (a toe' va kwone) is a synthetic naphthoquinone that acts by interfering with mitochondrial electron transport in susceptible organisms. Atovaquone is effective against chloroquine resistant P. falciparum, but is associated with a high rate of resistance, for which reason it is usually given in combination w... | Atovaquone has been linked to serum aminotransferase elevations in a small proportion of patients (1% to 6%). There have also been rare reports of clinically apparent, acute liver injury due to atovaquone. In one published case report (Case 1), the onset of injury was 25 days after starting (and a few days after stoppi... | The mechanism by which atovaquone might cause liver injury is unknown. Atovaquone is minimally metabolized by the liver, while proguanil is metabolized by the cytochrome P450 system (CYP 2C19). Either a toxic or an immunogenic metabolite may be responsible for the injury. | The severity of hepatic injury due to atovaquone varies from mild serum enzyme elevations that are asymptomatic and transient, to clinically apparent liver injury with jaundice. Acute liver failure, chronic hepatitis and vanishing bile duct syndrome have not been reported after atovaquone therapy. There does not seem t... | Atovaquone – Mepron® | Antimalarial Agents | null |
Posaconazole.nxml | Posaconazole | 2017-05-17 | Posaconazole is a potent triazole antifungal agent used in the prevention of invasive fungal infections due to aspergillosis and candida in high risk patients. Posaconazole therapy is associated with transient, asymptomatic serum aminotransferase elevations and is a suspected but rare cause of clinically apparent acute... | Posaconazole (poe" sa kon' a zole) is a synthetic triazole that is believed to act through inhibition of the fungal 14α-ergosterol demethylase, which is responsible for converting lanosterol to ergosterol and which blocks cell membrane synthesis. Posaconazole is active against a broad spectrum of fungal agents includin... | Transient elevations in serum aminotransferase levels occur in 2% to 12% of patients on posaconazole. These elevations are usually mild, asymptomatic and self-limited and rarely require discontinuation of the medication. Clinically apparent hepatotoxicity is very rare. Instances of jaundice and hepatitis during posacon... | The cause of the liver injury from posaconazole is unknown; however, it may have some correlation to the ability of voriconazole to alter human sterol synthesis. Because posaconazole inhibits CYP 3A4 activity, it can cause significant drug-drug interactions and including elevations in plasma levels of other medications... | The severity of the liver injury from posaconazole ranges from mild and transient enzyme elevations to hepatitis with jaundice. Fatal instances have not been described, but the drug has not been extensively used or studied. A single case report describes a patient with hepatotoxicity from voriconazole who was able to t... | Posaconazole – Noxafil® | Antifungal Agents | null |
Phenotypes_fail.nxml | Acute Liver Failure | 2019-12-11 | null | null | null | null | null | null | null | null |
ArnicaMontana.nxml | Arnica Montana | 2023-03-03 | Arnica montana, also known as wolf’s bane, is an herbal medication used topically for pain and inflammation but is of unproven efficacy. It is an extract of the flowering plant Arnica montana, a member of the daisy family. Arnica montana is used topically and as such has not been linked to serum aminotransferase elevat... | Arnica montana (also called wolf’s bane) is a tall perineal plant with large yellow flowers that belongs to the daisy family Asteraceae and is widespread across Europe. Arnica montana is used in small oral doses in homeopathic medicine and in low doses as treatment for pain, inflammation and fever, most often post-surg... | In multiple small, rather short term clinical trials of different preparations of Arnica montana extracts, adverse side effects were described as uncommon and local with no mention of either hepatotoxicity or ALT elevations. Despite widespread use, there have been no published reports of serum enzyme elevations or clin... | The mechanism by which Arnica montana might cause liver injury is unknown. | Hepatotoxicity from topically applied extracts of Arnica montana has not been reported.\n\nDrug Class: Herbal and Dietary Supplements\n\nOther names: Arnica, Wolf’s bane, Leopard’s bane, Mountain tobacco. | Arnica montana – Generic | Herbal and Dietary Supplements | null |
Demeclocycline.nxml | Demeclocycline | 2019-01-23 | Demeclocycline is a semisynthetic tetracycline derived from Streptococcus aureofaciens that is used as an antibiotic, but perhaps more frequently as an inhibitor of arginine vasopressin in the therapy of hyponatremia and the syndrome of inappropriate secretion of antidiuretic hormone (SIADH). While demeclocycline has n... | Demeclocycline (dem" e kloe sye' kleen) is a tetracycline antibiotic that is used for therapy of mild-to-moderate infections due to susceptible organisms. It is also used off-label as therapy of hyponatremia and SIADH. Its mechanism of action in SIADH is not well understood, but it appears to block the binding of argin... | No reports of liver injury due to demeclocycline have been published. However, demeclocycline is a tetracycline derivative and is likely to cause liver injury similar to other oral tetracyclines. Both hepatitis and liver failure are mentioned in the product label for demeclocycline, but details of the liver injury are ... | null | null | Demeclocycline – Generic, Declomycin® | Antiinfective Agents | null |
Telithromycin.nxml | Telithromycin | 2017-08-10 | Telithromycin is a ketolide, a novel form of macrolide antibiotic that is recommended for treatment of community acquired pneumonia. Telithromycin was approved for use in the United States in 2004 and subsequently linked to several cases of severe drug induced liver injury. | Telithromycin (tel ith" roe mye' sin) is a ketolide antibiotic, a novel form of macrolide antibiotic that is used to treated community acquired pneumonia. Telithromycin differs from erythromycin by several substitutions that render it less susceptible to erythromycin-resistant strains of bacteria. Telithromycin is acti... | As with other macrolide antibiotics, telithromycin has been associated with a low rate (1% to 2%) of transient serum enzyme elevations during therapy. These elevations, however, are usually transient and resolve even with drug continuation and a similar rate of serum enzyme elevations can occur with comparator agents. ... | The cause of hepatotoxicity from telithromycin is unknown, but the short latency period and abrupt onset of injury suggests hypersensitivity as the cause. Only a proportion of cases have been associated with eosinophilia, and rash, fever, adenopathy and facial edema are rarely described. | Severe cases of liver injury appearing within days of starting telithromycin have been described some of which have been associated with acute and rapid onset of ascites and liver failure requiring liver transplantation. Milder cases of injury and cases without jaundice have generally resolved rapidly over 4 to 6 weeks... | Telithromycin — Ketek® | Antiinfective Agents | null |
Zavegepant.nxml | Zavegepant | 2025-01-12 | Zavegepant is a small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Zavegepant is provided as a nasal spray and is approved for treatment of acute migraine attacks. In clinical trials, zavegep... | Zavegepant (za ve’ je pant) is a small molecule inhibitor of the receptor for the calcitonin gene-related peptide (CGRP), which is believed to play a role in the pathogenesis of migraine headaches. CGRP is a potent vasodilator and pain-signaling neurotransmitter that is found throughout the central and peripheral nervo... | In preregistration, controlled trials of zavegepant in several thousand patients, mild-to-moderate serum aminotransferase elevations arose in a small percentage of patients (1% to 2%) and overall rates were not different from those in placebo recipients. In the controlled trials and subsequently with general use, there... | Possible mechanisms of liver injury due to zavegepant are not known. It is metabolized in the liver largely by CYP 3A4 and is susceptible to drug-drug interactions with agents that induce or inhibit this microsomal enzyme. Lower doses should be used in patients receiving CYP 3A4 inhibitors. | Drug Class: Migraine Headache Agents\n\nOther Small Molecule Inhibitors of CGRP Receptors: Atogepant, Rimegepant, Ubrogepant | Zavegepant – Zavzpret® | Migraine Headache Agents | null |
Pimozide.nxml | Pimozide | 2020-07-01 | Pimozide is a conventional antipsychotic used largely in the therapy of Tourette syndrome. Pimozide therapy has not been associated with serum aminotransferase elevations nor with cases of clinically apparent acute liver injury. | Pimozide (pim' oh zide) is a diphenylbutylpiperidine derivative that differs structurally from the phenothiazines and appears to act by blocking dopamine type 2 (D2) receptors. Pimozide has other central and peripheral effects including anticholinergeric and alpha adrenergic blockade. Pimozide is indicated for the ther... | Liver test abnormalities have not been reported to occur in of patients on pimozide, but the degree and duration of monitoring done in initial studies were not clear. Instances of clinically apparent acute liver injury have not been reported due to pimozide, and thus must be rare if they occur at all.\n\nLikelihood sco... | Pimozide is extensively metabolized by the liver partially via the cytochrome P450 system (predominantly CYP 2D6) and levels can be seriously elevated in patients who concurrently receive CYP 2D6 inhibitors, particularly in persons who are poor metabolizers of CYP 2D6 substrates. The lack of hepatotoxicity may relate i... | null | Pimozide – Generic, Orap® | Antipsychotic Agents | null |
Tildrakizumab.nxml | Tildrakizumab | 2018-10-20 | Tildrakizumab is humanized monoclonal antibody to interleukin-23 that is used to treat moderate-to-severe plaque psoriasis. Tildrakizumab is associated with a low rate of transient and asymptomatic serum enzyme elevations during therapy, but has not been linked to cases of idiosyncratic, clinically apparent liver injur... | Tildrakizumab (til" dra kiz' ue mab) is a humanized monoclonal IgG1 antibody to interleukin (IL)-23, a cytokine that is an important mediator of autoimmune reactions. IL-23 is found in the skin lesions of psoriasis and in the affected gastrointestinal mucosa of patients with inflammatory bowel disease. Among the monocl... | Rates of serum aminotransferase elevations during tildrakizumab therapy have not been well defined, but rates of laboratory result abnormalities are said to be similar with tildrakizumab compared to placebo treatment. Neither during premarketing evaluation nor subsequently have there been case reports of clinically app... | null | Tildrakizumab has been linked to minor elevations in serum enzymes during therapy but not to clinically apparent liver injury or with reactivation of hepatitis B. The product label for tildrakizumab does not recommend routine screening for hepatitis B before initiation of therapy. However, guidelines prepared by some a... | Tildrakizumab – Ilumya® | Dermatologic Agents, Psoriasis Agents | null |
Clonazepam.nxml | Clonazepam | 2017-01-25 | Clonazepam is a benzodiazepine used predominantly as an anticonvulsant as adjunctive therapy in management of epilepsy. Therapy with clonazepam is not associated with serum aminotransferase elevations, and clinically apparent liver injury from clonazepam, if it occurs at all, must be exceedingly rare. | Clonazepam (kloe naz' e pam) is a benzodiazepine with particularly potent activity against spread of seizure activity in several animal models. The antiseizure activity of the benzodiazepines is mediated by their ability to enhance gamma-aminobutyric acid (GABA) mediated inhibition of synaptic transmission through bind... | Clonazepam, as with other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from clonazepam is extremely rare. However, at least one convincing case report of acute liver injury from clonazepam with recurrence on reexposure has been reported. Rare instances of drug in... | The liver injury from benzodiazepines is probably due to a rarely produced intermediate metabolite. Their relative safety may relate to the low daily doses used (typically 5 to 10 mg). | The case reports of hepatic injury due to clonazepam were followed by complete recovery, without evidence of residual or chronic injury. No cases of acute liver failure or chronic liver injury due to clonazepam have been described. There is no information about cross reactivity with other benzodiazepines (clobazam, clo... | Clonazepam – Klonopin® | Anticonvulsants | null |
Aripiprazole.nxml | Aripiprazole | 2023-06-05 | Aripiprazole is an atypical antipsychotic used in the treatment of schizophrenia and bipolar illness. Aripiprazole therapy has not been associated consistently with serum aminotransferase elevations and has yet to be linked to cases of clinically apparent acute liver injury. | Aripiprazole (ar" i pip' ra zole) is a partial agonist for dopamine type 2 (D2) and serotonin (5-HT1A) receptors and has antagonist activity against serotonin 5HT2A receptors. Aripiprazole is indicated for the therapy of schizophrenia and as either monotherapy or adjunctive therapy for manic and mixed episodes in bipol... | Liver test abnormalities have not been reported to occur in patients on long term therapy with aripiprazole, but most studies have not provided information on serum enzyme results. Despite its widescale use, aripiprazole has been implicated in only rare and isolated cases of clinically apparent liver injury in the lite... | Aripiprazole is extensively metabolized by the liver via the P450 system, largely by CYP 3A4 and 2D6 and is susceptible to drug-drug interactions with agents that induce or inhibit these microsomal enzymes. Weight gain is less prominent with aripiprazole than other atypical antipsychotic medications and the influence o... | null | Aripiprazole – Abilify® | Antipsychotic Agents | null |
Narajo.nxml | Adverse Drug Reaction Probability Scale (Naranjo) in Drug Induced Liver Injury | 2019-05-04 | null | null | null | null | null | null | null | null |
Vismodegib.nxml | Vismodegib | 2025-01-05 | Vismodegib is an orally available, small molecule inhibitor of the Hedgehog pathway that is used to treat unresectable or metastatic basal cell carcinoma. Vismodegib therapy is associated with a low rate or transient elevations in serum aminotransferase during therapy and has been linked to rare cases of clinically app... | Vismodegib (vis” moe deg’ ib) is an orally available, small molecule inhibitor of a key step in the hedgehog signaling pathway (activation of smoothened: SMO). Hedgehog is an important regulator of embryonic development, cell growth and differentiation. Mutations in this pathway have been identified in several malignan... | Most clinical trials of vismodegib included few patients, and rates of liver tests abnormalities were usually not reported. The product label for vismodegib includes no mention serum enzyme elevations or need for monitoring of routine liver tests. In a subsequent review of all published studies of vismodegib, liver enz... | The cause of liver injury from vismodegib is unknown, but likely due to hypersensitivity. Vismodegib has a prolonged half-life (~19 days) and is metabolized at least in part in the liver via multiple cytochrome P450 enzymes, including CYP 3A4, 2C8, 2C9 and 2C19. While it theoretically should have several drug-drug inte... | In using kinase and small molecule inhibitors for treatment of cancer, monitoring of routine liver tests before starting and at intervals during therapy is warranted. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) or any elevations accompanied by jaundice or symptoms should lea... | Vismodegib – Erivedge® | Antineoplastic Agents | null |
Topiramate.nxml | Topiramate | 2020-07-30 | Topiramate is a unique antiseizure medication that is widely used in treatment of partial and generalized seizures as well as for bipolar disorder, migraines and weight loss. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications. | Topiramate (toe pyre' a mate) is a sulfamate-substituted monosaccharide and belongs to an anticonvulsant class of its own. Topiramate is believed to act by reducing sodium channel currents and enhancing gamma aminobutyric acid A (GABA-A) receptor activity. Topiramate was approved for use in epilepsy in the United State... | Prospective studies suggest that less than 1% of subjects develop elevations in serum aminotransferase levels during long term topiramate therapy. Clinically apparent hepatotoxicity from topiramate is quite rare and usually arises in patients receiving multiple other anticonvulsants. Topiramate is metabolized by CYP 3A... | The mechanism of topiramate hepatotoxicity is thought to be due to its effects in inducing CYP 3A4 or inhibiting CYP 2C19 and possibly through the effects of a toxic metabolic intermediate. Cases with lactic acidosis and hyperammonemia may be caused by mitochondrial injury or dysfunction. | Topiramate hepatotoxicity is usually attributed to its effects on the metabolism of other anticonvulsants, and as such is rapidly reversible within a few days of either drug being stopped. Vanishing bile duct injury and chronic injury from topiramate therapy has not been reported.\n\nDrug Class: Anticonvulsants\n\nSee ... | Topiramate – Generic, Topamax® | Anticonvulsants | null |
