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|---|---|---|---|---|---|---|---|---|---|---|
Tamoxifen.nxml | Tamoxifen | 2020-08-20 | Tamoxifen is a nonsteroidal antiestrogen that is widely used in the treatment and prevention of breast cancer. Long term tamoxifen therapy has been associated with development of fatty liver, steatohepatitis, cirrhosis, and rare instances of clinically apparent acute liver injury. | Tamoxifen (ta mox' i fen) is referred to as a selective estrogen receptor modulator with tissue specific actions, having estrogenic agonist effects on bone, brain and liver, but antagonist activity on breast tissue. Tamoxifen may also have other, as yet undefined, anticancer effects. Adjuvant therapy with tamoxifen has... | Tamoxifen has been associated with rare instances of idiosyncratic, clinically apparent liver injury, typically arising within the first six months of treatment and having variable presentations with cholestatic, mixed or hepatocellular pattern of enzyme elevations. Immunoallergic features (fever, rash, eosinophilia) a... | The acute form of liver injury attributed to tamoxifen use is probably due to an idiosyncratic reaction to a metabolite of the medication rather than its estrogenic effects. In contrast, the induction of fatty liver and triggering of porphyria cutanea tarda are likely due to estrogenic effects on the liver in the setti... | While fatty liver arises in at least one third of women treated with tamoxifen for up to 5 years, clinically significant steatohepatitis is less common. Nevertheless, monitoring of serum aminotransferase levels during tamoxifen therapy is appropriate. In women with persistent elevations in ALT levels, the relative bene... | Tamoxifen – Generic, Nolvadex®, Tamone® | Antineoplastic Agents | null |
Bromelain.nxml | Bromelain | 2024-02-10 | Bromelain is a concentrated mixture of proteins and enzymes made from the stems and fruit of the pineapple plant (Ananas comosus) that has antiinflammatory and digestive properties, and is used topically to treat wounds and burns and orally for digestive problems and sinusitis. Bromelain is generally recognized as safe... | Bromelain is a concentrated mixture of proteolytic enzymes made from the stems and fruit of the pineapple plant (Ananas comosus) that has antiinflammatory and digestive properties, and is used topically to treat wounds and burns or orally for digestive complaints and sinusitis. Bromelain is typically concentrated, but ... | Oral bromelain has been evaluated in more than 100 clinical trials for conditions such as sinusitis, osteoarthritis, and rheumatoid arthritis, and is usually described as well tolerated and without significant side effects or adverse events. These studies have rarely reported results of liver enzyme testing, and most s... | null | null | Bromelain – Generic | Herbal and Dietary Supplements | null |
Flecainide.nxml | Flecainide | 2018-01-24 | Flecainide is an oral antiarrhythmic agent that has been in use for several decades. Long term flecainide therapy is associated with a low rate of serum enzyme elevations and is a very rare cause of clinically apparent acute liver injury. | Flecainide (fle kay' nide) is a benzamide derivative analogue of the local anesthetic procaine and has electrophysiological effects that resemble quinidine (antiarrhythmic Class IC). Flecainide appears to act by blocking open sodium channels and outward potassium channels. As a consequence, it decreases cardiac automat... | In clinical trials, flecainide was associated with a low rate of serum aminotransferase and alkaline phosphatase elevations. Despite wide scale use, flecainide has only rarely been linked to cases of clinically apparent liver injury. The typical presentation is with a cholestatic hepatitis arising within 1 to 6 weeks o... | The mechanism by which flecainide might cause liver injury is unknown. Flecainide is metabolized in the liver predominantly by CYP 2D6. In some instances, symptoms and liver test abnormalities may be due to worsening of congestive heart failure and hepatic congestion. | Liver injury due to flecainide is rare and usually mild. Cases of prolonged jaundice, but no reports of acute liver failure, chronic hepatitis or vanishing bile duct syndrome attributed to flecainide, have been published. There is little information about cross sensitivity to liver injury between flecainide and other o... | Flecainide – Generic, Tambocor® | Antiarrhythmic Agents | null |
