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Ephedra.nxml | Ephedra | 2018-02-10 | Ephedra is a genus of plants one species of which is known as Ma Huang (Ephedra sinica), which has been used in traditional Chinese medicine for centuries as a stimulant and antiasthmatic agent, and was recently introduced into use in the United States and Europe as a weight loss agent and aid in body building. Ma Huan... | Ephedra is prepared from the aerial parts of plants belonging to the genus Ephedra, family Ephedraceae. The 45 species of Ephedra are found worldwide, but Ephedra sinica is used predominantly and is native to China where it was first used therapeutically. Ephedra sinica is an herbaceous perennial with a strong pine odo... | Despite its apparent safe use for centuries in Chinese traditional medicine, Ma Huang was linked to many serious and potential fatal side effects since its widescale use in Western countries for weight loss. The major reported serious adverse events were cardiovascular, including hypertension, palpitations, myocardial ... | Ephedra sinica extracts contain multiple compounds including the sympathomimetic alkaloids ephedrine, pseudoephedrine, methylephedrine and norephedrine. The cardiovascular side effects and complications of ephedra use have been attributed to these sympathomimetic constituents. The liver injury has been attributed to ep... | The severity of liver injury due to ephedrine ranges from mild, asymptomatic elevations in serum enzymes to clinically apparent acute liver injury and to acute liver failure. Chronic use of Ma Huang has been linked to a chronic hepatitis-like syndrome, but recovery was prompt when ephedra was stopped. There have been n... | Ephedra – Generic | Herbal and Dietary Supplements | null |
ShouWuPian.nxml | Polygonum Multiflorum | 2020-08-18 | Polygonum multiflorum is an herb native to China, extracts of which has been used for centuries as a treatment for a wide range of conditions including backache, dizziness, liver disease, graying of the hair and constipation. P. multiflorum is also known as Shou Wu Pian, He Shou Pian, Fo-Ti and Chinese knotweed. Polygo... | Polygonum multiflorum is a commonly used and ancient Chinese herbal remedy prepared from the root of the tuber, Polygonum multiflorum, known as the Chinese climbing knotweed (Fo Ti). Fo Ti is a plant native to China which has been cultivated widely elsewhere, including the United States. Extracts of the roots of Polygo... | Several published cases and a large case series from China, Korea and Japan of clinically apparent acute liver injury have been attributed to use of Polygonum multiflorum. Indeed, in China Polygonum multiflorum is reported to be the most common cause of herbal product related liver injury. The latency to onset is usual... | The mechanism of hepatotoxicity of Polygonum multiflorum is not known, but the injury is usually attributed to the anthraquinones (such as emodin) which are major constituents in Polygonum multiflorum. In a single report, the major compound identified in the recovered tablets was a stilbene glycoside, tetrahydroxystilb... | Hepatotoxicity from Polygonum multiflorum is usually self-limited but can be prolonged and is occasionally fatal. Recurrence with restarting the herb is common and rechallenge should be avoided. There is little evidence for cross sensitivity to the hepatotoxic effects of other herbal medications. Use of corticosteroids... | Shou Wu Pian – Generic | Herbal and Dietary Supplements | null |
SickleCellAg.nxml | Sickle Cell Disease Agents | 2021-07-07 | Sickle cell disease is caused by an inherited mutation in the β globin gene that creates hemoglobin S, an abnormal form of hemoglobin which is prone to polymerization when exposed to low oxygen tension which results in sickling of red blood cells, hemolytic anemia, vascular occlusion of small vessels, ischemic tissue a... | Sickle cell disease is caused by an inherited mutation in the β globin gene that creates hemoglobin S, an abnormal form of hemoglobin which is prone to polymerization with deoxygenation resulting in sickling of red blood cells, hemolytic anemia, vascular occlusion of small vessels, ischemic tissue and organ injury and ... | None of the four approved drugs for sickle cell disease have been associated with serious hepatotoxicity. Low rates of transient, asymptomatic, mild-to-moderate serum enzyme elevations can occur with hydroxyurea and voxelotor, and rare instances of clinically apparent liver injury with jaundice have been reported with ... | null | null | null | null | null |
Dabigatran.nxml | Dabigatran | 2017-11-05 | Dabigatran is a direct inhibitor of thrombin and anticoagulant which is used for prevention of stroke and venous embolism in patients with chronic atrial fibrillation. Dabigatran therapy has been associated with a low rate of serum enzyme elevations and rare instances of liver enzyme elevations and jaundice. | Dabigatran (da" bi gat' ran) is a potent direct inhibitor of thrombin, the final intermediate in blood coagulation. Dabigatran binds to the active site of thrombin and inactivates both fibrin-bound and unbound thrombin, unlike heparin that binds to the unbound thrombin only. Inhibiting thrombin prevents the conversion ... | Chronic therapy with dabigatran is associated with moderate ALT elevations (greater than 3 times the upper limit of normal) in 1.5% to 3% of patients, an overall rate which is slightly lower than with low molecular weight heparin and similar to the rates with warfarin. While case reports of clinically apparent liver in... | The cause of liver injury during dabigatran oral anticoagulant therapy is unknown but is likely to be idiosyncratic and perhaps immunologic. Dabigatran undergoes little hepatic metabolism and does not affect CYP 450 activity. | Liver injury attributed to dabigatran varies from mild serum ALT elevations to liver injury with jaundice, but is usually mild and self-limited, resolving within 4 weeks of stopping. Recurrence of liver injury with rechallenge has not been described. There is no reason to suspect that there is cross sensitivity to hepa... | Dabigatran – Pradaxa® | Antithrombotic Agents | null |
Fostemsavir.nxml | Fostemsavir | 2023-06-20 | Fostemsavir is a unique antiretroviral agent that binds to an envelope antigen of the human immunodeficiency virus (HIV) inhibiting its attachment to cell surface receptors of CD4+ lymphocytes. It is used to treat patients with multidrug resistant infection and inadequate viral suppression despite optimized background ... | Fostemsavir (fos tem’ sa vir) is a unique antiretroviral drug that binds the gp120 subunit of the HIV envelope protein that mediates viral attachment to cell surface receptors on CD4+ lymphocytes, an initial and necessary step in HIV replication. Fostemsavir has both in vitro and in vivo activity against HIV and was de... | In registration clinical trials, fostemsavir was associated with alanine aminotransferase (ALT) elevations in up to 25% of patients, but levels above 5 times the upper limit of normal (ULN) arose in only 4% of subjects. Most ALT elevations were transient, asymptomatic, and did not require dose modification or discontin... | Fostemsavir is metabolized predominantly by esterase mediated hydrolysis and to a lesser extent by hepatic microsomal enzymes, predominantly CYP 3A4. Strong inducers of CYP 3A4 have the potential of lowering levels of fostemsavir and should be avoided if possible. | Serum enzyme elevations during fostemsavir therapy are generally transient, mild-to-moderate in severity, and often attributable to other causes. Because of the complexity of therapy for multidrug resistant HIV infection, caution should be used in altering the dose or discontinuation of fostemsavir unless the adverse e... | Fostemsavir – Rukobia® | Antiviral Agents | null |
Asparaginase.nxml | Asparaginase | 2023-09-19 | Asparaginase is a bacterial enzyme that is used as an antineoplastic agent, largely in the therapy of acute lymphocytic leukemia (ALL). Asparaginase has many side effects, one of which is hepatic injury that is characterized by inhibition of hepatic protein synthesis, marked cholestasis and steatosis, which is usually ... | Asparaginase (as par' a jin ase), often referred to as L-asparaginase, is a bacterial enzyme that acts to decrease tissue stores of asparagine, a secondary amino acid that is important in the growth of many cancers. Asparaginase, prepared from E. coli, was introduced into cancer chemotherapy over 50 years ago and remai... | Some abnormalities of liver test results occur in almost all patients treated with either asparaginase or pegaspargase. Most typical is a decrease in serum albumin and clotting factors (including II, V, VII, VIII, IX, prothrombin and fibrinogen) due to inhibition of hepatic protein synthesis. Most patients also have a ... | null | Asparaginase is typically given in 14 or 28 day cycles while pegaspargase is given at two-week intervals, and consequently the hepatic injury may first become clinically apparent after the drug is stopped. Further use of asparaginase (with dose reduction) should be delayed until hepatic function has been restored. Pati... | Asparaginase – Erwinaze® | Antineoplastic Agents | [
{
"cas_registry_number": "9015-68-3",
"molecular_formula": "Large protein",
"name": "Asparaginase"
},
{
"cas_registry_number": "130167-69-0",
"molecular_formula": "Large protein",
"name": "Pegaspargase"
}
] |
TisotumabVedotin.nxml | Tisotumab Vedotin | 2023-11-30 | Tisotumab vedotin is a human monoclonal antibody conjugate which is used in the therapy of refractory, recurrent or metastatic cervical cancer. Tisotumab vedotin has been linked to transient mild-to-moderate serum aminotransferase elevations during therapy but has not been implicated in cases of liver injury with jaund... | Tisotumab vedotin (ti” so’ tue mab) vedotin (ve doe’ tin) is a human IgG1 kappa monoclonal antibody to tissue factor (TF), a cell surface protein that is highly expressed in various forms of cancer and is associated with poor outcomes. The monoclonal antibody is conjugated using a linker sequence to a cytotoxic molecul... | In publications of the registration trials of tisotumab vedotin, serum aminotransferase elevations arose in 11% to 24% of treated patients but were above 5 times the upper limit of normal (ULN) in only 1% to 2%, and no patient developed clinically apparent liver injury attributed to therapy. The conjugated vedotin is a... | The cause of the serum aminotransferase elevations during tisotumab vedotin therapy is not known, but it is likely due to direct toxicity of the vedotin conjugate rather than the monoclonal antibody. It is not known whether the serum enzyme elevations are accompanied by hepatic steatosis. | The serum aminotransferase elevations that occur during tisotumab vedotin therapy are generally transient, mild and asymptomatic and rarely require dose modification or delay in therapy. Elevations above 5 times the upper limit of normal, if detected, should lead to more careful monitoring and suspension of further inf... | Tisotumab Vedotin – Tivdak® | Antineoplastic Agents | null |
Nelfinavir.nxml | Nelfinavir | 2017-09-01 | Nelfinavir is an antiretroviral protease inhibitor used in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Nelfinavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels and is a rare cause of clinically a... | Nelfinavir (nel fin' a vir) is a nonpeptidic protease inhibitor that acts by binding to the catalytic site of the HIV protease, thereby preventing the cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication. Nelfinavir was approved for use in the United States ... | Some degree of serum aminotransferase elevation occurs in a high proportion of patients taking nelfinavir containing antiretroviral regimens. Moderate-to severe elevations in serum aminotransferase levels (>5 times the upper limit of normal) are found in only 3% to 10% of patients, although rates may be higher in patie... | The cause of the clinical hepatotoxicity from nelfinavir is only partially known. Nelfinavir is extensively metabolized by the liver, largely by the cytochrome P450 system (CYP3A4), and toxic intermediates may be the cause of some liver injury. In patients with HIV infection who are coinfected with either HBV or HCV, i... | The severity of the liver injury from nelfinavir ranges from mild and transient enzyme elevations to more marked and symptomatic enzyme elevations and, rarely, to acute hepatitis which is usually self-limited, but can result in acute liver failure and death. Liver injury may be more common in persons without immune def... | Nelfinavir – Viracept® | Antiviral Agents | null |
Sertraline.nxml | Sertraline | 2020-04-08 | Sertraline is a selective serotonin reuptake inhibitor (SSRI) used in the therapy of depression, anxiety disorders and obsessive-compulsive disorder. Sertraline therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent ... | Sertraline (ser' tra leen) is a selective serotonin reuptake inhibitor (SSRI) that acts by blocking the reuptake of serotonin in CNS synaptic clefts, thus increasing serotonin levels in the brain which is associated with its psychiatric effects. Sertraline was approved for use in the United States in 1991, and it remai... | Liver test abnormalities have been reported to occur in up to 1% of patients on sertraline, but elevations are usually modest and infrequently require dose modification or discontinuation. Rare instances of acute, clinically apparent episodes of liver injury with marked liver enzyme elevations with or without jaundice ... | The mechanism by which sertraline causes liver injury is not known. Sertraline is metabolized at least in part by the liver, mainly via the cytochrome P450 system and PYP 2D6 and 2B6 which can cause drug-drug interactions. The hepatotoxicity of sertraline may be mediated by toxic intermediates of its metabolism. | The serum aminotransferase elevations that occur on sertraline therapy are usually self-limited and do not require dose modification or discontinuation of therapy. Rare instances of acute liver failure have been attributed to sertraline therapy. Rechallenge usually results in recurrence of liver injury and should be av... | Sertraline – Generic, Zoloft® | Antidepressant Agents | null |
Carboplatin.nxml | Carboplatin | 2020-09-15 | Carboplatin is an intravenously administered platinum coordination complex and alkylating agent which is used as a chemotherapeutic agent for the treatment of various cancers, mainly ovarian, head and neck and lung cancers. Carboplatin therapy is associated with a low rate of transient serum aminotransferase elevations... | Carboplatin (kar" boe pla' tin) is a cisplatin analog with a carboxy-cyclobutane moiety instead of the chloride atoms which makes it more stable and perhaps less toxic than cisplatin. Carboplatin and cisplatin act as alkylating agents causing cross linking between and within DNA strands, leading to inhibition of DNA, R... | Mild and transient elevations in serum aminotransferase levels are found in up to one-third of patients taking carboplatin. However, clinically apparent acute liver injury from carboplatin is extremely rare and the characteristics of such injury have not been well defined. In addition, carboplatin has been used in comb... | The cause of idiosyncratic hepatotoxicity from carboplatin is not known, but is possibly due to an intermediate in its metabolism. Sinusoidal obstruction syndrome is probably due to direct toxic effects of the myeloablative regimen on sinusoidal lining cells. | The severity of liver injury from carboplatin ranges from mild, reversible enzyme elevation to sinusoidal obstruction syndrome with acute liver failure and death. Liver injury from carboplatin is extremely rare. There is likely to be cross sensitivity to liver toxicities of the various platinum coordination complexes a... | Carboplatin – Generic, Paraplatin® | Antineoplastic Agents, Alkylating Agents | null |
Clozapine.nxml | Clozapine | 2023-06-05 | Clozapine was the first atypical antipsychotic approved for treatment of schizophrenia. Because it is associated with severe and potentially fatal side effects (agranulocytosis), its use is restricted to refractory schizophrenia, and monitoring during therapy is required. Clozapine therapy is associated with serum amin... | Clozapine (kloe" za peen) is an atypical antipsychotic medication that appears to act both as a dopamine (D) and serotonin (5-HT2) receptor antagonist. Clozapine was introduced into clinical practice in 1971, but subsequently withdrawn in 1975 after reports of fatal agranulocytosis with its use. Nevertheless, because o... | Serum enzyme elevations arise in up to two-thirds of patients on clozapine but are usually modest and resolve spontaneously after 6 to 12 weeks, often not requiring dose modification or discontinuation. ALT elevations above 3 times ULN arise in 10% to 20% of patients but are usually transient. Occasionally, serum enzym... | The mechanism by which clozapine causes liver injury is not known. Cases with features of hypersensitivity suggest that the injury is immunologically mediated. Clozapine is extensively metabolized by the liver, partially via the cytochrome P450 system (CYP 1A2 and others), and production of a toxic or immunogenic inter... | The serum aminotransferase elevations that occur on clozapine therapy are often self-limited and usually do not require dose modification or discontinuation of therapy. Most instances of clinically apparent liver injury due to clozapine have been mild-to-moderate in severity and rapidly resolve. Several cases of acute ... | Clozapine – Generic, Clozaril® | Antipsychotic Agents | null |