Echinacea.nxml | Echinacea | 2019-04-10 | Echinacea is a popular herbal medication and extract derived from a flowering plant (Echinacea purpurea) that is native to the United States, East of the Rocky Mountains. Echinacea has been used mostly for treating and preventing the common cold and other upper respiratory illnesses. While echinacea is generally well t... | Echinacea (ek" i nay' sha) is a widely used herb derived from the perennial plant, Echinacea purpurea, also known as American coneflower which is native to North America. The above ground parts and roots of the echinacea plant are used either fresh or dried to make teas, juice, extracts, capsules or tablets. The major ... | In multiple controlled trials, echinacea by itself has not been linked to liver injury, either in the form of transient serum enzyme elevations or clinically apparent acute liver injury. Nevertheless, there have been isolated case reports of clinically apparent liver injury with jaundice, and summary reports from natio... | The mechanism by which some preparations of echinacea might cause liver injury is not known but may be due to a contaminant or mislabeling of the product. However, because echinacea has been linked to rare instances of severe allergic reactions, the isolated cases of hepatitis may represent hepatic manifestations of hy... | Patients on echinacea who develop unexplained symptoms such as fatigue, nausea, abdominal pain or dark urine should have routine liver tests drawn and discontinue the herb if there are any abnormalities.\n\nDrug Class: Herbal and Dietary Supplements | Echinacea – Generic | Herbal and Dietary Supplements | null |
Senna.nxml | Senna | 2020-04-01 | Senna (Cassia species) is a popular herbal laxative that is available without prescription. Senna is generally safe and well tolerated, but can cause adverse events including clinically apparent liver injury when used in high doses for longer than recommended periods. | Senna (sen’ a) belongs to a large genus of flowering plants found throughout the tropics, commonly used species being Cassia acutifolia (Alexandrian senna) and C. angustifolio (Indian or Tinnevelly senna). Extracts of the leaves, flowers and fruit of senna have been used for centuries in folk medicine as a laxative and... | Use of senna in the recommended doses for a limited period of time has been associated with few side effects, most of which are mild and transient and related to its laxative action. With longer term and higher dose use of senna, however, adverse events have been described including several cases of clinically apparent... | The liver injury due to senna has been attributed to the anthraquinone derivatives present in the herbal extract, and most cases have been associated with taking excessive doses suggesting a direct hepatotoxic rather than idiosyncratic etiology. Other anthraquinones used to treat constipation have been implicated in ca... | Liver injury from long term senna use is rare, and most cases have been self-limited and rapidly reversible upon stopping the laxative. However, cases with a severe course with signs of acute liver failure have been described. There is no evidence of cross sensitivity to hepatic damage with other laxatives. Restarting ... | Senna – Generic | Herbal and Dietary Supplements | null |
Tigecycline.nxml | Tigecycline | 2025-04-15 | Tigecycline is a parenteral tetracycline antibiotic used for treatment of serious infections due to susceptible organisms. Tigecycline therapy is sometimes accompanied by minor aminotransferase elevations, but has not been definitely associated with clinically apparent liver injury with jaundice. | Tigecycline (tye" ge sye' kleen) is a glycycline, a tetracycline antibiotic used for treatment of serious infections due to susceptible organisms. Like other tetracyclines, tigecycline is a broad spectrum bacteriostatic agent that acts by binding to bacterial ribosomes inhibiting protein synthesis. Tigecycline has acti... | Tigecycline is reported to cause mild, transient elevations in serum aminotransferase levels in 2% to 5% of recipients, rates similar to those in patients treated with comparator antibiotics. Cases of clinically apparent liver injury with jaundice are rare. Product labels for tigecycline mention isolated cases of signi... | The cause of the serum enzyme elevations during intravenous therapy with tigecycline is unknown. High doses of intravenous tetracycline were associated with a severe direct hepatic injury. This syndrome has not been reported with limited courses of intravenous tigecycline or the other modified tetracyclines such as oma... | Patients with cirrhosis should be monitored during tigecycline therapy for evidence of worsening hepatic function. Patients on intravenous tigecycline who develop serum aminotransferase elevations that rise above 5 times the upper limit of normal or are accompanied by jaundice or symptoms should have tigecycline stoppe... | Tigecycline – Tygacil® | Antiinfective Agents | null |
Omadacycline.nxml | Omadacycline | 2020-01-09 | Omadacycline is an oral, tetracycline-like antibiotic used to treat moderate-to-severe infections including community-acquired pneumonia and acute bacterial skin and skin structure infections caused by susceptible organisms. Oral omadacycline use has been associated with serum enzyme elevations during therapy but has n... | Omadacycline (oh mad" a sye' kleen) is an oral, broad spectrum tetracycline like antibiotic with potent activity against both aerobic and anaerobic gram-positive and gram-negative organisms. Omadacyline is a semisynthetic derivative of minocycline that is classified as an aminomethylcycline. It has a broader spectrum o... | In clinical trials of omadacycline usually conducted in critically ill patients with major infections, serum aminotransferase elevations arose in 4% of patients and to above 5 times ULN in 1.5%. Nevertheless, the abnormalities were generally transient and asymptomatic and were no more frequent than with comparator anti... | The mechanism by which omadacycline might cause liver injury is unknown. Omadacycline is not metabolized in the liver to an appreciable extent which may explain its relative lack of hepatotoxicity. It does not appear to interact with cytochrome P450 enzymes and has not been reported to cause significant drug-drug inter... | Patients on intravenous omadacycline who develop serum aminotransferase elevations that rise above 5 times the upper limit of normal or are accompanied by jaundice or symptoms should have omadacycline discontinued. Whether there is cross sensitivity to hepatic injury among the various tetracyclines is not known but swi... | Omadacycline – Nuzyra® | Antiinfective Agents | null |
Amikacin.nxml | Amikacin | 2019-04-12 | Amikacin is a parenterally administered, broad spectrum aminoglycoside antibiotic typically used for severe gram negative infections. Despite widespread use, amikacin has not been associated with instances of acute liver injury. | Amikacin (am" i kay' sin) is a semisynthetic aminoglycoside with a particularly broad antimicrobial activity which is used for severe bacterial infections caused by sensitive agents including those resistant to gentamicin or tobramycin. Like other aminoglycosides, amikacin is thought to act by binding to bacterial ribo... | Intravenous and intramuscular therapy with amikacin has not been linked to serum alkaline phosphatase or aminotransferase elevations, and no convincing cases of symptomatic or icteric hepatotoxicity due to amikacin have been published. Other aminoglycosides have been linked to very rare cases of cholestatic hepatitis, ... | The cause of the rare occurrence of cholestatic jaundice after aminoglycoside therapy is unknown, but suspected to be a part of a generalized hypersensitivity reaction. Uptake of aminoglycosides into hepatocytes is limited and they are rapidly excreted in the urine; high concentrations are found in mainly in renal tubu... | The outcome of hepatic injury due to aminoglycosides is usually benign. Acute liver failure and chronic bile duct vanishing syndrome have been not been described after their use. Patients with any form of aminoglycoside hepatotoxicity should probably avoid future systemic aminoglycoside use.\n\nReferences to the safety... | Amikacin – Generic | Aminoglycosides | null |
Primidone.nxml | Primidone | 2020-08-12 | Primidone is an aromatic anticonvulsant used to treat complex, partial and generalized seizures. Therapy with primidone can be associated with increases in gamma glutamyltranspeptidase levels, but is not associated with serum aminotransferase elevations, and despite its similarity in structure to phenobarbital and phen... | Primidone (prim' i done) is a pyrimidinedione anticonvulsant and is partially metabolized to phenobarbital. Primidone is effective in suppressing seizure activity, but its mechanism of action is not well defined. It is believed to work centrally via interactions with voltage-gated sodium channels inhibiting repetitive ... | In clinical trials in epilepsy, therapy with primidone was not associated with an increased frequency of serum aminotransferase elevations or liver toxicity. Primidone therapy can lead to increases in gamma glutamyltranspeptidase (GGT) levels. Elevations in alkaline phosphatase levels were largely due to bone isoforms ... | Primidone, like phenobarbital, is extensively metabolized by the liver and can induce CYP 450 enzyme activities. Primidone can interfere with porphyrin metabolism and like phenobarbital and phenytoin can cause worsening of porphyria.\n\nDrug Class: Anticonvulsants | null | Primidone – Generic, Mysoline® | Anticonvulsants | null |
BlackCumin.nxml | Black Cumin Seed | 2023-04-27 | Black cumin also known as black seed and Nigella sativa is a flowering plant native to Eastern Europe and the Middle East that produces black seeds which are used to produce spice and flavoring of food and have been used in traditional medicine as therapy for a wide variety of conditions. Black cumin is well tolerated,... | Black Cumin (Nigella sativa) is a flowering annual plant native to Eastern Europe and the Middle East that is now cultivated in many areas of world and produces a black seed, extracts of which are used as a spice and for flavoring foods. In addition to its culinary uses, black cumin seeds and their extracts have also b... | In multiple, largely short term clinical studies of different preparations and concentrations of black cumin seed powdered extracts and oils, adverse side effects were usually described as uncommon and mild with either no change or slight improvement in serum aminotransferase and alkaline phosphatase levels. Furthermor... | The mechanism by which black cumin seed extracts might cause liver injury is unknown. | Hepatotoxicity from extracts of black cumin seeds has not been reported.\n\nDrug Class: Herbal and Dietary Supplements\n\nOther names: Black seed, Black caraway, Small fennel, Fennel flower, Roman Coriander, Nigella, Nigella sativa. | Black Cumin – Generic | Herbal and Dietary Supplements | null |
Atomoxetine.nxml | Atomoxetine | 2021-08-25 | Atomoxetine is a selective norepinephrine reuptake inhibitor used primarily for therapy of attention deficit hyperactivity disorder. Atomoxetine has been linked to a low rate of serum aminotransferase elevations and to rare cases of acute, clinically apparent liver injury. | Atomoxetine (a" toe mox' e teen) is a selective norepinephrine reuptake inhibitor that blocks the presynaptic norepinephrine transporter leading to an increase in levels of this potent neurotransmitter, predominantly in the central nervous system. Therapy with atomoxetine has been shown to lead to improvements in level... | Atomoxetine has been linked to serum aminotransferase elevations in a small proportion of patients (~0.5%). More importantly, there have been several reports of clinically apparent acute liver injury due to atomoxetine. The onset of injury was within 3 to 12 weeks of starting the medication. The typical pattern of seru... | The mechanism by which atomoxetine might cause liver injury is unknown. Atomoxetine is extensively metabolized in the liver by the cytochrome P450 system, predominantly CYP 2D6 and production of a toxic intermediate or immunogenic byproduct are reasonable explanations. Atomoxetine is susceptible to drug-drug interactio... | The liver injury due to atomoxetine varies from minor, transient and asymptomatic elevations in serum aminotransferase levels to clinically apparent hepatitis that can be prolonged and even fatal. Chronic liver injury and vanishing bile duct syndrome due to atomoxetine have not been described. Atomoxetine should be dis... | Atomoxetine – Generic, Strattera® | Central Nervous System Stimulants | null |
Lapatinib.nxml | Lapatinib | 2019-05-15 | Lapatinib is a small molecule inhibitor of several tyrosine kinase receptors involved in tumor cell growth that is used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent ac... | Lapatinib (la pa' ti nib) is a selective inhibitor of two tyrosine kinase receptors which are associated with tumor growth and angiogenesis. Lapatinib has special activity against the epidermal growth factor receptor (EGFR) and the human epidermal group factor receptor-2 (HER2). Tyrosine kinase receptors are often muta... | Elevations in serum aminotransferase levels are common during lapatinib therapy, occurring in up to half of patients. Values greater than 5 times the upper limit of normal (ULN) occur in 2% to 6% of patients but are usually transient and asymptomatic. Dose adjustments or temporary discontinuations are rarely required f... | The clinical and genetic findings associated with acute liver injury from the tyrosine kinase receptor inhibitors suggest that it is immune mediated. Lapatinib is metabolized in the liver largely through the CYP 3A4 and CYP 3A5 pathways, and liver injury may be due to production of a toxic or immunogenic intermediate. ... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. There does not appear to be cross reactivity of the hepatic injury among the tyrosine kinase receptor inhibitors and, in some situations, switching to another inhibitor may be a... | Lapatinib – Tykerb® | Antineoplastic Agents | null |
Salsalate.nxml | Salsalate | 2020-08-15 | Salsalate is a nonacetylated dimer of salicylic acid that is used in the treatment of chronic arthritis as an analgesic and antipyretic. Salsalate can cause moderate serum aminotransferase elevations when given in high doses in a manner similar to aspirin. | Salsalate (sal' sa late) is a dimer of salicylic acid that has antiinflammatory, analgesic and antipyretic actions similar to aspirin. The antiinflammatory and analgesic effects of salsalate are probably mediated by inhibition of prostaglandin synthesis. Although available for several decades, salsalate is not commonly... | Prospective studies show that a proportion of patients taking salsalate experience at least transient serum aminotransferase elevations particularly when it is given in higher doses. These abnormalities may resolve even with drug continuation or after dose reduction. Marked aminotransferase elevations (>10 fold elevate... | The mechanism of salsalate hepatotoxicity is likely a direct cytotoxic effect of high doses, similar to that of aspirin. | Salsalate hepatotoxicity has been marked by aminotransferase elevations without jaundice. Some patients have nonspecific symptoms or gastrointestinal upset. There have been no reported cases of acute hepatitis, acute liver failure or vanishing bile duct syndrome related to salsalate. Aminotransferase elevations during ... | Salsalate – Generic, Disalcid® (not available in US) | Antiinflammatory Agents | null |
Valerian.nxml | Valerian | 2020-04-05 | Valerian is a botanical extract derived from the roots of Valeriana officinalis, which is widely used in herbal medicine for insomnia, anxiety and digestive and urinary problems. Valerian has been linked to rare instances of clinically apparent liver injury. | Valerian (va ler' ee an) is the common name of the plant genus Valeriana, several species of which are used in herbal medicine, most typically Valeriana officinalis. Valerian has been used for centuries in Europe, usually for digestive and urinary problems. The name valerian derives from the Latin word valere, which me... | Valerian has been implicated in a small number of cases of clinically apparent liver injury, but usually in combination with other botanicals such as skullcap or black cohosh. In view of its wide scale use, valerian has to be considered a very rare cause of hepatic injury. In published cases, the latency to onset range... | The cause of the liver injury associated with valerian use is not known. Valerian extracts contain multiple ingredients, but none have been shown to be specifically hepatotoxic. | Hepatotoxicity from valerian is usually mild-to-moderate in severity and self-limiting. Only a small number of cases of liver injury attributed to valerian have been published, and there have been no instances of chronic hepatitis, cirrhosis or vanishing bile duct syndrome attributed to its use, and no convincing case ... | Valerian – Generic | Herbal and Dietary Supplements | null |
Dofetilide.nxml | Dofetilide | 2016-09-15 | Dofetilide is an oral class III antiarrhythmic agent used for treatment and prevention of atrial fibrillation and flutter. Dofetilide has had limited clinical use, but has not been linked to an increased rate of serum enzyme elevations during therapy or to instances of clinically apparent liver injury. | Dofetilide (doe fet' i lide) is a methanesulfonamide antiarrhythmic agent that is used to treat and prevent recurrence of atrial fibrillation and flutter. Dofetilide is considered a class III antiarrhythmic as it appears to act on a delayed rectifier of a specific potassium channel which results in prolongation of the ... | In clinical trials, serum aminotransferase and alkaline phosphatase elevations were no more common during dofetilide than placebo therapy. Some degree of ALT elevation was reported in 15% of dofetilide but a similar proportion of placebo recipients; these elevations were above 3 times the upper limit of normal in 1.5% ... | The mechanism by which dofetilide might cause liver injury is unknown. Dofetilide has a sulfonamide-like structure, but has not been linked to a high rate of hypersensitivity ("sulfa") reactions. The absence of hepatic side effects may be attributable to the low doses used (1 mg or less daily). Dofetilide is metabolize... | There is little evidence that dofetilide can cause liver injury, but it has a narrow therapeutic-toxic ratio in relation to cardiac arrhythmias, prolongation of the QTc interval and risk for torsades de pointes. There is little information about cross sensitivity to liver injury between other oral antiarrhythmics and d... | Dofetilide – Generic, Tikosyn® | Antiarrhythmic Agents | null |