Chenodiol.nxml | Chenodiol (Chenodeoxycholic Acid) | 2016-09-09 | Chenodeoxycholic acid (chenodiol) is a primary bile acid, synthesized in the liver and present in high concentrations in bile that is used therapeutically to dissolve cholesterol gallstones. Chronic therapy is associated with transient elevations in serum aminotransferase levels in up to 30% of patients, but chenodiol ... | Chenodeoxycholic acid or chenodiol (kee" noe dye' ol) is a naturally occurring bile acid that is used therapeutically to dissolve cholesterol gallstone in patients with a functioning gall bladder who have contraindications to cholecystectomy or refuse surgery. Chenodiol is the major bile acid synthesized by the liver a... | In multiple clinical trials of chenodiol therapy for dissolution of gallstones, serum aminotransferase elevations occurred in up to 30% of patients. The elevations generally arose within 2 months of starting therapy and were typically mild, transient and not accompanied by symptoms or jaundice. Liver biopsies done duri... | null | Patients on chenodiol should be monitored with liver tests, including serum bilirubin, ALT, AST and alkaline phosphatase at periodic intervals. Chenodiol should be discontinued for persistent increases in liver test abnormalities, ALT elevations above 8 times the upper limit of normal, elevations of bilirubin more than... | Chenodiol – Generic, Chenodal® | Gastrointestinal Agents | [
{
"cas_registry_number": "474-25-9",
"molecular_formula": "C24-H40-O4",
"name": "Chenodiol"
},
{
"cas_registry_number": "81-25-4",
"molecular_formula": "C24-H40-O5",
"name": "Cholic Acid"
}
] |
Vosoritide.nxml | Vosoritide | 2025-01-31 | Vosoritide is a modified recombinant C type natriuretic peptide analog which is used to promote linear growth in children and adolescents with achondroplasia who still have open epiphyses. Vosoritide is given in daily subcutaneous injections and its use has not been associated with elevations in serum aminotransferase ... | Vosoritide (voe’ soe re’ i tide) is a modified, recombinant 39 amino acid analogue of human C type natriuretic peptide which is used to increase linear growth in children and adolescents with achondroplasia. Achondroplasia is a rare (1:25,000 live births) autosomal dominant genetic disease marked by impaired conversion... | In the registration studies submitted in support of approval of vosoritide, “overall, there were no clinically meaningful changes in any laboratory parameter in the clinical program.” Serum ALT levels rose to above the upper limit of normal (ULN) in 22% of vosoritide treated participants vs 18% of controls, but there w... | The mechanism by which vosoritide might cause liver injury is unknown. It is a polypeptide and is metabolized to individual amino acids intracellularly in many tissues. Vosoritide is not metabolized by the cytochrome P450 system and has not been associated with drug-drug interactions. | Vosoritide has not been implicated in marked serum aminotransferase elevations or instances of acute liver injury. While minor elevations in serum enzymes may occur during therapy, these are generally transient, asymptomatic, and most likely unrelated to treatment.\n\nDrug Class: Genetic Disorder Agents | Vosoritide – Voxzogo® | Genetic Disorder Agents | null |
Disulfiram.nxml | Disulfiram | 2021-09-07 | Disulfiram is an alcohol deterrent used as an adjunct to treatment of chronic alcoholism, based upon its ability to cause an aversive reaction when taken with alcohol. Disulfiram has been associated with a low rate of with serum aminotransferase elevations during chronic therapy and has been linked to clinically appare... | Disulfiram (dye sul' fi ram) is tetraethylthiuram disulfide and is a potent inhibitor of aldehyde dehydrogenase activity, which interferes with the oxidative metabolism of alcohol resulting in accumulation of acetaldehyde. The elevations in serum acetaldehyde levels cause the aversive symptoms of disulfiram which inclu... | Chronic therapy with disulfiram is associated with mild serum aminotransferase elevations in up to 25% of patients, but elevations above 3 times the upper limit of normal (ULN) occur in 4% of patients or less. Importantly, disulfiram is a well established cause of clinically apparent liver injury, which can be severe a... | The mechanism of disulfiram hepatotoxicity is probably idiosyncratic hypersensitivity as suggested by the frequency of immunoallergic features (rash, fever, eosinophilia), the frequency of eosinophilic infiltrates seen on liver biopsy, and the prompt recurrence of enzyme elevation after rechallenge. Disulfiram is metab... | The severity of liver injury associated with disulfiram can range from asymptomatic elevations in serum aminotransferase levels, to symptomatic liver injury with jaundice, to acute liver failure and death. Disulfiram hepatotoxicity with jaundice is associated with high mortality and appearance of symptoms or signs of l... | Disulfiram – Generic, Antabuse® | Substance Abuse Treatment Agents | null |
