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Ifosfamide.nxml | Ifosfamide | 2018-04-15 | Ifosfamide is a parenterally administered alkylating agent similar to cyclophosphamide that is used in the treatment of several forms of cancer including lymphomas, sarcoma and advanced forms of solid organ cancer such as breast, testicular, ovarian, gastric and lung cancer. Ifosfamide therapy is associated with minor ... | Ifosfamide (eye fos' fa mide) is an analogue of cyclophosphamide and thus a nitrogen mustard-like alkylating agent that is used in the therapy of several forms of leukemia, lymphoma and solid organ cancer. Like cyclophosphamide, ifosfamide requires activation in the liver to form its active intermediaries which act by ... | The toxicity of ifosfamide seems to be similar to that of cyclophosphamide. Mild and transient elevations in serum aminotransferase levels are found in a high proportion of patients receiving ifosfamide. Because ifosfamide is typically given in combination with other antineoplastic agents, its role in causing the serum... | The cause of idiosyncratic hepatotoxicity from ifosfamide is not known. The sinusoidal obstruction syndrome induced by ifosfamide is probably related to the direct toxic effect of ifosfamide on sinusoidal cells in the liver, causing their necrosis and release into the sinusoids, obstruction and obliteration of hepatic ... | The severity of liver injury ranges from mild elevations in liver enzymes to massive, fatal hepatic necrosis due to sinusoidal obstruction syndrome. There is currently no specific therapy for veno-occlusive disease other than supportive management and avoidance of further damage. Rechallenge should be avoided.\n\nDrug ... | Ifosfamide – Generic, Ifex® | Antineoplastic Agents, Alkylating Agents | null |
Darifenacin.nxml | Darifenacin | 2023-07-12 | Darifenacin is an anticholinergic and antispasmotic agent used to treat urinary incontinence and overactive bladder syndrome. Darifenacin has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. | Darifenacin (dar" i fen' a sin) is an anticholinergic agent with a degree of selectivity for the M3 subtype of muscarinic acetylcholine receptors which are found predominantly in the smooth muscle of the bladder. Darifenacin increases bladder capacity and decreases bladder contractions and the urgency of urination. Dar... | Like most anticholinergic agents, darifenacin has not been linked to liver enzyme elevations during therapy or to instances of clinically apparent liver injury with symptoms or jaundice. In multiple prospective clinical trial of darifenacin in patients with overactive bladder syndrome, ALT elevations were reported in l... | Darifenacin has not been linked to liver injury. It is metabolized in the liver by microsomal P450 enzymes, predominantly CYP 3A4 and 2D6. Despite this, drug-drug interactions are uncommon. A major reason for its safety may relate to the low daily dose.\n\nDrug Class: Anticholinergic Agents | null | Darifenacin – Generic, Enablex® | Anticholinergic Agents | null |
Donepezil.nxml | Donepezil | 2020-01-15 | Donepezil is an oral acetylcholinesterase inhibitor used for therapy of Alzheimer disease. Donepezil is associated with a minimal rate of serum enzyme elevations during therapy and has only rarely been implicated as a cause of clinically apparent liver injury. | Donepezil (doe nep' e zil) is an acetylcholinesterase inhibitor which acts by inhibition of the metabolism of acetylcholine in the postsynaptic clefts, thus enhancing cholinergic neurotransmission. Alzheimer disease is associated with a cholinergic deficiency in the cerebral cortex, and the increase in concentration of... | In several large clinical trials, donepezil therapy was not associated with an increased rate of serum enzyme elevations compared to placebo treatment. Furthermore, escalation of the dose from 10 to 23 mg daily was not followed by an increased rate of ALT elevations compared to patients maintained on the lower dose. Ne... | Donepezil is extensively metabolized by the hepatic cytochrome P450 system (CYP 2D6 and 3A4) followed by glucuronidation. Hepatotoxicity is likely due to idiosyncratic metabolism to a toxic or immunogenic intermediate. Drug-drug interactions are not common, except with concurrent use of anticholinergic drugs. | Cases of hepatotoxicity from donepezil have been few and there have been no published reports of fatal acute liver failure, chronic hepatitis or vanishing bile duct syndrome attributed to donepezil. There is little information on the possible cross sensitivity to liver injury among the various acetylcholinesterase inhi... | Donepezil – Generic, Aricept® | Alzheimer Disease Agents | null |
Methenamine.nxml | Methenamine | 2021-01-22 | Methenamine is a urinary tract antiseptic that is used as suppressive therapy for chronic or recurrent urinary tract infections. Methenamine has not been linked to serum enzyme elevations or to instances of clinically apparent acute liver injury. | Methenamine (meth” en a mene’) also known as hexamethylenetetramine or urotropin is a heterocyclic molecule used as long term prophylaxis of recurrent urinary tract infections. Methenamine is rapidly absorbed and excreted in the urine where it decomposes at an acidic pH into formaldehyde and ammonia. Formaldehyde is di... | In prospective controlled trials, methenamine was generally well tolerated at conventional doses and no episodes of serum aminotransferase elevations or clinically apparent liver injury were reported. Since its approval and in over 100 years of general use, there have been no reports of clinically apparent liver injury... | The reason why methenamine rarely causes liver injury is probably due to its lack of hepatic metabolism and rapid unchanged urinary excretion.\n\nDrug Class: Antiinfective Agents, Urinary Tract Infection Agents\n\nOther Drugs in the Subclass: Fosfomycin, Nitrofurantoin, Sulfamethoxazole-Trimethoprim | null | Methenamine hippurate – Generic, Hiprex® | Antiinfective Agents | null |
CoQ10.nxml | Coenzyme Q10 | 2024-04-20 | Coenzyme Q10, also known as ubiquinone, is an enzyme cofactor found in virtually all cells of the body and participates in many essential energy-producing and antioxidant enzymatic actions. While normally synthesized in the body in adequate amounts, coenzyme Q10 is used as a nutritional supplement for conditions highly... | Coenzyme Q10, also known as ubiquinone, is an enzyme cofactor found in virtually all cells of the body where it participates in essential energy-producing and antioxidant actions. Coenzyme Q10 is a fat-soluble vitamin K-like molecule that is found in highest concentrations in the heart, liver, kidney, and brain. It is ... | Coenzyme Q10 is generally recognized as safe and has not been linked to elevations in serum aminotransferase, alkaline phosphatase, or bilirubin levels. Despite wide scale use for several decades, there have been no convincing reports of clinically apparent liver injury due to coenzyme Q10.\n\nLikelihood score: E (unli... | null | null | Coenzyme Q10 – Generic | Nutritional Supplements | null |
Dronedarone.nxml | Dronedarone | 2018-01-05 | Dronedarone is an antiarrhythmic and a synthetic derivative of amiodarone that is used for maintaining sinus rhythm for patients with atrial fibrillation or flutter. Dronedarone is associated with a variable rate of serum enzyme elevations during therapy and to rare instances of clinically apparent liver injury, which ... | Dronedarone (droe ne’ da rone) is a synthetic derivative of amiodarone, a benzofuran derivative that is a structural analogue of thyroid hormone. However, unlike amiodarone and thyroxine, dronedarone is not iodinated and was specifically designed to avoid some of the end-organ adverse effects associated with amiodarone... | Chronic therapy with dronedarone has been associated with mild serum enzyme elevations in up to 12% of patients, but similar rates were found in comparator arms and even in placebo recipients. The serum aminotransferase elevations that occur during chronic dronedarone therapy are generally mild-to-moderate in severity ... | The cause of dronedarone hepatotoxicity is not clear. The clinical presentation of injury is somewhat different than that described commonly associated with amiodarone which shares clinical features with alcoholic liver injury marked by insidious onset, minimal serum enzyme elevations, and liver histology showing steat... | The liver injury attributed to dronedarone can be severe and lead to liver failure and death. There are no known specific therapies for reversing dronedarone effects. There is also no information about cross sensitivity with hepatic injury from amiodarone, but other approaches to atrial arrhythmia control are probably ... | Dronedarone – Multaq® | Antiarrhythmic Agents | null |
Ciprofloxacin.nxml | Ciprofloxacin | 2024-05-09 | Ciprofloxacin is a second generation fluoroquinolone antibiotic that is widely used in the therapy of mild-to-moderate urinary and respiratory tract infections caused by susceptible organisms. Ciprofloxacin has been linked to rare but convincing instances of liver injury that can be severe and even fatal. | Ciprofloxacin (sip" roe flox' a sin) is an oral fluoroquinolone that is used to treat mild-to-moderate urinary and respiratory tract infections. Ciprofloxacin is also used for infectious diarrhea, typhoid fever, uncomplicated gonorrhea, treatment of Neisseria meningitides nasal carriage and prophylaxis against anthrax.... | Ciprofloxacin like other fluoroquinolones is associated with a low rate (1% to 3%) of serum enzyme elevations during therapy. These abnormalities are generally mild, asymptomatic and transient, resolving even with continuation of therapy. More importantly, ciprofloxacin has been linked to rare, but occasionally severe ... | The mechanism of ciprofloxacin hepatotoxicity is suspected to be hypersensitivity. Rechallenge leads to recurrence with a shorter time to onset and more severe course and should be avoided. | Severity ranges from mild and transient serum enzyme elevations to a self-limited hepatitis, to prolonged cholestatic hepatitis to a fulminant hepatic failure. If not fatal during the acute phase, complete recovery is expected after stopping the drug and is usually rapid (2 to 4 weeks) depending upon the severity and d... | Ciprofloxacin – Generic, Cipro®, Proquin® | Antiinfective Agents | null |
Flutamide.nxml | Flutamide | 2023-03-15 | Flutamide is a first generation, oral nonsteroidal antiandrogen that has been used widely in the therapy of prostate cancer. Flutamide is frequently associated with minor serum aminotransferase elevations and has been linked to numerous cases of acute liver injury, which are frequently severe and can be fatal. | Flutamide (floo' ta mide) is a synthetic, nonsteroidal antiandrogen that acts by competitive inhibition of the binding of testosterone and dihydrotestosterone to the intracellular androgen receptor, thus blocking the effects of endogenous androgen action. Flutamide acts by binding to and blocking intracellular androgen... | Chronic therapy with flutamide is associated with elevations in serum aminotransferase levels in up to 62% of patients, but marked elevations (above 5 times ULN) in only 3% to 5%. Most of these abnormalities are transient, asymptomatic and do not require dose adjustment or drug discontinuation. However, in 0.1% to 1% o... | The mechanism of injury due to flutamide is not clearly understood. Flutamide is extensively metabolized by the liver, and a common hypothesis is that flutamide is metabolized by the cytochrome P450 system (CYP 3A4) to a toxic intermediate. | The mortality rate of flutamide hepatotoxicity is considerable, particularly in cases with a hepatocellular pattern of injury and in elderly men. Generally, the injury begins to resolve within 1 to 2 weeks of stopping therapy. In severe cases, there can be progressive worsening with development of hypoalbuminemia, edem... | Flutamide – Generic, Eulexin® | Antineoplastic Agents | null |
Naproxen.nxml | Naproxen | 2020-03-20 | Naproxen is a popular over-the-counter nonsteroidal antiinflammatory drug (NSAID) that is widely used for therapy of mild-to-moderate pain and arthritis. Naproxen has been associated with rare cases of clinically apparent drug induced liver injury. | Naproxen (na prox' en) belongs to the propionic acid class of NSAIDs similar to fenoprofen, ibuprofen, ketoprofen and oxaprozin. The antiinflammatory and analgesic properties of NSAIDs such as naproxen are mediated by inhibition of tissue cyclo-oxygenases (Cox-1 and -2), which results in a decrease in pro-inflammatory ... | Serum aminotransferase levels can be elevated in as many as 4% of patients receiving prolonged courses of naproxen, particularly with high doses. Clinically apparent naproxen induced liver injury is very rare (~1-3 per 100,000 users), but convincing cases have been reported that resemble acute hepatitis and arise withi... | The mechanism of hepatotoxicity from naproxen is not known, but it is metabolized by the cytochrome P450 system and idiosyncratic injury may be due to a toxic metabolite. Cross sensitivity to hepatic injury with fenoprofen suggests that the propionic acid may be responsible for the injury. | Severity ranges from transient, asymptomatic elevations in serum aminotransferase levels, to hepatitis with jaundice, to fulminant liver failure leading to death or need for liver transplantation. In most cases, complete recovery is expected promptly after stopping the drug. Cross reactivity with other propionic acid d... | Naproxen – Generic, Aleve®, Anaprox®, Naprosyn® | Nonsteroidal Antiinflammatory Drugs | null |
Hyssop.nxml | Hyssop | 2018-03-30 | Hyssop is an herb prepared from the leaves and flowers of Hyssopus officinalis and is used for alleviation of symptoms of gastrointestinal and respiratory tract infections and the common cold. Hyssop is widely used and has not been implicated in causing liver injury. | Hyssop is an herb prepared from the aerial parts of the plant Hyssopus officinalis, which is a member of the mint family indigenous to Southern Europe and the Middle East. Hyssop has been used in folk medicine for centuries for stimulation of the circulation and for treatment of a variety of conditions including upper ... | Despite wide scale use, there is no evidence that Hyssop extracts cause liver injury and there have been no published reports of clinically apparent liver injury attributed to hyssop.\n\nLikelihood score: E (unlikely cause of clinically apparent liver injury).\n\nDrug Class: Herbal and Dietary Supplements | null | null | Hyssop – Generic | Herbal and Dietary Supplements | null |
Sirolimus.nxml | Sirolimus | 2020-02-17 | Sirolimus is macrocyclic antibiotic with potent immunosuppressive activity that is used alone or in combination with calcineurin inhibitors and corticosteroids to prevent cellular rejection after renal transplantation. Sirolimus therapy can be associated with mild serum enzyme elevations and it has been linked to rare ... | Sirolimus (sir oh' li mus) is a macrocyclic lactone antibiotic which also has profound immunosuppressive properties particularly affecting T cells and the cellular immune response. Sirolimus binds to the same intracellular receptor as tacrolimus and cyclosporine, but does not inhibit calcineurin, but rather blocks the ... | Serum enzyme elevations occur in a proportion of patients taking sirolimus, but the abnormalities are usually mild, asymptomatic and self-limiting, rarely requiring dose modification or discontinuation. Rare instances of cholestatic hepatitis have been reported with sirolimus use, but the clinical features of the clini... | Sirolimus undergoes extensive hepatic metabolism, largely via the cytochrome P450 system (CYP 3A4) and drug-drug interactions are common. Sirolimus may interfere with wound healing, which has been the usual reason cited for the increased rate of hepatic artery thrombosis with its use. | The liver injury associated with sirolimus therapy is usually mild and transient, resolving on its own or with dose modification or discontinuation. Sirolimus has not been linked to cases of acute liver failure or vanishing bile duct syndrome. There does not appear to be cross sensitivity to the hepatic injury between ... | Sirolimus – Generic, Rapamune® | Transplant Agents | null |
Perampanel.nxml | Perampanel | 2016-05-04 | Perampanel is glutamate receptor antagonist that is used as an anticonvulsant in the therapy of partial onset seizures. Perampanel has not been associated with serum aminotransferase elevations during therapy, and clinically apparent liver injury from perampanel has yet to be reported and must be rare, if it occurs at ... | Perampanel (per am' pan el) is a glutamate receptor antagonist that is used to treat severe or refractory partial onset seizures. Perampanel binds to the alpha-amino-3-hydroxyl-5-methyl-4-isooxazole-propionate receptor (AMPAR) for glutamate, a major central nervous system excitatory neurotransmitter. The inhibition of ... | Limited data are available on the hepatotoxicity of perampanel. In clinical trials, therapy with perampanel was not associated with an increased frequency of serum aminotransferase elevations as compared to placebo treatment, and there were no reported instances of clinically apparent liver injury. No individual case r... | The mechanism by which perampanel might cause liver injury is unknown. It is partially metabolized by the liver, largely by CYP 3A4 and is susceptible to drug interactions with agents that induce or inhibit this microsomal enzyme. | Liver injury from perampanel is rare, if it occurs at all. There is no reason to suspect cross sensitivity to hepatotoxicity between perampanel and other anticonvulsants such as phenytoin or carbamazepine with which it shares no structural similarity.\n\nDrug Class: Anticonvulsants | Perampanel – Fycompa® | Anticonvulsants | null |