Amantadine.nxml | Amantadine | 2020-06-22 | Amantadine is a primary amine that has both antiviral and dopaminergic activity and is used in the therapy of influenza A and management of Parkinson disease. Amantadine has not been associated with clinically apparent liver injury. | Amantadine (a man' ta deen) is a cyclic primary amine that has antiviral and anti-Parkinsonian activities. The antiviral activity of amantadine is attributed to inhibition of virion uncoating and release of viral RNA in the initial stages of viral replication. Amantadine is active only against influenza A virus and has... | Despite widespread use, there is little evidence that amantadine when given orally causes liver injury, either in the form of serum enzyme elevations or clinically apparent liver disease.\n\nLikelihood score: E (unlikely cause of clinically apparent liver injury). | Amantadine has minimal hepatic metabolism and is excreted largely unchanged in the urine, factors which perhaps explain the absence of significant hepatotoxicity.\n\nDrug Classes: Antiviral Agents; Antiparkinson Agents\n\nOther Drugs in the Class for Influenza: Baloxavir, Oseltamivir, Peramivir, Rimantadine, Zanamivir | null | Amantadine – Generic, Symmetrel® | Antiviral Agents; Antiparkinson Agents | null |
Teprotumumab.nxml | Teprotumumab | 2021-07-08 | Teprotumumab is a human monoclonal antibody to the insulin-like growth factor 1 receptor which is used to treat the ophthalmopathy of Graves disease. Teprotumumab is generally well tolerated and has not been associated with serum aminotransferase elevations during therapy or with instances of clinically apparent liver ... | Teprotumumab (tep” roe toom’ ue mab) is a human IgG1 monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF1R) that is used in the therapy of Graves ophthalmopathy (thyroid eye disease). Graves disease is an autoimmune disease associated with autoantibodies, hyperthyroidism and a distinctiv... | In preregistration trials of teprotumumab, abnormalities in serum aminotransferase levels were not reported. Furthermore, there were no reported hepatic serious adverse events or mention of clinically apparent liver injury. Since approval and more general use of teprotumumab there have been no reports of clinically sig... | Possible mechanisms of liver injury due to teprotumumab are not known. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids. On the other hand, IGF1 receptors are wide spread and have important functions in growth and development and may alte... | Drug Class: Monoclonal Antibodies, Antithyroid Agents | Teprotumumab – Tepezza® | Antithyroid Agents | null |
Ranitidine.nxml | Ranitidine | 2018-01-25 | Ranitidine is a histamine type 2 receptor antagonist (H2 blocker) which is widely used for treatment of acid-peptic disease and heartburn. Ranitidine has been linked to rare instances of clinically apparent acute liver injury. | Ranitidine (ra ni' ti deen) was the second H2 blocker introduced into clinical practice in the United States and remains a commonly used agent for treatment of duodenal and gastric ulcer and gastroesophageal reflux disease. The H2 blockers are specific antagonists of the histamine type 2 receptor, which is found on the... | Chronic therapy with ranitidine has been associated with minor elevations in serum aminotransferase levels in 1% to 4% of patients, but similar rates were reported in placebo recipients. The ALT elevations are usually asymptomatic and transient and may resolve without dose modification. Rare instances of clinically app... | Ranitidine 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. | The hepatic injury caused by ranitidine is usually rapidly reversible with stopping the medication (Case 1). Rare instances of acute liver failure have been attributed to it, but ranitidine has not been definitively linked to cases of prolonged cholestasis or vanishing bile duct syndrome. Rechallenge usually causes rec... | Ranitidine – Generic, Zantac® | Antiulcer Agents | null |
Phenotypes_Fatty.nxml | Nonalcoholic Fatty Liver | 2019-05-04 | null | null | null | null | null | null | null | null |
Ixekizumab.nxml | Ixekizumab | 2017-05-25 | Ixekizumab is a humanized monoclonal antibody to interleukin-17A which acts as an antiinflammatory agent and is used to treat moderate-to-severe plaque psoriasis. Ixekizumab has not been linked to serum enzyme elevations during therapy or to instances of idiosyncratic acute liver injury. | Ixekizumab (ix" ee kiz' ue mab) is a recombinant, humanized IgG4 monoclonal antibody to interleukin (IL)-17A, an important cytokine responsible for local release of proinflammatory mediators. The binding of the monoclonal antibody to the cytokine blocks its interaction with the receptor and thus decreases inflammatory ... | In large premarketing clinical trials, serum enzyme elevations were no more frequent with ixekizumab than with placebo injections and there were no instances of clinically apparent liver injury attributed to its use. Serum ALT elevations above 5 times the upper limit of normal were rare (<0.5%) and resolved without nee... | The mechanism by which ixekizumab might cause liver injury is unknown. Ixekizumab is a monoclonal antibody and, like other proteins, is metabolized into amino acids and is unlikely to have intrinsic toxicity. Because of its immunomodulatory activity, ixekizumab might induce an autoimmune reaction against hepatocytes, b... | null | Ixekizumab – Taltz® | Dermatologic Agents, Psoriasis Agents | null |
Ursodiol.nxml | Ursodiol (Ursodeoxycholic Acid) | 2017-09-25 | Ursodeoxycholic acid or ursodiol is a naturally occurring bile acid that is used dissolve cholesterol gall stones and to treat cholestatic forms of liver diseases including primary biliary cirrhosis. Ursodiol has been linked to rare instances of transient and mild serum aminotransferase elevations during therapy and to... | Ursodiol (ur" soe dye' ol) is a naturally occurring bile acid that is a minor fraction of the bile acid pool in humans, but a major fraction in bears and other hibernating animals. Ursodeoxycholic acid is more water soluble (hydrophilic) than cholic or chenodeoxycholic acid and is less inherently toxic to cells. When g... | n multiple clinical trials in a variety of conditions, ursodiol has not been found to cause increases in serum enzyme elevations, worsening of underlying liver disease or clinically apparent liver injury. Nevertheless, there have been rare reports of clinical decompensation in patients with advanced liver disease and c... | null | Patients with cirrhosis who are started on ursodiol should be monitored regularly for the first few months, and treatment discontinued if there is evidence of worsening of liver tests or of hepatic decompensation. There does not appear to be cross sensitivity to liver injury or adverse events between ursodiol and other... | Ursodiol – Generic, Actigall® | Gastrointestinal Agents | [
{
"cas_registry_number": "128-13-2",
"molecular_formula": "C24-H40-O4",
"name": "Ursodiol"
},
{
"cas_registry_number": "81-25-4",
"molecular_formula": "C24-H40-O5",
"name": "Cholic Acid"
}
] |
Cetirizine_Levocetir.nxml | Cetirizine | 2017-01-16 | Cetirizine and its enantiomer levocetirizine are second generation antihistamines that are used for the treatment of allergic rhinitis, angioedema and chronic urticaria. Cetirizine and levocetirizine have been linked to rare, isolated instances of clinically apparent acute liver injury. | Cetirizine (se tir' i zeen) is a second generation antihistamine (H1 receptor blocker) that is used widely to treat allergic symptoms associated with hay fever, seasonal allergies, urticaria, angioedema and atopic dermatitis. Levocetirizine (lee" voe se tir' i zeen) is the levorotatory R-enantiomer of cetirizine and it... | Cetirizine and levocetirizine use are not generally associated with liver enzyme elevations, but have been linked to rare instances of clinically apparent liver injury. In published reports, the time to onset varied widely, from 1 to 40 weeks and the pattern of injury ranged from cholestatic hepatitis to hepatocellular... | The cause of acute liver injury from cetirizine is not known. It is metabolized by the liver and a toxic metabolite may account for idiosyncratic injury. | null | Cetirizine/Levocetirizine – Generic, Zyrtec®/Generic, Xyzal® | Antihistamines | [
{
"cas_registry_number": "83881-51-0",
"molecular_formula": "C21-H25-Cl-N2-O3",
"name": "Cetirizine"
},
{
"cas_registry_number": "130018-77-8",
"molecular_formula": "C21-H25-Cl-N2-O3",
"name": "Levocetirizine"
}
] |
Lopinavir.nxml | Lopinavir | 2017-09-01 | Lopinavir is an antiretroviral protease inhibitor used in combination with ritonavir in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Lopinavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels and, ra... | Lopinavir (loe pin' a vir) is a peptidomimetic HIV protease inhibitor that acts by binding to the catalytic site of the HIV protease, thereby preventing the cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication. Lopinavir is usually given in combination with ... | Some degree of serum aminotransferase elevations occur in a high proportion of patients taking lopinavir containing antiretroviral regimens. Moderate-to-severe elevations in serum aminotransferase levels (>5 times the upper limit of normal) are found in 3% to 10% of patients, although rates may be higher in patients wi... | The cause of the clinical hepatotoxicity from lopinavir may be due to its metabolism by the liver, which is largely by the cytochrome P450 system (CYP3A4), which may result in production of a toxic intermediate. In patients with HBV or HCV coinfection, initiation of highly active antiretroviral therapy including lopina... | The severity of liver injury ranges from mild enzyme elevations to acute liver failure. In typical cases, recovery occurs within 1 to 2 months of stopping lopinavir. Rechallenge may lead to recurrence and should be avoided. There does not appear to be cross reactivity to hepatic injury with other protease inhibitors or... | Lopinavir – Kaletra® | Antiviral Agents | null |
MoxetumomabPasudotox.nxml | Moxetumomab Pasudotox | 2019-04-12 | Moxetumomab pasudotox is a mouse monoclonal antibody to CD22 conjugated with a toxic fragment of Pseudomonas exotoxin A which is used in the therapy of resistant forms of hairy cell leukemia. Moxetumomab pasudotox has been linked to transient serum enzyme elevations during therapy, but has not been linked to instances ... | Moxetumomab (mox" e toom' oh mab) pasudotox (pa soo' doe tox) is a recombinant mouse monoclonal antibody to the human CD22 cell surface marker which is highly expressed on the malignant B cells of hairy cell leukemia. The monoclonal antibody is conjugated to a fragment of a bacterial toxin, Pseudomonas exotoxin PE38 (p... | In publications on trials of moxetumomab pasudotox in hairy cell leukemia, serum ALT or AST elevations were frequent during therapy arising in 14% to 19% of patients, but to above 5 times the upper limit of normal (ULN) in only 3.8% to 5.5%. Serial testing for ALT and AST during moxetumomab therapy shows regular and re... | The serum enzyme elevations that occur during moxetumomab pasudotox therapy is not known, but it is likely direct toxicity of the conjugate. | null | Moxetumomab Pasudotox – Lumoxiti® | Antineoplastic Agents | null |
Tranylcypromine.nxml | Tranylcypromine | 2020-04-08 | Tranylcypromine is a nonhydrazine monoamine oxidase inhibitor (MAO inhibitor) used in therapy of severe depression. Tranylcypromine therapy is associated with rare instances of clinically apparent acute liver injury. | Tranylcypromine (tran" il sip' roe meen) is an antidepressant that acts through irreversible inhibition of monoamine oxidases, enzymes that inactivate several neurotransmitter amines such as norepinephrine and serotonin. Tranylcypromine is a nonspecific MAO inhibitor with activity against both MAO A (found in highest c... | Tranylcypromine, like most monoamine oxidase inhibitors, can cause transient serum aminotransferase elevations in a proportion of patients. These elevations are usually mild, asymptomatic and self-limited and do not require dose modification. Tranylcypromine has also been associated with rare cases of acute, clinically... | The mechanism by which tranylcypromine causes serum aminotransferase elevation is not known. It undergoes extensive hepatic metabolism and a possible cause of liver injury is production of a toxic intermediate of metabolism. Unlike other nonselective MAO inhibitors, tranylcypromine is not a hydrazine derivative which m... | The serum aminotransferase elevations that occur on tranylcypromine therapy are usually transient and mild and do not require dose modification or discontinuation of therapy. The acute liver injury caused by tranylcypromine is typically self-limited, but progressive and fatal instances of acute hepatitis have been repo... | Tranylcypromine – Parnate® | Antidepressant Agents | null |
Tolcapone.nxml | Tolcapone | 2021-10-25 | Tolcapone is a catechol-O-methyltransferase inhibitor used in the therapy of Parkinson disease as adjunctive therapy in combination with levodopa and carbidopa. Tolcapone has been associated with serum enzyme elevations during treatment and with several instances of clinically apparent acute liver injury, which can be ... | Tolcapone (tol' ka pone) is a specific inhibitor of cathechol-O-methyltransferase (COMT), which is a major enzyme in the pathway of levodopa metabolism. As a result, tolcapone slows the metabolism of levodopa and results in an increase in its bioavailability and duration of action. Tolcapone inhibits COMT activity both... | Tolcapone has been reported to cause serum aminotransferase elevations above 3 times the upper limit of normal in 1% to 5% of patients. While these abnormalities are usually asymptomatic and self-limiting, some persist if therapy is continued and resolved only with stopping tolcapone. More importantly, tolcapone has be... | Tolcapone is metabolized extensively in the liver and undergoes glucuronidation prior to excretion. The hepatotoxicity of tolcapone is likely due to production of a toxic intermediate that overwhelms the usual protective mechanisms of excretion. Increased likelihood of hepatic injury due to tolcapone has been linked to... | Liver injury caused by tolcapone ranges from mild, transient and asymptomatic serum enzyme elevations to clinically apparent hepatitis and acute liver failure. Tolcapone therapy has not been associated with chronic hepatitis or vanishing bile duct syndrome. Therapy of acute liver failure due to medications is largely s... | Tolcapone – Generic, Tasmar® | Parkinson Disease Agents | null |
Hydroxycut.nxml | Hydroxycut | 2018-04-12 | Hydroxycut is the commercial name a variety of multi-ingredient nutritional supplements (MINS) marketed for weight loss, body building and “fat burning”. In 2004, Hydroxycut products containing ephedra were withdrawn from use in the United States because of cardiovascular risks and in 2009 because of hepatotoxicity. Ne... | Hydroxycut is the proprietary name of a series of multi-ingredient nutritional supplements that are typically marketed as weight loss, body building, “fat burning” and performance enhancement aids. Initial ingredients in the products included caffeine and ephedra which in animal studies led to weight loss. In 2004, the... | Hydroxycut has been associated with at least 50 instances of clinically apparent acute liver injury, but the specific Hydroxycut product implicated in different cases has varied and the specific ingredients responsible for liver injury remain unclear. In reported cases, the onset of injury was generally within 2 to 12 ... | The cause of acute liver injury associated with Hydroxycut products was attributed to ephedra in the past and more recently to green tea extract (Camellia sinensis). Indeed, the clinical features of cases resemble those associated with the liver injury associated with green tea extracts. Green tea is rich in catechins,... | The acute hepatic injury associated with Hydroxycut exposure is usually self-limiting and resolves within 1 to 3 months. There is no evidence that corticosteroids are beneficial. Fatal cases of liver injury have been reported with Hydroxycut use. There is little information or cross reactivity to other weight loss prod... | Hydroxycut® | Herbal and Dietary Supplements | [
{
"cas_registry_number": "989-51-5",
"molecular_formula": "C22-H18-O11",
"name": "EGCG"
},
{
"cas_registry_number": "OM54525000",
"molecular_formula": "Unspecified",
"name": "Ephedra sinica"
}
] |
Infliximab.nxml | Infliximab | 2017-02-10 | Infliximab is a monoclonal antibody to human tumor necrosis factor alpha (TNFα) which has potent antiinflammatory activity and is used in the therapy of severe inflammatory bowel disease and rheumatoid arthritis. Infliximab has been linked to many instances of idiosyncratic acute liver injury and is a well known cause ... | Infliximab (in flix' i mab) is a mouse-human chimeric monoclonal antibody to TNFα which binds avidly to serum and tissue bound TNFα, causing its inactivation and degradation. Inhibition of TNFα activity leads to modulation of the inflammatory and pain pathways activated by this cytokine. Infliximab was approved for use... | Infliximab has been associated with at least four forms of hepatic injury which have quite separate causes and different clinical outcomes. First, infliximab can cause serum aminotransferase elevations, which generally arise after 2 to 5 infusions. These elevations can be transient and are usually asymptomatic, but in ... | The mechanism of liver injury caused by infliximab is probably due to autoimmunity caused by the immunomodulatory therapy. While a high proportion of patients develop autoantibodies either de novo or in rising titer, only rare persons develop clinically apparent autoimmune conditions, such as lupus-like syndrome or aut... | The liver injury caused by infliximab is usually mild and rapidly reversed once therapy is stopped. However, fatal instances of HBV reactivation and induction of autoimmune hepatitis due to infliximab have been reported, and regular monitoring of patients early during the course of infliximab is recommended. Patients w... | Infliximab – Remicade® | Antirheumatic Agents; Dermatologic Agents; Gastrointestinal Agents | null |