Phenotypes_intro.nxml | Phenotypes Of Drug Induced Liver Injury | 2019-05-04 | null | null | null | null | null | null | null | null |
Evinacumab.nxml | Evinacumab | 2021-07-08 | Evinacumab is a human monoclonal antibody to angiopoietin-like protein 3 which is approved for use in patients with homozygous familial hypercholesterolemia. Evinacumab is given intravenously every 4 weeks and is generally well tolerated, and has not been associated with serum aminotransferase elevations during therapy... | Evinacumab (e” vin ak’ ue mab) is a human monoclonal IgG4 antibody directed against angiopoietin-like protein 3 (ANGPTL3) which is a protein expressed largely in the liver that inhibits lipoprotein lipase and endothelial lipase activity, two endogenous lipases which break down lipids in serum. Inhibition of ANGPTL3 by ... | In preregistration randomized controlled studies, mild serum aminotransferase elevations arose a small percentage of treated patients but were generally asymptomatic and transient and did not require discontinuation or modification of dose. In addition, there were no reported instances clinically apparent liver injury ... | Possible mechanisms of liver injury due to evinacumab are not apparent. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids.\n\nDrug Class: Monoclonal Antibodies, Antilipemic Agents | null | Evinacumab – Evkeeza® | Antilipemic Agents | null |
AmprenavirFosampren.nxml | Fosamprenavir | 2017-09-01 | Amprenavir is an antiretroviral protease inhibitor used in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Fosamprenavir is a prodrug of amprenavir that has better oral bioavailability and that has largely replaced amprenavir in clinical use.... | Amprenavir (am pren' a vir) is sulfonamide nonpeptide HIV protease inhibitor that acts by binding to the catalytic site of the viral protease, thereby preventing the cleavage of HIV polyprotein precursors into mature, functional proteins that are necessary for viral replication. Fosamprenavir (fos" am pren' a vir) is a... | Some degree of serum aminotransferase elevations occur in a high proportion of patients taking amprenavir or fosamprenavir containing antiretroviral regimens. In large, multicenter trials of fosamprenavir based antiretroviral therapy, moderate-to-severe elevations in serum aminotransferase levels (>5 times the upper li... | The cause of the clinical hepatotoxicity from amprenavir or fosamprenavir is not well understood. Amprenavir is extensively metabolized by the liver, largely by the cytochrome P450 system (CYP 3A4), and toxic or immunogenic intermediates may be the cause of some liver injury. Clinically apparent cases of liver injury h... | null | Amprenavir – Agenerase® | Antiviral Agents | [
{
"cas_registry_number": "161814-49-9",
"molecular_formula": "C25-H35-N3-O6-S",
"name": "Amprenavir"
},
{
"cas_registry_number": "226700-79-4",
"molecular_formula": "C25-H36-N3-O9-P-S",
"name": "Fosamprenavir"
}
] |
GemtuzumabOzogamicin.nxml | Gemtuzumab Ozogamicin | 2023-11-30 | Gemtuzumab ozogamicin is a humanized monoclonal antibody conjugate that is used in the therapy of acute myelogenous leukemia. Gemtuzumab ozogamicin has been linked to transient serum enzyme elevations during therapy and not uncommon instances of acute sinusoidal obstruction syndrome, which can be severe and even fatal. | null | null | null | null | Gemtuzumab Ozogamicin – Mylotarg® | Antineoplastic Agents | null |
Doxazosin.nxml | Doxazosin | 2018-01-08 | Doxazosin is a nonselective alpha-1 adrenergic antagonist (alpha-blocker) used in the therapy of hypertension and benign prostatic hypertrophy. Doxazosin is associated with a low rate of transient serum aminotransferase elevations, but has not been linked to instances of clinically apparent acute liver injury. | Doxazosin (dox ay' zoe sin) was the third alpha-1 adrenergic antagonist to be approved for use in the United States and is still widely used for therapy of hypertension and benign prostatic hypertrophy. Doxazosin inhibits alpha-adrenergic receptors present on smooth muscle in arterioles (so-called alpha-1b adrenergic r... | Doxazosin has been associated with a low rate of serum aminotransferase elevations that in controlled trials was no higher than with placebo therapy. These elevations were transient and did not require dose modification. No instances of clinically apparent acute liver injury due to doxazosin have been published in the ... | The cause of the minor serum aminotransferase elevations associated with doxazosin is not known. Doxazosin is extensively metabolized by the liver and generation of a mildly toxic intermediate is a possible explanation.\n\nReferences on the safety and potential hepatotoxicity of doxazosin and other alpha-blockers are g... | null | Doxazosin – Generic, Cardura® | Antihypertensive Agents | null |