Kratom.nxml | Kratom | 2020-04-03 | Kratom is an herbal made from leaves of a tropical evergreen tree (Mitragyna speciosa) that is native to Southeast Asia. Extracts from the leaves of the kratom tree have psychotropic and opioid-like activity, which has led to their use as a recreational drug. Kratom has been linked to rare instances of clinically appar... | Kratom is a botanical extract derived from the leaves of a tropical evergreen tree (Mitragyna speciosa), which belongs to the coffee family and is indigenous to Thailand, Myanmar and Malaysia. In Southeast Asia, kratom has been used for decades as an herbal medication to treat chronic pain, increase energy and stamina,... | Chronic use of kratom recreationally has been associated with rare instances of acute liver injury. The onset of injury is usually within 1 to 8 weeks of starting regular use of kratom powder or tablets, with symptoms of fatigue, nausea, pruritus and dark urine followed by jaundice. The pattern of liver injury is typic... | The cause of liver injury due to kratom is unknown. It is often used with other agents, including drugs of abuse, and its causative relationship to liver injury in published cases is not always clear. | Patients who present with acute liver injury due to kratom usually recover once it is discontinued. There is no evidence that corticosteroids shorten the course of illness or improve outcomes. Patients should be warned against further use of kratom and multiingredient nutrition supplements that might contain it.\n\nDru... | Kratom – Generic | Herbal and Dietary Supplements | null |
GLP-1Analogues.nxml | Glucagon-Like Peptide-1 (GLP-1) Analogues | 2019-04-10 | null | null | null | null | null | null | null | null |
drugliverinjury.nxml | Agents Included in LiverTox by Drug Class | 2025-04-25 | null | null | null | null | null | null | null | null |
Amodiaquine.nxml | Amodiaquine | 2017-02-02 | Amodiaquine is an aminoquinoline used for the therapy of malaria. Amodiaquine has been linked to severe cases of acute hepatitis which can be fatal, for which reason it is recommended for use only as treatment and not for prophylaxis against malaria. | Amodiaquine (am" oh dye' 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 the asexual erythrocytic forms of Plasmodium species. Amodiaquine is related in structure to chloroquine, and... | Amodiaquine has been linked to serum aminotransferase elevations in a small proportion of patients (1%). More importantly, there have been multiple reports of idiosyncratic acute liver injury due to amodiaquine. The onset of injury is usually within 1 to 4 months and is often associated with agranulocytosis. The patter... | The mechanism by which amodiaquine causes liver injury is unknown, clinical factors and testing for serum antibodies suggest an idiosyncratic immunological reaction to a hepatic metabolite may be responsible. Amodiaquine is extensively metabolized by the liver to metabolites that are excreted 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 | Amodiaquine – Generic, Camoquin®, Flavoquine® | Antimalarial Agents | null |
Ozanimod.nxml | Ozanimod | 2021-07-15 | Ozanimod is an orally available immunomodulatory drug used to treat relapsing forms of multiple sclerosis. Ozanimod is associated with transient serum enzyme elevations during therapy but has not been linked to instances of clinically apparent liver injury with jaundice, although experience with its use has been limite... | Ozanimod (oh zan’ i mod) is an immunomodulatory agent used in the treatment of multiple sclerosis that is believed to act by modulating sphingosine-1-phosphate (S1P) receptors. Ozanimod is an analogue of sphingosine and is related in structure to fingolimod, the first S1P receptor inhibitor approved for use in multiple... | In large controlled trials of ozanimod in patients with multiple sclerosis, serum ALT elevations were common (~5% of recipients) but were typically mild and asymptomatic, and they returned to baseline values within a few months of stopping and often even with continuation of therapy. Aminotransferase elevations above 3... | The mechanism by which ozanimod might cause liver injury is not known. It is extensively metabolized by liver via the cytochrome P450 system, predominantly CYP 2C9 and 3A4 and drug-drug interactions with agents that induce or inhibit these enzymes are likely to occur. Serum enzyme elevations have been frequent with all... | While chronic therapy with ozanimod can be associated with mild-to-moderate serum aminotransferase elevations, it has not been linked to any cases of clinically apparent liver injury. Because of the frequency of enzyme elevations detected during therapy, the product label for ozanimod recommends obtaining baseline live... | Ozanimod – Zeposia® | Multiple Sclerosis Agents | null |
Atenolol.nxml | Atenolol | 2017-01-15 | Atenolol is a cardioselective beta-blocker that is widely used in the treatment of hypertension and angina pectoris. Atenolol has been linked to rare cases of drug induced liver injury, some of which have been fatal. | Atenolol (a ten' oh 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. Atenolol was approv... | Atenolol therapy has been associated with mild-to-moderate elevations of serum aminotransferase levels in 1% to 2% of patients. These elevations, however, are usually asymptomatic and transient and resolve even with continuation of therapy. A few instances of clinically apparent, acute liver injury attributable to aten... | The mechanism of drug induced liver injury from atenolol is not known. The agent has little hepatic metabolism and is excreted largely unchanged in the urine. The few cases of acute liver injury attributed to atenolol were likely idiosyncratic. | The severity of liver injury due to atenolol ranges from mild serum aminotransferase elevations to acute hepatitis with jaundice. In large case series of acute liver failure due to medications, atenolol has been listed as a rare cause. Rechallenge has not been reported, but should be avoided. There is little informatio... | Atenolol – Generic, Tenormin® | Beta-Adrenergic Receptor Antagonists | null |
Dinutuximab.nxml | Dinutuximab | 2018-01-03 | Dinutuximab is a recombinant chimeric monoclonal antibody to GD2 which is used as an anticancer agent in combination with other antineoplastic agents in the treatment of neuroblastoma. Transient asymptomatic elevations in serum aminotransferase levels are common during dinutuximab therapy, but it has not been linked to... | Dinutuximab (din" ue tux' i mab) is a mouse-human chimeric monoclonal IgG1 antibody to disialoganglioside (GD2), a cell surface glycolipid that is present in low concentrations on skin, neural or peripheral nerve cells and is overexpressed on neuroblastoma cells. Engagement of dinutuximab with GD2 triggers antibody dep... | Serum aminotransferase elevations are common during dinutuximab therapy occurring in at least 50% of patients, but the abnormalities are usually transient and asymptomatic, resolving spontaneously before the time for the next cycle of infusions. ALT elevations above 5 times the upper limit of normal occurred in 8% to 2... | The mechanism of liver injury caused by dinutuximab is not known. It is a recombinant protein and unlikely to be inherently hepatoxic, but may trigger liver injury by engagement of low levels of GD2 on hepatocytes or sinusoidal cells, triggering cell injury. The aminotransferase elevations with dinutuximab do not appea... | Patients with neuroblastoma receiving dinutuximab therapy require careful monitoring of both hematologic and clinical chemistry test results. Serum aminotransferase elevations that persist or rise above 5 times ULN should lead to delay in subsequent infusions until the abnormalities resolve. The appearance of symptoms ... | Dinutuximab – Unituxin® | Antineoplastic Agents | null |
Triheptanoin.nxml | Triheptanoin | 2024-06-10 | Triheptanoin is synthetic, medium-chain triglyceride that was developed for nutritional support of patients with long-chain fatty acid oxidation disorders. Triheptanoin is given orally by feeding tube titrated to provide approximately 30% of calories. Triheptanoin therapy has not been associated with elevations in seru... | Triheptanoin (trye hep’ ta noyn) is a synthetic, purified medium-chain triglyceride that has three 7-carbon chain length fatty acids that is used as a source of calories and fatty acids for adults and children with long-chain fatty acid oxidation disorders (LC-FAOD). The LC-FAODs are rare autosomal recessive disorders ... | Serum enzyme elevations during triheptanoin therapy are frequent, mostly reflecting the underlying condition of muscle and hepatic accumulation of toxic fatty acid products and lack of adequate energy production. Elevations in CPK were present in 81%, ALT in 72% and AST in 68% of subjects treated in preregistration stu... | Triheptanoin is a pure, pharmaceutical grade, synthetic medium-chain triglyceride with three 7 carbon fatty acid chains. There is no evidence that it causes liver injury but is used in patients who frequently have serum aminotransferase elevations. | The product label for triheptanoin does not recommend monitoring of routine liver tests during therapy. It is prudent to monitor routine liver tests before starting triheptanoin because preexisting abnormalities are frequent, and elevations found during therapy should be compared to pretreatment values.\n\nDrug Class: ... | Triheptanoin – Dojolvi® | Nutritional Supplements | null |
InotuzumabOzogamicin.nxml | Inotuzumab Ozogamicin | 2024-01-15 | Inotuzumab ozogamicin is a humanized monoclonal antibody-cytotoxin conjugate which is used in the therapy of refractory or relapsed acute lymphoblastic leukemia. Inotuzumab ozogamicin has been linked to frequent serum enzyme elevations during therapy and with instances of clinically apparent acute liver injury, includi... | Inotuzumab (in" oh tooz' ue mab) ozogamicin (oh" zoe ga mye' sin) is a humanized monoclonal antibody conjugate that is used in the therapy of B-cell precursor acute lymphoblastic leukemia. The monoclonal antibody is to the human CD22 cell surface marker which is highly expressed on malignant lymphoblastic leukemia cell... | In prelicensure clinical trials of inotuzumab ozogamicin, up to half of patients had serum ALT or AST elevations during therapy which were above 5 times the upper limit of normal (ULN) in 2% to 5%. Hyperbilirubinemia was also common during inotuzumab therapy, generally occurring without accompanying ALT or AST elevatio... | null | null | Inotuzumab Ozogamicin – Besponsa® | Antineoplastic Agents | null |
MoveFree.nxml | Move Free | 2020-02-26 | Move Free is a proprietary line of multi-ingredient dietary supplements (MIDS) marketed as aids for joint health and “to help ease joint discomfort, maintain strength and flexibility and help support and nourish cartilage”. The major ingredients in the products include glucosamine, chondroitin, hyaluronic acid and meth... | Move Free is a proprietary product name for an array of multi-ingredient herbal and dietary supplements (MIDS) meant to ease joint discomfort. The Move Free brand is currently produced by Reckitt Benckiser Group plc (Slough, England) which purchased its previous distributor, Schiff Nutrition International (Salt Lake Ci... | The initial reports of liver injury attributed to Move Free were published in 2010, with subsequent reports in 2012 and 2013, all from the United States. These publications described an acute hepatocellular injury arising within 1 to 3 weeks of starting a Move Free product that contained glucosamine, chondroitin and a ... | The liver injury attributed to Move Free products has been reported to be due to Chinese skullcap, but the mechanism by which this herb might cause liver injury is unexplained. Indeed, Chinese skullcap has hepatoprotective activity in animal models of liver disease. Contamination or misidentification of the herbal comp... | The liver injury that has been attributed to Move Free products has usually been mild-to-moderate in severity and self-limited in course, resolving in 1 to 2 months of stopping the preparations. Move Free has not been linked to instances of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. In pati... | Move Free® | Herbal and Dietary Supplements | [
{
"cas_registry_number": "9007-27-6",
"molecular_formula": "(C14-H21-N-O12)n-",
"name": "Chondroitin"
},
{
"cas_registry_number": "3416-24-8",
"molecular_formula": "C6-H13-N-O5",
"name": "Glucosamine"
},
{
"cas_registry_number": "9004-61-9",
"molecular_formula": "Unspecified"... |
Bezlotoxumab.nxml | Bezlotoxumab | 2017-09-28 | Bezlotoxumab is a human monoclonal antibody to the Clostridium difficile toxin B that is used to reduce the risk of recurrence in high risk patients being treated for C. difficile infection. Bezlotoxumab has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver i... | Bezlotoxumab (bez" loe tox' ue mab) is a human monoclonal antibody to the C. difficile toxin B that has high affinity for the toxin, blocking its binding to host cells. In several large clinical trials, bezlotoxumab given at the time of antibacterial therapy was found to decrease the rate of recurrence of C. difficile ... | In large clinical trials, bezlotoxumab was not associated with changes in serum aminotransferase levels during therapy, and rates of most adverse reactions were similar in patients who received placebo injections or standard care. There have been no published reports of clinically apparent acute liver injury attributed... | Bezlotoxumab is a human monoclonal antibody and is unlikely to be inherently hepatotoxic. Recombinant proteins are often metabolized in the cells on which they act, but are also metabolized in the liver, largely to small peptides and amino acids which may be reused to synthesize proteins and are unlikely to be toxic or... | null | Bezlotoxumab – Zinplava® | Antiinfective Agents | null |
CovidMonoclonals.nxml | Covid-19 Monoclonal Antibodies | 2022-04-05 | The severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) is a novel coronavirus that arose in late 2019 and led to a worldwide pandemic of respiratory illness (COVID-19) and, within the first year of its recognition, led to more than 100 million infections and at least 2 million deaths worldwide. SARS-CoV-... | Monoclonal antibodies to the spike protein of the SARS-CoV-2 virus have been developed and several have been shown to have neutralizing activity in vitro in cell culture as well as in vivo in animal models of COVID-19 infection. In clinical trials, administration of one or more of these monoclonal antibodies have been ... | In trials of monoclonal antibodies to the COVID-19 spike protein there have been no reports of ALT elevations or hepatotoxicity. Side effects may include rash and diarrhea and, in rare instances, hypersensitivity reactions.\n\nLikelihood score, all five monoclonal anti-SARs-CoV-2 antibodies: E (unlikely causes of clini... | Monoclonal antibodies have no specific hepatic metabolism and are broken down in cells to amino acids. The mechanism by which they might cause liver injury is unknown.\n\nDrug Class: Monoclonal Antibodies, Antiviral Agents | null | Bamlanivimab® (LY-CoV555) | Monoclonal Antibodies | null |
Cannabidiol.nxml | Cannabidiol | 2023-02-16 | Cannabidiol (CBD) is a non-psychoactive component of Cannabis sativa (marijuana), one of more than 80 cannabinoids identified in the plant, and the second most common constituent after Δ9-tetrahydrocannabinol (THC), the major psychoactive component. Cannabidiol is available as an FDA approved prescription medication (E... | Cannabidiol (kan" a bi dye' ol) is a natural cannabinoid, the second most common component in Cannabis sativa (marijuana). Unlike the most abundant cannabinoid, delta-9-tetrahydrocannabinol (THC), the psychoactive ingredient of marijuana, cannabidiol has minimal psychoactive properties and may actually decrease the ris... | In prelicensure studies, serum aminotransferase elevations arose during cannabidiol therapy for epilepsy in 34% to 47% of patients compared to 18% of controls who were receiving other anticonvulsant medications. Elevations above 3 times ULN occurred in 13% of cannabidiol treated compared to 1% on placebo. ALT and AST e... | The cause of serum aminotransferase elevations during cannabidiol therapy in doses used to treat epilepsy is not known, but may represent direct toxicity and be due to the molecule itself or to the production of a toxic intermediate in its metabolism. Cannabidiol is metabolized by the liver in large part by CYP 3A4 and... | High dose cannabidiol therapy can be associated with serum ALT and AST elevations that generally arise within the first 2 months of treatment and are mild-to-moderate in severity. The frequency of elevations is dose related and more frequent when given in combination with valproate and clobazam. The elevations, however... | Cannabidiol – Epidiolex® | Anticonvulsants | null |
Berotralstat.nxml | Berotralstat | 2024-06-20 | Berotralstat is a small molecule inhibitor of plasma kallikrein that is used to prevent acute attacks of hereditary angioedema (HAE) in adults and children 12 years of age or older. Berotralstat has been linked to occasional mild-to-moderate elevations in serum aminotransferase levels during therapy but has not been im... | Berotralstat (ber” oh tral’ stat) is an orally available, small molecule inhibitor of plasma kallikrein used to prevent acute attacks of hereditary angioedema (HAE), an autosomal dominant condition marked by intermittent episodes of swelling and pain affecting multiple organs and tissues. HAE is caused by mutations in ... | In preregistration trials, mild, transient serum aminotransferase elevations occurred in 2% to 5% of patients receiving berotralstat vs 10% of those on placebo. Values above 5 times the upper limit of normal (ULN) were uncommon (less than 1%). Furthermore, bilirubin levels remained normal and no patient developed sympt... | The causes of liver test abnormalities during berotralstat therapy of hereditary angioedema are often unrelated to the drug and are attributable to comorbidities, such as chronic viral hepatitis, gallstone disease, or malignancy. Nevertheless, berotralstat is metabolized in the liver, predominantly by CYP 2D6 and 3A4 a... | The product label for berotralstat does not recommend monitoring of routine liver tests during therapy, but testing patients before starting therapy is appropriate because of the frequency of comorbidities including liver disease in patients with HAE. A rise in serum aminotransferase levels during therapy should trigge... | Berotralstat – Orladeyo® | Genetic Disorder Agents | null |