Insulin.nxml | Insulin | 2018-04-26 | Insulin is a pancreatic hormone that plays an essential role in regulation of blood glucose as well as lipid and carbohydrate metabolism. Both natural and recombinant forms of insulin are used therapeutically to treat type 1 diabetes. While insulin itself is not hepatotoxic and has not been linked to serum enzyme eleva... | Insulin (in' su lin) is a polypeptide hormone produced by pancreatic islet β cells that is primarily responsible for regulation of blood glucose and storage of carbohydrates and lipids. Type 1 diabetes is due to inadequate production of insulin caused by destruction and loss of insulin producing pancreatic islet β cell... | Insulin in typical therapeutic doses is not associated with serum enzyme elevations or with episodes of clinically apparent liver injury. However, use of insulin in poorly controlled type 1 diabetes can result in a clinical syndrome known as glycogenosis or glycogenic hepatopathy, marked by varying degrees of hepatomeg... | null | The liver injury associated with insulin use or overdose is likely due to glycogenosis rather than inherent injury from insulin, and reverses rapidly when insulin and glucose are discontinued.\n\nDrug Class: Hormonal Agents; Antidiabetic Agents | Insulin – Generic, Lantus, Humulin® | Hormonal Agents; Antidiabetic Agents | null |
EnergyDrinks.nxml | Energy Drinks | 2020-06-20 | Energy drinks are defined as over-the-counter commercial beverages with high caffeine content that are advertised as boosting energy including mental alertness and physical performance. More than 50 brands of energy drinks are available in grocery stores, nutrition centers, beverage shops and on the internet. Consumpti... | Energy drinks are defined as beverages with high concentrations of caffeine that are purported to boost energy, physical and athletic performance and mental alertness. Energy drinks were first marketed in the late 1990s and have subsequently become popular and widely available. The commercial products vary greatly in c... | Caffeine containing energy drinks are widely used and generally well tolerated. Neverless, when taken in excessive amounts they can lead to caffeine toxicity with tremors, confusion, mania, stupor and coma and cardiac arrhythmias and cardiorespiratory failure. In addition, there have been several single case reports of... | Caffeine is metabolized by the microsomal P450 drug metabolizing enzymes, predominantly CYP 1A2. Patients with advanced cirrhosis may have delayed metabolism of caffeine and experience caffeine side effects (nervousness, insomnia, headache) at levels of intake that are well tolerated by patients without liver disease.\... | null | Energy Drinks – Monster®, NOS®, Red Bull®, Rockstar® | CNS Stimulants, Xanthine Derivatives | null |
Leuprolide.nxml | Leuprolide | 2023-05-28 | Leuprolide is a parenterally administered, gonadotropin releasing hormone (GnRH) agonist which causes an inhibition of estrogen and androgen production and is used predominantly to treat advanced prostate cancer. Leuprolide has been associated with a modest rate of serum enzyme elevations during therapy, but has not be... | Leuprolide (loo' proe lide), also called leuprorelin (loo" proe rel' in), is a nonapeptide analogue of gonadotropin releasing hormone (GnRH) that acts as a partial agonist of the gonadotropin receptors in the pituitary that induce secretion of luteinizing hormone (LH) and follicle stimulating hormone (FSH). These gonad... | Leuprolide has been associated with mild serum enzyme elevations during therapy in 3% to 5% of patients, but values above 3 times the upper limit of normal are rare, being reported in less than 1% of recipients. The serum enzyme elevations during leuprolide therapy have generally been transient and asymptomatic, resolv... | The cause of liver test abnormalities during leuprolide therapy is not known. Leuprolide is a short polypeptide and is metabolized locally in many tissues. It is not metabolized by the hepatic cytochrome P450 system and has not been associated with significant drug-drug interactions. Some serum enzyme elevations may be... | The serum enzyme elevations that occur on leuprolide therapy usually do not require dose adjustment or drug discontinuation, but should lead to a search for other causes of liver disease. There is no evidence to indicate that there is cross sensitivity to liver injury among the various GnRH analogues.\n\nDrug Class: An... | Leuprolide – Generic, Lupron® | Antineoplastic Agents | null |
Ibalizumab.nxml | Ibalizumab | 2018-08-08 | Ibalizumab is a humanized monoclonal antibody to CD4, the cell surface receptor for the HIV-1 envelope glycoprotein (gp120), which is used to treat patients with multidrug resistant HIV-1 infection. Ibalizumab therapy has not been associated with serum enzyme elevations or to instances of clinically apparent drug induc... | Ibalizumab (eye' ba liz' ue mab) is a recombinant humanized monoclonal antibody to CD4, the cell surface receptor for the HIV-1 envelope glycoprotein 120 (gp120). Ibalizumab does not block the binding of gp120 to CD4 but rather inhibits the conformation changes in the CD4/gp120 complex that allows binding to a second c... | The prelicensure clinical trials of ibalizumab included a limited number of patients, many of whom had other serious comorbidities including cirrhosis and chronic hepatitis B and C. In these trials, serum aminotransferase elevations occurred in 14% to 25% of patients, but the abnormalities were generally mild and self-... | null | null | Ibalizumab – Trogarzo® | Antiviral Agents | null |
Felbamate.nxml | Felbamate | 2018-01-29 | Felbamate is a dicarbamate derivative anticonvulsant that is typically used in combination with other antiepileptic medications for refractory partial onset or generalized seizures. Felbamate has been associated with multiple cases of aplastic anemia and acute liver failure and its use is now restricted. | Felbamate (fel bam' ate) is a dicarbamate that has unique anticonvulsant activity. Its exact mechanism of action has not been established. Felbamate was approved for use the United States in 1993, the first new anticonvulsant medication in more than a decade. Within a year of release, however, reports of aplastic anemi... | Prospective studies suggest that chronic felbamate therapy is not accompanied by significant elevations in serum aminotransferase levels. Nevertheless, clinically apparent hepatotoxicity from felbamate is well described, although uncommon, estimated to occur in 1 in 18,500 to 25,000 exposures, often with severe outcome... | The mechanism of felbamate hepatotoxicity is unknown but is likely to be due to idiosyncratic bioactivation of felbamate to a high reactive electrophilic toxic metabolite. | A case report of acute liver failure attributed to felbamate has been published as have several summarizes of severe cases of liver injury reported to the FDA. The fatality rate is high. Chronic injury from felbamate therapy has not been reported. There is no known cross sensitivity to liver injury between felbamate an... | Felbamate – Felbatol® | Anticonvulsants | null |
Ofloxacin.nxml | Ofloxacin | 2020-03-10 | Ofloxacin is a second generation fluoroquinolone that was previously used widely for therapy of mild-to-moderate bacterial infections, but which has been replaced by more potent and less toxic fluoroquinolones and is now used largely topically as eye and ear drops. Ofloxacin has been linked to rare instances of acute h... | Ofloxacin (oh flox' a sin) is an oral, second generation fluoroquinolone that was previously widely used to treat mild-to-moderate urinary and respiratory tract infections caused by susceptible organisms. Ofloxacin is a semisynthetic antibiotic and a racemic mixture; its l-enantiomer is available as levofloxacin which ... | Mild elevations in ALT and alkaline phosphatase levels occur in 1 to 2% of patients on ofloxacin. These abnormalities are generally mild, asymptomatic and transient, resolving even with continuation of therapy. Ofloxacin has also been linked to rare but occasionally severe and even fatal cases of acute liver injury. Th... | The cause of hepatic injury is unknown, but appears to be hypersensitivity. | The severity of ofloxacin induced liver injury ranges from mild and transient serum enzyme elevations to self-limited jaundice to acute liver failure. Recovery is usually rapid (2 to 8 weeks) after stopping the medication. Cross reactivity of the hepatic injury between different fluoroquinolones has not been well defin... | Ofloxacin – Generic, Floxin® | Antiinfective Agents | null |
Hydroxychloroquine.nxml | Hydroxychloroquine | 2021-04-15 | Hydroxychloroquine is a derivative of chloroquine that has both antimalarial and antiinflammatory activities and is now most often used as an antirheumatologic agent in systemic lupus erythematosis and rheumatoid arthritis. Hydroxychloroquine therapy has not been associated with liver function abnormalities and is an e... | Hydroxychloroquine (hye drox" ee klor' oh kwin) is a hydroxylated derivative of chloroquine and has similar antimalarial activity but is less toxic, allowing for use in higher doses for longer periods. Originally used as an antimalarial agent, hydroxychloroquine was later found to have antiinflammatory activity. Its me... | Hydroxychloroquine has not been associated with significant serum enzyme elevations during therapy of rheumatologic diseases. Furthermore, clinically apparent liver injury from hydroxychloroquine is rare. A single case series (two cases) of acute liver failure attributed to hydroxychloroquine was published twenty years... | Hydroxychloroquine is metabolized in the liver and may alter metabolism of other medications. Therapy is unlikely to cause liver injury in normal individuals, but can trigger an acute worsening of porphyria cutanea tarda in susceptible individuals.\n\nDrug Class: Antirheumatic Agents | null | Hydroxychloroquine – Generic, Plaquenil® | Antirheumatic Agents | null |
GnRHAnalogues.nxml | Gonadotropin Releasing Hormone (GnRH) Analogues | 2018-03-20 | The gonadotropin releasing hormone (GnRH) agonists and antagonists are short peptide analogues of GnRH that cause a profound inhibition of estrogen and androgen synthesis and are used predominantly as androgen deprivation therapy of advanced prostate cancer. Some of these agents are also used to treat benign conditions... | Gonadotropin releasing hormone is a decapeptide that is produced in the hypothalamus and acts upon GnRH receptors on the surface of gonadotropin cells in the pituitary gland, stimulating the release of luteinizing hormone (LH) and follicular stimulating hormone (FSH) which, in turn, stimulate the production and release... | null | null | null | null | null | null |
Brincidofovir.nxml | Brincidofovir | 2022-10-18 | Brincidofovir is an orally available antiviral agent with activity against smallpox and several other DNA viruses that is currently approved for use against smallpox virus (variola) infection in humans and has been given emergency use authorization for treatment of monkeypox (now renamed “mpox”) infection. Brincidofovi... | Mpox\n\ninhibits the orthopoxvirus DNA polymerase, which is required for its replication and is highly conserved among orthopoxviruses. The lipid conjugate consists of a lipophosphatidylcholine that allows intestinal absorption by lipid uptake pathways. Inside cells the lipid ester linkage is cleaved releasing cidofovi... | In preregistration clinical trials of brincidofovir as prevention of cytomegalovirus and adenovirus infection in adults and children after hematopoietic stem cell transplantation (HSCT), serum aminotransferase elevations were more frequent with brincidofovir (22%) than placebo (16%) treatment, the usual rate of hepatic... | The relative lack of serious adverse events and clinically apparent hepatic injury from brincidofovir may be due to its short duration of administration, being recommended for two doses only given one week apart. Whether longer term brincidofovir is also without serious hepatic adverse events remains to be seen. Brinci... | The product label for brincidofovir recommends screening for liver test abnormalities before starting therapy and repeating tests as clinically indicated. The mild ALT elevations associated with brincidofovir therapy are usually self-limited and do not require dose modification. Because brincidofovir is usually given o... | Brincidofovir – Tembexa® | Antiviral Agents | null |
Tagraxofusp.nxml | Tagraxofusp | 2019-04-12 | Tagraxofusp is a recombinant fusion protein consisting of the binding site of interleukin 3 [IL3] fused with diphtheria toxin and that is given by intravenous infusion and used as an antineoplastic agent for patients with blastic plasmacytoid dendritic cell neoplasm. Treatment with tagraxofusp is associated with a high... | Tagraxofusp (tag rax' oh fusp) is a recombinant fusion protein that combines the binding site domain of IL3 with the catalytic domain of diphtheria toxin. The IL3 domain targets cells with the IL3 receptor (CD122), which is highly expressed on some malignant myeloid cells and particularly cells of blastic plasmacytoid ... | In prelicensure clinical trials of tagraxofusp, serum enzyme elevations arose in 88% of patients and ALT or AST values were above 5 times ULN in 40%. Serum alkaline phosphatase elevations were also common [26%] as were bilirubin elevations [14%], but were usually mild and self-limited, resolving rapidly despite continu... | The possible cause of the liver injury due to tagraxofusp is not known. Tagraxofusp is a recombinant protein and is metabolized by many cells, but mostly those that have receptors for CD122 and take up the protein. The delivered diphtheria toxin is a direct cytoplastic toxin and would injure any cells that possess CD12... | Routine monitoring of liver tests is recommended in patients receiving tagraxofusp therapy at the time of each infusion. Patients with ALT or AST elevations of more than 5 times ULN should discontinue tagraxofusp at least temporarily and restarted only once the abnormalities have resolved.\n\nDrug Class: Antineoplastic... | Tagraxofusp – Elzonris® | Antineoplastic Agents | null |
Tetrabenazine.nxml | Vesicular Monoamine Transporter 2 (VMAT2) Inhibitors | 2019-04-02 | The vesicular monoamine transporter type 2 (VMAT2) inhibitors are agents that cause a depletion of neuroactive peptides such as dopamine in nerve terminals and are used to treat chorea due to neurodegenerative diseases (such as Huntington chorea) or dyskinesias due to neuroleptic medications (tardive dyskinesia). As of... | null | null | null | null | Deutetrabenazine – Austedo® | Genetic Disorder Agents | [
{
"cas_registry_number": "1392826-25-3",
"molecular_formula": "C19-H21-D6-N-O3 (USP)C19-H27-N-O3 (FDA)",
"name": "Deutetrabenazine"
},
{
"cas_registry_number": "58-46-8",
"molecular_formula": "C19-H27-N-O3",
"name": "Tetrabenazine"
},
{
"cas_registry_number": "1025504-45-3",
... |
Passionflower.nxml | Passionflower | 2020-03-28 | Passionflower is an extract of the flowers of the plant Passiflora incarnata that is claimed to have natural sedative properties and to be useful for treatment of anxiety and insomnia. Passionflower has not been implicated in causing serum enzyme elevations or clinically apparent liver injury. | Passionflower is a flowering plant, extracts of which have been used as a mild sedative and sleeping aid. The genus Passiflora includes more than 500 species which typically have complex and unique structures and flowers, and are found throughout much of the world. Passiflora incarnata (maypop) is indigenous to the Uni... | Despite widescale use, passionflower extracts have not been convincingly linked to instances of clinically apparent liver injury. However, there have been no placebo controlled and adequate sized trials with careful prospective assessment of adverse events and effects on laboratory test results.\n\nLikelihood score: E ... | null | null | Passionflower – Generic (OTC Products) | Herbal and Dietary Supplements | null |
Heparins.nxml | Heparins | 2017-11-13 | null | null | null | null | null | null | null | null |
Alpha_Peginterferon.nxml | Alpha Interferon | 2018-05-04 | Alpha interferon is a cytokine produced by the innate immune system in response to environmental exposures including viral infections. Alpha interferon in various formulations has been developed as therapy of several forms of cancer and viral infections, but its major use has been as therapy of chronic hepatitis C. Alp... | Alpha interferon (in"' ter feer' on) is a naturally occurring cytokine which is produced by cells of the innate immune system in reaction to viral infection or other environmental stresses. Alpha and beta interferon are considered type I interferons which share antiviral, immunomodulatory as well as antiproliferative e... | Therapy with interferon or peginterferon can be associated with transient and asymptomatic mild-to-moderate serum aminotransferase elevations in up to half of patients. Because the major use of peginterferon is for hepatitis C or in patients with cancer on multiple other medications, serum ALT elevations are often diff... | Interferon has diverse effects on multiple cell types. The autoimmune hepatitis-like syndrome that has been attributed to interferon therapy appears to occur in patients who are predisposed to autoimmune diseases, and is probably due to the immunomodulatory effects of alpha interferon in increasing cell surface display... | null | Alpha Interferon – Avonex® | Antiviral Agents | [
{
"cas_registry_number": "76543-88-9",
"molecular_formula": "C860-H1353-N227-O255-S9",
"name": "Alpha Interferon"
},
{
"cas_registry_number": "215647-85-1",
"molecular_formula": "Unspecified",
"name": "Peginterferon"
}
] |