Carmustine.nxml | Carmustine | 2017-01-17 | Carmustine (BCNU) is a parenterally administered alkylating agent used alone and in combination with other antineoplastic agents in the treatment of several forms of cancer including leukemias, lymphomas, and breast, testicular, ovarian, gastric and pancreatic cancer. Carmustine therapy is associated with minor transie... | Carmustine (kar mus' teen), which is also known as BCNU, is a nitrosourea that acts as an alkylating agent and is used in the therapy of several forms of leukemia, lymphoma and solid organ cancer. Like cyclophosphamide, carmustine requires activation in the liver to form its active intermediates which act by modifying ... | Mild and transient elevations in serum aminotransferase levels are found in up to 25% of patients treated with carmustine. Because carmustine is typically given in combination with other agents, its role in causing these serum enzyme elevations is not always clear. The abnormalities are generally transient, do not caus... | Most instances of hepatotoxicity from carmustine appear dose related and probably due to direct cytotoxicity. The sinusoidal obstruction syndrome induced by alkylating agents is probably related to their toxic effect on sinusoidal cells in the liver, causing their necrosis and release into the sinusoids, with subsequen... | The severity of liver injury from carmustine ranges from mild elevations in liver enzymes, to a self limited cholestatic hepatitis to massive, fatal hepatic necrosis due to sinusoidal obstruction syndrome. There is currently no specific therapy for veno-occlusive disease other than supportive management and avoidance o... | Carmustine – BiCNU, Gliadel® | Antineoplastic Agents, Alkylating Agents | null |
Bisphosphonates.nxml | Bisphosphonates | 2018-06-14 | The bisphosphonates are pyrophosphate analogues that become incorporated into bone matrix and suppress osteoclastic activity, thereby reducing bone turnover and increasing bone mass, which makes them valuable agents for the prevention and therapy of osteoporosis. Therapy with the bisphosphonates has been associated wit... | Bisphosphonates are pyrophosphate analogues that have two phosphonate groups attached to a central carbon atom that replaces the oxygen present in pyrophosphate. The bisphosphonates bind calcium and are rapidly taken up in bone matrix where they suppress osteoclastic activity and change the balance between bone resorpt... | In most large prospective trials, the bisphosphonates were associated with only rare and isolated instances of serum enzyme elevations and no cases of clinically apparent liver injury. Since their general availability and wide scale use, however, there have been occasional publications reporting clinically apparent acu... | The bisphosphonates are taken up by bone matrix and rapidly cleared from the serum by renal excretion. Hepatic metabolism is minimal, and thus it is somewhat surprising that they can be associated with hepatic injury. The mechanism of injury is likely to be metabolic idiosyncrasy as immunoallergic features are not typi... | The clinically apparent acute liver injury attributed to bisphosphonates has been mild-to-moderate in severity without published instances of acute liver failure or chronic liver disease. The possibility of cross reactivity of the hepatic injury among the various bisphosphonates has not been studied, nor is there publi... | Alendronate – Generic, Fosamax® | Osteoporosis Agents | [
{
"cas_registry_number": "121268-17-5",
"molecular_formula": "C4-H13-N-O7-P2.3H2-O.Na",
"name": "Alendronate"
},
{
"cas_registry_number": "2809-21-4",
"molecular_formula": "C2-H8-O7-P2",
"name": "Etidronate"
},
{
"cas_registry_number": "114084-78-5",
"molecular_formula": "C9-... |