Onasemnogene.nxml | Onasemnogene Abeparvovec | 2020-08-20 | Onasemnogene abeparvovec is a unique gene therapy agent used to correct the abnormal gene responsible for spinal muscular atrophy type 1, a rare progressive neuromuscular disorder that typically leads to disability and death within the first two years of life. Onasemnogene abeparvovec is given as a one-time intravenous... | Onasemnogene abeparvovec (on” a sem’ noe jeen a” be par’ voe vek) is a biologic agent and gene therapy designed to correct the gene defect of spinal muscular atrophy (SMA), a rare inherited disease that results in progressive neuromuscular disability leading to severe muscle weakness, paralysis, need for ventilatory su... | Prospective studies suggest that 90% of subjects who receive onasemnogene abeparvovec develop some degree of serum aminotransferase elevations during the 1 to 2 months after receipt of the infusion. In a small proportion of infants the elevations are as high as 10 to 20 times the ULN. These abnormalities can be amelior... | The mechanism of onasemnogene abeparvovec hepatotoxicity is thought to be an immunologic response to the expression of viral vector or SMN gene products by the liver. The liver injury typically arises concurrent with the appearance of anti-AAV9 antibodies. Of interest, cases of severe hepatotoxicity were also observed ... | Onasemnogene abeparvovec hepatotoxicity is usually responsive to an increase in dose of corticosteroids or their reinstitution if they have been discontinued. Infants receiving this gene therapy should be monitored before and at regular intervals for at least 3 months. Infants with ALT or AST elevations above 10 times ... | Onasemnogene Abeparvovec – Zolgensma® | Gene Therapy | null |
Corticosteroids.nxml | Corticosteroids | 2021-05-07 | The corticosteroids are a group of chemically related natural hormones and synthetic agents that resemble the human adrenal hormone cortisol and have potent antiinflammatory and immunosuppressive properties and are widely used in medicine. Corticosteroid therapy is associated with several forms of liver injury, some du... | The corticosteroids are hormones that have glucocorticoid (cortisol-like) and/or mineralocorticoid (aldosterone-like) activities and which are synthesized predominantly by the adrenal cortex. In clinical practice, the term “corticosteroids” usually refers to the glucocorticoids and are represented by a large group of n... | null | null | null | Betamethasone – Generic, Celestone® | Glucocorticoids, Synthetic | [
{
"cas_registry_number": "378-44-9",
"molecular_formula": "C22-H29-F-O5",
"name": "Betamethasone"
},
{
"cas_registry_number": "53-06-5",
"molecular_formula": "C21-H28-O5",
"name": "Cortisone"
},
{
"cas_registry_number": "50-02-2",
"molecular_formula": "C22-H29-F-O5",
"nam... |
PenicilllinGandV.nxml | Penicillin G and V | 2020-10-20 | Penicillin G and V are first generation penicillins that are used widely to treat infections due to susceptible organisms and have been linked rarely and only weakly with idiosyncratic liver injury. | Penicillin G benzathine, potassium, procaine and sodium are currently available in the United States in parenteral formulations for intravenous or intramuscular use. Penicillin V potassium (also called phenoxymethyl penicillin) is a more acid stable and can be administered orally. Both Penicillin G and V are available ... | Rare instances of idiosyncratic liver injury have been reported in persons receiving the first generation penicillins. Many case reports predated availability of serologic testing for viral hepatitis and many described patients with multiple reasons for having liver disease (such as sepsis) and who were receiving other... | The cause of the idiosyncratic, cholestatic liver injury associated with penicillin is probably hypersensitivity or allergy. No cases of rechallenge or reexposure have been reported. The serum aminotransferase elevations that occur with high doses of parenteral penicillin are likely due to direct hepatotoxicity. | The asymptomatic rise in serum aminotransferase levels that occurs with high dose penicillin therapy usually resolves rapidly once penicillin is stopped. These patients may tolerate another form of penicillin without recurrence. In the few cases of cholestatic hepatitis that have been described with the first generatio... | Various Generic | Antiinfective Agents | [
{
"cas_registry_number": "61-33-6",
"molecular_formula": "C16-H18-N2-O4-S",
"name": "Penicillin G (Benzylpenicillin)"
},
{
"cas_registry_number": "69-57-8",
"molecular_formula": "C16-H18-N2-O4-S",
"name": "Penicillin G Sodium"
},
{
"cas_registry_number": "113-98-4",
"molecula... |
Naloxone.nxml | Naloxone | 2020-03-24 | Naloxone is an opiate antagonist which is used intravenously in emergency situations to reverse the respiratory depression caused by overdoses of heroin, morphine or other opioids. Naloxone has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury. | Naloxone (nal ox’ one) is a derivative of the natural plant alkaloid thebaine and is similar to oxymorphone. Naloxone, however, is a competitive antagonist of the opiate receptors and has particularly high affinity for the μ opiate receptor and can displace morphine and other full agonists, thereby reversing their effe... | Therapy with naloxone has not been linked to serum enzyme elevations or to idiosyncratic acute, clinically apparent liver injury. Patients with opioid overdose often have underlying chronic liver diseases such as alcoholic liver disease, hepatitis B or C, but treatment with naloxone does not appear to exacerbate those ... | null | null | Naloxone – Generic, Narcan® | Opioid Antagonists | null |
Remdesivir.nxml | Remdesivir | 2022-02-03 | Remdesivir is an antiviral nucleotide analogue used for therapy of severe novel coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome (SARS) coronavirus 2 (CoV-2) infection. Remdesivir therapy is given intravenously for 3 to 10 days and is frequently accompanied by transient, reversible mild-t... | Remdesivir (rem de’ si vir) is a phosphoramidate prodrug of a substituted nucleotide analogue of adenosine which has potent activity against the SARS-CoV-1 and SARS-CoV-2 encoded RNA dependent RNA polymerases. Remdesivir is not well absorbed orally and must be given by intravenous infusion. Once absorbed into cells, re... | In human volunteer studies, remdesivir therapy given for 7 to 14 days was associated with minor serum aminotransferase elevations (less than 5 times ULN) but without other evidence of hepatic injury. In controlled trials of remdesivir in patients hospitalized with COVID-19, rates of serum ALT elevations were similar or... | Serum aminotransferase elevations are not uncommon with parenterally administered remdesivir and may be caused by direct toxicity possibly due to inhibition of mitochondrial RNA polymerase. On the other hand, idiosyncratic injury due to remdesivir has not been clearly shown. SARS-CoV-2 virus may infect the liver and ha... | The ALT and AST elevations associated with initiation of remdesivir therapy in patients with SARS-CoV-2 infection are generally mild-to-moderate in severity and self-limited in course without jaundice or symptoms. Careful monitoring of liver tests is recommended before and frequently during treatment. However, this rec... | Remdesivir – Veklury ® | Antiviral Agents | null |
Eravacycline.nxml | Eravacycline | 2019-04-10 | Eravacycline is a parenterally administered tetracycline-like antibiotic used to treat moderate-to-severe intraabdominal infections due to susceptible organisms. Eravacycline use has been associated with a low rate of serum enzyme elevations during therapy but has not been convincingly linked to instances of clinically... | Eravacycline (er" a va sye' kleen) is a parenterally administered, broad spectrum synthetic tetracycline-like antibiotic with potent activity against many gram-positive and gram-negative aerobic and anaerobic organisms including many multidrug resistant organisms. Eravacycline is similar to tigecycline both in structur... | In preclinical trials of intravenous eravacycline, serum aminotransferase elevations were mild and no more frequent than with placebo or comparator treatment arms. There were no instances of clinically apparent liver injury that could be attributed to eravacycline. Nevertheless, other tetracycline antibiotics are well ... | The mechanism by which eravacycline might cause liver injury is unknown. Eravacycline is metabolized in the liver by the microsomal cytochrome P450 system, largely via CYP 3A4. Eravacycline is susceptible to drug-drug interactions with modulators of CYP 3A4, inducers causing a decrease in eravacycline plasma levels. | Patients on intravenous eravacycline who develop serum aminotransferase elevations that rise above 5 times the upper limit of normal or are accompanied by jaundice or symptoms should have eravacycline discontinued. Whether there is cross sensitivity to hepatic injury among the various tetracyclines is not known, but sw... | Eravacycline – Xerava® | Antiinfective Agents | null |
Ezogabine.nxml | Ezogabine | 2018-02-18 | Ezogabine, which is known as retigabine in Europe, is a unique anticonvulsant used largely as an adjunctive agent in the treatment of partial seizures. Therapy with ezogabine has not been associated with serum aminotransferase elevations, and clinically apparent liver injury from ezogabine has yet to be reported and mu... | Ezogabine (e zog' a been) is an anticonvulsant with a unique mechanism of action, decreasing excitability and seizure activity by opening voltage-gated potassium channels in the brain. Ezogabine has been shown to be effective both as monotherapy and in combination with other anticonvulsants for partial seizures. Ezogab... | Limited data are available on the hepatotoxicity of ezogabine. In clinical trials, therapy with ezogabine was not associated with an increased frequency of serum aminotransferase elevations as compared to placebo treatment, and there were no instances of clinically apparent liver injury. No individual case reports of e... | Ezogabine is extensively metabolized by the liver, largely by glucuronidation and acetylation. However, its metabolism is independent of microsomal P450 system and it has no effect on P450 activity and lacks significant drug-drug interactions.\n\nDrug Class: Anticonvulsants | null | Ezogabine – Potiga® | Anticonvulsants | null |
Oxycodone.nxml | Oxycodone | 2020-11-24 | Oxycodone is a semisynthetic, moderately potent, orally available opioid that is widely used for acute or chronic management of moderate- or moderately severe pain either alone or in combination with acetaminophen. Oxycodone by itself has not been linked to serum enzyme elevations during therapy or to clinically appare... | Oxycodone (ox” i koe’ done) is a semisynthetic derivative of thebaine, a natural alkaloid found in the resin of poppy seeds (Papaver somniferum). It is well absorbed orally and has moderate opiate activity, acting as an agonist of the u type opiate receptor. Oxycodone alone or in combination with acetaminophen has been... | Despite wide scale use for many decades, oxycodone has not been convincingly linked to instances of clinically apparent acute liver injury. However, oxycodone and other opioid-acetaminophen combinations have become a common cause of acute liver injury, which is usually the result of excessive use of the medication for ... | null | null | Oxycodone – Generic, OxyContin® | Opioids | null |
Sunitinib.nxml | Sunitinib | 2018-06-27 | Sunitinib is multi-specific tyrosine kinase receptor inhibitor that is used in the therapy of gastrointestinal stromal tumors and advanced renal cell carcinoma. Sunitinib therapy is associated with transient elevations in serum aminotransferase and bilirubin levels and rare instances of clinically apparent acute liver ... | Sunitinib (soo ni' ti nib) is an inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis. The tyrosine kinase receptors of cancer cells are often mutated and can cause unregulated cell growth and proliferation. Sunitinib is one of several tyrosine kinase receptor inhibitor... | In large clinical trials of sunitinib, elevations in serum aminotransferase levels were common, occurring in 39% of sunitinib vs 23% of placebo recipients. Values greater than 5 times the upper limit of normal (ULN) occurred in only 2% to 3% of sunitinib recipients (and 1% of controls). These abnormalities were usually... | The clinical features of cases of severe acute liver injury due to sunitinib have suggested ischemic damage that may be related to hypotension and anoxia, rather than direct hepatic injury. Sunitinib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury may be related to production of a toxic... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. In some situations, therapy can be restarted particularly with concurrent prednisone (10-20 mg daily). In patients with clinically apparent liver injury and jaundice, restarting... | Sunitinib – Sutent® | Antineoplastic Agents | null |
Fenofibrate.nxml | Fenofibrate | 2017-01-24 | Fenofibrate is a fibric acid derivative used in the therapy of hypertriglyceridemia and dyslipidemia. Fenofibrate therapy is associated with mild and transient serum aminotransferase elevations and with rare instances of acute liver injury, which can be severe and prolonged and lead to significant hepatic fibrosis. | Fenofibrate (fen" oh fye' brate) is a fibric acid derivative. Its lipid lowering activity is probably mediated by its interactions with the peroxisome proliferator activated receptor alpha (PPARα), which regulates gene expression of enzymes involved in fatty acid oxidation. These fenofibrate induced changes cause an in... | Mild, transient serum aminotransferase elevations develop in up to 20% of patients receiving fenofibrate, but values above 3 times normal in only 3% to 5%. These abnormalities are usually asymptomatic and transient, resolving even with continuation of fenofibrate, but they occasionally may require drug discontinuation.... | The mechanism of hepatotoxicity of fenofibrate is not known but appears to be immunologic. Cases of autoimmune-like hepatitis due to fenofibrate suggest that there is induction of immune reactivity to altered metabolites or fenofibrate-protein haptens in the liver. | Several instances of chronic liver injury and fibrosis have been reported with fenofibrate use, typically in patients who were continued on therapy despite evidence of liver injury. However, in most cases, serum aminotransferase levels eventually fall to normal within 2 to as long as 12 months after stopping. Rechallen... | Fenofibrate – Antara®, Lipofen®, Lofibra®, Tricor®, Triglide® | Antilipemic Agents | null |
Edoxaban.nxml | Edoxaban | 2023-02-16 | Edoxaban is an oral, small molecule inhibitor of factor Xa which is used as an anticoagulant to decrease the risk of venous thromboses, systemic embolization and stroke in patients with atrial fibrillation, and as treatment of deep vein thrombosis and pulmonary embolism. Edoxaban has been linked to a low rate of serum ... | Edoxaban (e dox' a ban) is a selective inhibitor of the coagulation factor Xa, the last and rate controlling step in the generation of thrombin, the final intermediate in blood coagulation. Inhibiting thrombin prevents the conversion of fibrinogen to fibrin and subsequent cross linking of fibrin monomers, platelet acti... | Edoxaban is associated with serum aminotransferase elevations greater than 3 times the upper limit of normal in 2% to 5% of treated patients. This rate is similar or lower than rates with warfarin or comparator arms. The elevations are generally transient and not associated with symptoms or jaundice. In premarketing st... | Edoxaban is eliminated largely unchanged in the urine and has minimal hepatic metabolism. It is a substrate of P-glycoprotein, and its serum concentrations can be affected by inducers (rifampin) and inhibitors of this transport protein. The cause of the serum enzyme elevations during therapy with edoxaban is unknown, b... | The serum enzyme elevations during edoxaban therapy have been mild-to-moderate in severity, but asymptomatic and rapidly reversible often even without stopping therapy. Clinically apparent liver injury due to edoxaban appears to be rare and has not been well documented. There is no reason to suspect that there is cross... | Edoxaban – Savaysa® | Anticoagulants | [
{
"cas_registry_number": "480449-70-5",
"molecular_formula": "C24-H30-Cl-N7-O4-S",
"name": "Edoxaban"
}
] |
Atropine_Homatropine.nxml | Atropine | 2017-07-07 | Atropine is a natural alkaloid anticholinergic agent that has potent antimuscarinic effects and is used by injection to treat symptomatic bradycardia, severe bronchospasm and to reduce vagal stimulation. Atropine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. | Atropine (at' roe peen) is a natural alkaloid that is the prototypic anticholinergic agent found as a secondary metabolite in plants of the Solanaceae family, including deadly nightshade (Atropa belladonna) for which it is named. Atropine has potent and broad, nonspecific antimuscarinic activity. Because of its rapid o... | Despite widespread use over many decades, atropine has not been linked convincingly to episodes of liver enzyme elevations or clinically apparent liver injury. Atropine is metabolized by the liver, but is usually given in low doses (<1 mg) for short periods only.\n\nLikelihood score: E (unlikely cause of clinically app... | null | null | Atropine – Generic | Anticholinergic Agents | [
{
"cas_registry_number": "51-55-8",
"molecular_formula": "C17-H23-N-O3",
"name": "Atropine"
},
{
"cas_registry_number": "87-00-3",