Caffeine.nxml | Caffeine | 2020-06-18 | Caffeine is xanthine alkaloid that occurs naturally in seeds, leaves and fruit of several plants and trees that acts as a natural pesticide. Caffeine is a major component of coffee, tea and chocolate and in humans acts as a central nervous system (CNS) stimulant. Consumption of caffeine, even in high doses, has not bee... | Caffeine is a psychoactive xanthine alkaloid that is a major component of coffee, tea and some foods (chocolate) and is the most frequently used psychoactive agent. At least 90% of adults in the United States consume caffeine daily. Caffeine is also found in several herbs including yerba mate, green coffee beans, guara... | Some degree of caffeine intake is almost universal in modern society and an estimated 90% of adults in the United States consume caffeine daily, the average amount being 200 mg daily. Yet despite its widescale use, there is no evidence that regular consumption of caffeine or coffee has adverse effects on the liver. Ind... | Caffeine is metabolized by the microsomal P450 drug metabolizing enzymes, predominantly CYP 1A2. Patients with advanced cirrhosis may have delayed metabolism of caffeine and experience caffeine side effects (nervousness, insomnia, headache) at levels of intake that are well tolerated by patients without liver disease.\... | null | Caffeine – Generic, NoDoz® | CNS Stimulants, Xanthine Derivatives | null |
Lisinopril.nxml | Lisinopril | 2018-02-11 | Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor widely used in the therapy of hypertension and heart failure. Lisinopril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury that can be severe and even fatal. | Lisinopril (lye sin' oh pril) was the third ACE inhibitor to be approved for use in the United States and is still widely used for therapy of hypertension and heart failure. Like other ACE inhibitors, lisinopril inhibits the conversion of angiotensin I, a relatively inactive molecule, to angiotensin II which is the maj... | Lisinopril, like other ACE inhibitors, has been associated with a low rate of serum aminotransferase elevations (<2%) that, in controlled trials, was no higher than with placebo therapy. These elevations were transient and rarely required dose modification. Rare instances of clinically apparent acute liver injury have ... | The cause of the minor serum aminotransferase elevations associated with lisinopril therapy is not known. The cases of clinically apparent liver injury due to lisinopril are idiosyncratic and likely due to a reaction to a minor metabolite. Lisinopril has minimal hepatic metabolism. | Most instances of acute liver injury reported with lisinopril use have been self limited, but there have been reports of acute liver failure and death. Patients with severe lisinopril induced acute liver injury should avoid use of other ACE inhibitors, although cross sensitivity to liver injury among the members of thi... | Lisinopril – Generic, Prinivil®, Zestril® | Angiotensin-Converting Enzyme Inhibitors | null |
Adefovir.nxml | Adefovir | 2016-02-15 | Adefovir dipivoxil is an acyclic nucleotide analogue of adenosine used either alone or in combination with other agents as therapy of chronic hepatitis B. Adefovir does not appear to be a significant cause of drug induced liver injury, but initiation of therapy and sudden withdrawal of therapy can induce a transient ex... | Adefovir dipivoxil (bis-pom PMEA) is an acyclic nucleotide analog and prodrug of adefovir (a def' oh vir). The dipivoxil moiety is hydrolyzed after absorption, and adefovir is phosphorylated intracellularly to its active form, adefovir triphosphate, which competes with deoxyadenosine triphosphate for incorporation into... | Serum aminotransferase elevations are common during or after therapy of hepatitis B, but appear to be due to exacerbations of the underlying HBV infection rather than hepatotoxicity. Sudden withdrawal of adefovir therapy can lead to an acute flare of hepatitis as viral levels suddenly rise. These withdrawal flares are ... | The apparent absence of significant hepatotoxicity from adefovir may be due to its minimal hepatic metabolism and rapid urinary excretion. In vitro, adefovir demonstrates little inhibitory activity against mitochondrial polymerase gamma. | The mild-to-moderate ALT elevations associated with initiating adefovir use are usually asymptomatic and transient. Due to the high percentage of patients who have flares of hepatitis B after discontinuation of adefovir, serum aminotransferase testing should be monitored for several months and antiviral therapy resumed... | Adefovir – Hepsera® | Antiviral Agents | null |
intro.nxml | Introduction | 2019-11-20 | null | null | null | null | null | null | null | null |
Oxcarbazepine.nxml | Oxcarbazepine | 2020-07-30 | Oxcarbazepine is a keto analogue of carbamazepine and, like the parent drug, is a potent anticonvulsant used alone or in combination with other agents in the therapy of partial seizures. Oxcarbazepine has been linked to rare instances of clinically apparent acute drug induced liver injury which resembles carbamazepine ... | Oxcarbazepine (ox" kar baz' e peen) is a keto analog of carbamazepine and functions as a prodrug being rapidly converted to 10-hydroxycarbazepine. Oxcarbazepine and carbamazepine are iminostilbenes related chemically to the tricyclic antidepressants and unrelated in structure to most other anticonvulsants. They appear ... | Chronic therapy with oxcarbazepine is associated with elevations in serum aminotransferase levels in a small proportion of patients. These elevations are rarely clinically significant and do not usually require dose modification. Clinically apparent hepatotoxicity from oxcarbazepine is uncommon but described, and is le... | The mechanism of oxcarbazepine hepatotoxicity appears to be hypersensitivity or an immunological response to a metabolically generated drug-protein complex. Serious cutaneous reactions due to oxcarbazepine as with carbamazepine has been linked to the HLA-B*15.01 allele, particularly in Han Chinese subjects. Similar HLA... | Oxcarbazepine and carbamazepine hepatotoxicity is usually rapidly reversible with stopping therapy, improvements beginning within days. In cases of severe injury, progression to acute liver failure and death can occur. Corticosteroids have been used but with uncertain effectiveness. Cross reactivity with other aromatic... | Oxcarbazepine – Generic, Trileptal® | Anticonvulsants | null |
Natalizumab.nxml | Natalizumab | 2020-04-15 | Natalizumab is a monoclonal antibody to human alpha-4 integrin which has potent immune suppressive activity and is used in the therapy of severe inflammatory bowel disease and relapsing multiple sclerosis. Natalizumab has been linked to rare instances of idiosyncratic acute liver injury that has features of autoimmunit... | Natalizumab (na" ta liz' ue mab) is a humanized monoclonal antibody to alpha-4 integrin, which binds avidly to the cellular adhesion molecule found on leukocytes blocking their ability to migrate to inflammatory foci. Inhibition of alpha-4 integrin activity leads to modulation of inflammatory pathways that are activate... | In large clinical trials, serum aminotransferase elevations occurred in an average of 5% of patients on natalizumab therapy and in a slightly lower, although similar proportion (~3%) of those who received placebo. While there were no individual case reports of liver injury attributed to natalizumab therapy, at least 59... | The mechanism of liver injury caused by natalizumab is probably immunologically mediated, perhaps as a result of its effects on leukocyte function. It is a monoclonal antibody and like other proteins it is taken up by cells by endocytosis and is metabolized into amino acids. | The hepatotoxicity of natalizumab is usually moderate in severity and reversible with discontinuation of infusions. Recurrence of injury with a shorter latency and more severe course has been reported. In cases with persistent injury, the addition of prednisone has appeared to hasten recovery, but in most instances, co... | Natalizumab – Tysabri® | Gastrointestinal Agents; Multiple Sclerosis Agents | null |
ChloralHydrate.nxml | Chloral hydrate | 2017-01-23 | Chloral hydrate is a mild hypnotic that is used to treat simple insomnia. Despite many years of use, chloral hydrate has not been implicated in causing serum enzyme elevations or clinically apparent liver injury. | Chloral hydrate is a hypnotic agent that was developed in the 19th century and was commonly used as a sleeping aid into the 1970s, when it was replaced by the benzodiazepines. Chloral hydrate is a simple chlorinated molecule that is converted in the liver (by alcohol dehydrogenase) to trichloroethanol, which is the act... | Chloral hydrate has been in clinical use for many decades and has not been linked to serum enzyme elevations during therapy or instances of clinically apparent liver injury. While prospective studies of the effects of chloral hydrate on liver tests have not been done, the absence of reported instances of liver injury a... | null | null | Chloral Hydrate – Generic | Sedatives and Hypnotics | null |
Alefacept.nxml | Alefacept | 2021-09-15 | Alefacept is a recombinant fusion protein of lymphocyte function associated antigen-3 (LFA-3) and immunoglobulin G dimer that acts to block the activation of T cells, and is an immunosuppressive agent that was previously used to treat moderate-to-severe plaque psoriasis. Alefacept is associated with a low rate of serum... | Alefacept (a lef' a sept) is a recombinant fusion protein that combines the lymphocyte function associated antigen-3 (LFA3) with the heavy chain of immunoglobulin G. The fusion protein inhibits the binding of endogenous LFA3 to CD2 cells interfering with activation of memory T cells which play an important role in the ... | In prelicensure controlled trials, serum ALT or AST elevations greater than 3 times the upper limit of normal (ULN) occurred in <2% of alefacept and a similar proportion of placebo treated subjects. The elevations were usually mild-to-moderate in severity, asymptomatic and self-limited in course. ALT elevations accompa... | The mechanism of possible liver injury due to alefacept is unknown. Alefacept is a recombinant protein and unlikely to have intrinsic hepatotoxicity. However, because it is a potent immunomodulatory agent, it may be capable of causing reactivation of hepatitis B or autoimmune liver injury. | Liver injury attributed to alefacept has ranged from uncommon instances of transient serum enzyme elevations without symptoms or jaundice to rare cases of acute clinically apparent liver injury.\n\nDrug Class: Dermatologic Agents, Psoriasis Agents | Alefacept – Amevive® | Dermatologic Agents | null |
Erlotinib.nxml | Erlotinib | 2018-06-28 | Erlotinib is a tyrosine kinase receptor inhibitor that is used in the therapy of advanced or metastatic pancreatic or non-small cell lung cancer. Erlotinib therapy is associated with transient elevations in serum aminotransferase levels during therapy and rare instances of clinically apparent acute liver injury. | Erlotinib (er loe' ti nib) is a selective inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis. The tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation. Erlotinib is one of several tyrosine k... | Elevations in serum aminotransferase levels are common during erlotinib therapy of pancreatic and lung cancers, and values above 5 times the upper limit of normal occur in at least 10% of patients. Similar rates of ALT elevations, however, can occur with comparable antineoplastic regimens. The abnormalities are usually... | The abrupt and severe nature of the clinically apparent liver injury attributed to erlotinib suggests that it is immunologically mediated. In contrast, the transient serum enzyme elevations that occur during therapy may have a different cause and be the result of direct toxicity. Erlotinib is metabolized in the liver t... | Liver injury due to erlotinib varies in severity from minor, transient serum enzyme elevations to acute symptomatic hepatitis and acute liver failure. Monitoring of routine liver tests before starting and at regular intervals during erlotinib therapy is recommended. Serum aminotransferase elevations above 5 times the u... | Erlotinib – Tarceva® | Antineoplastic Agents | null |
Evolocumab.nxml | Evolocumab | 2018-02-19 | Evolocumab is a human monoclonal antibody to PCSK9 (proprotein convertase subtilisin/kexin type 9), a circulating protein that modulates the activity of the LDL cholesterol receptor in the liver. The monoclonal antibody lowers serum LDL cholesterol and is used to treat severe hypercholesterolemia. Evolocumab therapy ha... | Evolocumab (e" voe lok' ue mab) is a human IgG1 monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9), a serine protease that decreases the activity of the LDL cholesterol receptor in the liver. Inhibition of PCSK9 increases the low density lipoprotein (LDL) cholesterol receptor, leading to an in... | In premarketing studies, liver test abnormalities were uncommon in patients taking evolocumab and occurred at rates similar to those in patients receiving placebo injections or standard of care. Serum ALT or AST values greater than 3 times the upper limit of normal (ULN) occurred in 0.4% to 1.8% of persons on evolocuma... | Evolocumab is a human monoclonal antibody and is metabolized in many tissues to polypeptides and amino acids which are unlikely to be toxic. Monoclonal antibody therapy sometimes causes immune mediated liver injury, but such events have not been described in evolocumab. There appears to be no adverse consequences of in... | Therapy with evolocumab and other monoclonal antibodies to PCSK9 have been well tolerated with rates of adverse events similar to those with placebo or comparator treatments. Local injection site reactions occur with these agents, but are generally mild and improve with continued therapy. Monoclonal antibodies to PCSK9... | Evolocumab – Repatha® | Antilipemic Agents | null |
Oxacillin.nxml | Oxacillin | 2020-10-20 | Oxacillin is a parenteral, second generation penicillin antibiotic that is used to treat moderate-to-severe, penicillinase-resistant staphylococcal infections. Oxacillin has been linked to rare instances of clinically apparent, idiosyncratic liver injury, but it more commonly causes transient elevations in serum aminot... | Oxacillin (ox" a sil' in) is a second generation penicillin that is highly resistant to inactivation by penicillinases and is used to treat moderate-to-severe bacterial infections caused by penicillinase-producing bacteria, particularly staphylococcal infections. Oxacillin was approved for use in the United States in 1... | Oxacillin has been linked to two forms of hepatotoxicity, first an acute and transient elevation in serum aminotransferase levels occurring with high doses of intravenous therapy; and second, a more prolonged, usually cholestatic, idiosyncratic liver injury that is similar to the hepatotoxicity of other second-generati... | The cause of ALT elevations during high dose oxacillin therapy is not known, but may be due to a direct but mild injury to the liver. Fever is common, and eosinophilia and rash can occur. Liver biopsy during these episodes generally shows mild, focal cell injury. The idiosyncratic reaction to oxacillin (and other relat... | The serum aminotransferase elevations that appear during high dose intravenous therapy with oxacillin are usually benign, asymptomatic and resolve rapidly with stopping therapy or switching to other forms of penicillinase-resistant penicillins. The cholestatic hepatitis that occurs very rarely can be symptomatic and pr... | Oxacillin – Generic | Penicillin (Penicillinase-Resistant) | null |
Azilsartan.nxml | Azilsartan | 2017-01-13 | Azilsartan is an angiotensin II receptor blocker (ARB) used in the therapy of hypertension. It is associated with a low rate of transient serum aminotransferase elevations, but has yet to be linked to instances of acute liver injury. | Azilsartan (ay" sil sar' tan) is an ARB used alone or in combination with other agents for therapy of hypertension. Azilsartan inhibits the renin-angiotensin system by blocking the angiotensin II type 1 receptor (AT1), which prevents the vasoconstriction and volume expansion induced by circulating angiotensin II and wh... | Azilsartan has been associated with a low rate of serum aminotransferase elevations that, in controlled trials, was no higher than with placebo therapy. These elevations were transient and rarely required dose modification. No specific instances of clinically apparent acute liver injury have been reported in associatio... | The cause of the minor serum aminotransferase elevations with azilsartan is not known. Azilsartan is metabolized at least in part by the liver, largely via CYP 2C9, but it has minimal drug-drug interactions. | The instances of acute liver injury reported with ARB use have been self-limited and have not resulted in acute liver failure or chronic liver injury. While corticosteroids have been used in cases of severe cholestasis due to ARBs, their efficacy has not been shown and their use is best avoided. Patients with azilsarta... | Azilsartan – Edarbi® | Angiotensin II Receptor Antagonists | null |
Loperamide.nxml | Loperamide | 2019-04-25 | Loperamide is synthetic opioid that primarily affects opiate receptors in the intestine and is used to treat diarrhea. Loperamide has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury. | Loperamide (loe per’ a mide) is a synthetic piperidine derivative that acts as a mild opiate receptor agonist (predominant µ type receptors), but is used largely for the treatment of diarrhea rather than pain. Loperamide is not structurally related to morphine or codeine and has minimal or no euphoric or analgesic effe... | As with most opiates in current use, therapy with loperamide has not been linked to serum enzyme elevations. There have been no convincing cases of idiosyncratic acute, clinically apparent liver injury attributed to either agent. The reason for its lack of hepatotoxicity may relate to the low doses used and lack of sig... | null | null | Loperamide – Generic, Imodium® | Gastrointestinal Agents; Opioids | null |