Fosfomycin.nxml | Fosfomycin | 2018-02-06 | Fosfomycin is an orally available, broad spectrum antibiotic used largely for treatment of uncomplicated urinary tract infections. Fosfomycin is associated with a low rate of transient serum enzyme during therapy and with rare cases of clinically apparent acute liver injury with jaundice. | Fosfomycin (fos' foe mye. sin) is an oral, broad spectrum bactericidal antibiotic that is typically used as a single, large oral dose to treat acute cystitis. Fosfomycin (also known as phosphomycin) is a natural product of Streptomyces fradiae that acts by inactivation of a bacterial enzyme necessary for cell wall synt... | Serum aminotransferase elevations occur in a small proportion of patients after a single oral dose of fosfomycin (1-2%), but at rates similar to those with comparator antibiotics. Nevertheless, serum enzyme elevations are mentioned as potential adverse events in the product label for fosfomycin. In addition, a small nu... | The cause of the liver injury due to fosfomycin is unknown, but is likely to be immunologically mediated. Fosfomycin has minimal hepatic metabolism (mostly glucuronidation), and drug-drug interactions with it are not expected. | The severity of the liver injury linked to fosfomycin has ranged from transient, asymptomatic serum enzyme elevations to clinically apparent hepatitis. Severe but not fatal instances of acute hepatitis have been reported. In one publication, reexposure to fosfomycin after clinically apparent liver injury led to a rapid... | Fosfomycin – Monurol® | Antiinfective Agents | null |
ColonyStimulatingFac.nxml | Colony Stimulating Factors | 2017-10-30 | Granulocyte colony stimulating factor (G-CSF) and granulocyte-macrophage colony stimulating factor (GM-CSF) are glycosylated polypeptides that induce an increase in the proliferation and maturation of white blood cells including neutrophils and monocytes-macrophages. Recombinant forms of these colony stimulating factor... | Filgrastim (fil gra' stim) is a recombinant, non-glycosylated form of the 175 amino acid protein, granulocyte colony stimulating factor (G-CSF) that induces the proliferation and maturation of neutrophils. G-CSF is normally produced by multiple cell types including monocytes, fibroblasts, macrophages and stromal cells.... | Filgrastim and sargramostim have not been linked to instances of significant serum enzyme elevations during therapy and have not been implicated in cases of clinically apparent liver injury. In multiple large prelicensure studies, acute liver injury was not mentioned as an adverse event and serum aminotransferase eleva... | The mechanism by which the colony stimulating factors might cause liver injury is not known. Both filgrastim and sargramostim are polypeptides and are usually metabolized by the cells on which they act. | null | Filgrastim – Neupogen® | Hematologic Growth Factors | [
{
"cas_registry_number": "121181-53-1",
"molecular_formula": "Protein",
"name": "Filgrastim"
},
{
"cas_registry_number": "208265-92-3",
"molecular_formula": "Protein",
"name": "Pegfilgrastim"
},
{
"cas_registry_number": "123774-72-1",
"molecular_formula": "Protein",
"name... |
Avelumab.nxml | Avelumab | 2022-06-23 | Avelumab is a human monoclonal antibody to programmed cell death ligand 1 (PD-L1), which acts as a checkpoint inhibitor and is used in the immunotherapy of several forms of advanced or metastatic cancer. Avelumab therapy has major side effects and particularly immune related conditions, including acute hepatocellular a... | Avelumab (av el' ue mab) is a human recombinant monoclonal IgG1 antibody to the programmed cell death ligand-1 (PD-L1), which has distinctive immunomodulatory activity and is used as a checkpoint inhibitor in cancer immunotherapy. The programmed cell death receptor 1 (PD-1) is an important checkpoint molecule that is e... | Mild-to-moderate serum aminotransferase elevations are not uncommon during avelumab therapy, but are usually self-limited and resolve even with continuing cyclic therapy. These rates of serum enzyme elevations are similar to those with other forms of chemotherapy for advanced malignancies. Serum ALT elevations above 5 ... | The liver injury due to avelumab is likely immunologically mediated and is usually at least partially responsive to corticosteroid or immunosuppressive therapy. Liver biopsies in cases of hepatocellular injury and bile duct epithelial cell biopsies in cholangiopathic injury demonstrate necrosis and inflammatory cell in... | Guidelines for management of patients receiving avelumab recommend monitoring of liver tests and interrupting therapy for patients who develop serum aminotransferase elevations above 3 times the ULN and discontinuing treatment for values above 8 times the ULN in patients without preexisting abnormalities or tumor invol... | Avelumab – Bavencio® | Antineoplastic Agents | null |