"molecular_formula": "C16-H21-N-O3",
"name": "Homatropine"
}
] |
Isoflurane.nxml | Isoflurane | 2018-01-01 | Isoflurane is a commonly used inhalational anesthetic and has an excellent safety record. Isoflurane has been linked to rare instances of severe acute liver injury resembling halothane induced liver injury in small case series and individual case reports. | Isoflurane (eye" soe flur' ane) is a widely used major anesthetic agent with rapid onset of action and rapid dispersal. Isoflurane is a halogenated anesthetic, similar in structure and activity to halothane, desflurane, enflurane and sevofurane. Isoflurane is typically given in inhaled concentrations of 0.5% to 3% in o... | Prospective, serial blood testing often demonstrates minor transient elevations in serum aminotransferase levels in the 1 to 2 weeks after major surgery and halogenated anesthetic agents. Appearance of ALT levels above 10 times the upper limit of normal, however, is distinctly unusual and points to significant hepatoto... | The mechanism of isoflurane hepatotoxicity is suspected to be similar to that of halothane and associated with creation of reactive intermediates. Isoflurane is metabolized to some extent by the microsomal drug metabolizing enzyme CYP 2E1 to a trifluoroacetylated reactive intermediate (TFA) that is capable of binding t... | Severity ranges from mild and transient aminotransferase elevations without symptoms or other evidence of liver injury, to a self limited symptomatic acute hepatitis-like reaction to severe, acute hepatic failure. The severity and prognosis may relate in part of patient age, being more severe in the elderly and both mi... | Isoflurane – Generic, Forane® | Anesthetics, Halogenated | null |
EtoposideTeniposide.nxml | Etoposide | 2018-02-25 | Etoposide and teniposide are semisynthetic analogues of podophyllotoxin that are used as antineoplastic agents in the therapy of several forms of solid tumors, leukemia and lymphoma, usually in combination with other agents. Both etoposide and teniposide are associated with an appreciable rate of serum enzyme elevation... | Etoposide (e toe' poe side) and teniposide (ten" i poe' side) are semisynthetic derivatives of podophyllotoxin, an extract from the mandrake plant (American May Apple: Podophyllum peltatum). Both drugs appear to act by binding to and inhibiting topoisomerase II, preventing the healing of DNA breaks that occur during th... | Chemotherapy with etoposide or teniposide in combination with other agents is associated with serum enzyme elevations in 5% to more than 50% of patients, depending upon the dose and other agents used. The ALT elevations are usually asymptomatic and transient and may resolve without dose modification. In many instances,... | Etoposide is metabolized by the microsomal P450 drug metabolizing enzymes and inhibits the function of CYP 3A and 2D6, and injury may be the result of its activation to a toxic intermediate. Rapid recurrence with rechallenge is typical, but features of hypersensitivity are uncommon. In high doses, etoposide and tenipos... | null | Etoposide – Generic, Toposar® | Antineoplastic Agents | [
{
"cas_registry_number": "33419-42-0",
"molecular_formula": "C29-H32-O13",
"name": "Etoposide"
},
{
"cas_registry_number": "29767-20-2",
"molecular_formula": "C32-H32-O13-S",
"name": "Teniposide"
}
] |
Venetoclax.nxml | Venetoclax | 2017-04-04 | Venetoclax is an oral selective BCL-2 inhibitor and antineoplastic agent used in the therapy of refractory chronic lymphocytic leukemia (CLL). Venetoclax is associated with a low rate of transient serum enzyme elevations during therapy, but has not been implicated in cases of clinically apparent acute liver injury with... | Venetoclax (ven et' oh klax) is a small molecule inhibitor of BCL-2, an intracellular protein that inhibits apoptosis. BCL2 is overexpressed in cancer cells, particularly in chronic lymphocyte leukemia (CLL). Overexpression of BCL2 increases cancer cell survival and increases resistance to chemotherapy. Venetoclax bind... | In clinical trials in 240 patients with CLL, serum aminotransferase elevations occurred in 20% of subjects treated with venetoclax, but the elevations were generally transient, mild and not associated with jaundice or symptoms. In the preregistration trials, no cases of clinically apparent liver injury attributed to ve... | Venetoclax is unlikely to have direct hepatotoxic effects as dose escalation studies showed no dose related effect on liver test results. On the other hand, the immunosuppressive effects of venetoclax may cause liver related changes that could lead to viral or autoimmune reactions. Venetoclax is metabolized in the live... | Patients receiving venetoclax require careful monitoring largely for hematologic abnormalities and blood chemistry changes of tumor lysis syndrome. If serum aminotransferase levels rise to 5 times the upper limit of normal (ULN), therapy should be interrupted until levels fall to baseline or less than 1.5 times ULN.\n\... | Venetoclax – Venclexta® | Antineoplastic Agents | null |
Nicotine.nxml | Nicotine | 2020-03-25 | Nicotine is a natural alkyloid that is a major component of cigarettes and is used therapeutically to help with smoking cessation. Nicotine has not been associated with liver test abnormalities or with clinically apparent hepatotoxicity. | Nicotine (nik' oh teen) is a liquid alkyloid that has a variety of activities in the body and central nervous system (CNS), acting largely as a stimulant via activation of nicotinic receptors. Nicotine is a CNS stimulant and has both stimulatory and depressant actions on autonomic ganglia. Nicotine has multiple actions... | Nicotine used in cigarette cessation programs as well as nicotine containing e-cigarettes have not been associated with serum enzyme elevations during therapy at rates greater than occurred with placebo. Medical and recreational uses of nicotine have not been associated with cases of clinically apparent liver injury.\n... | Nicotine is metabolized extensively by many tissues including the liver and is rapidly excreted.\n\n[Agents in clinical use to aid in smoking cessation and to treat nicotine withdrawal symptoms include bupropion, nicotine, and varenicline.]\n\nDrug Class: Substance Abuse Treatment Agents | null | Nicotine – Generic, Commit®, Nicorette® (Oral); Habitrol® (Transdermal); Nicotrol® (Inhaler, Spray) | Substance Abuse Treatment Agents | null |
Pemetrexed.nxml | Pemetrexed | 2016-04-18 | Pemetrexed is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of... | Pemetrexed (pem" e trex' ed) is a folic acid analog 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 thymidine an... | Pemetrexed therapy is associated with a low-to-moderate rate of serum enzyme elevations, but these are generally mild, transient and without accompanying symptoms or jaundice. Serum ALT or AST elevations above 5 times ULN occur in 1% to 6% of patients, but are usually self-limited in course and rarely require dose modi... | The cause of the serum enzyme elevations that may occur during pemetrexed use is probably direct hepatotoxicity from the folate antagonism. Its hepatic metabolism is minimal and most of the administered dose is excreted unchanged in the urine. | Liver injury is rare after pemetrexed therapy. Persistent serum enzyme elevations above 5 times ULN should lead to temporary discontinuation of pemetrexed therapy, but should also lead to careful search for other possible causes of liver injury. There have been no instances of acute liver failure, chronic hepatitis or ... | Pemetrexed – Alimta® | Antineoplastic Agents | null |
Praziquantel.nxml | Praziquantel | 2020-07-20 | Praziquantel is an anthelmintic agent with activity against a broad spectrum of trematodes and cestodes that is used predominantly in the therapy of schistosomiasis, liver flukes, and cysticercosis. Praziquantel therapy has been reported to cause serum aminotransferase elevations during therapy, but clinically apparent... | Praziquantel (praz" i kown' tel) is a heterocyclic prazino-isoquinoline derivative with a broad spectrum of activity against several trematodes (Fasciola, Schistosoma) and cestodes (Taenia). Praziquantel is believed to act by interference with tegument calcium transport, resulting in paralysis of the parasitic worms wi... | Praziquantel therapy has been associated with elevations in serum aminotransferase levels in up to 27% of patients, but these abnormalities were self-limiting. Praziquantel has been rarely associated with clinically apparent liver injury, which generally accompanied hypersensitivity reactions such as rash and fever. In... | Praziquantel is extensively metabolized by the liver via the cytochrome P450 system and might cause hepatic injury as a result of a toxic intermediate of its metabolism. Plasma levels of praziquantel are affected by inducers (rifampin decreases drug levels) and inhibitors of P450 activity (cimetidine, ketoconazole and ... | Praziquantel is usually well tolerated and clinically apparent liver injury due to its use is rare. There is no evidence for cross sensitivity to other anthelmintic agents.\n\nDrug Class: Anthelmintic Agents | Praziquantel – Biltricide® | Anthelmintic Agents | null |
Gemcitabine.nxml | Gemcitabine | 2018-03-09 | Gemcitabine is a cytosine analogue and intravenously administered antineoplastic agent used in the therapy of several forms of advanced, pancreatic, lung, breast, ovarian and bladder cancer. Gemcitabine is associated with a high rate of transient serum enzyme elevations during therapy but is a very rare cause of acute,... | Gemcitabine (jem sye' ta been), 2,,2.-difluoro deoxycytidine, is a pyrimidine analogue that is widely used in solid tumor chemotherapy. Intracellularly, it is metabolized to diphosphate and triphosphate forms, both of which have antineoplastic activity inhibiting ribonucleotide reductase and competing with deoxycytidin... | Elevations in serum aminotransferase levels occur in 30% to 90% of patients receiving cyclic therapy with gemcitabine. The elevations are generally mild-to-moderate, asymptomatic and self-limited, frequently resolving without discontinuation or even interruption of therapy. ALT or AST elevations above 5 times the upper... | The frequent mild-to-moderate serum aminotransferase elevations that occur during gemcitabine therapy are likely due to direct hepatic toxicity. The clinically apparent liver injury linked to gemcitabine (cholestasis, HBV reactivation, sinusoidal obstruction syndrome) has occurred mostly in persons with underlying, pre... | The severity of the liver injury linked to gemcitabine therapy is usually mild and self-limited, and dose modification or discontinuation is rarely necessary. However, the clinically apparent liver injury described with gemcitabine therapy tends to be severe and several fatal instances have been described. Virtually al... | Gemcitabine – Generic, Gemzar® | Antineoplastic Agents | null |
Methylphenidate.nxml | Methylphenidate | 2021-08-24 | Methylphenidate is a central nervous system stimulant used for the therapy of attention deficit disorder and narcolepsy. Methylphenidate has been linked to a low rate of serum aminotransferase elevations during therapy and to rare instances of acute, clinically apparent liver injury, generally after its intravenous abu... | Methylphenidate (meth" il fen' i date) is a piperidine derivative that is structurally related to amphetamine which acts as a central nervous system (CNS) sympathomimetic stimulant, probably by causing release of norepinephrine at CNS nerve terminals promoting neurotransmission. Methylphenidate may also affect dopamine... | In prelicensure clinical trials, methylphenidate was not associated with serum aminotransferase elevations or instances of hepatic injury, but reports of enzyme elevations were received by the sponsor and appeared in publications after it was marketed. The elevations were transient, mild-to-moderate in severity and rar... | The mechanism by which methylphenidate might cause liver injury is unknown, but the injury occurring after intravenous use is likely due to direct toxicity. Methylphenidate is extensively metabolized in the liver and has many drug-drug interactions. | The liver injury due to oral methylphenidate is usually self-limited and resolves rapidity. Injury from intravenous use can be severe and fatalities have been reported. There have been no instances of chronic liver injury or vanishing bile duct syndrome associated with either oral or intravenous methylphenidate. Cross ... | Methylphenidate – Generic, Concerta®, Daytrana®, Jornay PM®, Ritalin® | Central Nervous System Stimulants | null |
Triazolam.nxml | Triazolam | 2023-06-22 | Triazolam is an orally available benzodiazepine used predominantly for therapy of insomnia. As with most benzodiazepines, triazolam has not been associated with serum aminotransferase or alkaline phosphatase elevations during therapy, and clinically apparent liver injury from triazolam has been reported but is very rar... | Triazolam (trye az" oh lam) is a benzodiazepine that was widely used as a sleeping aid in the therapy of insomnia for several decades but is now rarely used. The soporific activity of the benzodiazepines is mediated by their ability to enhance gamma-aminobutyric acid (GABA) mediated inhibition of synaptic transmission ... | Triazolam, like other benzodiazepines, is rarely associated with serum ALT and alkaline phosphatase elevations, and clinically apparent liver injury from triazolam is rare. There have been no well described case reports of acute liver injury from triazolam, except for a single report of severe and prolonged cholestatic... | Triazolam is metabolized by the liver to inactive metabolites that are excreted in the urine. Liver injury from benzodiazepines is probably due to a rarely produced intermediate metabolite. The relative safety of triazolam is probably related to its low daily dose (<1 mg). | 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. A single case of liver failure due to prolonged cholestatic hepatitis after triazolam therapy has been described in the literature. There ... | Triazolam – Generic, Halcion® | Sedatives and Hypnotics | null |
Baricitinib.nxml | Baricitinib | 2022-08-30 | Baricitinib is an orally available small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis, severe alopecia areata, and, in combination with remdesivir, severe COVID-19 in hospitalized patients requiring supplementary oxygen. Baricitinib is associated with transient and u... | Baricitinib (bar" i sye' ti nib) is an orally available, specific inhibitor Janus-associated kinases (mainly JAK1 and JAK2) that is used to treat moderate-to-severe rheumatoid arthritis and alopecia areata. The Janus kinases are critical steps in immune activation as well as in hematopoiesis. JAK1 is a critical kinase ... | In the large prelicensure clinical trials in rheumatoid arthritis, serum aminotransferase elevations occurred in up to 17% of baricitinib treated subjects compared to 11% in placebo recipients. The elevations were typically mild and transient and values above 3 times the upper limit of normal (ULN) occurred in 1% to 2%... | The cause of mild serum enzyme elevations during baricitinib therapy is not known. Baricitinib is largely excreted unchanged in urine and stool and less than 10% undergoes hepatic metabolism, largely via CYP 3A4. The metabolism of baricitinib is not affected by CYP inhibitors or inducers, but its renal excretion can be... | Monitoring of serum aminotransferase levels is recommended for patients starting baricitinib. De novo elevations in serum aminotransferases levels above 5 times the upper limit of normal should lead to temporary cessation. If serum enzyme elevations do not resolve or improve within a few weeks of stopping, or if sympto... | Baricitinib – Olumiant® | Antirheumatic Agents | [
{
"cas_registry_number": "1187594-09-7",
"molecular_formula": "C16-H17-N7-O2-S",
"name": "Baricitinib"
},
{
"cas_registry_number": "477600-75-2",
"molecular_formula": "C16-H20-N6-O",
"name": "Tofacitinib"
}
] |
Omalizumab.nxml | Omalizumab | 2020-12-28 | Omalizumab is a monoclonal antibody to human immunoglobulin E (IgE), which leads to a decrease in IgE binding to mast cells and basophils and a reduction in allergic symptoms of asthma and seasonal rhinitis. Omalizumab therapy has not been associated with serum enzyme elevations during therapy and has yet to be implica... | Omalizumab (oh” ma liz’ ue mab) is a recombinant, human monoclonal antibody to IgE which binds avidly to circulating immunoglobulin E, preventing its attachment to high affinity receptors on mast cells and basophils. This receptor inhibition prevents the release of histamine and other mediators of the allergic immune r... | In large clinical trials, omalizumab was not associated with changes in serum aminotransferase levels during therapy, and rates of most adverse reactions were similar in patients who received omalizumab or placebo. There have been no published reports of clinically apparent acute liver injury attributed to omalizumab t... | Omalizumab is a human monoclonal antibody and is unlikely to be inherently hepatotoxic. While most recombinant proteins are metabolized by the liver, the metabolism leads largely to small peptides and amino acids which may be reused to synthesize proteins and are unlikely to be toxic or immunogenic. Omalizumab lowers s... | null | Omalizumab – Xolair® | Antiasthmatic Agents | null |
StJohnsWort.nxml | St. John's Wort | 2020-03-28 | St. John’s wort is a popular herbal medication and extract derived from the plant Hypericum perforatum which is purported to be beneficial in depression and anxiety. St. John’s wort has not been implicated convincingly in cases of clinically apparent, acute liver injury, although it may increase the hepatotoxicity of o... | St. John’s wort (saynt jonz wort) is an extract prepared from the flowers and leaves of a flowering plant native to Europe commonly known as St. John’s wort, Tipton’s weed or chase-devil (Hypericum perforatum). St. John’s wort is a yellow flowering perennial herb indigenous to Europe that has been introduced elsewhere.... | Despite wide spread use, there have been no convincing case reports linking use of St. John’s wort and hepatotoxicity. In controlled trials, St. John’s wort has not been linked to serum enzyme elevations or to clinically apparent liver injury. Because of its many herb-drug interactions and effects on the P450 system an... | null | null | St. John’s Wort – Generic | Herbal and Dietary Supplements | null |