Trametinib.nxml | Trametinib | 2018-06-28 | Trametinib is a dual-kinase inhibitor that is used in the treatment of advanced malignant melanoma, usually in combination with darbafenib. Trametinib therapy is associated with transient elevations in serum aminotransferase and alkaline phosphatase levels during therapy, but has yet to be linked cases of clinically ap... | Trametinib (tra me’ ti nib) is an orally available, small molecule inhibitor of the mitogen activated extracellular signal regulated kinases 1 and 2 (MEK1 and MEK2), which are important components of the kinase cascade in the mitogen activated protein kinase (MAPK) pathway (RAS-RAF-MEK-ERK). Components of the MAPK path... | In large clinical trials, abnormalities in routine liver tests were common with serum aminotransferase elevations occurring in 39% to 60% and alkaline phosphatase in 24% to 67% of patients treated with trametinib. However, elevations in ALT above 5 times the ULN were uncommon, occurring in 0% to 5% of patients and gene... | The cause of serum enzyme elevations during trametinib therapy is not known. Trametinib is metabolized in the liver largely through the cytochrome P450 system, predominantly CYP 3A4 and CYP 2C8. Potent inducers or inhibitors of these P450 enzymes can alter serum levels of trametinib and serious drug-drug interactions c... | In using kinase inhibitors for treatment of cancer, monitoring of routine liver tests before starting and during therapy is warranted. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) or elevations accompanied by jaundice or symptoms should lead to temporary cessation. Therapy sh... | Trametinib – Mekinist® | Antineoplastic Agents | null |
Pyrazinamide.nxml | Pyrazinamide | 2020-12-20 | Pyrazinamide is a first line antituberculosis medication, but is used only in combination with other antituberculosis medications such as isoniazid or rifampin. Pyrazinamide is associated with transient and asymptomatic elevations in serum aminotransferase levels and is a well known cause of clinically apparent, acute ... | Pyrazinamide (pir" a zin' a mide) is a synthetic pyrazine analogue of nicotinamide that has potent activity against mycobacterium tuberculosis. Its mechanism of action is unknown, but it appears to be both bactericidal and bacteriostatic. Pyrazinamide is considered an adjunctive therapy of tuberculosis and is always us... | Combination therapy for tuberculosis using pyrazinamide is commonly associated with transient and asymptomatic elevations in the serum aminotransferase levels. These elevations are usually less than five times the upper limit of the normal range. Because pyrazinamide is used only in combination with other antituberculo... | The mechanism of hepatic injury by pyrazinamide is not known, but the drug is extensively metabolized by the liver and injury may be caused by a metabolic intermediate. Hepatotoxicity from pyrazinamide appears to be more frequent with higher doses, suggesting a direct toxic effect, at least in part. | The appearance of liver injury with symptoms and serum aminotransferase levels above 3 times the ULN or any elevation in aminotransferase levels above 5 times the ULN should prompt withdrawal of pyrazinamide. Many cases of pyrazinamide hepatotoxicity are severe and prolonged, and fatal instances have occurred. Pyrazina... | Pyrazinamide – Generic, Tebrazid® | Antituberculosis Agents | null |
Tribulus.nxml | Tribulus | 2022-08-08 | Tribulus is herbal product prepared from the leaves, fruit and roots of Tribulus terrestris, extracts of which have been used as an aphrodisiac, general tonic and mood stimulant in traditional medicine. The native plant causes serious liver injury in grazing animals, and but tribulus extracts have not been linked convi... | Tribulus is prepared from the leaves and roots of the low-growing shrub and common weed Tribulus terrestris that is found in dry habitats in many parts of the world, including Asia, Africa, Australia and North and South America. Extracts of the shrub have been used in traditional medicine as an aphrodisiac, general ton... | Tribulus terrestris has been not been reported to cause serum enzyme elevations in persons taking the herbal extract, but prospective studies with regular monitoring of liver tests have not been done. Isolated case reports of renal injury with serum aminotransferase elevations have been published but may have represent... | Leaf extracts of Tribulus contain many components, but none has been shown to be particularly hepatotoxic in humans. In grazing animals Tribulus terrestris has been linked to bile duct injury and the toxic component of the plant is believed to be steroidal sapogenins which form crystals in bile ducts and renal tubules. | Clinically apparent liver injury from Tribulus in humans has not been convincingly shown.\n\nDrug Class: Herbal and Dietary Supplements | Tribulus – Generic | Herbal and Dietary Supplements | null |
Ruxolitinib.nxml | Ruxolitinib | 2022-08-30 | Ruxolitinib is a small molecule Janus kinase inhibitor that is used in the treatment of intermediate or high risk myelofibrosis and resistant forms of polycythemia vera and graft-vs-host disease. Ruxolitinib is associated with transient and usually mild elevations in serum aminotransferase during therapy and to rare in... | Ruxolitinib (rux” oh li’ ti nib) is an orally available, specific inhibitor of Janus kinase subtypes 1 and 2 (JAK1 and JAK2). JAK1 and JAK2 are non-receptor tyrosine kinases that are critical components of pathways that lead to production and secretion of hematologic growth factors and inflammatory cytokines. These pat... | In the large clinical trials, serum ALT elevations occurred in 25% to 48% of ruxolitinib treated subjects versus 7% to 9% of placebo recipients. The ALT elevations were generally self-limited, asymptomatic and mild and were above 5 times ULN in only 1.3% of patients. In the prelicensure clinical trials, no cases of cli... | The causes of serum enzyme elevations during ruxolitinib therapy are not known. Ruxolitinib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury may be related to production of a toxic intermediate. Ruxolitinib is susceptible to drug-drug interactions with agents that inhibit or induce hepat... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) or any elevations accompanied by jaundice or symptoms should lead to dose reduction or temporary cessation. There does not appear to be cross reactivity in risk for hepatic injury between ruxolitinib and other kinase inhibitors. Ru... | Ruxolitinib – Jakafi® | Antineoplastic Agents | null |
Nedosiran.nxml | Nedosiran | 2025-03-05 | Nedosiran is a synthetic small interfering RNA molecule directed against the mRNA of lactic dehydrogenase A that is used to treat the rare genetic disease primary hyperoxaluria type 1. Nedosiran has not been linked to serum aminotransferase elevations during therapy or to instances of clinically apparent liver injury w... | Nedosiran (ned” oh sir' an) is a synthetic, double-stranded, small interfering RNA (siRNA) directed against the mRNA of lactic dehydrogenase A (LDH-A), an enzyme made in the liver, the inhibition of which decreases the production of oxalate, a stable molecule that is excreted in the kidneys. Nedosiran was developed to ... | In the small registration trial of nedosiran in 35 children and adults with primary hyperoxaluria type 1, therapy was well tolerated and side effects attributed to the drug were few, transient and generally mild. Rates of ALT and AST elevations during therapy were similar with nedosiran vs placebo and usually less than... | The possible cause of hepatic injury from nedosiran or other siRNA therapeutics is not known. Nedosiran, like other siRNA therapeutic agents, is metabolized intracellularly by nucleases and is not a substrate of cytochrome P450 enzymes or hepatic transporters. | Nedosiran has not been linked to liver test abnormalities or to clinically apparent liver injury and regular monitoring of routine liver tests is not recommended.\n\nDrug Class: Genetic Disorder Agents, siRNA and Antisense Agents\n\nOther Therapeutic siRNA-based Agent for Hyperoxaluria: Lumasiran | Nedosiran – Rivfloza® | Genetic Disorder Agents | null |
Melphalan.nxml | Melphalan | 2020-01-15 | Melphalan is an orally and parenterally administered nitrogen mustard-like alkylating agent used in the therapy of multiple myeloma and ovarian cancer. Melphalan therapy has been associated with low rates of serum enzyme elevations during therapy, but when used in high doses as myeloablative therapy in preparation for ... | Melphalan (mel' fa lan) is a phenylalanine derivative of nitrogen mustard and an alkylating agent that resembles cyclophosphamide and chlorambucil. It acts by causing modification and cross linking of DNA, thus inhibiting DNA, RNA and protein synthesis and causing programmed cell death (apoptosis) in rapidly dividing c... | Mild and transient elevations in serum aminotransferase levels are uncommon with standard doses of melphalan, but occur more commonly with high dose intravenous regimens. The enzyme elevations are usually mild and asymptomatic and do not require dose modification. Clinically apparent liver disease has not been reported... | The mechanism of hepatotoxicity from melphalan is probably direct cytotoxic injury to sinusoidal endothelial cells causing their death and extrusion into sinusoids, with subsequent obstruction of sinusoids and small hepatic veins. The cytotoxic and immunosuppressive activity of melphalan may also be responsible for the... | The severity of sinusoidal obstruction syndrome varies considerably, from transient mild asymptomatic liver injury to acute liver failure that is rapidly fatal. There is no known specific therapy of proven efficacy for sinusoidal obstruction syndrome and management should focus on avoidance of further injury and suppor... | Melphalan – Generic, Alkeran® | Antineoplastic Agents, Alkylating Agents | null |
JinBuHuan.nxml | Jin Bu Huan | 2018-04-26 | Jin Bu Huan is a Chinese herb used for centuries as a mild sedative and analgesic, recently marketed for insomnia, arthritic and orthopedic pain and gastrointestinal complaints. Jin Bu Huan products have been implicated in more than a dozen cases of idiosyncratic, clinically apparent, acute liver injury but the hepatot... | Jin Bu Huan is a popular and widely used Chinese herbal medication which can contain several unrelated herbal species including Lycopodium serratum, Panax, Pseudo ginseng, Polygala chinensis and two species of Stephania. Jin Bu Huan has been used for centuries in China for multiple purposes including as a sedative, ana... | More than a dozen cases of hepatotoxicity attributable to products sold as Jin Bu Huan have been reported, with onset of liver test abnormalities or jaundice within 2 to 24 weeks of starting the herbal supplement. The enzyme pattern was typically hepatocellular, and the clinical syndrome resembled acute viral hepatitis... | The mechanism of hepatotoxicity of Jin Bu Huan is not known, but some extracts are usually rich in levo-tetrahydropalmatine, which may have hepatotoxic potential. On the other hand, the majority of cases of hepatotoxicity from Jin Bu Huan have had features of an idiosyncratic reaction and may have been due to an adulte... | The severity of hepatotoxicity from Jin Bu Huan ranges from serum enzyme elevations without symptoms to acute hepatitis with marked jaundice. The injury is usually self-limited and rapidly reversible with stopping the herbal. Rechallenge leads to recurrence of injury and should be avoided. There is no evidence that the... | Jin Bu Huan – Generic | Herbal and Dietary Supplements | null |
Fluvoxamine.nxml | Fluvoxamine | 2021-05-11 | Fluvoxamine is a selective serotonin reuptake inhibitor (SSRI) used in the therapy of obsessive-compulsive disorder. Fluvoxamine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury. | Fluvoxamine (floo vox' a meen) is a selective serotonin reuptake inhibitor (SSRI) that was developed largely for use in obsessive-compulsive disorder. Fluvoxamine acts by blocking the reuptake of serotonin in CNS synaptic clefts, thus increasing serotonin levels in the brain which is associated with its psychiatric eff... | Liver test abnormalities have been reported to occur in up to 1% patients on fluvoxamine, but elevations are usually modest and usually do not require dose modification or discontinuation. A few instances of acute, clinically apparent episodes of liver injury with marked liver enzyme elevations with no or minimal jaund... | The mechanism by which fluvoxamine causes liver injury is not known. Fluvoxamine is extensively metabolized by the liver, mainly via the cytochrome P450 system, and hepatotoxicity may be mediated by toxic intermediates of their metabolism. In addition, fluvoxamine inhibits several CYP enzymes and has significant drug-d... | The serum aminotransferase elevations that occur on fluvoxamine therapy are usually self-limited and do not require dose modification or discontinuation of therapy. No instances of acute liver failure or chronic liver injury have been attributed to fluvoxamine therapy. Restarting fluvoxamine has been reported to cause ... | Fluvoxamine – Generic, Luvox® | Antidepressant Agents | null |
Tedizolid.nxml | Tedizolid | 2016-04-02 | Tedizolid is an oxazolidinone antibiotic, similar to linezolid, which has a broad spectrum of activity against gram positive bacteria including methicillin resistant Staphyloccocal aureus (MRSA). Tedizolid has been associated with a low rate of transient serum aminotransferase elevations during therapy, but has not bee... | Tedizolid (te diz' oh lid) is a synthetic, second generation oxazolidinone antibiotic, similar to linezolid, that has broad bactericidal activity against gram positive organisms such as enterococci and staphylococci and most streptococci. Importantly, tedizolid has potent activity against Methicillin resistant strains ... | Therapy with tedizolid has been associated with mild and transient elevations in serum aminotransferase and alkaline phosphatase levels in 1% to 4% of patients, although similar rates of elevations occur in patients with infections treated with comparable agents including linezolid. In all instances, the elevations occ... | The etiology of serum enzyme elevations during tedizolid therapy is not known and may relate more to the underlying condition rather than injury from tedizolid. Lactic acidosis and peripheral neuropathy from oxazolidinones are probably due to inhibition of mitochondrial ribosomal function and protein synthesis. Indeed,... | The serum aminotransferase and alkaline phosphatase elevations that occur during tedizolid therapy are self-limited and resolve once therapy is stopped. There are no reports of cross sensitization and hepatic injury from tedizolid in persons with hepatic injury from other antibiotics or sulfonamides. The lactic acidosi... | Tedizolid – Sivextro® | Antiinfective Agents | [
{
"cas_registry_number": "856866-72-3",
"molecular_formula": "C17-H15-F-N6-O3",
"name": "Tedizolid"
},
{
"cas_registry_number": "165800-03-3",
"molecular_formula": "C16-H20-F-N3-O4",
"name": "Linezolid"
}
] |
Gefitinib.nxml | Gefitinib | 2018-03-06 | Gefitinib is a selective tyrosine kinase receptor inhibitor used in the therapy of non-small cell lung cancer. Gefitinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury. | Gefitinib (ge fi' ti nib) is a selective inhibitor of the tyrosine kinase receptor of epidermal growth factor (EGFR), which is often mutated and over expressed in cancer cells, particularly non-small cell lung cancer and some forms of breast cancer. The mutated EGF tyrosine kinase receptor is constitutively expressed w... | In large early clinical trials, elevations in serum aminotransferase levels occurred in 9% to 13% of patients treated with standard doses of gefitinib, and 2% to 4% of patients had to stop therapy because of elevations above 5 times the upper limit of normal. Serum enzyme elevations typically arise after 4 to 12 weeks ... | The cause of the liver injury due to gefitinib is unknown. Gefitinib is metabolized in the liver largely via CYP 3A4, and liver injury may be due to accumulation of a toxic or immunogenic intermediate. | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose interruption. If changes persist, are severe, or reoccur on restarting, gefitinib should be discontinued. There have been no published reports of acute liver failure, chronic hepatitis or vanishing bile duct syn... | Gefitinib – Iressa® | Antineoplastic Agents | null |
Flavocoxid.nxml | Flavocoxid | 2018-01-30 | Flavocoxid is a medical food consisting of plant derived flavonoids which have antiinflammatory activity and are used to treat chronic osteoarthritis. Flavocoxid has been linked to minor elevations in serum enzyme levels during therapy and to rare instances of clinically apparent liver injury. | Flavocoxid (flay" voe kox' id) is a proprietary blend of purified plant derived bioflavonoids including baicalin and catechins. Flavocoxid inhibits cyclooxygenases (both Cox-1 and Cox-2) as well as lipoxygenases (5-Lox) in vitro and in animal models, which may account for its antiinflammatory and antioxidant activity. ... | In premarketing clinical trials, serum aminotransferase elevations occurred in up to 10% of patients on flavocoxid therapy, but elevations above 3 times the upper limit of normal occurred in only 1% to 2% of recipients. Since its release, however, there have been several reports of clinically apparent acute liver injur... | Flavocoxid is a proprietary mixture of plants and herbs and it is unclear which component(s) might be responsible for liver injury. The mixture includes extracts from Scutellaria baicalensis (skullcap, containing the phytochemical baicalin) and Acacia catechu (catechin), both of which have been implicated in causing ra... | No instances of acute liver failure or chronic liver injury have been linked to flavocoxid use and all cases have been self-limited, without subsequent chronic hepatitis or vanishing bile duct syndrome. Recurrence upon reexposure has been reported and rechallenge should be avoided. There is no information on possible c... | Flavocoxid – Limbrel® | Herbal and Dietary Supplements | [