Cabozantinib.nxml | Cabozantinib | 2017-01-04 | Cabozantinib is orally available kinase inhibitor and antineoplastic agent that is used in treatment of advanced, metastatic medullary thyroid cancer and refractory renal cell carcinoma. Cabozantinib is associated with a low rate of serum enzyme elevations during treatment and has been implicated with rare instances of... | Cabozantinib (ka" boe zan' ti nib) is an orally available, small molecule, multi-kinase inhibitor with activity against hepatocyte growth factor receptor (MET), vascular endothelial growth factor receptor 2 (VEGFR-2), and rearranged during transfection (RET), cell surface tyrosine kinase receptors which are overexpress... | In large clinical trials of cabozantinib, elevations in serum aminotransferase levels were common, occurring in 16% to 97% of patients. Values greater than 5 times the upper limit of normal (ULN), however, occurred in only 2% to 8% of recipients. Serum alkaline phosphatase elevations were also common and were above 3 t... | The mechanisms of liver injury accounting for serum enzyme elevations during cabozantinib therapy are not known, but may be a direct effect of inhibition of cellular kinases by this multi-specific tyrosine kinase inhibitor. Cabozantinib is metabolized in the liver, predominantly by the cytochrome P 450 system and espec... | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. Clinically apparent liver injury should prompt immediate interruption of cabozantinib therapy. There is little information on cross reactivity in risk for hepatic injury between... | Cabozantinib – Cometriq®, Cabometyx® | Antineoplastic Agents | null |
MinElements.nxml | Elements Needed In Reporting Cases Of Drug-Induced Liver Injury | 2019-05-04 | null | null | null | null | null | null | null | null |
Probenecid.nxml | Probenecid | 2020-07-10 | Probenecid is a uricosuric agent used for the treatment of gout usually in combination with other agents. Probenecid has been associated with minor serum aminotransferase elevations and very rarely with hypersensitivity reactions which, even more rarely, can be accompanied by acute liver injury. | Probenecid (proe ben' e sid) is a sulfonamide derivative that acts as an inhibitor of inorganic acid transport in the distal renal tubule, causing blockage of reabsorption of uric acid. Therapy leads to lowering of serum uric acid levels within a few weeks, and chronic therapy has been shown to decrease uric acid level... | There are no reports on the frequency of liver test abnormalities during probenecid therapy, but they are probably rare as the drug is largely secreted unchanged in the urine. A single case report of a severe hypersensitivity reaction from probenecid and rechallenge with a rapid and severe recurrence of jaundice was re... | The mechanism of probenecid hepatotoxicity is probably hypersensitivity. Most cases of hypersensitivity to probenecid are marked by skin rash alone, without liver damage. | Chronic hepatitis and vanishing bile duct syndrome have not been reported from probenecid therapy. Hypersensitivity reactions (largely rash and urticaria) to probenecid can occur and rechallenge should be avoided as the single case of severe liver injury reported was in a patient who was retreated with probenecid after... | Probenecid – Generic, Benemid® | Antigout Agents/Gout Suppressants | null |
Naxitamab.nxml | Naxitamab | 2024-07-12 | Naxitamab is a monoclonal antibody to GD2 that is used in combination with granulocyte-macrophage colony stimulating factor to treat children with relapsed or refractory high risk neuroblastoma of the bone or bone marrow. Naxitamab therapy is associated with transient serum aminotransferase elevations during therapy bu... | Naxitamab (nax it’ a mab) is a humanized, cytolytic monoclonal antibody to glycolipid disialoganglioside (GD2), an adhesion molecule widely expressed on cell membranes of neuroectoderm derived tumors including neuroblastoma, the most common extra-cranial cancer of children. Naxitamab was found to be cytolytic to neurob... | Naxitamab was evaluated in small, prospective open label trials in children and adults with refractory neuroblastoma, a rare but often fatal cancer. Abnormal laboratory results were common during therapy including elevations in serum ALT levels in 55% of subjects which were 5 times ULN or greater than the upper limit o... | The causes of the frequent liver test abnormalities during naxitamab therapy are not known but may be due to the cytotoxic monoclonal antibody and low level expression of GD2 on hepatocytes. Some of the abnormalities are no doubt due to the underlying condition and other treatments administered. Naxitamab can cause hyp... | The product label for naxitamab does not recommend monitoring of routine liver tests during therapy, and considerations of the severity of the underlying tumor and its poor prognosis generally outweigh concerns about serum aminotransferase elevations not accompanied by jaundice or symptoms of liver injury.\n\nDrug Clas... | Naxitamab – Danyelza® | Antineoplastic agents | null |
Germander.nxml | Germander | 2018-03-12 | Germander refers to about 250 species of plants in the mint family (genus: Teucrium) used for centuries in herbal teas and more recently marketed as a germander extract as an aid for weight control and management of diabetes and hyperlipidemia. Germander extracts have been linked to multiple instances of clinically app... | Germander is derived from aerial parts of a perennial aromatic plant of the mint family (Teucrium Lamiaceae) which has been used in Europe for centuries to treat inflammatory and digestive disorders. Germander is also widely used in gardening for its attractive flowers and uniform shape. Only some species have been use... | Liver injury attributable to germander was first reported in a series of publications from France in 1992, a few years after a weight loss supplement containing germander ("Tealine") was commercially marketed in that country. The onset of acute injury varied from 2 to 18 weeks (averaging 9 weeks) after starting germand... | Germander and other Teucrium extracts have many components including glycosides, flavonoids, saponins, volatile oils and furan containing neoclerodane diterpenoids, the last of which (Teucrin A and Teuchmaedryn A) are considered the hepatotoxins responsible for its liver injury. The furano neoclerodane diterpenoids are... | Hepatotoxicity from germander and other Teucrium extracts or tea preparations is usually self-limiting once the herbal is discontinued. Nevertheless, several cases of acute liver failure and death or liver transplantation after germander use have been reported as well as several instances of chronic hepatitis and cirrh... | Germander – Generic | Herbal and Dietary Supplements | null |
Pramlintide.nxml | Pramlintide | 2016-06-06 | Pramlintide is a recombinant DNA produced polypeptide analogue of human amylin that is used in combination with insulin in the therapy of diabetes. Pramlintide has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury. | Pramlintide (pram' lin tide) is a synthetic analogue of human amylin that is used in combination with insulin in the treatment of diabetes. Amylin is a human pancreatic hormone which, like insulin, is produced in pancreatic beta cells and aids in the control of blood sugar after meals by delaying gastric emptying, decr... | In large clinical trials, serum enzyme elevations were rare (<1%) during pramlintide/insulin therapy and no more common than with placebo and there were no reports of clinically apparent liver injury among treated patients. Since licensure, there have been no published case reports of hepatotoxicity due to pramlintide ... | Pramlintide is a polypeptide and is metabolized to amino acids by serum and tissue proteases, and is unlikely to have any direct hepatotoxic potential.\n\nDrug Class: Antidiabetic Agents | null | Pramlintide – Symlin® | Antidiabetic Agents | null |
Lovastatin.nxml | Lovastatin | 2021-12-01 | Lovastatin is a commonly used cholesterol lowering agent (statin) that is associated with mild, asymptomatic and self-limited serum aminotransferase elevations during therapy and rarely with clinically apparent acute liver injury. | Lovastatin (loe" va stat' in) is an orally available inhibitor of hepatic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the major rate-limiting enzyme in cholesterol synthesis. Like other members of its class (the “statins”), lovastatin lowers total serum cholesterol and low density lipoprotein (LDL) conce... | Lovastatin therapy is associated with mild, asymptomatic and usually transient serum aminotransferase elevations. In summary analyses of large scale studies with prospective monitoring, ALT elevations above normal occurred in 3% to 5% of patients, but were above 3 times the upper limit of normal (ULN) in only 0.4% comp... | The cause of hepatic injury from lovastatin is unknown. Lovastatin is largely metabolized in the liver (via CYP 3A4) and metabolites are excreted in bile. Lovastatin is susceptible to drug-drug interactions and strong inhibitors of CYP 3A4 can result in higher plasma lovastatin levels which increases the risk of muscle... | The product label for lovastatin recommends screening for liver test abnormalities before starting therapy and repeating tests as clinically indicated. The ALT elevations that occur with lovastatin therapy usually resolve spontaneously within a few weeks even without discontinuation. The product label for lovastatin me... | Lovastatin – Generic, Altoprev®, Mevacor® | Antilipemic Agents | null |
Dasatinib.nxml | Dasatinib | 2017-12-05 | Dasatinib is a selective tyrosine kinase receptor inhibitor that is used in the therapy of chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome. Dasatinib is commonly associated with transient elevations in serum aminotransferase levels during treatment, but with only rare instances of clinically... | Dasatinib is an orally available, small molecule 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 re... | In large clinical trials, elevations in serum aminotransferase levels during dasatinib therapy occurred in up to 50% of patients, but were usually mild and self-limited. Elevations above 5 times the upper limit of normal (ULN) occurred in 1% to 9% of patients and generally responded to dose adjustment or temporary disc... | Dasatinib 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, dasatinib is susceptible to drug-drug interactions when used with agents that induce or inhibit CYP 3A4. | 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 to 20 mg daily). In patients with clinically apparent liver injury and jaundice, restar... | Dasatinib – Sprycel® | Antineoplastic Agents | null |
Phentermine.nxml | Phentermine | 2020-06-04 | Phentermine is a sympathomimetic amine and anorectic agent used for the short term therapy of obesity. Phentermine which has been in clinical use for more than 50 years has not been linked convincingly to either serum enzyme elevations during therapy or to instances of clinically apparent liver injury. | Phentermine (fen' ter meen) is a structural analogue to amphetamine and has similar activity in suppressing appetite, but has few of the other central nervous system effects of amphetamines and only mild abuse potential. Its effect in increasing weight loss is probably mediated by anorectic activity that is the result ... | Phentermine has not been linked to an increased rate of serum enzyme elevations during therapy; however, results of ALT monitoring during phentermine therapy have rarely been reported. Despite long term availability and wide use of phentermine, there have been no published reports linking it to clinically apparent acut... | null | null | Phentermine – Generic, Adipex-P®, Lonamin® | Weight Loss Agents | null |
Pirfenidone.nxml | Pirfenidone | 2025-04-25 | Pirfenidone is an orally available pyridinone derivative that inhibits collagen formation and is used to treat idiopathic pulmonary fibrosis. Elevations in serum enzyme levels during pirfenidone therapy are not uncommon, but it has yet to be implicated in cases of clinically apparent liver injury with jaundice. | Pirfenidone (pir fen' i done) is an orally available, antiinflammatory and antifibrotic agent that is used to treat idiopathic pulmonary fibrosis. It is a small molecular weight phenyl substituted pyridinone that has antifibrotic activity both in vitro and in vivo. In animal models, pirfenidone decreases fibroblast pro... | In large randomized controlled trials, serum aminotransferase elevations more than 3 times the upper limit of normal (ULN) occurred in 4% of pirfenidone- compared to less than 1% of placebo-treated patients. The elevations were generally asymptomatic and short lived, resolving with or without dose modification and requ... | The mechanism by which pirfenidone might cause liver injury is not known. It is 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. Pirfenidone is also susceptible to drug-drug interactions with strong in... | While chronic therapy with pirfenidone can be associated with mild-to-moderate serum aminotransferase elevations, it has only rarely been linked to cases of clinically apparent liver injury. Nevertheless, monitoring of serum aminotransferase levels monthly during the first 6 months and every 3 months thereafter is reco... | Pirfenidone – Esbriet® | Pulmonary Fibrosis Agents | null |
Dalfampridine.nxml | Dalfampridine | 2017-11-13 | Dalfampridine is a pyrimidine analogue used in the treatment of relapsing multiple sclerosis. Dalfampridine has had limited clinical use, but has not been linked to serum enzyme elevations during treatment nor to instances of clinically apparent liver injury with jaundice. | Dalfampridine (dal fam' pri deen) is a pyrimidine analogue (4-aminopyridine) and potassium channel blocker that is used to improve mobility and walking speed in patients with multiple sclerosis. Dalfampridine appears to act by prolonging neuronal action potentials and thus improving conduction in demyelinated nerve fib... | Dalfampridine has been associated with infrequent serum aminotransferase elevations during therapy and has not been convincingly linked to instances of clinically apparent liver injury. In analyses of safety of dalfampridine in pre-registration controlled trials with 1922 patients with multiple sclerosis, there were no... | The possible mechanisms by which dalfampridine could be hepatotoxic are not clear. Dalfampridine is eliminated largely unchanged in the urine and appears to have little hepatic metabolism.\n\nDrug Class: Multiple Sclerosis Agents (Symptomatic Therapies) | null | Dalfampridine – Generic, Ampyra® | Multiple Sclerosis Agents | null |
Clofibrate.nxml | Clofibrate | 2017-01-24 | Clofibrate is a fibric acid derivative used in the therapy of hypertriglyceridemia and dyslipidemia. Clofibrate therapy is associated with mild and transient serum aminotransferase elevations and with rare instances of acute liver injury. | Clofibrate (kloe fye' brate) is a fibric acid derivative. The lipid lowering activity of clofibrate 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. Clofibrate increases lipoprotein li... | Mild, transient serum aminotransferase elevations develop in a small proportion of patients receiving clofibrate, but values above 3 times normal occur in 2% or less. These abnormalities are usually asymptomatic and transient, resolving even with continuation of clofibrate. There have been rare reports of clinically ap... | The mechanism of hepatotoxicity of clofibrate is not known but may relate to formation of toxic intermediates or interference with normal hepatic enzyme function. The development of gallstones during clofibrate therapy may relate to its effects in increasing cholesterol while lowering bile acid secretion in bile, thus ... | There have been no reports of acute liver failure, chronic hepatitis, cirrhosis or vanishing bile duct syndrome related to clofibrate therapy. There is likely to be some degree of cross reactivity to hepatotoxic reactions to fibrates, but not to statins.\n\nDrug Class: Antilipemic Agents, Fibrates | Clofibrate – Atromid-S® | Antilipemic Agents | null |
Ramipril.nxml | Ramipril | 2018-02-11 | Ramipril is an angiotensin-converting enzyme (ACE) inhibitor used in the therapy of hypertension and heart failure. Ramipril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. | Ramipril (ra' mi pril) is an ACE inhibitor widely used in the therapy of hypertension, heart failure and for reduction in risk of myocardial infarction and stroke. Like other ACE inhibitors, ramipril inhibits the conversion of angiotensin I, a relatively inactive molecule, to angiotensin II which is the major mediator ... | Ramipril, like other ACE inhibitors, has been associated with a low rate of serum aminotransferase elevations (<2%) that, in controlled trials, was no higher than with placebo therapy. These elevations were transient and rarely required dose modification. Rare instances of clinically apparent acute liver injury have be... | The cause of the minor serum aminotransferase elevations associated with ramipril therapy is not known. The clinically apparent acute liver injury due to ramipril is idiosyncratic and is likely due to a reaction to a minor metabolite. Ramipril is hydrolyzed in the liver to its active carboxylic metabolite ramiprilat, b... | Only a few cases of ramipril associated liver injury have been reported, but the rare instances that have been published have resembled typical ACE inhibitor related hepatic injury. Most instances of acute liver injury related to ACE inhibitors have been self limited, but severe cases of cholestatic hepatitis can resul... | Ramipril – Generic, Altace® | Angiotensin-Converting Enzyme Inhibitors | null |
BileAcidResins.nxml | Bile Acid Resins or Sequestrants | 2017-09-28 | null | null | null | null | null | null | null | null |