Phenotypes_bland.nxml | Bland Cholestasis | 2019-05-04 | null | null | null | null | null | null | null | null |
Palbociclib.nxml | Palbociclib | 2020-05-10 | Palbociclib is a unique cyclin-dependent kinase inhibitor that is used in combination with aromatase inhibitors in the treatment of postmenopausal women with metastatic breast cancer. Palbociclib is associated with transient and usually mild elevations in serum aminotransferase during therapy and to an unusual form of ... | Palbociclib (pal" boe sye' klib) is an orally available, specific inhibitor of cyclin-dependent kinases that is used in combination with aromatase inhibitors in the therapy of postmenopausal women with metastatic breast cancer that is positive for the estrogen receptor (ER+), but negative for human epidermal growth fac... | In the large clinical trials, adverse events were common and led to dose reductions in one-third of patients and discontinuation in 8%. Publications on the efficacy and safety of palbociclib rarely mentioned serum ALT elevations or hepatotoxicity. In a study of women with refractory, metastatic breast cancer, serum ALT... | The possible causes of serum enzyme elevations or liver injury from palbociclib therapy are not known. Palbociclib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury might be caused by production of a toxic or immunogenic intermediate. Because it is a substrate for CYP 3A4, palbociclib is ... | 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 is no evidence to suggest a cross reactivity in risk for adverse events, hypersensitivity or hepatic injury between p... | Palbociclib – Ibrance® | Antineoplastic Agents | null |
Valproate.nxml | Valproate | 2020-07-31 | Valproate or valproic acid is a branched chain organic acid that is used as therapy of epilepsy, bipolar disorders and migraine headaches and is a well known cause of several distinctive forms of acute and chronic liver injury. | Valproate (val proe' ate) is a carboxylic acid derivative that appears to act by increasing brain levels of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the human brain. Valproate has been shown to be effective in several forms of seizures. Valproate was approved for therapy of epilepsy in a... | Prospective studies suggest that 5% to 10% of persons develop ALT elevations during long term valproate therapy, but these abnormalities are usually asymptomatic and can resolve even with continuation of drug. Unlike phenytoin and carbamazepine, valproate does not induce elevations in serum GGT levels. More importantly... | The mechanism of valproate hepatotoxicity is thought to be due to mitochondrial toxicity, perhaps from inhibition of beta oxidation and subsequent loss of mitochondrial function. Valproate is extensively metabolized by the liver and excreted in urine. Valproate therapy lowers tissue carnitine levels which may affect mi... | Valproate hepatotoxicity varies in severity from minimal and asymptomatic ALT elevations to severe liver injury with progressive jaundice, hepatic synthetic dysfunction, coma and death. Monitoring of symptoms and serum aminotransferase levels is recommended for children for the first 6 months of valproate therapy. Valp... | Valproate – Generic, Depakene®, Depakote® | Anticonvulsants | null |
Nicardipine.nxml | Nicardipine | 2017-01-11 | Nicardipine is a second generation calcium channel blocker used in the treatment of hypertension and stable angina pectoris. Nicardipene therapy has been associated with a low rate of transient serum enzyme elevations, but has not been linked convincingly to instances of clinically apparent liver injury with jaundice. | Nicardipine (nye kar' di peen) belongs to the dihydropyridine class of calcium channel blockers and is used in the treatment of both angina pectoris and hypertension. Like other calcium channel blockers, nicardipine acts by blocking the influx of calcium ions into vascular smooth muscle and cardiac cells during depolar... | Nicardipine has not been associated with significant increases in rates of elevations in serum aminotransferase or alkaline phosphatase levels, even with chronic long term therapy. Cases of idiosyncratic liver injury have not been published, although a single instance of marked serum enzyme elevations without jaundice ... | null | null | Nicardipine – Generic, Cardene® | Cardiovascular Agents | null |
Daclizumab.nxml | Daclizumab | 2017-11-10 | Daclizumab is a humanized monoclonal antibody to CD25, the alpha subunit of the IL2 receptor on T lymphocytes, which was used in the past to treat and prevent acute cellular rejection after solid organ transplantation and is currently approved as a second line therapy of refactory relapsing multiple sclerosis. Daclizum... | Daclizumab (da kliz’ ue mab) is a humanized monoclonal immunoglobulin G1 antibody to the alpha subunit of the IL2 receptor (CD25). The IL2 receptor is found on T cells and its engagement results in activation and proliferation of T cells and generation of proinflammatory cytokines. Inhibition of the receptor by antibod... | When given as a part of induction therapy for solid organ transplantation, daclizumab was not linked to instances of serum enzyme elevations or clinically apparent liver injury. While adverse events at the time of organ transplantation are common, they were not found to be more frequent in patients receiving induction ... | null | null | Daclizumab – Zinbryta® | Transplant Agents | null |
Nystatin.nxml | Nystatin | 2020-04-29 | Nystatin is a topical and oral antifungal agent with activity against many species of yeast and candida albicans, which is used largely to treat skin and oropharyngeal candidiasis. Nystatin is not absorbed orally and has not been linked to drug induced liver injury. | Nystatin (nye stat' in) is a polyene macrolide antibiotic that acts by binding to sterols in the plasma membranes of fungi causing the cells to leak, eventually leading to fungal cell death. Nystatin is indicated for the treatment of candidal infections of the skin, mucous membranes and gastrointestinal tract. It is no... | Nystatin therapy has been associated with a low rate of serum enzyme abnormalities, although it has been difficult to attribute these elevations to nystatin. Despite its use for several decades, there have been no convincing cases of acute hepatic injury linked to nystatin therapy. While nystatin is usually is not norm... | The absence of hepatotoxicity from nystatin is probably largely due to lack of absorption.\n\nDrug Class: Antifungal Agents | null | Nystatin – Generic, Mycostatin®, Nystat® | Antifungal Agents | null |
Ivermectin.nxml | Ivermectin | 2021-04-09 | Ivermectin is an antiinfective agent with activity against several parasitic nematodes and scabies and is the treatment of choice for onchocerciasis (river blindness). It is typically given as one or two oral doses. Ivermectin therapy has been associated with minor, self-limiting serum aminotransferase elevations and v... | Ivermectin (eye" ver mek" tin) is a macrocyclic lactone and semisynthetic derivative of avermectin which is produced by Streptomyces avermitilis. Ivermectin has potent activity against several parasites and arthropods. It believed to act by interference with a glutamate gated chloride channel, which interferes with the... | Single dose therapy with ivermectin has been associated with a low rate of serum aminotransferase elevations. A single case of clinically apparent liver injury has been reported after ivermectin use (Case 1). The onset of injury occurred 1 month after a single dose and was characterized by a hepatocellular pattern of s... | Ivermectin acts by interference with chloride channels that are important in neuromuscular activity in parasitic worms and protozoa, but has little activity against mammalian neural transmission. The mechanism by which it might cause liver injury is unknown. | Ivermectin is usually well tolerated and the liver injury reported with its use has been mild and self-limited in course. Ivermectin has not been associated with acute liver failure or chronic liver injury.\n\nDrug Class: Anthelmintic Agents | Ivermectin – Generic, Stromectol® | Anthelmintic Agents | null |
Ponatinib.nxml | Ponatinib | 2020-05-10 | Ponatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of refractory chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome. Ponatinib is commonly associated with transient elevations in serum aminotransferase levels during treatment, but with only rare instances of clinicall... | Ponatinib (poe na’ ti nib) is a broad spectrum inhibitor of the unique BCR-ABL tyrosine kinase receptor, which is the product of a fusion gene resulting from the translocation between chromosomes 9 and 22 that underlies the Philadelphia chromosome of chronic myelogenous leukemia (CML). The abnormal tyrosine kinase rece... | In large clinical trials, elevations in serum aminotransferase levels during ponatinib therapy occurred in up to 56% of patients and were above 5 times upper limit of normal (ULN) in 8% of patients. While these abnormalities were reversible in most patients, they were prolonged or severe in some. Instances of clinicall... | Ponatinib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury may be related to production of a toxic intermediate. Because of this pathway of metabolism, ponatinib is susceptible to drug-drug interactions when using agents that induce or inhibit CYP 3A4. Studies of ponatinib in vitro sugge... | Serum aminotransferase elevations above 3 times the upper limit of normal should lead to dose reduction or temporary cessation, with resumption at a lower dose once levels return to normal. In patients with clinically apparent liver injury and jaundice, ponatinib should be discontinued permanently. Ponatinib, like imat... | Ponatinib – Inclusig® | Antineoplastic Agents | null |
AmpicillinSulbactam.nxml | Ampicillin-Sulbactam | 2020-10-20 | null | The combination of ampicillin (am" pi sil' in) with sulbactam (sul bak' tam) is a parenterally administered, broad spectrum, potent antibiotic which combines a third generation, aminopenicillin with a beta lactamase inhibitor. This combination was approved for use in the United States in 1986. Current indications are f... | Parenteral therapy with ampicillin-sulbactam has been reported to cause transient low level elevations in serum aminotransferase levels in 5% to 10% of patients, but these resolve rapidly once the therapy is stopped, and similar rates of enzyme elevations are found with comparable agents. Clinically apparent liver inju... | The cause of the liver injury associated with ampicillin use is probably hypersensitivity or allergy. Recurrence of hepatic injury has been reported after ampicillin induced liver injury with reexposure. | null | Ampicillin-Sulbactam – Generic, Unasyn® | Antiinfective Agents | null |
Gilteritinib.nxml | Gilteritinib | 2019-01-20 | Gilteritinib is an orally available small molecule inhibitor of FMS-like tyrosine kinase 3 (FLT3) which is used as an antineoplastic agent in the treatment of acute myeloid leukemia with FLT3 mutations. Gilteritinib is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected ... | Gilteritinib (gil" te ri' ti nib) is a potent small molecule inhibitor of FLT3 (FMS-like tyrosine kinase 3), a tyrosine kinase receptor that is mutated in to up one-third of patients with acute myeloid leukemia (AML). The mutated FLT3 activates an intracellular signaling cascade of RAS-MEK-PI3K-AKT-STAT-5, promoting un... | Elevations in serum aminotransferase levels are common during gilteritinib therapy occurring in 78% of patients and rising above 5 times the upper limit of the normal range in 12%. Gilteritinib has had limited clinical use but has not been linked to instances of acute liver injury with symptoms or jaundice. Because of ... | The possible cause of the liver injury due to gilteritinib is not known. Gilteritinib 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. | Gilteritinib 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 discontinuatio... | Gilteritinib – Xospata® | Antineoplastic Agents | null |
Dronabinol.nxml | Dronabinol | 2018-01-15 | Dronabinol is an orally available cannabinoid agonist that is used to treat nausea and vomiting and to stimulate appetite, particularly in patients with wasting disease or cachexia. Dronabinol is associated with a minimal rate of serum enzyme elevations during therapy and has not been linked to cases of clinically appa... | Dronabinol (droe nab’ i nol) is the main isomer of tetrahydrocannabinol, the principal psychoactive constituent of the marijuana plant (Cannabis sativa). Dronabinol is a partial agonist of the cannabinoid receptors which are found in the central nervous system (CB1 receptor), but also peripherally (largely CB2 receptor... | Serum aminotransferase elevations during dronabinol therapy were reported to occur in 6% of treated patients compared to 4.3% in controls who receiving cancer chemotherapy. The aminotransferase elevations were transient, mild-to-moderate in severity, and not associated with symptoms or jaundice. There have been no conv... | Dronabinol is metabolized by the liver and undergoes extensive first-pass metabolism to both active and inactive metabolites. Despite its hepatic metabolism and high level of plasma protein binding, it has not been implicated in causing drug-drug interactions. The lack of reported cases of liver injury due to dronabino... | null | Dronabinol – Generic, Marinol® | Gastrointestinal Agents | null |
VitaminC.nxml | Vitamin C | 2021-05-27 | Vitamin C (ascorbic acid) is a water soluble vitamin found in citrus fruits and green vegetables and deficiency of which is the cause of scurvy. There is no evidence that vitamin C, in physiologic or in moderately high doses, causes acute liver injury or jaundice. | Vitamin C is a water soluble vitamin known chemically as L-ascorbic acid (as kore' bik as' id). The major role of ascorbic acid is as an electron donor and intracellular antioxidant protecting critical intracellular molecules and enzymes systems against reactive oxygen species. Vitamin C also plays a role as a cofactor... | Neither normal nor moderately high intakes of vitamin C are associated with liver injury or liver test abnormalities. In long term clinical trials, serum enzyme and bilirubin elevations were no more frequent with vitamin C therapy than with placebo. Indeed, in many animal models, vitamin C is protective against hepatot... | The serum ALT elevations that occur with extremely high doses of vitamin C are likely due to a direct but minimal toxic effect on the liver. The injury is, however, short lived and has not been linked to cases of acute or chronic hepatitis, acute liver failure or cirrhosis.\n\nDrug Class: Vitamins\n\nOther Drugs in the... | null | Vitamin C – Generic, Combination Products | Vitamins | null |
Desirudin.nxml | Desirudin | 2018-01-03 | Desirudin is a parenterally administered, selective thrombin inhibitor that is used to decrease the risk of deep vein thrombosis and pulmonary embolus in patients undergoing hip replacement surgery. Desirudin has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury with jaund... | Desirudin (des" i roo' din) is a recombinant 65 amino acid peptide analogue of hirudin, the naturally occurring anticoagulant found in the salivary glands of leeches (Hirudo medicinalis). Hirudin is a mixture of similar peptides that actively bind to and inactivate thrombin. Like human antithrombin, hirudin binds to bo... | In the large prelicensure clinical trials of desirudin, serum aminotransferase and alkaline phosphatase elevations were not reported. Furthermore, there have been no case reports of clinically apparent liver injury attributable to desirudin therapy. There have been reports of hypersensitivity reactions to desirudin the... | Desirudin is a recombinant protein and is unlikely to have intrinsic hepatotoxicity. Liver injury during desirudin therapy is clearly rare, if it occurs at all, and would most likely be part of an immunologic reaction to the foreign protein. | There appears to be cross sensitivity to allergic reactions to various preparations of recombinant hirudins and retreatment with desirudin should be avoided.\n\nDrug Class: Antithrombotic Agents, Anticoagulants\n\nOther Drugs in the Subclass, Anticoagulants, Thrombin Inhibitors: Dabigatran | Desirudin – Iprivask® | Antithrombotic Agents | null |
Antithyroid.nxml | Antithyroid Agents | 2014-02-16 | null | null | null | null | null | null | null | null |
Bromocriptine.nxml | Bromocriptine | 2017-07-20 | Bromocriptine is an oral dopamine receptor agonist used predominantly in the therapy of Parkinson disease, but which has other activities including inhibition of prolactin and growth hormone release which has led to its use in acromegaly, infertility and galactorrhea. Bromocriptine therapy is associated with low rate o... | Bromocriptine (broe" moe krip' teen) is a semisynthetic ergot alkaloid derivative which acts as a dopamine receptor agonist. Bromocriptine has strong agonist activity on the D2 class of dopamine receptors and partial antagonist of the D1 receptors in central nervous system. Bromocriptine was approved for use in the Uni... | Bromocriptine has been reported to cause serum aminotransferase elevations in a small proportion of patients, but these abnormalities are usually mild, asymptomatic and self-limiting even without dose adjustment. In rare instances, more marked elevations occur that may require dose modification or discontinuation and w... | Bromocriptine is rapidly removed from the serum by the liver with extensive first pass metabolism. Bromocriptine is metabolized to inactive forms largely by hydrolysis and excreted rapidly. | Most instances of suspected hepatotoxicity of bromocriptine have been mild and self-limited. There have been no reports of acute liver failure or chronic hepatitis due to bromocriptine. There is likely cross sensitivity to hypersensitivity reactions among the different ergot alkaloids, such as pergolide.\n\nDrug Class:... | Bromocriptine – Generic, Parlodel® | Antiparkinson Agents | null |