{
"cas_registry_number": "21967-41-9",
"molecular_formula": "C21-H18-O11",
"name": "Baicalin"
},
{
"cas_registry_number": "154-23-4",
"molecular_formula": "C15-H14-O6",
"name": "Catechin"
}
] |
Gabapentin.nxml | Gabapentin | 2020-07-30 | Gabapentin is a unique anticonvulsant that is used as adjunctive therapy in management of epilepsy and for neuropathic pain syndromes. Therapy with gabapentin is not associated with serum aminotransferase elevations, but several cases of clinically apparent liver injury from gabapentin have been reported. | Gabapentin (gab" a pen' tin) is a structural analogue of gamma-aminobutyric acid (GABA), but demonstrates little or no interaction with GABA receptors and does not appear to alter GABA uptake, synthesis or metabolism. While initially believed to act on the GABA-ergic neurotransmitter system, the actual mechanism of act... | Limited data are available on the hepatotoxicity of gabapentin. In clinical trials in diabetic neuropathy and epilepsy, therapy with gabapentin was not associated with an increased frequency of serum aminotransferase elevations or liver toxicity. Rare individual case reports of liver injury from gabapentin have been pu... | The apparent absence or low rate of significant hepatotoxicity from gabapentin may be due to its minimal hepatic metabolism and rapid urinary excretion. | The case reports of hepatic injury due to gabapentin were followed by complete recovery without evidence of residual or chronic injury. No cases of acute liver failure or chronic liver injury due to gabapentin have been described. There is no information about cross reactivity with other compounds having similar struct... | Gabapentin – Generic, Neurontin® | Anticonvulsants | null |
Arsenic.nxml | Arsenic | 2017-07-25 | Arsenic is a nonessential trace element that is widely distributed in nature. Arsenic was used in medicinal agents in the 19th and early 20th centuries, but has been replaced by safer and more effective agents and has not been in use for over 50 years. Nevertheless, arsenic is found widely in nature and accidental or i... | Arsenic is a nonessential trace element and well known poison that is found widely in low concentrations in the environment. Typical arsenic concentrations are 2 to 5 parts per billion in soil and sea water. In the United States, the maximal allowable concentration of arsenic in well and drinking water is 50 parts per ... | Acute poisoning with arsenic is marked by severe abdominal pain, nausea and vomiting, diarrhea, muscle cramps, metallic taste and extreme thirst, followed by stupor, coma, cardiovascular collapse and death. Death can occur within 24 hours of exposure, but with sublethal doses, survival is possible and liver injury may ... | Arsenic uncouples oxidative phosphorylation and is a general cytoplasmic toxin binding to and inhibiting sulfhydryl groups on essential enzymes. With acute exposures, the skin, cardiac and neurologic toxicities are most prominent. With chronic exposure, skin and hepatic manifestations may dominant the clinical picture. | Arsenic poisoning is often treated with chelation, with uncertain efficacy. Both dimercaprol and succimer have been used, but their efficacy in ameliorating symptoms and signs and speeding clinical recovery has not been documented. The major invention should be directed at detection and elimination of the source of ars... | Arsenic – Trisenox® | Trace Elements and Metals | null |
Diphenhydramine.nxml | Diphenhydramine | 2017-01-16 | Diphenhydramine is a first generation antihistamine that is used for symptoms of allergic rhinitis and the common cold. It is also commonly used as a mild sleeping aid. Diphenhydramine has not been linked to instances of clinically apparent acute liver injury. | Diphenhydramine (dye" fen hye' dra meen) is a first generation antihistamine that is used widely in the therapy of the symptoms of allergic rhinitis and the common cold, including sneezing, cough, runny note, watery eyes and itching. Because of its sedating side effects, it is also used as a mild sleeping aid. In intra... | Despite widespread use over many decades, diphenhydramine has not been linked to liver test abnormalities or to clinically apparent liver injury. The reason for its safety may relate its short half-life and limited duration of use.\n\nLikelihood score: E (unlikely to be a cause of clinically apparent liver injury).\n\n... | null | null | Diphenhydramine – Generic, Benadryl® | Antihistamines | null |
Efavirenz.nxml | Efavirenz | 2018-02-10 | Efavirenz is a nonnucleoside reverse transcriptase inhibitor used in combination with other agents in the therapy of human immunodeficiency virus (HIV) infection. Efavirenz is associated with a low rate of serum enzyme elevations during therapy and is an uncommon, but well established cause of clinically apparent acute... | Efavirenz (ef" a vir' enz) is an antiretroviral agent that acts by noncompetitive binding to and inhibition of the HIV reverse transcriptase. Efavirenz is a nonnucleoside reverse transcriptase inhibitor and is similar to nevirapine in its mechanism of action, but has little or no structural similarity. Efavirenz was ap... | Serum aminotransferase elevations above 5 times the upper limit of normal occur in 1% to 8% of patients on efavirenz, and this rate is higher in patients who have HCV coinfection. Clinically apparent hepatotoxicity due to efavirenz is rare, but many convincing cases have been published. The liver injury is usually immu... | The cause of the clinically apparent hepatotoxicity from efavirenz appears to be hypersensitivity. Features such as eosinophilia, skin rash and biopsy findings suggest that the injury is due to an immunoallergic reaction. Efavirenz is metabolized by the cytochrome P450 system including CYP 3A and 2B6 and has significan... | The severity of the liver injury due to efavirenz ranges from mild and transient enzyme elevations to acute hepatocellular jaundice and even fulminant liver failure and death. Typically, improvements start within a few days of stopping efavirenz and full recovery is expected within 2 to 8 weeks. Corticosteroids are oft... | Efavirenz – Sustiva® | Antiviral Agents | null |
UvaUrsi.nxml | Uva Ursi | 2020-03-28 | Uva ursi is an herbal extract derived from the leaves of the Arctostaphylos, a small evergreen shrub, which has been used in Native American traditional medicine for treatment of urinary tract symptoms and as a diuretic. Treatment with extracts of uva ursi has not been specifically linked to serum aminotransferase elev... | Uva ursi is an herbal product derived from the fresh or dried leaves of the plant Arctostaphylos uva-ursi or bearberry, named for the grape-like clusters of orange berries that are commonly eaten by bears. Both Arctostaphylos and uva-ursi mean “grape of the bears”, the former in Greek and the latter in Latin. Uva ursi ... | Uva ursi has not been linked to serum enzyme elevations during therapy although there have been few prospective studies of its adverse effects on laboratory test results. There have been no convincing published instances of clinically apparent liver injury attributed to uva ursi. The frequency of hypersensitivity react... | null | null | Uva Ursi – Generic | Herbal and Dietary Supplements | null |
Sotorasib.nxml | Sotorasib | 2023-09-02 | Sotorasib is a small molecule inhibitor of the KRAS G12C mutant protein which is found in up to 13% of refractory cases of non-small cell lung cancer. Serum aminotransferase elevations are common during therapy with sotorasib, and a proportion of patients develop clinically apparent liver injury that can be severe. | Sotorasib (soe toe ras’ ib) is an orally available, small molecule inhibitor of the KRAS gene product which is a frequently mutated oncogene found in several forms of cancer, most commonly in non-small cell lung cancer (NSCLC). The KRAS (Kristen rat sarcoma viral oncogene homolog) G12C mutation produces a constituently... | In the prelicensure clinical trials of sotorasib in patients with solid tumors harboring KRAS G12C mutations, liver test abnormalities were frequent although usually self-limited and mild. Some degree of ALT elevations arose in 38% of sotorasib treated patients and were above 5 times the upper limit of normal (ULN) in ... | The cause of serum aminotransferase elevations from sotorasib is unknown, but the pattern of abnormalities suggests immune-mediated liver injury. Several retrospective analyses have found that significant ALT and AST elevations arise most frequently in patients who had received checkpoint inhibitor therapy (usually ant... | The product label for sotorasib recommends monitoring for routine liver tests before starting treatment, at 3 week intervals during the first 3 months of treatment and monthly thereafter as clinically indicated. Serum aminotransferase elevations above 5 times the upper limit of normal should lead to dose reduction or t... | Sotorasib – Lumakras® | Antineoplastic Agents | null |
Fidaxomicin.nxml | Fidaxomicin | 2017-08-08 | Fidaxomicin is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury. | Fidaxomicin (fye dax" oh mye' sin) is a semisynthetic macrolide antibiotic that is minimally absorbed and has potent bactericidal activity against Clostridia, but minimal or no antibacterial activity against normal gastrointestinal flora. Because of its lack of oral absorption and restricted antibacterial activity, fid... | In large clinical trials, therapy with fidaxomicin for ten days was associated with a low rate of serum aminotransferase elevations [1% to 3.2%], but rates with comparator agents such as vancomycin were similar [up to 2.7%]. There have been no reports of clinically apparent liver injury attributed to fidaxomicin. Howev... | Fidaxomicin is minimally absorbed systematically and the cause of serum enzyme elevations or liver injury from its use is unknown. | The minor serum aminotransferase elevations that appear during therapy with fidaxomicin are usually benign, asymptomatic and resolve rapidly once fidaxomicin is stopped. It is unclear whether there is cross sensitivity to hepatic injury about the different macrolide antibiotics, but after severe injury from one macroli... | Fidaxomicin – Dificid® | Antiinfective Agents | null |
Abrocitinib.nxml | Abrocitinib | 2022-06-13 | Abrocitinib is an orally available, small molecule inhibitor of Janus kinase 1 (JAK1) that is used to treat moderate-to-severe atopic dermatitis. Abrocitinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy, but has not been linked to cases of clinically apparent ... | Abrocitinib (ab” roe sye' ti nib) is an orally available, small molecule, specific inhibitor of Janus-associated kinase 1 (JAK1) that is used to treat refractory, moderate-to-severe atopic dermatitis. The JAK proteins are intracellular tyrosine kinases that provide critical steps in pathways of immune activation as wel... | In the large registration clinical trials, serum aminotransferase elevations occurred rarely and were not attributed to abrocitinib. These elevations were typically mild and transient, and values above 3 times the upper limit of normal (ULN) occurred in less than 1% of patients on abrocitinib. In prelicensure studies, ... | The causes of serum enzyme elevations during abrocitinib therapy are not known. Abrocitinib is metabolized in the liver largely by CYP 2C9 and 3A4 pathways and may be susceptible to drug-drug interactions with agents that inhibit or induce these specific hepatic microsomal enzymes. | There is no recommendation for monitoring of routine liver tests during abrocitinib therapy. Because abrocitinib may cause reactivation of hepatitis B, patients starting long term therapy should be screened for HBsAg and anti-HBc. Patients with preexisting HBsAg in serum should undergo evaluation and prophylaxis agains... | Abrocitinib – Cibinqo® | Dermatologic Agents | [
{
"cas_registry_number": "1622902-68-4",
"molecular_formula": "C14-H21-N5-O2-S",
"name": "Abrocitinib"
},
{
"cas_registry_number": "477600-75-2",
"molecular_formula": "C16-H20-N6-O",
"name": "Tofacitinib"
}
] |
Zafirlukast.nxml | Zafirlukast | 2019-06-04 | Zafirlukast is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma. Zafirlukast has been linked to rare, but occasionally severe cases of acute liver injury. | Zafirlukast (za" fir loo' kast) is a leukotriene receptor antagonist that binds to the CysLT1 and CysLT2 receptors, thereby interfering with inflammatory pathways that are involved in the pathogenesis of asthma and allergic rhinitis. Pretreatment with single oral doses of zafirlukast inhibits bronchoconstriction and th... | Prospective studies have shown that ALT elevations occur in 1.5% of patients receiving zafirlukast, most of which are mild, asymptomatic and self limited even with continuing therapy. A similar rate of transient ALT elevations is often found in placebo recipients. Clinically apparent liver disease from zafirlukast is r... | null | Monitoring of routine liver tests for liver injury is recommended but has not been shown to be effective in preventing the rare instances of hepatic injury due to zafirlukast and the optimal timing and frequency of such testing is not well define. Patients should be alerted to the signs and symptoms of liver injury and... | Zafirlukast – Generic, Accolate® | Antiasthma Agents | null |
Ketamine.nxml | Ketamine | 2018-04-25 | Ketamine is a parenterally administered, general anesthetic used largely for short term diagnostic and surgical procedures, but which has been limited in use because of its psychological side effects including vivid hallucinations, agitation and confusion. Ketamine also has major abuse potential and is used illicitly a... | Ketamine (kee' ta meen) is an arylcyclohexylamine anesthetic that acts as a noncompetitive inhibitor of N-methyl-D-apartate (NMDA) receptors in the brain. Ketamine infusions rapidly produce anesthesia and a unique cataleptic state with profound analgesia, amnesia and unresponsiveness, but often with maintenance of musc... | Short term use of ketamine for anesthesia has been associated with rare instances of serum enzyme elevations, but not with clinically apparent liver injury. With chronic or intermittent use, however, unusual biliary and hepatic complications have been described. In a manner similar to its effects on the urinary tract, ... | The mechanism by which ketamine causes urinary and biliary abnormalities is not known, but the high concentrations of ketamine metabolites in urine and bile may cause direct toxic injury to surface epithelium with repeated use. Ketamine undergoes extensive hepatic metabolism, largely via the cytochrome P450 system (CYP... | Clinically apparent hepatobiliary injury associated with ketamine arises during chronic rather than acute exposure, and is most commonly associated with ketamine abuse or experimental applications as in the therapy of chronic pain syndromes. Most patients improve once ketamine is stopped and no instances of cirrhosis o... | Ketamine – Generic, Ketalar® | Anesthetic Agents | null |
Atorvastatin.nxml | Atorvastatin | 2025-03-03 | Atorvastatin is a commonly used cholesterol lowering agent (statin) that is associated with mild, asymptomatic and self-limited serum aminotransferase elevations during therapy and rarely with clinically apparent acute liver injury. | Atorvastatin (a tor" va stat' in) is a potent, orally available inhibitor of hepatic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the major rate-limiting enzyme in cholesterol synthesis. Like other members of its class (the “statins”), atorvastatin lowers total serum cholesterol and low density lipoprotei... | Atorvastatin therapy is associated with mild, asymptomatic and usually transient serum aminotransferase elevations in 1% to 3% of patients but levels above 3 times ULN in less than 1%. In summary analyses of large scale studies with prospective monitoring, ALT elevations above 3 times the upper limit of normal (ULN) oc... | The cause of hepatic injury from atorvastatin is unknown. Atorvastatin is largely metabolized in the liver via CYP 3A4 and is excreted in bile. The mild, self-limited ALT elevations are likely due to a toxic intermediate of drug metabolism and the reversal of these elevations due to adaptation. The idiosyncratic, clini... | The product label for atorvastatin recommends screening for liver test abnormalities before starting therapy and repeating tests as clinically indicated. The mild ALT elevations associated with atorvastatin therapy are usually self-limited and do not require dose modification. Atorvastatin should be stopped if ALT leve... | Atorvastatin – Generic, Lipitor® | Antilipemic Agents | null |
Bictegravir.nxml | Bictegravir | 2019-04-10 | Bictegravir is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor, the fourth in this class of agents that target the viral integrase. Bictegravir is used only in combination with other antiretroviral agents in the treatment of HIV infection and it has had limited use. Bictegravir is associated wi... | Bictegravir (bic teg' ra vir) is a relatively new antiretroviral drug that targets the HIV integrase, one of the three viral enzymes involved in replication. Bictegravir blocks the binding site of the HIV integrase and prevents the strand transfer activity and integration of the provirus into the host genome. Bictegrav... | In large clinical trials, therapy with bictegravir combined with emtricitabine and tenofovir alafenamide was associated with alanine aminotransferase (ALT) elevations (above 1.5 times ULN) in 11% patients, but these rates were similar to those in comparator groups (12% to 15%) receiving matched background optimized ant... | The mechanism by which bictegravir might cause liver injury is not known. Bictegravir is metabolized by the liver, largely by glucuronidation with subsequent urinary clearance. Bictegravir has little or no effect on microsomal cytochrome P450 enzymes. Reconstitution of immune reactivity by antiretroviral therapy in pat... | If bictegravir hepatotoxicity occurs, it must be rare. Bictegravir has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. Patients receiving antiviral therapy for HIV infection should be screened for evidence of hepatitis B and C and treated accordingly.\n\nDrug Class: A... | Bictegravir – Biktarvy® | Antiviral Agents | [