Tramadol.nxml | Tramadol | 2020-11-24 | Tramadol is an opioid analgesic used for the therapy of mild-to-moderate pain. Tramadol overdose can cause acute liver failure. Pharmacologic doses of tramadol has not been associated with cases of clinically apparent drug induced liver disease. | Tramadol is a synthetic codeine analog that acts as a weak opioid agonist in addition to mildly inhibiting serotonin and norepinephrine reuptake. Tramadol is effective against mild-to-moderate pain, but is not as effective as standard opioids and not recommended for severe pain. Tramadol was approved for use in the Uni... | Serum aminotransferase levels can be elevated in a small proportion of patients receiving tramadol, particularly with high doses. Intentional and accidental overdoses of tramadol can cause respiratory arrest as well as acute liver failure, several fatal instances of which have been reported. In these cases, however, th... | The mechanism of hepatotoxicity from overdoses of tramadol is not known, but is likely due to direct hepatocellular injury, either as a result of ischemia or mitochondrial toxicity. Tramadol is metabolized by the liver, predominantly by CYP 2D6 and 3A4 to its active form and it can result in troublesome drug-drug inter... | The minor enzyme elevations that occur with tramadol use are usually mild, asymptomatic and self-limited, resolving even with continuation of therapy. Cases of acute liver failure due to tramadol overdose require intensive medical management and can be fatal. In acute overdoses, there may be interaction with other agen... | Tramadol – Generic, Ultram® | Opioids | null |
Allopurinol.nxml | Allopurinol | 2020-12-26 | Allopurinol is a xanthine oxidase inhibitor and a widely used medication for gout. Allopurinol is a rare but well known cause of acute liver injury that has features of a hypersensitivity reaction and can be severe and even fatal. | Allopurinol (al' oh pure' i nol) is an analog of hypoxanthine and a potent inhibitor of the enzyme xanthine oxidase that is responsible for converting hypoxanthine to xanthine and xanthine to uric acid in the breakdown pathway of purines. Allopurinol lowers serum and tissue uric acid levels and has potent activity agai... | Chronic therapy with allopurinol is associated with transient and minor liver test abnormalities in 2% to 6% of patients, which resolve spontaneously or with drug discontinuation. More importantly, allopurinol has been linked to a very distinctive form of acute liver injury that is accompanied by prominent immunoallerg... | The mechanism of allopurinol hepatotoxicity is believed to be immunoallergic. Many cases resemble those of anticonvulsant hypersensitivity. Recently, several cases have been linked to concurrent infection with human herpesvirus-6, EBV or CMV infections. Severe allopurinol hypersensitivity skin reactions have been close... | While most cases of acute liver injury attributed to allopurinol are self-limited and start to resolve within 7 to 10 days of stopping the medication, other cases are protracted, severe and even fatal. Instances of chronic vanishing bile duct syndrome due to allopurinol have been reported. Because of the accompanying a... | Allopurinol – Generic, Aloprim®, Zyloprim® | Antigout Agents/Gout Suppressants | null |
GreenTea.nxml | Green Tea | 2020-11-20 | Green tea is a popular and commonly consumed drink and its extract is found in many herbal and dietary supplements (HDS). Green tea extract and, more rarely, ingestion of large amounts of green tea have been implicated in cases of clinically apparent acute liver injury, including instances of acute liver failure and ei... | Both green tea and black tea are produced from the leaves of the Chinese tea tree Camellia sinensis. Green tea, unlike black tea, is unfermented, which helps to preserve its antioxidant polyphenolic catechols. Green tea has long been believed to have health restoring properties and its ingredients to have antioxidant a... | Drinking green tea has not been associated with liver injury or serum aminotransferase elevations; indeed, cross sectional studies suggest that regular use of green tea is associated with lower serum ALT and AST values. Nevertheless, case series and a systematic review by the United States Pharmacopeia have raised the ... | Preclinical and human data implicate the catechin component of green tea as the culprit of hepatotoxicity. Approximately 10% of the green tea extract is composed of catechins; of these, epigallocatechin-3-gallate (EGCG) is present in highest concentration. There is great variability in the concentration of green tea ex... | Given the wide spread consumption of green tea and its extract in various HDS, liver injury from green tea is rare. Patients who present with acute liver injury, particularly with a hepatocellular pattern without an obvious cause, should be asked about the use of HDS and green tea extract, and should be advised to stop... | Green Tea – Generic | Herbal and Dietary Supplements | null |
ObeticholicAcid.nxml | Obeticholic Acid | 2019-12-10 | Obeticholic acid (OCA) is a synthetically modified bile acid and potent agonist of the farnesoid X nuclear receptor (FXR) that is used to treat liver diseases including primary biliary cholangitis. Obeticholic acid has not been linked to elevations in serum enzyme levels during therapy, but has been linked to an increa... | Obeticholic (oh bet" i koe' lik) acid is a synthetically modified bile acid that is a potent agonist of the farnesoid X nuclear receptor (FXR), a nuclear receptor with major effects on bile acid synthesis and transport as well as lipid metabolism and glucose homeostasis. Obeticholic acid has been shown to improve serum... | In multiple preregistration clinical trials, obeticholic acid was found to decrease serum enzyme elevations in a high proportion of patients with different liver diseases. Instances of paradoxical worsening of liver disease or further increases in serum ALT or AST were not reported. However, the product label for obeti... | null | Patients on obeticholic acid should be monitored with liver tests, including serum bilirubin, ALT, AST and alkaline phosphatase, during the first few months of therapy to assess both its efficacy and safety. Patients with paradoxical worsening of the liver disease, with persistent worsening of serum enzyme elevations a... | Obeticholic Acid – Ocaliva® | Gastrointestinal Agents | null |
Cholestyramine.nxml | Cholestyramine | 2017-09-28 | Cholestyramine is a nonabsorbed bile acid sequestrant that is used a therapy of hyperlipidemia and for the pruritus of chronic liver disease and biliary obstruction. Cholestyramine has been associated with mild and transient serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent... | Cholestyramine (koe" le stye' ra meen) is a large, highly positively charged anion exchange resin that binds to negatively charged anions such as bile acids (as well as other organic compounds and some medications). The binding of bile acids to cholestyramine creates an insoluble compound that cannot be reabsorbed and ... | There is little evidence that cholestyramine causes significant liver injury. However, mild elevations in serum aminotransferase levels occur in a proportion of patients on cholestyramine. The elevations have been mild, transient and without accompanying symptoms or jaundice. In one prospective study, cholestyramine th... | The mechanism by which cholestyramine causes serum aminotransferase elevations is not known. Because cholestyramine is not absorbed, it is surprising that it might cause liver injury, even mild and asymptomatic serum enzyme elevations. There is also little evidence that the contraction of the bile acid pool caused by i... | null | Cholestyramine – Generic, Questran® | Antilipemic Agents | null |
Pramipexole.nxml | Pramipexole | 2017-07-20 | Pramipexole is a selective dopamine receptor agonist used in the therapy of Parkinson disease. Pramipexole therapy is associated with a low rate of transient serum enzyme elevations during treatment, but has not been implicated in cases of clinically apparent acute liver injury. | Pramipexole (pram" i pex' ole) is synthetic, nonergot derivative and dopamine receptor agonist that has selective activity for the D2 class of dopamine receptors and little agonist activity for the D1 class. For this reason, pramipexole may be better tolerated than bromocriptine or pergolide which have activity for bot... | Pramipexole 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. Pramipexole has not been implicated in cases of clinically apparent acute liver injury which must be rare, if... | Pramipexole is minimally metabolized by the liver and is excreted largely unchanged in the urine. | Instances of liver injury attributed to pramipexole have been mild, asymptomatic and self-limiting. No instances of acute liver failure or chronic injury have been reported.\n\nDrug Class: Antiparkinson Agents\n\nOther Drugs in the Subclass, Dopamine Receptor Agonists: Apomorphine, Bromocriptine, Pergolide, Ropinirole,... | Pramipexole – Generic, Mirapex® | Antiparkinson Agents | null |
Moxifloxacin.nxml | Moxifloxacin | 2020-03-10 | Moxifloxacin is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria as well as atypical pathogens. Moxifloxacin has been linked to mild ALT elevations during therapy and to rare instances of idiosyncratic acute liver injury with symptoms and jaundice. | Moxifloxacin (mox" i flox' a sin) is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria including multidrug resistant strains of Streptococcus pneumoniae. Like other fluoroquinolones, moxifloxacin is active against a wide range of aerobic gram-positive and gram-negative organisms.... | Moxifloxacin, 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. Moxifloxacin has been linked to rare but occasionally severe and even fatal case... | The cause of hepatic injury is unknown but is likely to be immune-mediated as many cases occur in the context of a system hypersensitivity reaction. Moxifloxacin is metabolized by sulfate or glucuronide conjugation and has no effect on cytochrome P450 enzymes. | Mild-to-moderate hepatic injury due to moxifloxacin should be followed by full recovery within 4 to 8 weeks. Fulminant cases and chronic cholestatic forms with vanishing bile duct syndrome have been described. Cross reactivity of the hepatic injury between different fluoroquinolones has not been demonstrated, but is su... | Moxifloxacin – Generic, Avelox® | Antiinfective Agents | null |
Erenumab.nxml | Erenumab | 2018-08-08 | Erenumab is a monoclonal antibody to the receptor for calcitonin gene related peptide which plays a role in inducing migraine headaches. Erenumab is used for prevention of migraine in patients with episodic or chronic migraine headaches. Erenumab therapy has not been associated with serum enzyme elevations during thera... | Erenumab (e ren' ue mab) is a recombinant, human monoclonal IgG1 antibody to the calcitonin gene related peptide (CGRP) receptor which plays an important role in migraine headaches. CGRP is a neuropeptide found throughout the central and peripheral nervous systems which has potent vasodilator and pain signaling activit... | In large clinical trials, erenumab was not associated with changes in serum aminotransferase levels during therapy and rates of most adverse reactions were similar to those in patients who received placebo. There have been no published reports of clinically apparent acute liver injury attributed to erenumab therapy. Th... | null | null | Erenumab – Aimovig® | Migraine Headache Agents | null |
Fosphenytoin.nxml | Fosphenytoin | 2020-11-08 | Fosphenytoin is a prodrug of phenytoin available in parenteral forms only. While not specifically associated with cases of drug induced liver injury, fosphenytoin is converted to phenytoin which is a well known cause of acute idiosyncratic drug induced liver disease. | Fosphenytoin (fos' fen i toyn") is a hydantoin derivative that is a prodrug of phenytoin that is rapidly converted to phenytoin and is likely to have the same mechanisms of activity, efficacy and side effects as phenytoin. Phenytoin acts by stabilization of neuronal membranes through increasing the efflux and decreasin... | Hepatic injury has not been specifically ascribed to use of fosphenytoin, but because it is metabolized to phenytoin, it is likely to cause similar hepatic injury. Cases of typical immunoallergic hepatitis and DRESS syndrome have been reported in patients initially treated with fosphenytoin and then converted to the or... | The mechanism of fosphenytoin and phenytoin hepatotoxicity is not known, but is thought to be immunoallergic. | The course and outcome of hepatotoxicity from fosphenytoin should be similar to that of phenytoin.\n\nReferences on the safety and hepatotoxicity of fosphenytoin are included in the Annotated Bibliography of Phenytoin, last updated in July 2020.\n\nDrug Class: Anticonvulsants; see also Phenytoin | Fosphenytoin – Generic, Cerebyx® | Anticonvulsants | null |
Daridorexant.nxml | Daridorexant | 2025-02-05 | Daridorexant is an orexin receptor antagonist currently used in the treatment of insomnia in adults. Daridorexant is associated with rare instances of elevations in serum aminotransferase levels during therapy but has not been implicated in cases of clinically apparent liver injury. | Daridorexant (da ree” doe rex’ ant) is an orexin receptor antagonist used for therapy of insomnia in adults. Orexin is a neuropeptide that plays a role in wakefulness and central nervous system neurons, with orexin receptors that are activated during wakeful periods and are inactive during sleep. Engagement of the orex... | In two controlled trials conducted in support of approval of daridorexant in the United States, there were no changes in serum ALT, AST, alkaline phosphatase or bilirubin levels during treatment and no instances of drug induced liver injury. Since its approval and more widespread clinical use, there have been no publis... | The mechanism by which daridorexant might cause serum aminotransferase elevations is not known. It is metabolized in the liver by the P450 system, largely by CYP 3A4 and is susceptible to drug-drug interactions. The dose of daridorexant may have to be adjusted if there is concurrent therapy with moderate or strong CYP ... | There is no evidence that daridorexant can cause liver injury, and development of ALT or AST elevations or clinical evidence of liver injury during therapy should lead to search for another cause.\n\nDrug Class: Sedatives and Hypnotics; Drugs for Insomnia\n\nOther Orexin Receptor Antagonists: Lemborexant, Suvorexant | Daridorexant – Quviviq® | Sedatives and Hypnotics | null |
Rifaximin.nxml | Rifaximin | 2018-06-14 | Rifaximin is a nonabsorbable antibiotic that is used as treatment and prevention of travelers’ diarrhea and, in higher doses, for prevention of hepatic encephalopathy in patients with advanced liver disease and to treat diarrhea in patients with irritable bowel syndrome. Rifaximin has minimal oral absorption and has no... | Rifaximin (rif ax' i min) is a synthetic antibiotic and derivative of rifamycin specifically designed to have minimal gastrointestinal absorption (<0.4%). It is a broad spectrum antibiotic with activity against both aerobic and anaerobic organisms, both gram negative and gram positive. The antibiotic activity of rifaxi... | Despite widespread use, there is little evidence that rifaximin when given orally causes liver injury, either in the form of serum enzyme elevations or clinically apparent liver disease.\n\nLikelihood score: E (unlikely cause of clinically apparent liver injury). | Rifaximin has minimal systemic absorption and is unlikely to reach serum concentrations that might be hepatotoxic or induce CYP 3A4 enzyme activity or inhibit hepatic organic anion transport proteins, which the native compound has been shown to affect.\n\nOther agents used for hepatic encephalopathy include neomycin an... | null | Rifaximin – Xifaxan® | Antiinfective Agents | null |
FentanylAndAnalogues.nxml | Fentanyl | 2019-04-25 | Fentanyl is a fully synthetic opioid that is more potent that morphine and is commonly used for management of severe pain and as an adjunct to general anesthesia. Alfentanil, remifentanil and sufentanil are phenylpiperidine analogues of fentanyl and have a similar spectrum of activity, but differ in their pharmacokinet... | Fentanyl (fen’ tan il) is a synthetic phenylpiperidine which shares similar pain relieving activities with morphine, but is 50 to 100 times more potent. Like morphine, fentanyl is an agonist for the µ type opiate receptors which are found in the central nervous system but also on heart, lung, vascular and intestinal ce... | Although fentanyl has many serious side effects and has been implicated in deaths from overdose and inadvertent use, it has not been linked to cases of clinically apparent liver injury. In large clinical trials, chronic fentanyl therapy for pain has not been associated with serum enzyme elevations or cases of hepatotox... | null | null | Fentanyl – Generic, Duragesic®, Sublimaze® | Opioids | [
{
"cas_registry_number": "437-38-7",
"molecular_formula": "C22-H28-N2-O",
"name": "Fentanyl"
},
{
"cas_registry_number": "71195-58-9",
"molecular_formula": "C21-H32-N6-O3",
"name": "Alfentanil"
},
{
"cas_registry_number": "132875-61-7",
"molecular_formula": "C20-H28-N2-O5",
... |
Axatilimab.nxml | Axatilimab | 2024-11-07 | Axatilimab is a humanized monoclonal antibody to the colony stimulating factor-1 receptor that is used to treat patients with chronic graft-versus-host disease who have active disease despite having received at least two previous systemic therapies. Axatilimab therapy is often accompanied by transient serum enzyme elev... | Axatilimab (axe” a til’ i mab) is a humanized monoclonal IgG4 antibody directed against the colony stimulating factor-1 receptor (CSF-1R) which is used to treat adults with active, refractory chronic graft-vs-host disease (GvHD). Axatilimab binds to CSF-1R on monocytes and macrophages, blocking their activation and ind... | In preregistration controlled trials, elevations in serum aminotransferase levels arose in 12.7% of patients treated with 0.3 mg/kg and in higher rates with higher doses, 21.5% at 1 mg/kg and 40% at 3 mg/kg. Elevations in aminotransferase levels above 5 times the ULN occurred in only 1.3% of patients and all of the ele... | Serum ALT elevations may be a direct result of inhibition of CSF-1R because elevations occur in many enzyme levels including alkaline phosphatase, GGT, creatine phosphatase, amylase and lipase, but rarely result in organ injury. These transient laboratory abnormalities may be explained by Kupffer cells depletion and re... | It is appropriate to monitor patients with chronic GvHD for liver test abnormalities before starting and at intervals during therapy. The serum aminotransferase elevations that were reported during axatilimab therapy were generally transient, mild and asymptomatic and did not require dose modification or delay in thera... | Axatilimab – Niktimvo® | Immunosuppressive Agents | null |