Mirtazapine.nxml | Mirtazapine | 2020-02-26 | Mirtazapine is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine 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. | Mirtazapine (mir taz' a peen) is a tetracyclic derivative with a somewhat unique antidepressant activity in comparison to the selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants. Its mechanism of action is not well defined, but it is a potent antagonist of serotonin 5-HT2 and 5-HT3 receptors a... | Liver test abnormalities have been reported to occur in up to 10% of patients on mirtazapine, but elevations are usually modest and rarely require dose modification or discontinuation. Rare instances of acute, clinically apparent episodes of liver injury with marked liver enzyme elevations with or without jaundice have... | The mechanism by which mirtazapine causes liver injury is not known. Mirtazapine is extensively metabolized by the liver, mainly via the cytochrome P450 system, predominantly CYP 3A4, and is susceptible to multiple drug-drug interactions with agents that induce or inhibit CYP activity. The metabolic intermediates of mi... | The serum aminotransferase elevations that occur on mirtazapine 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 mirtazapine therapy. Persons with intolerance to mirtazapine may have s... | Mirtazapine – Generic, Remeron® | Antidepressant Agents | null |
Cenobamate.nxml | Cenobamate | 2021-08-18 | Cenobamate is a tetrazole carbamate anticonvulsant used as therapy of partial onset seizures in adults. Cenobamate is associated with a low-to-moderate rate of serum aminotransferase elevations during therapy and has been linked to cases of clinically apparent liver injury usually in the context of a multiorgan hyperse... | Cenobamate (sen” oh bam’ ate) is a novel tetrazole alkyl carbamate anticonvulsant that reduces repetitive neuronal firing by inhibiting voltage-gated sodium channels. It also is a positive allosteric modulator of GABAA ion channels. In several controlled trials, cenobamate was shown to be effective in reducing focal-on... | In controlled clinical trials, addition of cenobamate to standard anticonvulsant therapy was associated with transient, mild-to-moderate serum aminotransferase elevations in 1% to 4% of patients. In the preregistration trials of cenobamate, there were no cases of clinically apparent liver injury with jaundice. However,... | Cenobamate is a carbamate anticonvulsant and is metabolized extensively in the liver via several of the cytochrome P450 enzymes. Cenobamate is a weak inhibitor of CYP 2C19 and an inducer of CYP 2B6, 2C8 and 3A4 and thus capable of causing drug-drug interactions. In higher doses it can cause euphoria and it is classifie... | Patients who have developed serious hypersensitivity reactions to cenobamate should discontinue therapy promptly and avoid reexposure. The potential cross reactivity of hypersensitivity reactions to cenobamate with the aromatic anticonvulsants, such as phenytoin, carbamazepine and lamotrigine, is unknown. The structure... | Cenobamate – Xcopri® | Anticonvulsants | null |
Idelalisib.nxml | Idelalisib | 2022-07-12 | Idelalisib is an oral kinase inhibitor that is approved for use in combination with rituximab in relapsed or refractory chronic lymphocytic leukemia (CLL) and as monotherapy for relapsed follicular B cell, small lymphocytic lymphoma and indolent non-Hodgkin lymphoma. Idelalisib is associated with a high rate of serum e... | Idelalisib (eye del" a lis' ib) is an orally available, small molecule inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), which is an essential component in the B cell signaling pathways that drive migration of B cells to lymph nodes and bone marrow. Inhibition of this pathway inhibits B cell chemotaxis and adhe... | In clinical trials of idelalisib combined with rituximab in patients with CLL and lymphoma, the rates of serum enzyme elevations during therapy ranged from 25% to 35% and were above 5 times the ULN in 5% to 8% (compared to 1% with placebo and rituximab). Severe instances of severe acute hepatocellular injury and acute ... | The reason why idelalisib causes serum enzyme elevations is not known, but may be a direct toxicity to hepatocytes caused by inhibition of PI3K activity or the result of change in B cell activity and caused by induction of autoimmunity. Idelalisib is metabolized primarily by aldehyde oxidase which is present in many ti... | Serum enzyme elevations are not uncommon during cancer chemotherapy with idelalisib and may be dose limiting. Idelalisib should not be used with other agents with hepatotoxic potential. Furthermore, regular monitoring of liver tests every 2 to 4 weeks is recommended during the first six months of idelalisib therapy and... | Idelalisib – Zydelig® | Antineoplastic Agents | null |
Heparin.nxml | Heparin | 2017-11-13 | Standard or unfractionated heparin is a complex mixture of naturally occurring glycosaminoglycans and is used as an anticoagulant to treat venous thrombosis or to prevent thrombosis in high risk patients. Heparin therapy is associated with frequent elevations in serum aminotransferase levels that are typically transien... | Heparin (hep' a rin) is a complex mixture of naturally occurring glycosaminoglycans that have potent anticoagulant activity. Heparin has been used to treat or prevent venous thromboses for more than 50 years. Multiple generic forms of heparin are available, usually in ampoules or vials of 1000 to 40,000 units per mL. H... | Heparin has been associated with transient serum aminotransferase elevations in 10% to 60% of patients, but values are usually less than 5 times the upper limit of normal and are rarely associated with symptoms or jaundice. Values above 5 times the upper limit of normal occur in ~2% of those receiving the high doses of... | The cause of the serum aminotransferase elevations during heparin therapy is not known, but it is likely due to a direct hepatotoxic effect on the liver. The elevations may be accompanied by decreases in platelet counts, another know side effect of heparin therapy. | The serum aminotransferase elevations that occur on heparin therapy are usually self-limited and do not require dose modification or discontinuation of therapy. No convincing instances of clinically apparent, severe acute liver injury have been linked to heparin therapy in the published literature.\n\nReferences to hep... | Heparin – Generic | Antithrombotic Agents | null |
Sulfadiazine.nxml | Sulfadiazine | 2017-12-05 | Sulfadiazine is a sulfonamide antibacterial agent used in the therapy of mild-to-moderate infections due to sensitive organisms. Sulfadiazine, like other sulfonamides, is a well known cause of clinically apparent, idiosyncratic liver injury. | Sulfadiazine (sul" fa dye' a zeen) is an orally administered sulfonamide antibiotic that acts by inhibition of folic acid synthesis, which is required for bacterial replication and growth. Different forms of sulfonamides have been used in clinical medicine since the 1930s. Sulfadiazine was approved for use in the Unite... | Sulfadiazine, like other sulfonamides, causes a characteristic idiosyncratic liver injury which has features of drug-allergy or hypersensitivity. The typical onset is sudden development of fever and rash followed by jaundice within a few days or weeks of starting the medication. The pattern of injury is typically mixed... | The clinical pattern of injury with sulfadiazine suggests a drug-allergy or hypersensitivity mechanism, perhaps through its metabolism to a toxic, reactive or antigenic metabolite. | Sulfadiazine induced liver injury ranges in severity from anicteric and asymptomatic liver enzyme elevations, to symptomatic hepatitis with jaundice to severe acute hepatic failure. Sulfadiazine hepatotoxicity can result in acute liver failure, but most cases resolve rapidly with discontinuation of drug and full recove... | Sulfadiazine – Generic, Microsulfon® | Antiinfective Agents | null |
Trifluridine.nxml | Trifluridine | 2017-04-16 | Trifluridine/tipiracil is the combination of an antineoplastic pyrimidine analogue (trifluridine) with an inhibitor of its metabolism (tipiracil) that is used in the therapy of refractory, metastatic colorectal cancer. Trifluridine/tipiracil is associated with a low rate of transient serum enzyme elevations during ther... | Trifluridine (trye flure' i deen)/tipiracil (tye pir’ a sil) combines an antineoplastic pyrimidine analogue (2-deoxy-5-trifluoromethyl uridine) with a thymidine phosphorylase inhibitor that blocks its rapid metabolism, thus increasing the bioavailability of trifluridine. Trifluridine is absorbed orally and converted in... | Pooled analyses of preregistration clinical trials reported that serum enzyme elevations occurred in up to 24% of patients on trifluridine/tipiracil therapy, but were also elevated in 27% of controls. Similarly, ALT values above 5 times ULN occurred in 2% of trifluridine/tipiracil treated compared to 4% of placebo trea... | Hepatotoxicity from trifluridine/tipiracil appears to be rare and liver test abnormalities are most likely to be due to the underlying condition rather than the drug itself. Trifluridine is metabolized in most cells by thymidine phosphorylase to 5-trilfuorosmethyluracil, which is inactive. Tipiracil is excreted largely... | The serum aminotransferase and alkaline phosphatase elevations that occur during trifluridine/tipiracil therapy are usually transient, asymptomatic and mild. Trifluridine/tipiracil has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. There is no information on cross se... | Trifluridine/Tipiracil – Lonsurf® | Antineoplastic Agents | [
{
"cas_registry_number": "70-00-8",
"molecular_formula": "C10-H11-F3-N2-O5",
"name": "Trifluridine"
},
{
"cas_registry_number": "183204-74-2",
"molecular_formula": "C9-H11-Cl-N4-O2",
"name": "Tipiracil"
}
] |
Lingzhi.nxml | Lingzhi, Reishi | 2024-10-05 | Lingzhi (Ganoderma lingzhi), also known as Reishi (usually Ganoderma lucidum), is a large, reddish-brown mushroom with a distinctive fan-like appearance that is used in traditional Chinese medicine for improving health, restoring vitality, and preventing illness. Lingzhi is well tolerated and has not been associated wi... | Lingzhi (Ganoderma lingzhi or lucidum) is a large, reddish-brown mushroom that grows at the base of trees or on tree stumps. Because it is rare in the wild, it is cultivated using logs, sawdust, or wood chips from deciduous trees. Lingzhi has a distinctive bitter taste, and is used in cooking and in making herbal tea. ... | In multiple small, short term placebo-controlled trials of Lingzhi or Reishi, serum aminotransferase levels did not change during treatment, and there were no reported instances of clinically apparent liver injury or jaundice. Furthermore, Lingzhi and Reishi are not listed in the many reviews of causes of liver injury ... | The mechanism and the ingredient in Reishi and Lingzhi responsible for the liver injury have not been identified. The most characteristic ingredients are polysaccharides and triterpenoids which have been extensively studied in animals and not been linked to liver injury. | Cases of liver injury from Reishi have ranged in severity from minimally symptomatic elevations in serum aminotransferase levels to cases of mild hepatitis resolving rapidly upon stopping to severe hepatitis with symptoms and signs of acute liver failure. Liver injury from Reishi is typically hepatocellular but self-li... | Lingzhi – Generic | Herbal and Dietary Supplements | null |
Levofloxacin.nxml | Levofloxacin | 2020-03-10 | Levofloxacin is a third generation fluoroquinolone that is widely used in the treatment of mild-to-moderate respiratory and urinary tract infections due to sensitive organisms. Levofloxacin has been linked to rare instances of clinically apparent hepatic injury marked by a short latency period and a hepatocellular patt... | Levofloxacin (lee" voe flox' a sin) is the L-enantiomer of ofloxacin and is considered a third generation fluoroquinolone. Like other fluoroquinolones, levofloxacin is active against a wide range of aerobic gram-positive and gram-negative organisms. The fluoroquinolones are believed to act by inhibition of type II DNA ... | In short term studies, levofloxacin has been associated with minor elevations in serum ALT and AST levels in 2% to 5% of patients. The abnormalities were usually asymptomatic and transient and rarely require dose modification. With its wide scale use, levofloxacin has been implicated in in at least 50 instances of clin... | The rapid onset and severe course of levofloxacin associated liver injury suggests hypersensitivity, although allergic manifestations are not always present and are generally mild and transient. | The severity of levofloxacin liver injury ranges from mild and transient serum enzyme elevations to self-limited hepatocellular injury, cholestatic hepatitis, to acute liver failure. In milder cases, complete recovery is expected after stopping the drug and resolution of clinical symptoms and signs is usually rapid (4 ... | Levofloxacin – Generic, Levaquin® | Antiinfective Agents | null |
Fingolimod.nxml | Fingolimod | 2021-08-10 | Fingolimod is an orally available immunomodulatory drug used to treat relapsing multiple sclerosis. Fingolimod is associated with transient serum enzyme elevations during therapy and with rare instances of clinically apparent, acute liver injury that can be severe and even fatal. | Fingolimod (fin gol' i mod) is an immunomodulatory agent that is believed to act by its interaction and binding to sphingosine-1-phosphate (S1P) receptors. Fingolimod is a derivative of myriocin, a metabolite of the fungus Isaria sinclairii and is a structural analogue of sphingosine. Once phosphorylated intracellularl... | In large randomized controlled trials of fingolimod in patients with multiple sclerosis, serum ALT elevations above 3 times ULN were reported in 8% to 14% of fingolimod compared to 2% to 3% of placebo recipients. The enzyme elevations were usually transient and not associated with symptoms or jaundice and required drug... | The mechanism by which fingolimod might cause liver injury is not known. It is extensively metabolized by liver via the cytochrome P450 system, predominantly CYP 4F2, and liver injury may be caused by a toxic or immunogenic intermediate of its metabolism. Despite its interaction with the P450 system, drug-drug interact... | Chronic therapy with fingolimod is associated with mild-to-moderate serum aminotransferase elevations in approximately 10% of patients, and clinically apparent liver injury has occurred with its use, usually shortly after initiation of treatment. Because of the frequency of enzyme elevations detected during therapy and... | Fingolimod – Generic, Gilenya® | Multiple Sclerosis Agents | null |
Kelp.nxml | Kelp | 2024-03-10 | Kelp is a form of seaweed belonging to the order Laminariales that is used as a food and a source of vitamins and minerals, administered as a botanical supplement, and employed in food processing and production of fertilizers. Preparations of kelp are generally recognized as safe, and there is no evidence that they can... | Kelp is a seaweed that grows in nutrient rich coastal waters in temperate and subtropical zones of the world. Kelp is a subgroup of seaweed and refers to several genera of the order Laminariales. The kelp most commonly found in the United States is Laminaria hyperborea. Kelp has multiple uses including as a food, as a ... | While kelp is generally recognized as safe, it has not been formally assessed for hepatic adverse effects or elevations of serum aminotransferase, alkaline phosphatase, or bilirubin levels. However, despite common use, there have been no published case reports of liver injury convincingly attributed to kelp. Large case... | null | null | Kelp – Generic | Herbal and Dietary Supplements | null |
Herbalife.nxml | Herbalife | 2018-04-11 | Herbalife is weight management and nutritional supplement manufacturer that markets herbal and dietary supplements (HDS) for a wide range of conditions, including weight loss, digestive health, heart health, personal care, energy and fitness, general health, wellbeing, and boosting of energy and immunity. There have be... | Herbalife is a for-profit, publically traded company (Herbalife International of America, Inc., Torrance CA) that produces an array of multi-ingredient herbal and nutritional supplements (MINS). The products are not sold in conventional stores or nutrition outlets, but by independent distributors or via the internet. T... | The initial reports of liver injury attributed to Herbalife were from Spain and Israel, with subsequent case series from Latin America, Switzerland, Iceland and the United States. At least 50 instances of clinically apparent liver injury have been described in persons taking Herbalife products. The typical latency has ... | The liver injury attributed to Herbalife products remains unexplained. There was no clear commonality in the products themselves, much less their constituents. Some products contained green tea or aloe vera extracts, both which have been implicated in other forms of HDS liver injury. | The liver injury that has been attributed to Herbalife products has usually been mild-to-moderate in severity and self-limited in course, resolving in 1 to 2 months of stopping the preparations. Rare instances of acute liver failure and even progressive fibrosis and cirrhosis have been reported, but are uncommon and no... | Herbalife® | Herbal and Dietary Supplements | null |