{
"cas_registry_number": "1611493-60-7",
"molecular_formula": "C21-H18-F3-N3-O5",
"name": "Bictegravir"
},
{
"cas_registry_number": "1051375-16-6",
"molecular_formula": "C20-H19-F2-N3-O5",
"name": "Dolutegravir"
},
{
"cas_registry_number": "697761-98-1",
"molecular_formula": ... |
Momelotinib.nxml | Momelotinib | 2023-12-28 | Momelotinib is a small molecule Janus kinase inhibitor that is used in the treatment of intermediate or high risk, primary or secondary myelofibrosis. Momelotinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy and has also been linked to instances of clinically ... | Momelotinib (moe” me, loe’ ti nib) is an orally available, small molecular inhibitor of Janus kinase subtype 1 and 2 (JAK1/2) including mutant JAK2V617F and is used to treat resistant forms of myelofibrosis including secondary forms related to polycythemia vera and essential thrombocythemia. Myelofibrosis is a cancerou... | In the published preregistration clinical trials of momelotinib, rates of serum ALT or AST elevations ranged from 21% to 31% and were above 5 times the upper limit of normal (ULN) in 0.5% to 2.0%, and above 20 times ULN in 0.5%. Two of 448 momelotinib treated patients evaluated in the safety cohort developed clinically... | Momelotinib therapy has been clearly linked to serum enzyme elevations and to rare instances of clinically apparent liver injury. It is metabolized in the liver, and liver injury may be due to its metabolism to an immunogenic or toxic intermediate. Momelotinib is a weak inducer of CYP 2B6 and competes for hepatic uptak... | Momelotinib has been clearly linked to serum aminotransferase elevations and significant liver injury. For this reason, routine monitoring of liver tests is recommended in the product label every month for six months, and “as needed” thereafter. Serum aminotransferase elevations above 5 times ULN should lead to dose re... | Momelotinib – Ojjaara® | Antineoplastic Agents | null |
Buprenorphine.nxml | Buprenorphine | 2020-11-24 | Buprenorphine is a sublingually and transdermally available, semisynthetic opioid analgesic, which is used as an analgesic and for management of opioid dependence. Therapy with buprenorphine is associated with mild and transient serum enzyme elevations, and with moderate-to-severe clinically apparent liver injury when ... | Buprenorphine (bue" pre nor' feen) is a semisynthetic opioid that is 25 to 50 times more potent than morphine and has been used as an analgesic as well as therapy of opioid addiction. Buprenorphine is a partial µ-opioid receptor agonist and a κ-receptor antagonist accounting for its benefit for opioid deterrence. Bupre... | Buprenorphine therapy has been associated with a low rate of serum enzyme elevations during treatment, although the populations studied (opioid dependent) often have coexisting chronic liver diseases which complicate such assessments. Nevertheless, rates of ALT elevations during treatment with buprenorphine (with or wi... | Buprenorphine undergoes extensive first pass hepatic extraction and is metabolized primarily by the cytochrome P450 system (CYP 3A4). The low doses used and rapid metabolism may account for its relative lack of hepatotoxicity when used in conventional doses. The appearance of an acute hepatic necrosis after intravenous... | The severity of liver injury attributed to buprenorphine has ranged from mild-to-severe hepatitis, and fatal instances have been reported. Interestingly, most patients subsequently tolerated restarting buprenorphine at doses used prior to the toxic event, and some patients continued to misuse it by intravenous injectio... | Buprenorphine – Generic, Buprenex®, Subutex® (SL Tablets) | Substance Abuse Treatment Agents | null |
ScopolamineMethscop.nxml | Scopolamine | 2017-07-07 | Scopolamine as a natural plant alkaloid that has potent anticholinergic effects and is used to treat mild to moderate nausea, motion sickness and allergic rhinitis. Scopolamine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. | Scopolamine (skoe pol' a meen) is a derivative of natural alkaloid found in plants of the nightshade family (henbane, jimson weed). Scopolamine has potent anticholinergic activity and broadly and nonspecifically inhibits muscarinic transmission. It has been used for decades as an antiemetic, antisecretory and antispasm... | Despite widespread use over many decades, neither scopolamine nor methscopolamine have been linked to episodes of liver enzyme elevations or clinically apparent liver injury. Scopolamine is metabolized by the liver, but is usually given in low doses (<1 mg) for short periods only.\n\nReferences on the safety and potent... | null | null | Methscopolamine – Generic, Pamine® | Gastrointestinal Agents | [
{
"cas_registry_number": "13265-10-6",
"molecular_formula": "C18-H24-N-O4",
"name": "Methscopolamine"
},
{
"cas_registry_number": "51-34-3",
"molecular_formula": "C17-H21-N-O4",
"name": "Scopolamine"
}
] |
Glasdegib.nxml | Glasdegib | 2019-01-20 | Glasdegib is an orally available small molecule inhibitor of the signaling molecule hedgehog which is used as an antineoplastic agent in the treatment of acute myeloid leukemia. Glasdegib is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected to cause rare instances of c... | Glasdegib (glas deg' ib) is a potent small molecule inhibitor of hedgehog, a signaling molecule that is frequently overexpressed in cancer cells including leukemia stem cells in patients with acute myeloid leukemia (AML). The hedgehog intracellular signaling cascade promotes cell growth and proliferation. Mutations in ... | Elevations in serum ALT levels are common during glasdegib therapy, occurring in 31% of patients and rising above 5 times the upper limit of the normal range in 11%. Glasdegib has had limited clinical use but has not been linked to instances of acute liver injury with symptoms or jaundice. Because of the limited clinic... | The possible cause of the liver injury due to glasdegib is not known. Glasdegib is metabolized in the liver largely by the cytochrome P450 system (largely CYP 3A4) and is susceptible to drug-drug interactions with inhibitors or inducers of the microsomal enzyme system. | Glasdegib therapy has been associated with transient serum aminotransferase elevations during therapy, but has not been linked to instances of acute liver injury with jaundice or symptoms. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to temporary discontinuation, ... | Glasdegib – Daurismo® | Antineoplastic Agents | null |
Boceprevir.nxml | Boceprevir | 2022-01-26 | Boceprevir is an oral, direct acting hepatitis C virus (HCV) protease inhibitor that was used in combination with peginterferon and ribavirin in the treatment of chronic hepatitis C, genotype 1. Initially approved for use in 2012, it was withdrawn in 2015 because of the availability of more effective and better tolerat... | The hepatitis C virus is a small RNA virus that is a major cause of chronic hepatitis, cirrhosis and hepatocellular carcinoma in the United States as well as worldwide. Various approaches to antiviral therapy of chronic hepatitis C have been developed, starting in the 1980s with interferon alfa which was replaced in th... | In large randomized controlled trials, triple therapy with boceprevir, peginterferon and ribavirin was associated with a high rate of adverse events that often required dose adjustments and led to early discontinuation in 5% to 20% of patients. However, serum ALT elevations and clinically apparent liver injury were not... | The mechanism by which boceprevir might cause liver injury is not known. It is metabolized in the liver largely via the cytochrome P450 system, predominantly CYP 3A4. It is also a substrate of P-glycoprotein (P-gp). It is susceptible to drug-drug interactions, but largely for those agents that have major effects or are... | Triple therapy using boceprevir is no longer used, but it was considered inadvisable in patients with preexisting cirrhosis, particularly those with a prior history of hepatic decompensation. A similar high rate of decompensation of preexisting cirrhosis was reported with triple therapy using telaprevir and simeprevir,... | Boceprevir – Victrelis® | Hepatitis C Agents | null |
Carisoprodol.nxml | Carisoprodol | 2017-01-30 | Carisoprodol is a centrally acting muscle relaxant that has been in use for more than fifty years without significant evidence for causing hepatic injury. | Carisoprodol (kar eye" soe proe' dol) is a carbamate derivative similar to meprobamate. Its mechanism of action as a muscle relaxant is unknown, but it is a sedative and may act centrally by modifying perception of pain without affecting pain reflexes. Carisoprodol is recommended for treatment of acute, painful disorde... | There have been no adequate prospective studies demonstrating the rates of aminotransferase elevations on carisoprodol therapy or convincing case reports of clinically apparent liver injury due to carisoprodol. Thus, the hepatotoxic potential of this medication is low. It has been increasingly reported as a substance o... | null | null | Carisoprodol – Generic, Soma® | Autonomic Agents: Muscle Relaxants, Central | null |
Pralatrexate.nxml | Pralatrexate | 2016-05-01 | Pralatrexate is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of peripheral T cell lymphomas. Pralatrexate has been associated with a modest rate of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liv... | Pralatrexate (pral" a trex' ate) is a folate analogue which acts as an antagonist to the enzymes involved in folate dependent synthetic pathways such as thymidine synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. Inhibition of these enzymes leads to decrease in intracellular concentrat... | Pralatrexate is associated with serum enzyme elevations during therapy, but these abnormalities are generally mild and self-limited, rising to above 5 times ULN in 2% to 6% of patients and rarely requiring dose adjustment. No instances of clinically apparent acute liver injury attributed to pralatrexate have been repor... | The cause of the serum enzyme elevations that may occur during pralatrexate use is probably direct hepatotoxicity from the folate antagonism. Its hepatic metabolism by the microsomal P450 system is minimal and much of the administered drug is excreted unchanged in the urine. | Liver injury is rare after pralatrexate therapy. Confirmed serum enzyme elevations above 5 times ULN should lead to temporary discontinuation of pralatrexate therapy or adjustment of dose, but should also lead to careful search for other possible causes of liver injury. There have been no instances of acute liver failu... | Pralatrexate – Folotyn® | Antineoplastic Agents | null |
Efalizumab.nxml | Efalizumab | 2018-02-10 | Efalizumab is a humanized monoclonal antibody to human CD11a subunit of the lymphocyte function-associated antigen 1, which acts as an immunosuppressant agent blocking lymphocyte activation and was formerly used to treat severe plaque psoriasis. Efalizumab has been linked to rare instances of idiosyncratic acute liver ... | Efalizumab (ef” al iz’ ue mab) is a recombinant, humanized monoclonal antibody to CD11a, a subunit of the lymphocyte function-associated antigen 1 (LFA-1), which is present on lymphocytes and causes activation and proliferation of lymphocytes. Blocking of CD11a inhibits lymphocyte activation and decreases migration of ... | In large clinical trials of efalizumab, serum alkaline phosphatase levels were often reported to be mildly elevated (by 2-3 U/L) compared to baseline, but serum aminotransferase values did not change and there were no reports of marked ALT elevations or clinically apparent liver injury due to the monoclonal antibody th... | The mechanism of liver injury caused by efalizumab is probably immunologically mediated, perhaps as a result of its effects on leukocyte function in causing an autoimmune reaction or reactivation of hepatitis B. Efalizumab is a monoclonal antibody and, like other proteins, is metabolized into amino acids and is unlikel... | The hepatotoxicity of efalizumab is not well established, but in some instances resembles autoimmune hepatitis and warrants corticosteroid therapy. Other cases of liver injury during efalizumab therapy may represent reactivation of hepatitis B and call for antiviral therapy with drugs active against HBV.\n\nOther immun... | Efalizumab – Raptiva® | Immunomodulatory Agents | null |
Gentamicin.nxml | Gentamicin | 2019-04-12 | Gentamicin is a parenterally administered, broad spectrum aminoglycoside antibiotic typically used for moderate to severe gram negative infections. Despite its wide use, gentamicin has not been definitively linked to instances of clinically apparent liver injury. | Gentamicin (jen" ta mye' sin) is a aminoglycoside with broad bacteriocidal activity against many aerobic gram negative and some aerobic gram positive organisms. Gentamicin is the most commonly used aminoglycoside antibiotic and is indicated for moderate-to-severe bacterial infections caused by sensitive agents, primari... | Intravenous and intramuscular therapy with gentamicin has been linked to mild and asymptomatic elevations in serum alkaline phosphatase levels, but rarely affects aminotransferase levels or bilirubin, and changes resolve rapidly once gentamicin is stopped. Only isolated case reports of acute liver injury with jaundice ... | The cause of symptomatic, icteric hepatic injury from gentamicin is not known, but likely to be immunoallergic. Uptake of aminoglycosides into hepatocytes is limited and they are rapidly excreted in the urine; high concentrations are found in mainly in renal tubular cells and hair cells of inner ear perhaps explaining ... | The outcome of hepatic injury due to aminoglycosides is usually benign. Acute liver failure has not been associated with gentamicin use and no convincing cases of chronic bile duct vanishing syndrome have been described after its use. Patients with clinical apparent reactions to gentamicin should probably avoid all sys... | Gentamicin – Generic | Aminoglycosides | null |
Tolvaptan.nxml | Tolvaptan | 2020-09-02 | Tolvaptan is a vasopressin 2 receptor antagonist which is used for short term treatment of severe hyponatremia in patients with heart failure, cirrhosis or syndrome of inappropriate secretion of antidiuretic hormone (SIADH). It has been used experimentally to prevention progression of disease in autosomal dominant poly... | Tolvaptan (tol vap' tan) is a vasopressin 2 receptor antagonist (vaptan) that is used for treatment of hyponatremia caused by elevated levels of arginine vasopressin (also known as antidiuretic hormone: ADH), commonly found in patients with inappropriate ADH syndrome (SIADH) or with fluid overload from heart failure or... | In prelicensure clinical trials, tolvaptan was not implicated in causing serum enzyme elevations or clinically apparent liver injury. However, instances of worsening of hepatic failure and complications of portal hypertension were reported in a small proportion of patients with cirrhosis treated with tolvaptan. These c... | Tolvaptan is metabolized by the microsomal P450 drug metabolizing enzyme CYP 3A4 liver injury from tolvaptan may be due to activation of a toxic intermediate. Inhibitors of CYP 3A4 (such as ketoconazole) can raise levels of tolvaptan and should be avoided. | The hepatic injury caused by tolvaptan is usually reversible with stopping the medication. Tolvaptan has not been linked to cases of acute liver failure, chronic hepatitis, prolonged cholestasis or vanishing bile duct syndrome. Rechallenge usually causes recurrence and should be avoided. There is no information on poss... | Tolvaptan – Jynarque®, Samsca® | Diuretics, Vasopressin Antagonists | null |
Naltrexone.nxml | Naltrexone | 2020-03-24 | Naltrexone is a synthetic opioid antagonist used in prevention of relapse of opiate addiction and alcoholism. Naltrexone has been associated with low rates of serum enzyme elevations during therapy and with rare instances of clinically apparent liver injury. | Naltrexone (nal trex' one) is orally available opioid antagonist which blocks the euphoric effects of administered opiates. Naltrexone is a relatively pure antagonist and has no analgesic activity. Naltrexone has been shown to aid in maintenance of an opioid-free state in detoxified patients and to help in other addict... | Naltrexone therapy is typically given to patients with a high background rate of liver disease (injection drug use or alcoholism) and has been associated with variable rates of serum enzyme elevations (0% to 50%), values above 3 times the upper limit of normal occurring in approximately 1% of patients and occasionally ... | Naltrexone is a relatively pure opioid antagonist and is rapidly metabolized by the liver to inactive forms. The cause of hepatic injury is not known, but may be partially dose dependent direct toxicity.\n\nAgents in clinical use in therapy of alcohol abuse and dependence include acamprosate, disulfiram, methadone, and... | null | Naltrexone – Generic, Revia®, Vivitrol® | Substance Abuse Treatment Agents; Opioid Antagonists | null |