Elagolix.nxml | Elagolix | 2019-01-31 | Elagolix is an oral, nonsteroidal gonadotropin releasing hormone (GnRH) antagonist that decreases estrogen production and is used to treat painful forms of endometriosis in women. Elagolix therapy is associated with a low rate of serum enzyme elevations during therapy and has yet to be linked to instances of clinically... | Elagolix (el ag" o lix') is a synthetic nonsteroidal antagonist of gonadotropin releasing hormone (GnRH) that blocks GnRH stimulation of luteinizing hormone (LH) and follicular stimulating hormone (FSH) production by the pituitary gland, thereby decreasing the synthesis of estrogen by the ovaries in women and testoster... | Elagolix therapy has been associated with serum enzyme elevations in a small proportion of patients, rates of ALT elevations above 3 times the upper limit of normal being 0.2% with 150 mg once daily and 1.1% with 200 mg twice daily. The elevations, however, are generally mild and self-limited, resolving even without do... | The mechanism by which elagolix might cause liver injury is unknown. Elagolix has multiple complex interactions with several hepatic drug metabolizing enzymes, is a mild inducer and a substrate of CYP 3A4 and drug levels can be significantly increased by OATP1B1 and CYP 3A4 inhibitors. | Serum aminotransferase elevations during elagolix therapy are usually mild and self-limited, rarely requiring dose adjustment or drug discontinuation. Routine monitoring of liver tests is not recommended except in patients with known, preexisting liver disease. There is no evidence of cross sensitivity to liver injury ... | Elagolix – Orilissa® | Obstetrical and Gynecological Agents | null |
Nifedipine.nxml | Nifedipine | 2017-01-11 | Nifedipine is a first generation calcium channel blocker used to treat hypertension and angina pectoris. Nifedipine therapy is associated with a low rate of serum enzyme elevations and has been linked to several instances of clinically apparent acute liver injury. | Nifedipine (nye fed' i peen) belongs to the dihydropyridine class of calcium channel blockers (first in its class and similar to amlodipine, felodipine and nicardipine) and is used for the treatment of hypertension and angina pectoris. Like other calcium channel blockers, nifedipine acts by inhibiting the transmembrane... | Mild and transient elevations in serum aminotransferase levels may occur during nifedipine therapy, but often resolve even with continuation of therapy. Clinically apparent acute liver injury with jaundice due to nifedipine is rare and described only in isolated case reports. The time to onset of injury is typically 1 ... | The mechanism of nifedipine hepatotoxicity is not known, but is likely to be due to production of a toxic or immunogenic intermediate during its metabolism by the liver. | The severity of liver injury from nifedipine ranges from mild and transient serum enzyme elevations to self-limited jaundice to an alcoholic hepatitis-like syndrome. Complete recovery is expected after stopping the drug and recovery is usually rapid (3 to 8 weeks). There is little information on cross sensitivity to li... | Nifedipine – Generic, Adalat®, Procardia® | Cardiovascular Agents | null |
SndGenSulfonylureas.nxml | Sulfonylureas, Second Generation | 2018-03-16 | The second generation sulfonylureas include glyburide (also known as glibenclamide), gliclazide, glipizide, and glimepiride, which are oral hypoglycemic agents that are widely used in therapy of type 2 diabetes. These agents are known, but infrequent causes of clinically apparent liver injury. | The sulfonylureas are substituted arylsulfonylureas, their differences being in the types of substitutions at the two ends of the molecule. The sulfonylureas lower blood glucose through an increase in secretion of insulin from pancreatic beta cells. They may also have other extra-pancreatic hypoglycemic actions that ar... | Minor enzyme elevations have been reported to occur during sulfonylurea therapy in less than 1% of patients, rates that are similar to what occurs with placebo therapy. Clinically apparent liver injury from the sulfonylureas is rare, but has been reported for virtually all of the currently available forms and appears t... | The mechanism of liver injury due to sulfonylureas is unknown, but suspected to be due to hypersensitivity. Cross reactivity to reactions to sulfonamides can occur, but not invariably and the overall pattern of injury and outcome of sulfonylurea associated hepatic injury does not resemble the acute, immunoallergic patt... | null | Gliclazide – Diamicron® | Antidiabetic Agents | [
{
"cas_registry_number": "21187-98-4",
"molecular_formula": "C15-H21-N3-O3-S",
"name": "Gliclazide"
},
{
"cas_registry_number": "93479-97-1",
"molecular_formula": "C24-H34-N4-O5-S",
"name": "Glimepiride"
},
{
"cas_registry_number": "29094-61-9",
"molecular_formula": "C21-H27-... |
Flurbiprofen.nxml | Flurbiprofen | 2018-01-25 | Flurbiprofen is a nonsteroidal antiinflammatory drug (NSAID) used in treatment of mild-to-moderate pain and symptoms of chronic arthritis. Flurbiprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury. | Flurbiprofen (flur" bi proe' fen) belongs to the propionic acid derivative class of NSAIDs, similar to fenoprofen, naproxen and ibuprofen. Like other NSAIDs, flurbiprofen is a cyclo-oxygenase (Cox-1 and -2) inhibitor that blocks the formation of prostaglandins that are important in pain and inflammatory pathways. Flurb... | Prospective studies show that mild elevations in serum aminotransferase levels can occur in up to 15% of patients taking flurbiprofen, but these are generally transient, mild and asymptomatic, often resolving even with drug continuation. Marked aminotransferase elevations (>3 fold elevated) occur in <1% of patients. Cl... | The mechanism of flurbiprofen hepatotoxicity is not known, but likely to be due to an idiosyncratic hypersensitivity reaction to an intermediate of its metabolism. Flurbiprofen is extensively metabolized by the liver, largely through the cytochrome P450 pathway (CYP 2C9). | Severity ranges from asymptomatic elevations in serum aminotransferase levels, to symptomatic hepatitis with or without jaundice, to acute liver failure and death. There are no convincing cases of chronic hepatitis or vanishing bile duct syndrome attributable to flurbiprofen use in the published literature. Patients wi... | Flurbiprofen – Generic, Ansaid® | Nonsteroidal Antiinflammatory Drugs | null |
Aprepitant.nxml | Aprepitant | 2024-02-28 | Aprepitant and its prodrug fosaprepitant are antiemetic agents that are used to prevent cancer chemotherapy related nausea and vomiting. Both aprepitant and fosaprepitant are associated with a low rate of serum enzyme elevations after treatment which are similar to rates with comparator therapies, and neither agent has... | Aprepitant (a pre’ pi tant) is a substance P antagonist that blocks the neurokinin 1 (NK1) receptor, which is found in the central nervous system and induces the vomiting reflex when activated by its ligand, substance P. Aprepitant has been shown to inhibit both acute and delayed nausea and vomiting associated with can... | In preregistration clinical trials of aprepitant, serum aminotransferase elevations occurred in 6% of treated patients compared to 4.3% in controls receiving cancer chemotherapy. The aminotransferase elevations were transient, mild-to-moderate in severity, and not associated with symptoms or jaundice. There have been n... | The serum aminotransferase elevations that occur after aprepitant therapy are more likely due to the chemotherapy rather than the antiemetic. The lack of reported cases of liver injury due to aprepitant and fosaprepitant may be due to the low doses and short duration of typical therapy. Aprepitant is metabolized by and... | null | Aprepitant – Generic, Emend® | Gastrointestinal Agents | null |
Clomiphene.nxml | Clomiphene | 2017-10-17 | Clomiphene is an oral agent used to treat infertility in women desiring pregnancy. Clomiphene has been linked to a low rate of transient serum aminotransferase elevations during therapy and to rare instances of clinically apparent liver injury, which can be severe and even fatal. | Clomiphene (kloe' mi feen) is an orally available, nonsteroidal antiestrogen that stimulates ovulation and is used largely as therapy of infertility in women. Clomiphene interacts with estrogen receptors in many tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina and cervix. The inhibition of est... | There is little information on serum aminotransferase levels during clomiphene therapy which is typically given in low doses for a short time only. There have been a few reports of mild serum enzyme elevations in patients taking clomiphene, but no convincing instances of idiosyncratic, clinically apparent liver injury ... | The mechanism of injury accounting for serum enzyme elevations during clomiphene therapy is not known. Clomiphene is metabolized in the liver and has a prolonged half-life. The liver test abnormalities found during OHSS may be due to fluid shifts, hypovolemia and ischemia. | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. Clomiphene has not been implicated in cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. There does not appear to be cross reactivity in risk for h... | Clomiphene – Generic, Clomid® | Infertility Agents | null |
Stiripentol.nxml | Stiripentol | 2019-04-10 | Stiripentol is a structurally unique anticonvulsant that has been introduced as adjuvant therapy of Dravet syndrome, a rare form of severe childhood epilepsy. There is limited information on the safety of stiripentol, but it has not been associated with serum aminotransferase elevations or linked to cases of clinically... | Stiripentol (stir" i pen' tol) is an aromatic alcohol, structurally unrelated to other anticonvulsants that is approved for use in the United States as adjunctive therapy of seizures in patients with Dravet syndrome, a rare childhood-onset disorder marked initially by hemiclonic seizures, often triggered by fever and f... | Limited data are available on the safety of stiripentol, based mainly on open-label and small, placebo controlled clinical trials in children with Dravet syndrome. In these studies, addition of stiripentol to chronic clobazam therapy was not associated with an increased frequency of serum aminotransferase elevations, a... | The mechanism by which stiripentol might cause liver injury is not known. Stiripentol is extensively metabolized by the liver via the microsomal P450 system, and it is a moderate inhibitor of CYP 2C 19 and, to a lesser extent, CYP 3A4 and 1A2. Stiripentol has major drug-drug interactions and can alter metabolism of man... | There is no reason to suspect cross sensitivity to hepatotoxicity of stiripentol with other drugs for epilepsy such as the benzodiazepines or aromatic anticonvulsants.\n\nDrug Class: Anticonvulsants | Stiripentol – Diacomit® | Anticonvulsants | null |
Daptomycin.nxml | Daptomycin | 2017-12-04 | Daptomycin is an intravenously administered, broad spectrum antibiotic used to treat complex skin and tissue infections, endocarditis and bacteremia. Daptomycin is associated with a low to modest rate of serum enzyme elevations during therapy, but is a very rare cause of clinically apparent liver injury. | Daptomycin (dap" toe mye' sin) is a cyclic lipopeptide antibiotic that is poorly absorbed orally and must be given intravenously. Daptomycin appears to act by binding to bacterial membranes causing their depolarization and disruption and cell death. Daptomycin has been shown to be highly effective in treating severe gr... | Elevations in serum aminotransferase levels occur in 2% to 6% of patients receiving daptomycin, rates that are minimally higher than with placebo or comparator drugs. The elevations are generally mild-to-moderate, asymptomatic and self-limited, frequently resolving without discontinuation or even interruption of therap... | null | The severity of the liver injury linked to daptomycin therapy is usually mild and self-limited, and dose modification or discontinuation is rarely necessary. No instances of acute liver failure, chronic hepatitis or vanishing bile duct syndrome have been attributed to daptomycin therapy. The outcome of reexposure to da... | Daptomycin – Generic, Cubicin® | Antiinfective Agents | null |
Protriptyline.nxml | Protriptyline | 2020-04-05 | Protriptyline is a tricyclic antidepressant that was previously widely used in the therapy of major depression. Most of the tricyclic antidepressants have been shown to cause a low rate of mild and transient serum enzyme elevations and rare cases of clinically apparent acute cholestatic liver injury. The potential hepa... | Protriptyline (proe trip' ti leen) is a tricyclic antidepressant which acts by inhibition of serotonin and norepinephrine reuptake within synaptic clefts in the central nervous system, thus increasing brain levels of these neurotransmitters. Protriptyline is indicated for therapy of major depression and was approved fo... | Liver test abnormalities have been reported to occur in 10% to 12% of patients on tricyclic antidepressants, but elevations are uncommonly above 3 times the upper limit of normal. The aminotransferase abnormalities are usually mild, asymptomatic and transient, reversing even with continuation of medication. The rate of... | The mechanism by which protriptyline might cause liver injury is not known. It undergoes extensive hepatic metabolism and a possible cause of liver injury is production of a toxic intermediate of metabolism. Many cases have features of hypersensitivity, and more rapid recurrence with reexposure and some instances of tr... | The serum aminotransferase elevations that occur on protriptyline therapy are usually self-limited and do not require dose modification or discontinuation of therapy. The acute liver injury caused by tricyclic antidepressants is typically self-limited, but progressive and fatal instances of acute hepatitis and prolonge... | Protriptyline – Generic, Vivactil® | Antidepressant Agents | null |
Fluoxetine.nxml | Fluoxetine | 2018-02-02 | Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) widely used as an antidepressant. Fluoxetine 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. | Fluoxetine (floo ox' e teen) is an antidepressant which was one of the first of the class of selective serotonin reuptake inhibitors (SSRIs) introduced into clinical use. By blocking the reuptake of serotonin in CNS synaptic clefts, SSRIs increase serotonin levels in the brain which is associated with their antidepress... | Liver test abnormalities have been reported to occur rarely in patients on fluoxetine (less than 1%), and elevations are usually modest and usually do not require dose modification or discontinuation. Rare instances of acute, clinically apparent episodes of liver injury with marked liver enzyme elevations with or witho... | The mechanism by which fluoxetine causes liver injury is not known. Fluoxetine is extensively metabolized by the liver, mainly via the cytochrome P450 system, and hepatotoxicity may be mediated by toxic intermediates of their metabolism. | The serum aminotransferase elevations that occur on fluoxetine 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 fluoxetine therapy. Persons with intolerance to fluoxetine may have simi... | Fluoxetine – Generic, Prozac® | Antidepressant Agents | null |
Entacapone.nxml | Entacapone | 2021-10-25 | Entacapone is a catechol-O-methyltransferase inhibitor used in the therapy of Parkinson disease as adjunctive therapy in combination with levodopa and carbidopa. Entacapone has been associated with a low rate of serum enzyme elevations during treatment, but has yet to be implicated in cases of clinically apparent acute... | Entacapone (en tak' a pone) is a specific inhibitor of cathechol-O-methyltransferase (COMT) which is a major enzyme in the pathway of levodopa metabolism. As a result, entacapone slows the metabolism of levodopa, causing an increase in its bioavailability and duration of action. Entacapone inhibits COMT activity only p... | Entacapone therapy has been associated with serum aminotransferase elevations (above 3 times the upper limit of normal) in only 0.3% to 0.5% of patients, which is similar or minimally higher than the rate in subjects receiving placebo. The elevations were usually transient and asymptomatic and rarely required dose adju... | Entacapone is extensively metabolized by the liver and eliminated though biotransformation, mostly by glucuronidation via UDP-glucuronosyl transferase. Polymorphisms of this enzyme have been linked to liver enzyme elevations during therapy, but the relationship between dose, metabolism and liver injury due to entacapon... | The cases of hepatotoxicity attributed to entacapone have been mild and self-limiting. There have been no reports of acute liver failure, chronic liver injury or vanishing bile duct syndrome associated with entacapone therapy. In at least one case report, a patient who developed raised serum enzymes during tolcapone th... | Entacapone – Generic, Comtan® | Parkinson Disease Agents | null |