Hyoscyamine.nxml | Hyoscyamine | 2017-07-07 | Hyoscyamine as a natural plant alkaloid derivative and anticholinergic that is used to treat mild to moderate nausea, motion sickness, hyperactive bladder and allergic rhinitis. Hyoscyamine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. | Hyoscyamine (hye" oh sye' a meen) is a derivative of natural alkaloid found in plants of the Solanacea family such as henbane (Hyoscyamus niger, for which it is named), jimson weed (Datura stramonium), tomatoes (Soanum lycopersicum) and deadly nightshade (Atropa belladonna). Hyoscyamine is the levorotary isomer of atro... | Despite widespread use over many decades, hyoscyamine has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. A major reason for its safety may relate to the low daily dose and limited duration of use.\n\nReferences on the safety and potential hepatotoxicity of anticholinergics a... | null | null | Hyoscyamine – Generic, Anaspaz® | Gastrointestinal Agents | null |
Acrivastine.nxml | Acrivastine | 2017-01-16 | Acrivastine is a second generation antihistamine that is used for the treatment of allergic rhinitis. Acrivastine has not been linked to instances of clinically apparent acute liver injury. | Acrivastine (ak" ri vas' teen) is a second generation antihistamine (H1 receptor blocker) that is used to treat allergic symptoms associated with hay fever, seasonal allergies, urticaria, angioedema and atopic dermatitis. Acrivastine, like other second generation antihistamines, is considered to be nonsedating, and pro... | Acrivastine has not been linked to liver enzyme elevations or to instances of clinically apparent liver injury. Its relative safety may relate to its rapid metabolism and use in low dosages.\n\nLikelihood score: E (unlikely cause of clinically apparent liver injury).\n\nReferences on the safety and potential hepatotoxi... | null | null | Acrivastine (with Pseudoephrine) – Semprex-D® | Antihistamines | null |
Penbutolol.nxml | Penbutolol | 2017-01-15 | Penbutolol is a nonselective beta-adrenergic receptor blocker (beta-blocker) used for the therapy of hypertension. Penbutolol has yet to be convincingly associated with clinically apparent liver injury. | Penbutolol (pen bue' toe 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 ca... | Mild-to-moderate elevations in serum aminotransferase levels occur in less than 2% of patients on penbutolol and are usually transient and asymptomatic, resolving even with continuation of therapy. Despite its wide spread use, penbutolol has not been convincingly linked to instances of clinically apparent liver injury.... | Penbutolol undergoes extensive metabolism by the liver and is excreted in the urine as inactive metabolites. The reason why penbutolol 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\nReferences t... | null | Penbutolol – Levatol® | Beta-Adrenergic Receptor Antagonists | null |
Nateglinide.nxml | Nateglinide | 2019-05-21 | Nateglinide is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury. | Nateglinide (na teg' li nide) is an insulin secretagogue that is similar in action but different in structure from the sulfonylureas. It is a derivative of phenylalanine and stimulates insulin secretion by blocking ATP sensitive potassium channels in pancreatic beta-cells, causing cell membrane depolarization which res... | In several large clinical trials, serum aminotransferase elevations were no more common with nateglinide than with placebo. The enzyme elevations that occurred were asymptomatic and resolved rapidly with stopping therapy. Since its approval and with wide scale use, the FDA and the sponsor have received reports of clini... | The mechanism of nateglinide induced liver injury is not known, but nateglinide is extensively metabolized by the liver via the P450 system (CYP 2C9 and 3A4), and liver injury may be the result of production of a toxic or immunoreactive intermediate. | There is no information on results of rechallenge on cross sensitivity to hepatic damage among the various metiglinides. Reexposure and use of other metiglinides after clinically apparent liver injury related to nateglinide should be done with caution.\n\nReferences regarding the safety and hepatotoxicity of nateglinid... | Nateglinide – Generic, Starlix® | Antidiabetic Agents | null |
Mavyret.nxml | Mavyret | 2022-02-07 | Mavyret is an oral, fixed combination of two antiviral agents, glecaprevir and pibrentasivir used to treat chronic hepatitis C virus (HCV) infection due to any genotype (1 through 6). This combination has not been linked to instances or worsening of serum enzymes during therapy or with de novo appearance of clinically ... | Mavyret is the commercial name for a fixed combination of oral antiviral agents used to treat chronic hepatitis C virus infection of all genotypes (1 through 6). The hepatitis C virus encodes several nonstructural (NS) polypeptides that are essential for its replication, including NS3/4 that has protease and helicase a... | In large randomized controlled trials, serum aminotransferase levels decreased rapidly during Mavyret therapy and there were only rare instances of late, de novo elevations in ALT or AST that were usually mild-to-moderate in degree and rising to more than 5 times ULN in less than 1% of treated subjects. In addition, Ma... | The mechanism by which glecaprevir and pibrentasvir might cause liver injury is not known. Both are metabolized in the liver largely via the cytochrome P450 system, predominantly CYP 1A2, and liver injury may be due to production of a toxic or immunogenic metabolite. Mavyret is also susceptible to drug-drug interaction... | While 8 to 16 weeks of therapy with Mavyret can be associated with transient mild-to-moderate serum aminotransferase elevations, it has not been convincingly linked to cases of clinically apparent idiosyncratic liver injury. Nevertheless, Mavyret is labelled as having the potential of causing decompensation of preexist... | Glecaprevir, Pibrentasvir – Mavyret® | Hepatitis C Agents | [
{
"cas_registry_number": "1365970-03-1",
"molecular_formula": "C38-H46-F4-N6-O9-S",
"name": "Glecaprevir"
},
{
"cas_registry_number": "1353900-92-1",
"molecular_formula": "C57-H65-F5-N10-O8",
"name": "Pibrentasvir"
}
] |
Orlistat.nxml | Orlistat | 2020-06-04 | Orlistat is an inhibitor of pancreatic and gastric lipase and a commonly used weight loss agent that is available both by prescription and over-the-counter. Orlistat has been linked to rare instances of acute liver injury, some of which have been severe. | Orlistat (or' li stat) is a tetrahydrolipstatin, a saturated derivative of lipstatin which is a potent natural inhibitor of gastric and pancreatic lipase. Orlistat when taken with meals inhibits the digestion of dietary fats and prevents their absorption, thus reducing caloric intake. When used in conjunction with calo... | Orlistat acts my binding pancreatic and gastric lipase in the intestinal tract. Systemic absorption is not needed for its effect. Indeed, little of orally administered orlistat is absorbed (1% to 3%) and plasma levels are usually undetectable or less than 4 ng/mL (too little to inhibit serum lipase activities). Thus, s... | The mechanism by which orlistat causes liver injury is not known. Because only small amounts of orlistat are absorbed, hypersensitivity is likely the mechanism by which the liver is damaged. However, typical features of hypersensitivity have not been prominent in case reports. | The liver injury that occurs during orlistat therapy ranges in severity from minor serum aminotransferase elevations to acute symptomatic hepatitis to severe acute liver failure that can be fatal or require emergency liver transplantation. There is no known therapy for orlistat induced liver injury. Recurrence of injur... | Orlistat – Generic, Alli®, Xenical® | Weight Loss Agents | null |
Dacomitinib.nxml | Dacomitinib | 2019-04-15 | Dacomitinib is a multi-kinase receptor inhibitor used in the therapy of cases of non-small cell lung cancer that harbor activating mutations in the epidermal growth factor receptor gene (EGFR). Dacomitinib is associated with high rate of transient serum aminotransferase elevations during therapy but has not been linked... | Dacomitinib (dak" oh mi' ti nib) is a multi-kinase inhibitor with potent activity against epidermal growth factor receptor 2 genes (HER1, HER2 and HER4), members of the ErbB family of EGFRs. These receptors are often mutated and over expressed in cancer cells, particularly non-small cell lung cancer (NSCLC) and some fo... | In large early clinical trials, elevations in serum aminotransferase levels were common during dacomitinib therapy, arising in 40% of patients treated with standard doses. However, most elevations were transient and asymptomatic, and they rarely led to dose modification or discontinuation. Serum ALT elevations above 5 ... | The cause of the liver injury due to dacomitinib is unknown. Serum enzyme elevations are common during antineoplastic therapy with tyrosine kinase inhibitors, particularly those that target EGFR. The mechanism of injury is unknown but may relate to inhibition of other kinase activities. Dacomitinib is metabolized in th... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose interruption. If changes persist, are severe or associated with symptoms or jaundice, or reoccur on restarting, dacomitinib should be discontinued. There have been no published reports of acute liver failure, ch... | Dacomitinib – Vizimpro® | Antineoplastic Agents | null |
Deuruxolitinib.nxml | Deuruxolitinib | 2024-11-07 | Deuruxolitinib is an orally available small molecule inhibitor of Janus kinases that is used to treat severe alopecia areata. Deuruxolitinib is associated with a low rate of transient and usually mild elevations in serum aminotransferase levels during therapy but has not been linked to cases of clinically apparent acut... | Deuruxolitinib (dew rux” oh li’ ti nib) is an orally available, specific inhibitor of Janus-associated kinases (greater inhibition of JAK1, JAK2, and TYK2 relative to JAK3) that is used to treat moderate-to-severe alopecia areata. Alopecia areata is an autoimmune disorder that is characterized by hair loss resulting in... | In the prelicensure clinical trials in alopecia areata, serum aminotransferase elevations occurred in less than 1% of deuruxolitinib-treated subjects and there were no instances of ALT or AST elevations accompanied by symptoms or jaundice. The elevations were typically mild and transient and did not lead to dose adjust... | The mechanism by which deuruxolitinib might cause liver injury is not known. It is metabolized in the liver, largely via CYP 2C9 and to a lesser extent by 3A4. High levels can arise in patients who are slow metabolizers by CYP 2C9 and the product label recommends testing patients for CYP 2C9 metabolized status before i... | Serum aminotransferase elevations are uncommon during deuruxolitinib therapy, and routine monitoring of liver tests is not recommended in the product label. If aminotransferase elevations above 5 times the upper limit of normal (ULN) arise, deuruxolitinib therapy should be interrupted, at least temporarily, until level... | Deuruxolitinib – Leqselvi® | Dermatologic Agents | null |
Enfuvirtide.nxml | Enfuvirtide | 2018-02-10 | Enfuvirtide is an HIV fusion inhibitor, the first of this class of agents active against the human immunodeficiency virus (HIV). Enfuvirtide has not been associated with serum aminotransferase elevations during therapy or episodes of acute, clinically apparent liver injury. | Enfuvirtide (en fue' vir tide) is relatively new antiretroviral drug that blocks the fusion of HIV to target cell, preventing viral entry and subsequent infection. Enfuvirtide is a 36 amino acid biomimetic peptide that resembles the HIV proteins that are responsible for the fusion of the virus to cell membranes and sub... | Enfuvirtide has not been reported to cause serum aminotransferase elevations at rates higher than in controls receiving similar antiretroviral therapy. No instances of clinically apparent liver injury due to enfuvirtide have appeared in the published literature. Enfuvirtide has, however, not been a widely used agent. P... | Enfuvirtide is a polypeptide and is catabolized to its constituent amino acids and rapidly cleared from the circulation. Hepatic metabolism is minimal and enfuvirtide does not affect the CYP 450 system. | If enfuvirtide hepatotoxicity occurs independent of minor aminotransferase elevations accompanying hypersensitivity reactions, it must be rare. Nevertheless, the product label for enfuvirtide mentions the possibility of toxic hepatitis and steatosis.\n\nDrug Class: Antiviral Agents | Enfuvirtide – Fuzeon® | Antiviral Agents | null |
Daclatasvir.nxml | Daclatasvir | 2022-02-07 | Daclatasvir is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and was used in combination with other oral antiviral agents to treat chronic hepatitis C before its withdrawal in 2019. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has y... | 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 t... | In large randomized controlled trials, daclatasvir was not associated with serum enzyme elevations during therapy. A difficulty in assessing side effects of daclatasvir and other anti-HCV agents, however, was that they are never used as monotherapy, but were also combined with agents active against other HCV targets, s... | The mechanism by which daclatasvir might cause liver injury is not known. It is metabolized in the liver largely via the cytochrome P450 system, predominantly CYP 3A4 and liver injury may be due to production of a toxic or immunogenic metabolite. Daclatasvir is also susceptible to drug-drug interactions with strong CYP... | Daclatasvir in combination with other potent direct acting agents for hepatitis C (such as sofosbuvir) has been associated with instances of hepatic decompensation in patients with preexisting cirrhosis. For these reasons, monitoring of liver tests is recommended, particularly during the first 4 weeks of therapy. Treat... | Daclatasvir – Daklinza® | Hepatitis C Agents | null |
Ampicillin.nxml | Ampicillin | 2020-10-20 | null | Ampicillin (am" pi sil' in) is an oral, third generation penicillin that is one of the most commonly used antibiotics worldwide. Ampicillin has been available in the United States since the mid-1960s and continues to be widely used for bacterial infections in both children and adults. Ampicillin is indicated for mild-t... | Rare instances of idiosyncratic liver injury have been reported in persons receiving the aminopenicillins. The incidence is far lower with ampicillin than occurs with amoxicillin, occurring probably in less than 1 in 100,000 exposed persons. Cases are characterized by a short latency period of a few days to as long as ... | The cause of the liver injury associated with ampicillin use is probably hypersensitivity or allergy. Cases of recurrence upon rechallenge or reexposure have been reported. | In the few cases of ampicillin related acute liver injury that have been described, most patients have recovered, although recovery has been slow in some cholestatic instances (2 to 6 months). Rare instances of acute liver failure and several cases of vanishing bile duct syndrome have been reported with ampicillin indu... | Ampicillin – Generic, Principen® | Antiinfective Agents | null |
VitaminB.nxml | Vitamin B | 2021-05-27 | Vitamin B refers to several water soluble vitamins often found together in foods, all of which are necessary for normal growth and metabolism, but none of which are synthesized in adequate amounts by humans. The common forms of vitamin B include vitamin B1 (thiamine), B2 (riboflavin), B3 (niacin), B6 (pyridoxine) and B... | null | null | null | null | Vitamin B1, Thiamine – Generic, Combination Products | Vitamins | [
{
"cas_registry_number": "58-85-5",
"molecular_formula": "C10-H16-N2-O3-S",
"name": "Biotin"
},
{
"cas_registry_number": "62-49-7",
"molecular_formula": "C5-H14-N-O",
"name": "Choline"
},
{
"cas_registry_number": "68-19-9",
"molecular_formula": "C63-H88-Co-N14-O14-P",
"na... |
Streptomycin.nxml | Streptomycin | 2021-09-15 | Streptomycin is a broad spectrum aminoglycoside antibiotic typically used for treatment of active tuberculosis, always in combination with other antituberculosis agents. Streptomycin is usually used in combination with agents that are known to be hepatotoxic and the role of streptomycin in liver injury has been difficu... | Streptomycin (strep" toe mye' sin), an aminoglycoside antibiotic, must be given by parenteral injection and is now considered a second line antituberculosis agent, used largely when toxicity has limited use of first line agents. Like other aminoglycosides, streptomycin is thought to act by binding to bacterial ribosome... | Intravenous and intramuscular therapy with streptomycin has been linked to mild and asymptomatic elevations in serum alkaline phosphatase, but therapy rarely affects aminotransferase levels or bilirubin and changes typically resolve rapidly once streptomycin is stopped. Only isolated case reports of acute liver injury ... | 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 the inner ear, perhaps explaining why they are more likely to cause nephro- or oto- rather than hepatotoxicity.\n\n[First line medications us... | null | Streptomycin – Generic | Antituberculosis Agents | null |
Leflunomide.nxml | Leflunomide | 2019-04-15 | Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis. Leflunomide therapy is associated with frequent elevations in serum aminotransferase levels and with rare instances of clinically apparent acute liver injury which can be severe and even fatal. | Leflunomide (le floo' noe mide) is an isoxazole derivative that is rapidly converted to its active metabolite teriflunomide (ter" i floo' noe mide: A77-1726) in the gut wall and liver. Leflunomide acts by inhibition of dihydroorotate dehydrogenase, which is a rate limiting step in pyrimidine synthesis necessary for DNA... | Up to 15% of subjects treated with leflunomide develop transient serum aminotransferase elevations that are usually asymptomatic and mild, in the range of 1 to 3 times the upper limit of normal (ULN). Elevations above 3 times the ULN occur in 1% to 4% of patients.\n\nIn addition, leflunomide is associated with rare ins... | The hepatic injury due to leflunomide is thought to be due to production of a toxic intermediate. Leflunomide is extensively metabolized by the liver and is a potent inhibitor of CYP 2C9. Hepatotoxicity of leflunomide has been linked to the cytochromic alleleic variants CYP 2C9*2 and *3, both of which are associated wi... | The mild ALT elevations associated with leflunomide therapy are usually asymptomatic, self limited and rarely require dose modification or discontinuation. Nevertheless, monitoring of serum enzymes is recommended, monthly for the first 6 months and then every other month. In instances in which ALT levels rise above 3 t... | Leflunomide – Generic, Arava® | Antirheumatic Agents | null |