Metoprolol.nxml | Metoprolol | 2017-01-15 | Metoprolol is a cardioselective beta-blocker that is widely used in the treatment of hypertension and angina pectoris. Metoprolol has been linked to rare cases of drug induced liver injury. | Metoprolol (met" oh proe' lol) is considered a “selective” beta-adrenergic receptor blocker in that it has potent activity against beta-1 adrenergic receptors which are found in cardiac muscle, but has little or no activity against beta-2 adrenergic receptors found on bronchial and vascular smooth muscle. Metoprolol wa... | Metoprolol therapy has been associated with a low rate of mild-to-moderate elevations of serum aminotransferase levels which are usually asymptomatic and transient and resolve even with continuation of therapy. A few instances of clinically apparent, acute liver injury attributable to metoprolol have been reported. In ... | The mechanism of drug induced liver injury from metoprolol is not known. The agent is metabolized in the liver via the cytochrome P450 (largely CYP 2D6). The rare instances of liver injury due to beta-blockers are likely to be idiosyncratic. | The severity of liver injury due to metoprolol ranges from mild serum aminotransferase elevations to mild acute hepatitis with jaundice. In large case series of acute liver failure due to medications, metoprolol has not been listed as a cause. Rechallenge has been reported to result in recurrence of injury and should b... | Metoprolol – Generic, Lopressor®, Toprol® | Beta-Adrenergic Receptor Antagonists | null |
HAEAgents.nxml | Hereditary Angioedema Agents | 2024-06-20 | Multiple parenterally administered agents are available as prophylaxis or treatment of acute attacks of hereditary angioedema (HAE), including plasma derived and recombinant preparations of the C1-esterase Inhibitor as well as small protein and monoclonal antibody inhibitors of kallikrein and bradykinin activity. While... | Hereditary angioedema (HAE) is an autosomal dominant condition caused by mutations in the gene that encodes C1-esterase inhibitor and is marked clinically by intermittent episodes of moderate-to-severe swelling and pain affecting the gastrointestinal tract, genitourinary tract, skin, hands, feet, face, or larynx. The a... | Cinryze is the proprietary name for a human plasma derived preparation of C1-esterase inhibitor that was approved for prevention of acute attacks of HAE in 2008 and remains available as a lyophilized powder for reconstitution in single use vials of 500 IU. The recommended dose for adults and adolescents is 1000 IU intr... | null | The product labels for the various parenteral therapies of acute attacks of HAE do not recommend monitoring of routine liver tests during therapy, but testing HAE patients before starting long term prophylaxis therapy is appropriate because of the frequency of comorbidities including liver disease in patients with HAE.... | Human Plasma Derived C1-Esterase Inhibitor – Cinryze® | Genetic Disorder Agents | [
{
"cas_registry_number": "80295-38-1",
"molecular_formula": "Protein",
"name": "C1-Esterase Inhibitor"
},
{
"cas_registry_number": "460738-38-9",
"molecular_formula": "C305-H442-N88-O91-S8",
"name": "Ecallantide"
},
{
"cas_registry_number": "138614-30-9",
"molecular_formula":... |
Pindolol.nxml | Pindolol | 2017-01-15 | Pindolol is a nonselective beta adrenergic receptor blocker that is widely used for the therapy of hypertension and angina pectoris. Pindolol has yet to be convincingly associated with clinically apparent liver injury. | Pindolol (pin' doe lol) is a nonselective beta blocker, acting on both beta-1 and beta-2 adrenergic receptors. Beta-1 adrenergic blockade reduces the heart rate and myocardial contractility by slowing the AV conduction and suppressing automaticity. Beta-2 blockade affects peripheral vascular resistance and can cause br... | Mild-to-moderate elevations in serum aminotransferase levels occur in less than 2% of patients on pindolol and are usually transient and asymptomatic, resolving even with continuation of therapy. Despite its wide spread use, pindolol has not been convincingly linked to instances of clinically apparent liver injury. Oth... | Pindolol undergoes metabolism by the liver and is excreted in the urine both unchanged and as inactive metabolites. The reason why pindolol rarely causes liver injury is unknown; other beta-blockers with similar chemical structures have been linked to cases of clinically apparent, idiosyncratic liver injury.\n\nReferen... | null | Pindolol – Generic, Visken® | Beta-Adrenergic Receptor Antagonists | null |
Eprosartan.nxml | Eprosartan | 2017-01-13 | Eprosartan is an angiotensin II receptor blocker used in the therapy of hypertension. Eprosartan is associated with a low rate of transient serum aminotransferase elevations but has yet to be linked to instances of acute liver injury. | Eprosartan (ep" roe sar' tan) is an angiotensin II receptor blocker (ARB) used alone or in combination with other agents for therapy of hypertension. Eprosartan inhibits the renin-angiotensin system by blocking the angiotensin II type 1 receptor (AT1), which prevents the vasoconstriction and volume expansion induced by... | Eprosartan has been associated with a low rate of serum aminotransferase elevations (<2%) that in controlled trials was no higher than with placebo therapy. These elevations were transient and rarely required dose modification. No specific instances of clinically apparent acute liver injury have been reported in associ... | The cause of the minor serum aminotransferase elevations with eprosartan is not known. Eprosartan is metabolized in the liver to a glucuronide which is excreted in the urine. Eprosartan does not appear to be metabolized by the cytochrome P450 system and has minimal drug-drug interactions. | The instances of acute liver injury reported with ARB use have been self limited and have not resulted in acute liver failure or chronic liver injury. While corticosteroids have been used in cases of severe cholestasis due to ARBs, their efficacy has not been shown and their use is best avoided. Patients with eprosarta... | Eprosartan – Teveten® | Angiotensin II Receptor Antagonists | null |
Benznidazole.nxml | Benznidazole | 2023-07-20 | Benznidazole is an orally available, broad spectrum antimicrobial agent used in the treatment of Chagas disease (American trypanosomiasis). Benznidazole is a nitroimidazole similar to metronidazole and is associated with serum enzyme elevations during therapy in up to 10% of patients but has not linked to cases of clin... | Benznidazole (benz nid' a zole) is an oral, broad spectrum nitroimidazole antimicrobial that has activity against bacteria as well as several parasites. Like other nitroimidazoles such as metronidazole, benznidazole is activated intracellularly by bacterial or parasitic enzymes to a radical anion, which damages large p... | Benznidazole therapy is associated with an appreciable rate of serum enzyme elevations, found in at least 10% of patients. The abnormalities, however, are generally mild, transient and without accompanying symptoms or jaundice. In clinical trials there were no reported instances of clinically apparent liver injury with... | The cause of the serum enzyme elevations during benznidazole therapy is unknown. Benznidazole is metabolized in the liver where it undergoes glucuronidation but has not been found to lead to significant drug-drug interactions. | The severity of the liver injury linked to benznidazole therapy has been mild and self-limited, usually with transient, asymptomatic serum enzyme elevations, occasionally accompanied by hypersensitivity reactions or jaundice. However, the use of benznidazole has been limited. In instances of allergic reactions or anaph... | Benznidazole – Generic | Antiinfective Agents | null |
LevodopaCarbodopa.nxml | Levodopa | 2021-10-25 | Levodopa (L-Dopa) is an amino acid precursor of dopamine and is the most effective and commonly used drug in the treatment of Parkinson disease. Levodopa is usually combined with carbidopa, which is an inhibitor of L-amino acid decarboxylase, the plasma enzyme that metabolizes levodopa peripherally. Treatment with the ... | Levodopa (lee" voe doe' pa) is a derivative of phenylalanine and is a metabolic precursor of dopamine. Levodopa crosses the blood brain barrier where it is converted to dopamine by decarboxylation in the presynaptic terminals of dopaminergic neurons. After release, it is transported back into the dopaminergic terminals... | The combination of levodopa and carbidopa has been reported to cause serum aminotransferase elevations in up to 9% of patients, but these abnormalities are usually mild, asymptomatic and self-limiting. In rare instances, the aminotransferase elevations rise above 5 to 10 times the ULN and require discontinuation or dos... | The metabolism of levodopa and carbodopa is largely through peripheral or intracellular amino acid decarboxylases, and by catechol-O-methyltransferase and monoamine oxidase in the brain. They have minimal hepatic metabolism which perhaps accounts for its lack of hepatotoxicity.\n\nDrug Class: Parkinson Disease Agents | null | Levodopa – L-Dopa® | Parkinson Disease Agents | [
{
"cas_registry_number": "59-92-7",
"molecular_formula": "C9-H11-N-O4",
"name": "Levodopa"
},
{
"cas_registry_number": "38821-49-7",
"molecular_formula": "C10-H14-N2-O4.H2-O",
"name": "Carbidopa"
}
] |
Carfilzomib.nxml | Carfilzomib | 2017-01-17 | Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma. Carfilzomib is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which ... | Carfilzomib (kar filz’ oh mib) is an orally available, small molecule inhibitor of the 26S proteasome, the intracellular complex that degrades proteins involved in cell signaling and cell cycle regulation. Blocking proteasome activity prevents activation of factors involved in cell growth and resistance to chemotherapy... | In large clinical trials of carfilzomib, elevations in serum aminotransferase levels were common, occurring in 8% to 13% of patients. However, values greater than 5 times the upper limit of normal (ULN) were uncommon, occurring in 1% to 2% of recipients. In several studies there were reports of clinically apparent live... | The mechanisms of liver injury accounting for serum enzyme elevations and hepatic toxicity during carfilzomib therapy are not known. Carfilzomib is metabolized peripherally by plasma peptidases and only a proportion is metabolized in the liver through the CYP 3A4 pathway. Carfilzomib has minimal effect on CYP 3A4 activ... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. Clinically apparent liver injury should prompt immediate interruption of carfilzomib therapy. There is little information on cross reactivity in risk for hepatic injury between ... | Carfilzomib – Kyprolis® | Antineoplastic Agents | null |
AlphaGlucosidaseInhi.nxml | Alpha Glucosidase Inhibitors | 2021-01-12 | null | null | null | null | null | null | null | null |
Spironolactone.nxml | Spironolactone | 2021-10-14 | Spironolactone is an aldosterone receptor antagonist and potassium-sparing diuretic widely used in the therapy of edema, particularly in patients with cirrhosis in which hyperaldosteronism appears to play a major role. Spironolactone has been linked to rare cases of clinically apparent drug induced liver disease. | Spironolactone (spir on oh lak' tone) is a competitive inhibitor of the mineralocorticoid receptor in the late distal tubule and collecting duct of the kidneys, which causes a decrease in sodium reabsorption and potassium excretion in the distal tubule. As a result, spironolactone promotes a sodium diuresis, but mainta... | Clinically apparent liver injury from spironolactone is rare and only a few instances have been reported as isolated case reports. The liver injury typically arises after 4 to 8 weeks of therapy and the pattern of serum enzyme elevations is usually hepatocellular or mixed. Immunoallergic features (rash, fever, eosinoph... | The mechanism of spironolactone hepatic injury is unknown, but is most likely due to a metabolic idiosyncrasy. | Reported cases of liver injury due to spironolactone have been mild with either no or minimal jaundice, and recovery within a few months of stopping the medication. Recurrence on rechallenge has been reported, but there is no information or cross reactivity to the hepatic injury with other diuretics. Because eplerenone... | Spironolactone – Generic, Aldactone® | Diuretics | null |
Satralizumab.nxml | Satralizumab | 2024-05-14 | Satralizumab is a cytolytic monoclonal antibody to the interleukin 6 receptor that is used to treat adolescents and adults with neuromyelitis optica spectrum disorder accompanied by an autoantibody to aquaporin-4. Satralizumab therapy has been associated with serum aminotransferase elevations during therapy but has not... | Satralizumab (sa’ tra liz’ ue mab) is a humanized, cytolytic monoclonal antibody to the interleukin 6 receptor (IL-6r) that is used to treat adolescents and adults with neuromyelitis optica spectrum disorder (NMOSD), a rare and severe neurologic disease marked by bilateral optic neuritis and transverse myelitis and acc... | In registration, controlled trials, serum ALT elevations occurred in 20% to 37% of satralizumab vs 13% to 15% of placebo recipients but were rarely above 3 times the upper limit of normal (ULN). In these trials, satralizumab was discontinued in only two patients due to elevated liver enzymes, and one case was confounde... | The causes of the mild liver test abnormalities during satralizumab therapy are not clearly known but appear to be related to the underlying condition or comorbidities. Satralizumab can cause hypersensitivity reactions including urticaria and rash, and liver injury might be a part of the immunoallergic reaction. Cases ... | The product label for satralizumab recommends monitoring of routine liver tests during therapy every 4 weeks for 3 months, followed by every 3 months for one year and thereafter as clinically indicated. Despite this, marked elevations of serum ALT levels during therapy are rare, and long term studies have reported no i... | Satralizumab – Enspryng® | Immunomodulatory Agents | null |
Sotalol.nxml | Sotalol | 2017-01-15 | Sotalol is a nonselective beta-adrenergic blocker used largely in the therapy cardiac arrhythmias. Sotalol has been linked to at least one instance of clinically apparent liver injury. | Sotalol (soe' ta lol) is a nonselective beta-blocker, acting on both beta-1 and beta-2 adrenergic receptors. Beta-1 adrenergic blockade reduces the heart rate and myocardial contractility by slowing the AV conduction and suppressing automaticity. Beta-2 blockade affects peripheral vascular resistance and can also cause... | Mild-to-moderate elevations in serum aminotransferase levels occur in less than 2% of patients on sotalol and are usually transient and asymptomatic, resolving even with continuation of therapy. Sotalol has been linked to a single case of clinically apparent liver injury, with onset of an acute hepatitis-like syndrome ... | Sotalol undergoes minimal metabolism by the liver and is excreted largely unchanged in the urine. The reason why sotalol might cause liver injury is unknown. The acute liver injury attributed to other beta-blockers is likely to be idiosyncratic.\n\nReferences to the safety and potential hepatotoxicity of sotalol are pr... | null | Sotalol – Generic, Betapace® | Beta-Adrenergic Receptor Antagonists | null |
Oxazepam.nxml | Oxazepam | 2023-06-22 | Oxazepam is an orally available benzodiazepine used in the therapy of anxiety and acute alcohol withdrawal syndromes. As with most benzodiazepines, oxazepam has not been associated with serum aminotransferase or alkaline phosphatase elevations during therapy, and clinically apparent liver injury from oxazepam has not b... | Oxazepam (ox az' e pam) is a benzodiazepine that is used largely in the therapy of anxiety and alcohol withdrawal states. The antianxiety (anxiolytic) activity of the benzodiazepines is mediated by their ability to enhance gamma-aminobutyric acid (GABA) mediated inhibition of synaptic transmission through binding to th... | Oxazepam, like other benzodiazepines, is rarely associated with serum ALT or alkaline phosphatase elevations, and clinically apparent liver injury from oxazepam is extremely rare, if it occurs at all. Despite its availability for more than 50 years, there have been no case reports of symptomatic, acute liver injury fro... | Oxazepam is metabolized by the liver to inactive metabolites which are excreted in the urine. Liver injury from benzodiazepines is probably due to the toxic effects of a rarely produced intermediate metabolite. | The case reports of hepatic injury due to benzodiazepines were followed by prompt and complete recovery upon stopping the medication, without evidence of residual or chronic injury. No cases of acute liver failure or chronic liver injury due to oxazepam have been described. There is no information about cross reactivit... | Oxazepam – Generic, Serax® (Trade name discontinued) | Benzodiazepines | null |
Sorafenib.nxml | Sorafenib | 2018-06-22 | Sorafenib is an oral multi-kinase inhibitor that is used in the therapy of advanced renal cell, liver and thyroid cancer. Sorafenib has been associated with a low rate of transient elevations in serum aminotransferase levels during therapy that are generally mild and asymptomatic. Sorafenib has also been linked to rare... | Sorafenib (soe raf’ e nib) is an orally available, small molecule, multi-specific tyrosine kinase inhibitor with activity against vascular endothelial growth factors (VEGF) receptors -1, -2 and -3 as well as against the receptor for platelet derived growth factor (PDGF) and several Raf kinases. Inhibition of these kina... | In large clinical trials of sorafenib, elevations in serum aminotransferase levels were common, occurring in up to half of patients, but values greater than 5 times the upper limit of normal (ULN) occurred in only 1% to 3% of treated subjects. In addition, there have been several single case reports of clinically appar... | The mechanism of injury accounting for serum enzyme elevations during sorafenib therapy is not known. Sorafenib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury may be related to production of a toxic intermediate. Sorafenib is susceptible to drug-drug interactions with agents that inhib... | Monitoring of routine liver tests is recommended during sorafenib therapy. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) or any elevations accompanied by jaundice or symptoms should lead to dose reduction or temporary cessation. Sorafenib has been implicated in cases of acute ... | Sorafenib – Nexavar® | Antineoplastic Agents | null |