Prochlorperazine.nxml | Prochlorperazine | 2020-07-01 | Prochlorperazine is a phenothiazine used primarily as an antiemetic agent. In rare instances, prochlorperazine can cause clinically apparent acute and chronic cholestatic liver injury. | Prochlorperazine (proe" klor per' a zeen) is a tricyclic aliphatic phenothiazine which acts by postsynaptic inhibition of dopamine receptors. Prochlorperazine has other peripheral and central nervous system effects, producing both alpha adrenergic stimulation and blocking histamine- and serotonin-mediated effects. Proc... | Liver test abnormalities are uncommon during prochlorperazine therapy, perhaps because it is rarely given long term or in high doses chronically. Aminotransferase elevations can occur during therapy, but they are usually mild, asymptomatic and transient and reversible even with continuation of medication. Rare instance... | The mechanism by which prochlorperazine causes serum aminotransferase elevations is not known but is likely shared with other phenothiazines. Several features of the clinical presentation of prochlorperazine hepatotoxicity (short latency period, fever, eosinophilia) suggest a hypersensitivity reaction, and rechallenge ... | The serum aminotransferase elevations that occur on prochlorperazine therapy are usually transient and do not require dose modification or discontinuation of therapy. The acute cholestatic hepatitis caused by prochlorperazine is typically self-limited and benign but should prompt immediate discontinuation. A small prop... | Prochlorperazine – Generic, Compazine®, Compro® | Gastrointestinal Agents; Antipsychotic Agents | null |
Atazanavir.nxml | Atazanavir | 2017-09-01 | Atazanavir is an antiretroviral protease inhibitor that is used in the therapy and prevention of human immunodeficiency virus (HIV-1) infection and the acquired immunodeficiency syndrome (AIDS). Atazanavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels, mild elevations in indir... | Atazanavir (a" ta zan' a vir) is proteinomimetic, azapeptide that binds to the active, catalytic site of the HIV-1 protease preventing cleavage and processing of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication. Atazanavir, in combination with other antiretroviral a... | Atazanavir can cause several forms of liver injury including transient serum enzyme elevations, indirect hyperbilirubinemia, idiosyncratic acute liver injury and exacerbation of underlying chronic viral hepatitis.\n\nSome degree of serum aminotransferase elevations occurs in a high proportion of patients taking atazana... | The cause of the clinical hepatotoxicity from atazanavir is only partially known. The indirect hyperbilirubinemia associated with its use is caused by inhibition of hepatic conjugation of bilirubin, similar to what occurs in Gilbert syndrome and is not indicative of liver injury. Atazanavir is extensively metabolized b... | The severity of liver injury from atazanavir ranges from asymptomatic unconjugated hyperbilirubinemia to moderate serum aminotransferase elevations to acute hepatitis. In typical cases, recovery occurs within 1 to 2 months and neither chronic hepatitis nor vanishing bile duct syndrome have been reported due to atazanav... | Atazanavir – Reyataz®, Evotaz® (with Cobicistat) | Antiviral Agents | null |
Apremilast.nxml | Apremilast | 2017-07-25 | Apremilast is an orally available, small molecule inhibitor of phosphodiesterase-4 (PDE-4) and an immunomodulating agent that is used for treatment of refractory psoriatic arthritis. Apremilast has been linked to a low rate of serum enzyme elevations during therapy, but has not been implicated in cases of clinically ap... | Apremilast (a pre' mi last) is a small molecule inhibitor of the enzyme phosphodiesterase-4 (PDE-4) that is responsible for the degradation of cyclic adenosine monophosphate (cAMP), thereby blocking an important step in the inflammatory signaling of immune effector cells including T lymphocytes, monocytes and macrophag... | In multiple, large scale randomized controlled trials of apremilast in psoriasis and psoriatic arthritis, serum enzyme elevations were no more frequent among recipients of apremilast than placebo treatment. In these studies, serum ALT values rose above 150 U/L (3 to 4 times ULN) in 0.4% of apremilast- compared to 0.2% ... | The mechanism by which apremilast might cause serum aminotransferase elevations or liver injury is not known. It is extensively metabolized by the liver predominantly by the cytochrome P450 system and is susceptible to drug-drug interactions with agents that induce or inhibit CYP 3A4 activity.\n\nDrug Class: Dermatolog... | null | Apremilast – Otezla® | Dermatologic Agents, Psoriasis Agents | null |
CarbonicAnhydraseInh.nxml | Carbonic Anhydrase Inhibitors | 2021-10-13 | Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. Both acetazolamide and methazolamide have been linked to rare cases of clinically apparent drug induced liver disease. | Acetazolamide (a seet" a zol' a mide) and methazolamide (meth" a zol' a mide) are inhibitors of carbonic anhydrase, an enzyme that converts carbon dioxide and water to carbonic acid. Inhibition of this enzyme in the kidney causes an alkalization of the urine and diuresis. In the eye, inhibition of carbonic anhydrase ca... | Idiosyncratic, clinically apparent liver injury from acetazolamide and methazolamide is rare, but several instances have been reported as isolated case reports. Acetazolamide is a sulfonamide and cross reactivity to sulfonamide reactions have been reported. The liver injury typically arises after a few days to weeks of... | The mechanism of acetazolamide hepatic injury is believed to be due to hypersensitivity with shared pathogenesis with the sulfonamides. | null | Acetazolamide – Generic, Diamox® | Diuretics | [
{
"cas_registry_number": "59-66-5",
"molecular_formula": "C4-H6-N4-O3-S2",
"name": "Acetazolamide"
},
{
"cas_registry_number": "554-57-4",
"molecular_formula": "C5-H8-N4-O3-S2",
"name": "Methazolamide"
}
] |
Copper.nxml | Copper | 2017-10-30 | Copper is an essential trace element that is included in some over-the-counter multivitamin and mineral supplements, even though copper deficiency is quite rare and supplementation is rarely needed. The amounts of copper found in typical supplements has not been associated with serum enzyme elevations or with clinicall... | Copper is a heavy metal and essential trace element that is found in many human enzymes and transcription factors. The recommended dietary allowance is approximately 1.5 mg per day. Adequate amounts of copper are found in most Western diets, with highest levels found in shellfish, chocolate and nuts. Total body copper ... | Acute hepatotoxicity of copper is usually the result of ingestion of toxic amounts (1 to 10 g), often as a suicide attempt. In children, accidental poisoning can occur, particularly with ingestion of coins. Initial symptoms may be metallic taste and gastrointestinal distress due to gastric or small bowel erosions. Acut... | null | null | Copper Sulfate – Generic | Trace Elements and Metals | null |
Viltolarsen.nxml | Viltolarsen | 2022-11-29 | Viltolarsen is a synthetic antisense oligonucleotide designed to cause skipping of abnormal exons in the synthesis of the dystrophin gene and that is used to treat Duchenne muscular dystrophy. Viltolarsen has not been reported to cause ALT elevations during therapy and has not been linked to instances of acute liver in... | Viltolarsen (vil” toe lar’ sen) is a synthetic antisense oligonucleotide designed to cause exon 53 skipping during the processing of the mRNA of the dystrophin gene, which encodes an essential protein for muscle integrity and is mutated in Duchenne muscular dystrophy. Patients with Duchenne muscular dystrophy typically... | Duchenne muscular dystrophy is rare affecting ~1:5000 newborn boys, and those with deletion mutants in exon 53 that would be amenable to viltolarsen therapy account for only 8% of patients with the disease. The pivotal trials of viltolarsen were conducted in rather small numbers of patients, and the full spectrum of he... | The reason why viltolarsen or other RNA antisense therapeutics for Duchenne muscular dystrophy might cause hepatic injury is unknown. One possibility is that exon skipping may cause disruption of translation of other genes in hepatocytes. Viltolarsen and other antisense molecules are largely excreted unchanged in the u... | Viltolarsen therapy has not been associated with liver injury, either in the form of minor serum enzyme elevations or clinically apparent liver injury. There is no reason to suspect cross reactivity of the hepatic injury with other antisense therapies or drugs used to treat Duchenne muscular dystrophy. Regular monitori... | Viltolarsen – Viltepso® | Genetic Disorder Agents | null |
Pacritinib.nxml | Pacritinib | 2023-12-28 | Pacritinib is a small molecule Janus kinase inhibitor that is used in the treatment of intermediate or high risk, primary or secondary myelofibrosis. Pacritinib is associated with transient and usually mild elevations in serum aminotransferase during therapy but has not been linked instances of clinically apparent acut... | Pacritinib (pak ri’ ti nib) is an orally available, small molecular inhibitor of Janus kinase subtype 2 (JAK2) and the FLT3 tyrosine kinase that is used to treat symptomatic or advanced forms of myelofibrosis, a cancerous or pre-cancerous condition marked by scarring and progressive bone marrow failure with splenomegal... | In the published preregistration clinical trials of pacritinib, rates of serum ALT elevations were not provided, and no mention of ALT elevations are given in the product label or FDA review of efficacy and safety for its approval. Nevertheless, rates of ALT or AST elevations in several small clinical trials were said ... | Pacritinib therapy has not been clearly linked to serum enzyme elevations or instances of clinically apparent liver injury. It is metabolized in the liver largely through CYP 3A4 and is potentially susceptible to drug-drug interactions with agents that inhibit or induce hepatic CYP 3A4 activity. Because of its effects ... | Pacritinib has not been clearly linked to serum aminotransferase elevations and routine monitoring of liver tests is not recommended in the product label. However, serum ALT and AST elevations occur with most JAK kinase inhibitors. If detected, serum aminotransferase elevations above 5 times ULN should lead to dose red... | Pacritinib – Vonjo® | Antineoplastic Agents | null |
Viloxazine.nxml | Viloxazine | 2021-08-20 | Viloxazine is a selective norepinephrine reuptake inhibitor that is used in the therapy of attention deficit/hyperactivity disorder in children. Viloxazine has been associated with uncommon and mild serum enzyme elevations during therapy but not with occurrence of clinically apparent liver injury. | Viloxazine (vye lox” a zeen) is a selective norepinephrine reuptake inhibitor (SNRI) that is used to treat pediatric attention deficit/hyperactivity disorder (ADHD). ADHD is marked by variable degrees of inattention, impulsivity and hyperactivity that is inconsistent with developmental levels and that impairs daily lif... | In four placebo-controlled trials of viloxazine in children with ADHD, minor serum aminotransferase elevations occurred in 5% to 10% of recipients but were more than 2 times the upper limit of normal in less than 1%. In the preregistration trials, there were no instances of clinically apparent liver injury or serum ami... | The mechanism by which viloxazine might cause liver injury is not known but may be due to a toxic or immunogenic intermediate product of its metabolism. Viloxazine is metabolized in the liver largely via the cytochrome P450 system. It is a strong inhibitor CYP 1A2 and weak inducer of CYP 2D6 and 3A4 and is susceptible ... | null | Viloxazine – Qelbree® | Drugs for ADHD | null |
Lomitapide.nxml | Lomitapide | 2019-05-20 | Lomitapide is a cholesterol lowering agent that acts by inhibition of the microsomal triglyceride transfer protein and is used to treat the severe lipid abnormalities of familial hypercholesterolemia. Lomitapide is associated with mild, asymptomatic and self-limited serum aminotransferase elevations during therapy that... | Lomitapide (loe mi' ta pide) is a potent, orally available inhibitor of the hepatic microsomal triglyceride transfer protein (MTTP) and is used to treat severe forms of familial hypercholesterolemia. MTTP is responsible for transferring triglyceride to apolipoprotein B in the liver which is necessary for the assembly o... | Lomitapide is associated with a moderately high rate of serum aminotransferase elevations during therapy, levels above 3 times the upper limit of normal (ULN) occurring in 34% of patients. Aminotransferase elevations above 10 times ULN have also been reported which can necessitate drug discontinuation. Despite the freq... | The cause of hepatic injury from lomitapide appears to be a direct effect of its mechanism of action in inhibiting triglyceride transport out of hepatocytes, which leads to hepatocyte steatosis and, in some instances, liver injury. Lomitapide is also extensively metabolized in the liver, primarily via CYP 3A4 and is ve... | The ALT elevations associated with lomitapide therapy are not uncommon and are often accompanied by increases in hepatic steatosis which may ultimately lead to steatohepatitis and significant chronic liver injury. The REMS management program calls for dose adjustment or drug discontinuation based upon the degree of ser... | Lomitapide – Juxtapid® | Antilipemic Agents | null |
Saxagliptin.nxml | Saxagliptin | 2018-01-03 | Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents. Saxagliptin is a relatively new medication and has yet to be implicated in causing clinically apparent live... | Saxagliptin (sax' a glip' tin) is an inhibitor of dipeptidyl peptidase-4, which is the major enzyme responsible for the degradation of glucagon-like peptide-1 (GLP-1), an important gastrointestinal hormone (incretin) that increases glucose dependent insulin secretion by the pancreas. By prolonging the effect of GLP-1, ... | In large clinical trials, rates of serum enzyme elevations were similar with saxagliptin therapy (<1%) as with placebo, and no instances of clinically apparent liver injury were reported. Nevertheless, postmarketing experience suggests that some DPP-4 inhibitors can cause hepatic enzyme elevations and rare instances of... | The cause of possible liver injury during saxagliptin therapy is not known. The drug is metabolized by the liver, largely by the cytochrome P450 system (CYP 3A4), and a toxic or immunogenic intermediate of metabolism might be produced that could cause liver injury. | The instances of liver injury associated with the DPP-4 inhibitors have been rare and self-limited, and have resolved rapidly and completely with stopping the medication. The similarity in activity among the DPP-4 inhibitors suggests that there may be cross sensitivity to hepatic injury among the different agents, but ... | Saxagliptin – Onglyza® | Antidiabetic Agents | null |
InterferonGamma.nxml | Interferon Gamma | 2018-05-03 | Interferon gamma is a recombinant cytokine with a multitude of actions including stimulation of T cell immunity, increase in innate immune responses, induction of Class II major histocompatibility complex molecules, and inhibition of fibrosis. Interferon gamma is used for its immune enhancing properties as therapy of c... | Interferon gamma (in' ter feer" on) is human cytokine produced by macrophages and lymphocytes that plays a critical role in both innate and adaptive immune responses. While also known as type II interferon, interferon gamma has only modest direct antiviral activity and is unrelated in structure, genetic linkage and fun... | In multiple phase 2 and 3 clinical trials, interferon gamma was found to cause mild-to-moderate serum enzyme elevations in in small portion of patients. The elevations were generally transient and without jaundice or obvious symptoms of liver injury, but rose to levels above 5 to 10 times ULN and necessitated dose modi... | The mechanism by which interferon gamma infusions might cause liver injury is unclear as it is a recombinant human protein and thus is unlikely to have direct hepatotoxicity. The induction of activated T cells, however, may be associated with some degree of hepatic inflammation and injury, but is not likely to cause fr... | The serum enzyme elevations during interferon gamma therapy are generally self-limited and benign. However, such elevations are more frequent and more marked in children less than one year of age, in whom monthly monitoring of liver tests is recommended. In situations in which ALT or AST levels rise above 5 times ULN, ... | Interferon gamma – Actimmune® | Antineoplastic Agents | null |
Cycloserine.nxml | Cycloserine | 2017-11-03 | Cycloserine is a broad spectrum antibiotic used as a second line agent for treatment of drug resistant tuberculosis, always in combination with other antituberculosis agents. Cycloserine is appears to have little or no hepatotoxic potential, but it is usually used in combination with agents that are known to be hepatot... | Cycloserine (sye" kloe ser' een) is an antibiotic that is currently used largely in the therapy of tuberculosis caused by multidrug resistant mycobacteria. Cycloserine is a d-alanine analogue of isoxazolidone that was isolated initially from Streptococcus orchidaceus and has moderate activity in vitro against mycobacte... | Cycloserine is reported to be associated with a low rate of serum aminotransferase elevations that are usually transient and asymptomatic and do not require dose modification. Cycloserine is usually used in combination with agents that are more clearly linked to liver test abnormalities, and it generally plays little o... | Cycloserine undergoes minimal hepatic metabolism, perhaps accounting for the absence of significant hepatotoxicity. Allergic reactions have been reported with cycloserine and, if severe, these may be accompanied by mild serum enzyme elevations. | Cycloserine blood levels are typically monitored during therapy and the product label recommends monitoring of blood counts, renal function and routine liver tests as well.\n\n[First line medications used in the therapy of tuberculosis in the US include ethambutol, isoniazid, pyrazinamide, rifabutin, rifampin, and rifa... | Cycloserine – Generic, Seromycin® | Antituberculosis Agents | null |