Mefloquine.nxml | Mefloquine | 2017-02-07 | Mefloquine is a quinoline derivative used for the prevention and therapy of P. falciparum malaria. Mefloquine therapy is associated with a low rate of transient and asymptomatic serum enzyme elevations and is a rare cause of clinically apparent acute liver injury. | Mefloquine (mef' loe kwin) is a quinoline methanol similar to quinine and is active against the asexual stages of malaria. Its exact mechanism of activity is unknown. Mefloquine is effective as prophylaxis against malaria and is widely used in therapy against chloroquine-resistant P. falciparum infection. Unfortunately... | Chronic therapy with mefloquine is associated with asymptomatic, transient serum enzyme elevations in up to 18% of patients. These elevations are usually mild and resolve without dose modifications. Despite widespread use, mefloquine has rarely been linked to clinically apparent acute liver injury and too few reports a... | The cause of the hepatic injury from mefloquine is unknown, but may relate to a metabolic intermediate with direct toxicity or ability to induce an immune mediated hepatotoxicity. Mefloquine undergoes extensive hepatic metabolism to an inactive metabolite that is excreted 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 | Mefloquine – Generic, Lariam® | Antimalarial Agents | null |
Lumateperone.nxml | Lumateperone | 2023-06-05 | Lumateperone is a second generation (atypical) antipsychotic agent that is used in the treatment of schizophrenia. Lumateperone 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. | Lumateperone (loo” ma te’ per one) is a second generation antipsychotic agent which appears to act as a serotonin (5-HT)-2A receptor and dopamine type 2 (D2) antagonist and is similar in structure and mechanism of action to paliperidone. It has low affinity for histamine-1 and alpha adrenergic-1 receptors and also is a... | In preregistration controlled trials, ALT elevations arose in 2% of patients receiving lumateperone compared to less than 1% of placebo controls. The elevations, however, were usually mild, transient and typically resolved without dose modification or drug discontinuation. In preregistration trials, there were no insta... | The mechanism by which lumateperone might cause serum ALT elevations or liver injury is not known. Lumateperone is metabolized in the liver by multiple enzymes include CYP 3A4, 2C8 and 1A2 and drug-drug interactions may occur with agents that are strong inhibitors or inducers of hepatic microsomal enzymes. | The serum aminotransferase elevations that occur on lumateperone therapy are usually self-limited and often do not require dose modification or discontinuation. No instances of acute liver failure, chronic hepatitis or vanishing bile duct syndrome have been attributed to lumateperone. Cross sensitivity to liver related... | Lumateperone – Caplyta® | Antipsychotic Agents | [
{
"cas_registry_number": "313368-91-1",
"molecular_formula": "C24-H28-F-N3-O",
"name": "Lumateperone"
},
{
"cas_registry_number": "144598-75-4",
"molecular_formula": "C23-H27-F-N4-O3",
"name": "Paliperidone"
}
] |
Prasugrel.nxml | Prasugrel | 2020-09-15 | Prasugrel is an inhibitor of platelet aggregation that is used to decrease the risk of myocardial infarction and stroke in patients with acute coronary syndromes. Prasugrel has been linked to mild and transient serum enzyme elevations during therapy and to rare instances of hypersensitivity reactions accompanied by mil... | Prasugrel (pra' soo grel) is a thienopyridine inhibitor of adenosine diphosphate (ADP) receptors (P2Y12) on platelets, and is used as an anticoagulant to decrease the risk of recurrent coronary thromboses in patients who undergo interventions during an acute coronary syndrome. Activated platelets release ADP which bind... | Prasugrel is associated with low rates of serum enzyme elevations during therapy, which are similar to those with clopidogrel. In premarketing studies, no instances of clinically apparent liver injury were reported. Since marketing and release, there has been several reports of liver injury attributed to prasugrel ofte... | The mechanism of prasugrel hepatotoxicity is not known, but is likely to be immunologically mediated and due to hypersensitivity. Prasugrel requires metabolic activation for its antiplatelet effects, which occurs in the liver primarily via the cytochrome P450 system, CYP 3A4 and 2B6. Inhibitors of CYP 3A4 (such as clar... | The severity of liver injury associated with prasugrel has been mild and rapidly reversible with stopping therapy. In one instance, switching anticoagulant therapy to clopidogrel was tolerated without recurrence. Rechallenge should be avoided.\n\nDrug Class: Antithrombotic Agents, Antiplatelet Agents\n\nOther Drugs in ... | Prasugrel – Generic, Effient® | Antithrombotic Agents | null |
Linezolid.nxml | Linezolid | 2019-06-06 | Linezolid is an oxazolidinone class antibiotic that is used for serious or problematic infections caused by resistant enterococcal or staphylococcal organisms. Prolonged therapy with linezolid has been linked to rare instances of lactic acidosis and liver injury probably as a result of hepatic mitochondrial toxicity. | Linezolid (lin ayz' oh lid) is a synthetic antibiotic that belongs to the oxazolidinone class. It has broad bacteriocidal activity against gram positive organisms such as enterococci and staphylococci and most streptococci. It also has moderate activity against Mycobacterium tuberculosis. Linezolid acts by blocking bac... | Therapy with linezolid has been associated with mild and transient elevations in serum aminotransferase and alkaline phosphatase levels in 1% to 10% of patients, although similar rates of elevations occur in patients with infections treated with comparable agents, and enzyme elevations were not found in normal voluntee... | The etiology of serum enzyme elevations during linezolid therapy is not known and may relate more to the underlying condition rather than injury from linezolid. Lactic acidosis and peripheral neuropathy from linezolid are probably due to inhibition of mitochondrial ribosomal function and protein synthesis. Indeed, a mi... | The serum aminotransferase and alkaline phosphatase elevations that occur during linezolid therapy are self-limited and resolve once therapy is stopped. There are no reports of cross sensitization and hepatic injury from linezolid in persons with hepatic injury from other antibiotics or sulfonamides. The lactic acidosi... | Linezolid – Zyvox® | Antiinfective Agents | null |
BempedoicAcid.nxml | Bempedoic Acid | 2023-07-15 | Bempedoic acid is a small molecule inhibitor of adenosine triphosphate-citrate lyase that is used as a cholesterol lowering agent in patients with hypercholesterolemia and high risk or with known atherosclerotic cardiovascular disease who fail to have an adequate response or are intolerant of conventional statin therap... | Bempedoic (bem” pe doe’ ik) acid is an orally available, small molecule inhibitor of adenosine triphosphate-citrate lyase (ACL), a hepatic enzyme involved in cholesterol synthesis. Inhibition of ACL results in a lowering of intrahepatic cholesterol levels which leads to an increase in LDL cholesterol (LDL-C) receptors ... | Bempedoic acid is associated with low rate of mild, asymptomatic and typically transient serum aminotransferase elevations during therapy. In prelicensure controlled trials, elevations in either ALT or AST arose in 2% of treated patients compared to less than 1% of placebo recipients. ALT elevations above 3 times the u... | The potential cause of hepatic injury from bempedoic acid is unknown. It is metabolized in the liver (via CYP 2C9). The mild, self-limited ALT elevations may be due to a toxic intermediate of drug metabolism and the reversal of these elevations due to adaptation. | The serum enzyme elevations that sometimes arise in patients taking bempedoic acid generally resolve even without dose modification or discontinuation. There is no evidence for cross sensitivity to hepatic injury among the various cholesterol lowering drugs.\n\nDrug Class: Antilipemic Agents\n\nOther Drugs in the Subcl... | Bempedoic Acid – Nexletol® | Antilipemic Agents | null |
Voclosporin.nxml | Voclosporin | 2021-08-30 | Voclosporin is an orally available calcineurin inhibitor and potent immunosuppressive agent which is used in combination with mycophenolate mofetil and corticosteroids to treat acute lupus nephritis. Voclosporin may be associated with low rate of transient serum enzyme elevations during treatment but has not been linke... | Voclosporin (voe” kloe spor’ in) is a potent immunosuppressive agent that is used as therapy for patients with systemic lupus erythematosus and acute lupus nephritis. Voclosporin is a derivative of cyclosporin A, a cyclic polypeptide of 11 amino acids, initially isolated from a fungus species (Beauveria nivea). Cyclosp... | In large randomized controlled trials of voclosporin, serum aminotransferase levels were transiently elevated in 3% of patients, but rates were similar in controls receiving conventional therapy (2%). Similar to cyclosporine, voclosporin therapy is associated with minor increases in alkaline phosphatase and bilirubin l... | The mechanism by which voclosporin might cause liver injury is unknown. Other calcineurin inhibitors such as cyclosporine and tacrolimus are associated with serum enzyme elevations and rare instances of cholestatic liver injury. Voclosporin is metabolized in the liver, largely by CYP 3A4 and is susceptible to drug-drug... | Serum enzyme elevations during therapy with voclosporin are generally mild and without accompanying symptoms or jaundice. Appearance of liver injury during therapy should lead to a search for other possible causes. But if none are found, dosing should be interrupted if values rise above 5 times the upper limit of norma... | Voclosporin – Lupkynis® | Immunosuppressive Agents | [
{
"cas_registry_number": "515814-01-4",
"molecular_formula": "C63-H111-N11-O12",
"name": "Voclosporin"
},
{
"cas_registry_number": "59865-13-3",
"molecular_formula": "C62-H111-N11-O12",
"name": "Cyclosporine"
}
] |
Panobinostat.nxml | Panobinostat | 2020-09-25 | Panobinostat is an oral histone deacetylase inhibitor and antineoplastic agent that is approved for use in combination with other agents in refractory or relapsed multiple myeloma. Panobinostat is associated with modest rate of minor serum enzyme elevations during therapy, but has not been linked to cases of clinically... | Panobinostat (pan" oh bin' oh stat) is an oral small molecule inhibitor of histone deacetylases, thereby preventing removal of acetyl groups from histones. The accumulation of acetyl groups on histones causes cell cycle arrest and apoptotic cell death. Malignant cells are particularly sensitive to the effects of inhibi... | Most clinical trials of panobinostat have not reported rates of serum enzyme elevations during therapy and it is typically given in combination with other antineoplastic agents that can cause serum ALT and AST elevations. In the large controlled trial of panobinostat vs placebo in combination with bortezomib and dexame... | The reason why panobinostat might cause serum enzyme elevations is not known, but may be a direct toxicity to hepatocytes caused by inhibition of histone deacetylase or other enzyme activities. Panobinostat is extensively metabolized in the liver by the cytochrome P450 system (predominantly CYP 3A4 and 2D6) and drug-dr... | Serum enzyme elevations are uncommon during panobinostat therapy and are rarely dose limiting. Nevertheless, regular monitoring of liver tests with each course of therapy is recommended with more frequent monitoring if serum aminotransferase values rise. Panobinostat should be held if ALT or AST values rise above 5 tim... | Panobinostat – Farydak® | Antineoplastic Agents | null |
Tenofovir.nxml | Tenofovir | 2020-10-20 | Tenofovir is an acyclic nucleotide analogue of adenosine used in combination with other agents in the therapy of the human immunodeficiency virus (HIV) and as single agent in hepatitis B virus (HBV) infection. Tenofovir does not appear to be a significant cause of drug induced liver injury. | Tenofovir (ten of' oh vir) is an acyclic nucleotide analogue of adenosine, but is poorly absorbed orally. For this reason, the prodrug is used, either tenofovir disoproxil fumarate or more recently tenofovir alafenamide, which are well absorbed from the intestines, rapidly hydrolyzed to tenofovir intracellularly and th... | Like all nucleoside analogues used as therapy of hepatitis B, tenofovir can cause transient increases in serum aminotransferases during or after therapy. These abnormalities appear to be due to an exacerbation or flare of the underlying hepatitis B. Three types of flares due to nucleoside analogue therapy have been des... | The majority of cases of lactic acidosis and hepatic failure in patients receiving tenofovir appear to be due to didanosine, stavudine or zidovudine coadministration. Addition of tenofovir to an antiretroviral regimen including didanosine concurrently can increase didanosine concentrations by up to 60%, thus amplifying... | The minor ALT elevations associated with initiation of tenofovir therapy in chronic hepatitis B are usually asymptomatic and transient. Care should be taken in stopping tenofovir therapy in patients with chronic HBV infection. If administered concurrently with tenofovir, didanosine should be reduced in dosage and patie... | Tenofovir (Tenofovir disoproxil fumarate) – Generic, Viread® | Antiviral Agents | null |
Decitabine.nxml | Decitabine | 2023-07-27 | Decitabine is a cytosine analogue and an intravenously administered antineoplastic agent used in the therapy of myelodysplastic syndromes. Decitabine is associated with a low rate of transient serum enzyme elevations during therapy, but has not been implicated in causing clinically apparent liver injury with jaundice. | Decitabine (dee sye' ta been) is a pyrimidine analogue (5-aza-deoxy-cytidine) which is the deoxyribose form of 5-azacitidine. Decitabine is converted intracellularly to a triphosphate which becomes incorporated into DNA and appears to inhibit DNA methylation, resulting in increased expression of silenced genes includin... | In early clinical trials using high doses of decitabine, serum enzyme elevations occurred in up to 16% of patients with underlying liver disease or liver metastases, but rarely in persons without hepatic illness. In subsequent studies, serum ALT elevations were reported in 5% to 15% of treated patients, but all were se... | Hepatotoxicity from decitabine appears to be rare and confined mostly to asymptomatic elevations in serum enzymes in patients receiving the highest doses or with underlying liver disease. Thus, the liver injury is likely due to direct toxicity which is generally minimal or mild except in susceptible patients. | The severity of the liver injury linked to decitabine therapy is usually mild in severity and without accompanying symptoms or jaundice. Decitabine has not been linked to cases of severe acute hepatitis, acute liver failure, chronic hepatitis or vanishing bile duct syndrome. There is no information on cross sensitivity... | Decitabine – Generic, Dacogen® | Antineoplastic Agents | null |
Pasireotide.nxml | Pasireotide | 2017-04-20 | Pasireotide is a synthetic polypeptide analogue of somatostatin that resembles the native hormone in its ability to suppress levels and activity of growth hormone, insulin, glucagon and many other gastrointestinal peptides. Because its half-life is longer than somatostatin, pasireotide can be used clinically to treat n... | Pasireotide (pa" ze ree' oh tide) is a synthetic octapeptide and analogue of somatostatin that is used for its ability to suppress levels and activities of hormones (growth hormone, insulin, gastrin, secretin, glucagon) or active neuropeptides (serotonin, vasoactive intestinal polypeptide [VIP]). Natural somatostatin i... | Mild, transient, asymptomatic elevations in serum aminotransferase levels occur in up to 29% of patients receiving pasireotide LAR, but elevations above 5 times the upper limit of normal are rare (<1%) and no case of clinically apparent liver injury with jaundice was reported in the preregistration trials of pasireotid... | Pasireotide, like somatostatin, decreases cholecystokinin secretion, gall bladder contractility and bile secretion, perhaps accounting for the high rate of gall bladder sludge and stone formation with long term use. How infusions of pasireotide might cause acute liver injury independent of its effect on bile flow and g... | The product label for pasireotide recommends evaluation of “liver enzyme test prior to and during treatment.” The liver test abnormalities during pasireotide therapy generally resolve rapidly with stopping therapy, but may resolve even with drug continuation. Patients should be monitored if pasireotide is restarted aft... | Pasireotide – Signifor®, Signifor LAR® | Hormonal Agents | [
{
"cas_registry_number": "108736-35-2",
"molecular_formula": "C54-H69-N11-O10-S2",
"name": "Lanreotide"
},
{
"cas_registry_number": "83150-76-9",
"molecular_formula": "C49-H66-N10-O10-S2",
"name": "Octreotide"
},
{
"cas_registry_number": "396091-73-9",
"molecular_formula": "C... |
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