Edaravone.nxml | Edaravone | 2019-04-09 | Edaravone is a free radical scavenger and neuroprotective agent used for therapy of amyotrophic lateral sclerosis. Edaravone is associated with a low rate of serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent, acute liver injury. | Edaravone (e dar' a vone) is a free radical scavenger that has been used as a neuroprotective agent in patients with ischemic stroke and amyotrophic lateral sclerosis. The mechanism by which it protects neurons from toxic injury is unknown, but it appears to eliminate lipid peroxide and hydroxyl radicals by electron tr... | Serum aminotransferase elevations occur in a small proportion of patients on edaravone therapy, but the frequency, timing of onset, duration and severity of these elevations has not been defined. The rates of abnormal liver tests during edaravone therapy were said to be similar to those during placebo treatment. Most e... | The mechanism by which edaravone might cause hepatotoxicity is unclear. Edaravone is extensively metabolized by the liver to sulfate and glucuronide conjugates that also demonstrate no toxicity in animal models. Edaravone has not been found to have significant drug-drug interactions. | The liver injury arising during edaravone therapy has consisted of minor and transient elevations in serum aminotransferase levels in a small proportion of patients. Routine monitoring of serum aminotransferase levels is not recommended. However, if aminotransferase elevations greater than 5 times ULN are detected duri... | Edaravone – Radicava® | Amyotrophic Lateral Sclerosis Agents | null |
Turmeric.nxml | Turmeric | 2024-06-01 | Turmeric is a popular herb derived from the roots of the plant Curcuma longa found mostly in India and Southern Asia. Turmeric has an intense yellow color and distinct taste and is used as a dye as well as a spice in the preparation of curry. Turmeric and its purified extract curcumin are also used medically for their ... | Turmeric (tur mer' ik) is a widely used herbal product derived from the roots of Curcuma longa, a perennial plant belonging to the ginger family (Zingiberaceae) that is native to India but grown throughout Southern Asia and in central America. Extracts of the rhizomes of turmeric contain volatile oils and curcuminoids ... | Both turmeric and curcumin were considered to be generally safe and for many years had not been linked to instances of liver injury in any consistent way. Studies of its use in various diseases showed low rates of transient and asymptomatic serum enzyme elevations during therapy, but without instances of clinically app... | The acute hepatotoxicity caused by turmeric appears to be due to an idiosyncratic injury, perhaps immunologically mediated. The association with HLA-B*35:01 suggests that the injury is linked to the immune system and perhaps interaction with curcumin or another component of turmeric with the HLA molecule leading to T c... | Most cases of acute hepatic injury from turmeric resolve within 1 to 3 months of stopping the medication. In some instances, however, the injury is severe and unremitting, leading to acute liver failure and either death or need for liver transplantation. A severe outcome is more likely if turmeric is continued after th... | Turmeric – Generic | Herbal and Dietary Supplements | null |
Afamelanotide.nxml | Afamelanotide | 2024-03-05 | Afamelanotide is a melanocortin-1 receptor agonist that stimulates melanin production in the skin and is used to decrease pain and itching from light exposure in patients with erythropoietic protoporphyria and X-linked protoporphyria. Afamelanotide has not been linked to serum aminotransferase elevations during therapy... | Afamelanotide (a fa mel” ano tide’) is a melanocortin-1 receptor (MC1-R) agonist that stimulates melanin production in the skin and is used to decrease pain and itching from light exposure in patients with erythropoietic protoporphyria (EPP) or X-linked protoporphyria (XLPP). EPP and XLPP are rare genetic diseases of h... | Erythropoietic protoporphyria and X-linked protoporphyria are rare genetic diseases, and the pivotal trials of afamelanotide were conducted in a limited number of patients, so the full spectrum of hepatotoxicity may not be fully known. Furthermore, a proportion of untreated persons with EPP/XLPP have liver disease with... | The reasons why afamelanotide might cause liver injury are not clear. It is a small, modified polypeptide that mimics melanocyte stimulating hormone. After uptake, it is metabolized intracellularly by proteases to its component amino acids by many cells. Allergic reactions and antibodies to afamelanotide are uncommon a... | Afamelanotide has not been linked to liver injury, and monitoring of liver enzymes is not recommended during treatment. However, persons with EPP/XLPP are at an increased risk for developing liver disease and gallstones due to accumulation of toxic protoporphyrin for which reason screening for liver disease and ongoing... | Afamelanotide – Scenesse® | Genetic Disorder Agents | null |
Primaquine.nxml | Primaquine | 2017-02-02 | Primaquine is an aminoquinoline that has been used for the prevention and therapy of malaria for more than 50 years. Primaquine is not associated with serum enzyme elevations during therapy and has yet to be linked to instances of clinically apparent acute liver injury. | Primaquine (prim' a kwin) is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis; it is active against several of the stages in the development of the plasmodia including liver schizonts, hypnozoites and gametocytes and... | Despite use for more than 50 years, primaquine has not been linked to significant serum aminotransferase elevations or to clinically apparent acute liver injury. Primaquine can cause hemolysis in patients with G6PD deficiency, which can result in mild jaundice.\n\nLikelihood score: E (unlikely cause of clinically appar... | Hepatic reactions to quinine are usually due to hypersensitivity reactions, but have been rarely reported with primaquine. Primaquine undergoes metabolism by the liver to its active metabolite that is excreted unchanged in the urine. | There does not seem to be cross reactivity to hepatic injury among the various antimalarial agents and switching to other drug can be done.\n\nDrug Class: Antimalarial Agents | Primaquine – Generic | Antimalarial Agents | null |
Eluxadoline.nxml | Eluxadoline | 2017-04-20 | Eluxadoline is a mixed opioid receptor agonist (mu) and antagonist (delta) that is used to treat diarrhea-predominant irritable bowel disease. Eluxadoline is associated with a low rate of serum aminotransferase elevations that appear to be due to isolated instances of sphincter of Oddi spasm and/or pancreatitis that oc... | Eluxadoline (el" ux ad' oh leen) is mixed opioid receptor agonist and antagonist, having agonist activity for the mu (µ) receptor and antagonist activity for the delta (δ) receptor. This combination of activities leads to its activity in reducing bowel transit and decreasing pain without the side effects that occur wit... | In preregistration clinical trials, serum aminotransferase elevations were uncommon during eluxadoline therapy and in pooled analyses ALT elevations above 3 times the upper limit of normal occurred in 2% to 3% of eluxadoline- vs 1% of placebo-treated subjects. More detailed analysis found rare instances of marked ALT a... | Eluxadoline is minimally absorbed and unlikely to have direct hepatotoxic effects. Most instances of serum aminotransferase elevations attributed to eluxadoline therapy have been accompanied by evidence of acute pancreatitis or sphincter of Oddi spasm or both. | Eluxadoline has been shown to cause sphincter of Oddi spasm and pancreatitis and its use should be limited to patients with a gallbladder and without known preexisting pancreatitis, hepatobiliary disease or advanced cirrhosis. It should also be avoided in persons who drink alcohol to excess.\n\nDrug Classes: Gastrointe... | Eluxadoline – Viberzi® | Gastrointestinal Agents | null |
Eribulin.nxml | Eribulin | 2018-02-20 | Eribulin mesylate is an inhibitor of microtubule function and is used as an antineoplastic agent for refractory, metastatic breast cancer and liposarcoma. Despite its cytotoxic activity against cancer cells, eribulin has rarely been implicated in causing clinically apparent acute liver injury. | Eribulin (er' i bue' lin) is a synthetic macrocyclic analogue of halichondrin B, a naturally occurring inhibitor of mitotic division found in a species of marine sponges (Halichondria okadai). Eribulin binds to the growing ends of microtubules preventing cell division (mitotic arrest) which leads to tubulin sequestrati... | Eribulin is a cytotoxic chemotherapeutic agent and serum aminotransferase and alkaline phosphatase elevations are common during cyclic therapy of breast cancer and liposarcoma. The reported rates of ALT elevations have ranged from 8% to 83% with values above 5 times the upper limit or normal (ULN) in 2% to 5%. Isolated... | Eribulin causes mitotic arrest in rapidly dividing cells and likely causes similar changes in some hepatocytes, perhaps accounting for the frequent occurrence of mild serum aminotransferase elevations during therapy. Eribulin undergoes minimal hepatic metabolism and is mostly excreted unchanged. It also has little or n... | Serum enzyme elevations are frequent during cancer chemotherapy with eribulin, but are rarely dose limiting. Serum aminotransferase elevations above 5 times ULN should lead to dose interuption or modification. Serum ALT or AST elevations above ten times ULN or any elevations accompanied by symptoms of liver disease or ... | Eribulin – Halaven® | Antineoplastic Agents | null |
Rifabutin.nxml | Rifabutin | 2018-06-10 | Rifabutin is a rifamycin antibiotic that is similar in structure and activity to rifampin and rifapentine and which is used largely in the prevention of Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. Rifabutin is associated with transient and asymptomatic elevations in serum aminotra... | Rifabutin (rif" a bue' tin) is a rifamycin antibiotic and a synthetic derivative of natural products of the bacterium, Amycolatopsis mediterranei. The rifamycins are complex macrocyclic antibiotics that have activity against several bacteria, but most prominently M. tuberculosis and several atypical mycobacterial speci... | Because of its limited use, the effects of rifabutin on the liver have been less well defined than those of rifampin, but they are likely to be similar. Thus, studies on the prevention of MAC in HIV infected patients with rifabutin, minor, transient elevations in serum aminotransferase levels occurred in 3% to 8% of pa... | The mechanism of rifamycin associated hepatotoxicity is not known, but these agents are extensively metabolized by the liver and induce multiple hepatic enzymes. Thus, the cause of injury is likely to be due to idiosyncratic metabolic products that are either directly toxic or induce an immunologic reaction. | For the rifamycins, the severity of hepatic injury ranges from asymptomatic elevations in serum aminotransferase levels, jaundice without apparent hepatic injury, symptomatic self-limited hepatitis to severe fulminant liver failure and death. In most cases, complete recovery is expected after stopping the drug and is u... | Rifabutin – Mycobutin® | Antituberculosis Agents | null |
Bleomycin.nxml | Bleomycin | 2017-09-05 | Bleomycin is a cystotoxic antibiotic that is used as an anticancer agent in the therapy of testicular and germ cell cancers, Hodgkin disease, lymphomas and tumors of the head and neck. Therapy with bleomycin in combination with other agents is often associated with mild-to-moderate serum enzyme elevations, but is a rar... | The bleomycins are a group of glycopeptide antibiotics that were initially derived from Streptomyces verticillus and later found to have antitumor activity in vitro and in vivo. Bleomycin (blee” oh mye’ sin) is actually a mixture of water soluble glycopeptides that have similar chemical structures and metabolic activit... | Chemotherapy with bleomycin in combination with other agents is associated with serum enzyme elevations in 10% to 40% of patients and with levels above 5 times ULN in 1% to 7% of patients, depending upon the dose and other agents used. The ALT elevations are usually asymptomatic and transient, resolving within a month ... | The mechanism by which bleomycin might cause liver injury is not known. Bleomycin is generally cytotoxic, and the minor serum enzyme elevations that occur during therapy are likely due to a direct toxic effect on hepatocytes. Bleomycin is not concentrated in the liver and has minimal hepatic metabolism. | The hepatic injury caused by bleomycin is usually mild, asymptomatic and rapidly reversible. Chemotherapeutic regimens that include bleomycin have been implicated in causing reactivation of hepatitis B and sinusoidal obstruction syndrome, but bleomycin has not been specifically implicated in these forms of liver injury... | Bleomycin – Blenoxane® | Antineoplastic Agents | null |
Deferasirox.nxml | Deferasirox | 2017-12-26 | Deferasirox is an oral iron chelating agent used to treat chronic iron overload. Deferasirox has been linked to a low rate of transient serum aminotransferase elevations during therapy and to rare instances of clinically apparent liver injury, which can be severe and even fatal. | Deferasirox (dee fer’ a sir ox) is an orally available iron chelating agent that is selective for ferric iron and binds iron with a high affinity. Deferasirox binds two iron molecules and is eliminated in the feces after hepatic metabolism by glucuronidation. Deferasirox also binds zinc and copper, but to a far lower e... | In large clinical trials of deferasirox, elevations in serum aminotransferase levels above 5 times the upper limit of normal (ULN) occurred in 6% of patients and led to drug discontinuation in 1% to 2%. In addition, there have been several single case reports of clinically apparent liver injury arising during deferasir... | The mechanism of injury accounting for serum enzyme elevations during deferasirox therapy is not known. The injury may be due to direct, intrinsic toxicity and to have a more severe outcome in patients with pre-existing liver disease as a result of iron overload or concurrent hepatitis B or C. Deferasirox is metabolize... | Deferasirox is well known to cause transient serum aminotransferase elevations that are usually self-limited and benign. However, it has also been implicated in cases of clinically apparent liver injury and acute liver failure.. The product label recommends monitoring of serum aminotransferase levels and bilirubin befo... | Deferasirox – Exjade® | Hematological Agents | null |
Donanemab.nxml | Donanemab | 2024-10-04 | Donanemab is a humanized monoclonal antibody to aggregated amyloid β which has been approved for use in Alzheimer disease with mild cognitive impairment or mild dementia. Donanemab is associated with a minimal rate of serum aminotransferase elevations during therapy and has not been linked to instances of clinically ap... | Donanemab (doe nan’ e mab) is a humanized monoclonal IgG1 antibody directed against insoluble N-truncated pyroglutamate amyloid β which was developed as therapy for Alzheimer disease, based upon the theory that the dementia and neurological decline in Alzheimer disease is caused by accumulation of amyloid β oligomers a... | Serum aminotransferase elevations were infrequent in the controlled trials of donanemab in Alzheimer disease and no more frequent than with placebo treatment. The elevations were transient, asymptomatic, and mild-to-moderate in severity (1 to 3 times upper limit of normal). In the preregistration trials there were no i... | The possible mechanisms by which donanemab might cause liver injury are unclear. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids. There is no evidence to suggest that inhibition of amyloid β accumulation or increase in its clearance woul... | null | Donanemab – Kisunla® | Alzheimer Disease Agents | null |
Anastrozole.nxml | Anastrozole | 2017-07-25 | Anastrozole is a nonsteroidal inhibitor of aromatase which effectively blocks estrogen synthesis in postmenopausal women and is used as therapy of estrogen receptor positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent... | Anastrozole (an as' troe zole) is a nonsteroidal inhibitor of aromatase, the enzyme responsible for the conversion of testosterone to estrone (E1) and of androstenedione to estradiol (E2). Highest levels of aromatase are found in the ovary and placenta, which are the major sources of estrogen in premenopausal women. Ho... | Serum enzymes are reported to be elevated in 2% to 4% of women treated with anastrozole, but these elevations are usually mild, asymptomatic and self-limited, rarely requiring dose modification. There have been rare instances of clinically apparent liver injury associated with anastrozole therapy, typically arising wit... | The liver injury attributed to anastrozole use is probably due to a toxic or immunoallergic intermediate of its metabolism. Anastrozole is metabolized in the liver by the cytochrome P450 system and is a strong inhibitor of CYP 2A6 and to a lesser extent CYP 2C19. | Liver injury attributed to anastrozole is usually mild and self-limited, typically a transient, asymptomatic elevation in serum enzymes. Cases of severe hepatitis have been reported in women on anastrozole, but acute liver failure has not. There is little evidence for cross sensitivity to liver injury between anastrozo... | Anastrozole – Generic, Arimidex® | Antineoplastic Agents | null |
MonoclonalAntibodies.nxml | Monoclonal Antibodies | 2025-04-09 | null | null | null | null | null | null | null | null |
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