Varenicline.nxml | Varenicline | 2020-07-22 | Varenicline is a partial agonist of the nicotinic acetylcholine receptor and is used to help in smoking cessation. Varenicline has been associated with a low rate of serum enzyme elevations during therapy and, since approval and its widescale use, with rare instances of clinically apparent mild liver injury. | Varenicline (var en' i kleen) is a partial agonist of the α4 β2 nicotinic acetylcholine receptor and appears to act by blocking the binding of nicotine to this receptor while providing partial agonist effect thus relieving nicotine craving. Use of varenicline in a program to stop smoking has been shown to increase the ... | Varenicline has not been associated with rates of serum enzyme elevations during therapy greater than occurs with placebo therapy, but information on these abnormalities is limited and occasional instances of asymptomatic ALT elevations leading to drug discontinuation have been reported. In prelicensure pivotal registr... | The mechanism by which varenicline might cause liver injury is not known. Varenicline undergoes minimal hepatic metabolism and is excreted largely unchanged in the urine. | The rare reports of hepatotoxicity attributed to varenicline therapy have been mild and self-limiting. Varenicline has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome.\n\nAgents in clinical use to aid in smoking cessation and to treat nicotine withdrawal symptoms inclu... | Varenicline – Chantix® | Substance Abuse Treatment Agents | null |
Hydrocodone.nxml | Hydrocodone | 2020-11-24 | Hydrocodone is a semisynthetic, moderately potent, orally available opioid that, in combination with acetaminophen, is widely used for treatment of acute or chronic pain, and in combination with antihistamines or anticholinergics used to treat cough. Hydrocodone by itself has not been linked to serum enzyme elevations ... | Hydrocodone (hye” droe koe’ done) is a semisynthetic derivative of codeine or thebaine, natural alkaloids derived from the resin of poppy seeds (Papaver somniferum). It is well absorbed orally and has moderate opiate activity (approximately 6 times that of codeine), acting an agonist of the µ opiate receptor. The combi... | Despite wide scale use for many decades, hydrocodone by itself has not been convincingly linked to instances of clinically apparent acute liver injury. However, when combined with acetaminophen, hydrocodone combinations have become a common cause of acetaminophen acute liver injury. The typical history is of a patient ... | null | null | Hydrocodone (with Acetaminophen) – Generic, Co-Gesic®, Vicodin® | Opioids | null |
Vardenafil.nxml | Vardenafil | 2017-08-02 | Vardenafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction. Vardenafil has not been associated with serum aminotransferase elevations nor with clinically apparent liver injury. | Vardenafil (var den' a fil) is a selective inhibitor of phosphodiesterase type 5 (PDE5), an intracellular enzyme that mediates the breakdown of cyclic guanosine monophosphate (cGMP) inducing smooth muscle relaxation in the corpus cavernosum of the penis and in the pulmonary vasculature where this specific phosphodieste... | Despite fairly extensive use, vardenafil has not been associated with clinically apparent cases of liver injury and serum enzyme elevations during therapy are rare. The related PDE5 inhibitors, sildenafil and tadalafil have been linked to isolated, rare instances of acute liver injury and jaundice. The latency to onset... | While vardenafil has not been associated with hepatotoxicity, its potential for causing hypotension and use in patients with cardiac disease may lead to instances of acute ischemic liver injury. Vardenafil, like the other PDE5 inhibitors, is metabolized in the liver via the cytochrome P450 system (CYP 3A4). | While sildenafil and tadalafil have been linked to rare instances of clinically apparent acute liver injury, vardenafil has not. There is no known cross sensitivity in idiosyncratic adverse effects between vardenafil and the other PDE5 inhibitors currently in use in the United States. However, switching to another PDE5... | Vardenafil – Levitra® | PDE5 Inhibitors | null |
Telbivudine.nxml | Telbivudine | 2020-10-20 | Telbivudine is a nucleoside analogue and antiviral inhibitor of hepatitis B virus (HBV) replication which is used alone and in combination with other agents in the therapy of the hepatitis B. Telbivudine does not appear to be a significant cause of drug induced liver injury, but can be associated with flares of the und... | Telbivudine (tel biv' ue deen) is the L-enantiomer of deoxythymidine (LdT) and has antiviral activity against HBV replication both in vitro and in vivo. Telbivudine is phosphorylated intracellularly to the triphosphate which inhibits the HBV polymerase and competes with deoxythymidine for incorporation into the growing... | Telbivudine shares many features with the other L-nucleosides (lamivudine, emtricitabine) and has been linked to transient flares of hepatitis B during and after treatment of chronic hepatitis B. Serum ALT elevations above 3 times normal occurred in 5% to 10% of patients on telbivudine, which was comparable to other nu... | The apparent absence of significant hepatotoxicity from telbivudine may be due to its lack of hepatic metabolism. In vitro, telbivudine has little activity against mitochondrial polymerase gamma, inhibition of which has been implicated in the syndrome of hepatic mitochondrial injury with lactic acidosis, steatosis and ... | Flares of hepatitis B during and after telbivudine therapy can range in severity from mild, transient ALT elevations to severe acute liver injury resulting in hepatic failure and death. Flares occurring at initiation of therapy are usually mild and not associated with symptoms or jaundice. Flares associated with develo... | Telbivudine – Tyzeka® | Antiviral Agents | null |
Candesartan.nxml | Candesartan | 2017-01-13 | Candesartan is an angiotensin II receptor blocker used widely in the therapy of hypertension and heart failure. Candesartan is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. | Candesartan (kan" de sar' tan) is an angiotensin II receptor blocker (ARB) that is widely used alone or in combination with other agents as therapy of hypertension and heart failure. Candesartan inhibits the renin-angiotensin system by blocking the angiotensin II type 1 receptor (AT1), which prevents the vasoconstricti... | Candesartan has been associated with a low rate of serum aminotransferase elevations (<1%) that in controlled trials was no higher than with placebo therapy. These elevations were transient and rarely required dose modification. Rare instances of clinically apparent acute liver injury have been reported in association ... | The cause of the minor serum aminotransferase elevations and the acute liver injury associated with candesartan is not known, but resembles idiosyncratic liver injury due to a hypersensitivity reaction. Candesartan has minor liver metabolism through the cytochrome P450 system (CYP 2C9) and has minimal drug-drug interac... | The instances of acute liver injury reported with candesartan use have been self limited and have not resulted in acute liver failure or chronic liver injury. While corticosteroids have been used in cases of severe cholestasis due to ARBs, their efficacy has not been shown and their use is best avoided. Patients with c... | Candesartan – Atacand® | Angiotensin II Receptor Antagonists | null |
Brigatinib.nxml | Brigatinib | 2018-08-03 | Brigatinib is a tyrosine kinase receptor inhibitor and antineoplastic agent used in the therapy of selected forms of advanced non-small cell lung cancer. Brigatinib is associated with a moderate rate of transient elevations in serum aminotransferase levels during therapy but has yet to be linked to instances of clinica... | Brigatinib (bri ga' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against anaplastic lymphoma kinase (ALK) that is rearranged and mutated in some cancers including approximately 5% of non-small cell lung cancer (NSCLC). The mutated, rearranged ALK promotes unregulated cell growth a... | In preregistration trials of brigatinib, ALT elevations occurred in up to 40% of patients but values above 5 times the upper limit of normal (ULN) were found in only 1% to 3%. Brigatinib therapy was also associated with frequent elevations in alkaline phosphatase (15% to 29%), but the serum enzyme elevations were usual... | Serum enzyme and bilirubin elevations are frequent during therapy with tyrosine kinase inhibitors, but their cause is unknown. The liver injury may be due to direct activity against essential intracellular kinases or to production of a toxic metabolite during metabolism of the kinase inhibitor. Brigatinib is metabolize... | Brigatinib has been shown to cause transient serum aminotransferase elevations but has not been linked to cases of clinically apparent liver injury, acute liver failure or chronic hepatitis. The product label recommends monitoring of serum glucose, CPK and pancreatic enzymes, but not specifically routine liver tests. S... | Brigatinib – Alunbrig® | Antineoplastic Agents | null |
Cysteamine.nxml | Cysteamine | 2017-11-03 | Cysteamine is a simple aminothiol molecule that is used to treat nephropathic cystinosis, due to its ability to decrease the markedly elevated and toxic levels of intracellular cystine that occur in this disease and cause its major complications. Cysteamine has been associated with serum enzyme elevations when given in... | Cysteamine (sis tee' a meen) is a simple aminothiol molecule which is used to treat nephropathic cystinosis, a rare autosomal recessive disorder characterized by progressive renal tubular dysfunction and growth retardation, and which eventually leads to renal failure and need for dialysis or renal transplantation often... | During long term use of cysteamine in preregistration studies, serum ALT elevations occurred in a small proportion of treated subjects, but the background rate of serum enzyme elevations in this population is high and was not defined in the open label studies. There have been reports of more marked enzyme elevations du... | The mechanism by which cysteamine might lead to serum enzyme elevations or liver injury is not known. Cysteamine is metabolized in most cells and it does not seem to be a substrate for or affect the hepatic cytochrome P450 system. In clinical trials of cysteamine, no evidence of drug-drug interactions was identified. | Serum enzyme elevations during cysteamine therapy are generally mild and self-limited, resolving even without drug interruption or dose reduction. Other causes of liver injury should be sought before assuming that the abnormalities are due to cysteamine.\n\nDrug Class: Genetic Disorder Agents | Cysteamine Bitartrate – Cystagon® | Genetic Disorder Agents | null |
Nizatidine.nxml | Nizatidine | 2018-01-25 | Nizatidine is a histamine type 2 receptor antagonist (H2 blocker) which is widely used for treatment of acid-peptic disease and heartburn. Nizatidine has been linked to rare instances of clinically apparent acute liver injury. | Nizatidine (nye za' ti deen) was the fourth histamine type 2 receptor blocker (H2 blocker) introduced into clinical practice in the United States and is a commonly used agent for treatment of duodenal and gastric ulcer and gastroesophageal reflux disease. Other H2 blockers in clinical use include cimetidine, ranitidine... | Chronic therapy with nizatidine and other H2 blockers is associated with minor elevations in serum aminotransferase levels in 1% to 4% of patients, but similar rates have been reported in placebo recipients. The ALT elevations are usually asymptomatic and transient and may resolve without dose modification. Rare instan... | Nizatidine is metabolized by the microsomal P450 drug metabolizing enzymes and injury may be the result of its activation to a toxic intermediate. Despite its metabolism by the P450 system, nizatidine does not result in significant inhibitor or induction of the enzymes and thus is less likely to cause drug-drug interac... | The hepatic injury caused by nizatidine is usually rapidly reversible with stopping the medication, but an instance of severe hepatitis with incomplete recovery and cirrhosis has been reported (Case 1). Nizatidine has been in use for a shorter time than cimetidine or ranitidine and remains unknown whether there is cros... | Nizatidine – Generic, Axid® | Antiulcer Agents | null |
Selumetinib.nxml | Selumetinib | 2021-01-21 | Selumetinib is an oral, small molecule inhibitor of the mitogen activated protein kinase 1 and 2 (MEK1/2) that is used to treat symptomatic, refractory fibromas in neurofibromatosis type 1. Selumetinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy, but has not ... | Selumetinib (sel" ue me’ ti nib) is an orally available, specific inhibitor of mitogen activated protein kinase 1 and 2 (MEK1/2) and is used to treat neurofibromatosis. Neurofibromatosis type 1 is marked by a mutation in the neurofibromin, a tumor suppressor gene which is a negative regulator of the RAS/MAPK signaling ... | In the prelicensure clinical trials conducted in children and adults with neurofibromatosis, serum aminotransferase elevations occurred in 35% of treated subject but rose to above 5 times the upper limit of normal (ULN) in only 4%. However, there were no liver related serious adverse events and no patient had a concurr... | The causes of serum enzyme elevations during selumetinib therapy are not known. Selumetinib is metabolized in the liver largely through the cytochrome P450 pathway and specifically by CYP 3A4, and liver injury may be related to production of a toxic or immunogenic intermediate. Because it is a substrate for CYP 3A4, se... | Monitoring of laboratory tests (particularly CPK) is recommended for patients treated with selumetinib. 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 are no data t... | Selumetinib – Koselugo® | Genetic Disorder Agents, Antineoplastic Agents | null |
Rivastigmine.nxml | Rivastigmine | 2020-01-15 | Rivastigmine is an oral acetylcholinesterase inhibitor used for therapy of Alzheimer disease. Rivastigmine is associated with a minimal rate of serum enzyme elevations during therapy and is a rare cause of clinically apparent liver injury. | Rivastigmine (riv" a stig' meen) is a selective acetylcholinesterase inhibitor which acts by inhibition of the metabolism of acetylcholine in the postsynaptic clefts, thus enhancing cholinergic neurotransmission. Rivastigmine has selective activity for acetylcholinesterase in the central nervous system with little effe... | In large placebo controlled trials, rivastigmine therapy was not associated with an increased rate of serum enzyme elevations compared to placebo treatment and no instances of clinically apparent liver injury with jaundice were reported. Nevertheless, since its introduction into clinical use, rivastigmine (administered... | Rivastigmine differs from the other acetylcholinesterase inhibitors in not having major hepatic metabolism. The mechanism of potential hepatotoxicity of rivastigmine is not known, but is likely to be immunological idiosyncrasy. | Cases of hepatotoxicity from rivastigmine have been too few to characterize clinically. There have been no published reports of acute liver failure, chronic hepatitis or vanishing bile duct syndrome attributed to rivastigmine. There is no information on the possible cross sensitivity to liver injury among the various a... | Rivastigmine – Generic, Exelon® | Alzheimer Disease Agents | null |
L-Glutamine.nxml | L-Glutamine | 2021-07-12 | L-glutamine is an essential amino acid and precursor of major intracellular antioxidant molecules that is used in high doses to prevent vaso-occlusive crises in patients with sickle cell disease. L-glutamine has not been associated with serum enzyme elevations during therapy or to instances of idiosyncratic acute liver... | L-glutamine (el gloo’ ta mene) is a conditionally essential amino acid that is approved for use in the treatment of sickle cell disease to prevent painful crises. Sickle cell disease is caused by an inherited mutation in the β globin gene that creates hemoglobin S, an abnormal form of hemoglobin which is prone to polym... | In clinical trials of L-glutamine in patients with sickle cell disease, serum aminotransferase elevations were not mentioned, and there were no reports of clinically apparent liver injury. Patients with sickle cell disease frequently have jaundice, largely due to chronic hemolysis which raises serum indirect bilirubin ... | The mechanism by which L-glutamine might cause liver injury is unknown. L-glutamine is an amino acid that is used in protein synthesis in virtually all tissues and organs. | Elucidating the cause of liver test abnormalities in patients with sickle cell disease on therapies to prevent vaso-occlusive crises is difficult, as they are susceptible to several forms of liver injury including acute viral hepatitis, hemosiderosis, gallstone disease, congestive hepatopathy and ischemic liver injury ... | L-Glutamine – Endari® | Sickle Cell Disease Agents | null |
Dapsone.nxml | Dapsone | 2017-12-05 | Dapsone is a sulfonamide related drug used for the therapy of leprosy and dermatitis herpetiformis. Dapsone has been linked with rare cases of idiosyncratic liver injury, similar to that seen with the sulfonamides. | Dapsone (dap' sone) is 4,4’ diaminodiphenylsulfone and is bacteriostatic for Mycobacterium leprae. Like other sulfonamides, dapsone is believed to act by inhibition of folate synthesis. Bacteria including M. leprae are acutely sensitive to this inhibition as folate is necessary for protein, DNA and RNA synthesis. In co... | Dapsone, like other sulfonamides, causes a characteristic idiosyncratic liver injury that 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. Eosinophilia or lymphocytosis are also common.... | The clinical pattern of injury with dapsone suggests a drug-allergy or hypersensitivity mechanism, perhaps through its metabolism to a toxic, reactive or antigenic metabolite. | Dapsone induced liver injury can result in acute liver failure, but most cases resolve rapidly with discontinuation of drug and full recovery is expected within 2 to 8 weeks. Severe cholestatic injury may be prolonged. Rechallenge should not be done, and patients should be told that they are allergic to sulfonamides (“... | Dapsone – Generic | Antiinfective Agents | null |
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