Baloxavir.nxml | Baloxavir | 2020-06-22 | Baloxavir is an inhibitor of the influenza cap-dependent endonuclease enzyme and is used as therapy of influenza A and B. Baloxavir is given as a single, one-time dose and has not been associated with serum enzyme elevations or with clinically apparent liver injury. | Baloxavir (ba lox' a vir) marboxil (mar box' il) is an oral, influenza cap-dependent endonuclease inhibitor that blocks the initiation of mRNA synthesis in influenza viruses, which results in a decrease in influenza virus particle production. Baloxavir is active against both influenza A and B viruses but has no activit... | In clinical trials, there was little evidence that baloxavir caused liver injury, either in the form of serum enzyme elevations or clinically apparent liver disease. A proportion of patients with acute influenza A may have minor serum enzyme elevations during the acute illness, but these are independent of therapy and ... | How baloxavir might cause liver injury is not known. Baloxavir marboxil is a prodrug that is converted to the active agent baloxavir in the intestines. Baloxavir is metabolized by the liver by UGT1A3 with a minor contribution of CYP 3A4 but demonstrates no significant drug-drug interactions. Baloxavir is administered a... | null | Baloxavir – Xofluza® | Antiviral Agents | null |
Phenotypes_ahn.nxml | Acute Hepatic Necrosis | 2019-05-04 | null | null | null | null | null | null | null | null |
DimethylFumarate.nxml | Dimethyl Fumarate | 2022-09-07 | Dimethyl fumarate, monomethyl fumarate and diroximel fumarate are antiinflammatory and immunomodulatory agents that are used to treat relapsing multiple sclerosis and have similar beneficial as well as adverse effects. Dimethyl fumarate is associated with low rates of transient serum enzyme elevations during treatment,... | Dimethyl fumarate (dye meth' il fue' ma rate) is a methylated, unsaturated dicarboxylic acid which has distinctive antiinflammatory and immunomodulatory activities, both in vitro and in vivo. Its mechanism of action is believed to be via activation of the nuclear factor E2-related factor (NrF2) pathway, which is import... | In large randomized controlled trials of dimethyl fumarate in patients with psoriasis and multiple sclerosis, serum ALT elevations were frequent, occurring in up to 25% of patients. The elevations, however, were generally mild-to-moderate and resolved rapidly even without dose modification. Elevations above 3 times ULN... | The mechanism by which dimethyl fumarate causes liver injury is not known but is likely to be idiosyncratic. It is extensively metabolized by serum and tissue esterases to monomethyl fumarate, which is further metabolized in the liver to fumarate which enters the tricarboxylic acid (TCA) cycle. Dimethyl fumarate metabo... | While chronic therapy with dimethyl fumarate can be associated with mild-to-moderate serum aminotransferase elevations, it has been linked only rarely to cases of clinically apparent liver injury. There is reason to suspect that there is cross sensitivity of the hepatic injury from dimethyl fumarate and either diroxime... | Dimethyl Fumarate – Generic, Tecfidera® | Multiple Sclerosis Agents | null |
Prucalopride.nxml | Prucalopride | 2019-04-25 | Prucalopride is a serotonin type 4 (5-HT4) receptor agonist that has potent prokinetic activity and is used as therapy for chronic idiopathic constipation. Prucalopride has been associated with a minimal rate of transient serum enzyme elevations during therapy and has not been implicated in cases of clinically apparent... | Prucalopride (proo kal' oh pride) is a highly selective serotonin type 4 (5-HT4) receptor agonist that increases the release of serotonin by the specialized enterochromaffin cells in the mucosa of the gut and stimulates intestinal peristalsis and tone. Serotonin (5-HT) is released in response to chemical and mechanical... | Prucalopride therapy was associated with a low rate of serum enzyme elevations during therapy (<1%) that was not different from that of placebo recipients. The elevations noted were mild and transient and did not required dose adjustment. In the many large clinical trials of prucalopride therapy in patients with chroni... | The mechanism by which prucalopride might cause liver injury is unknown. It is used in low total doses which may explain its relative lack of hepatotoxicity. Prucalopride is metabolized in the liver, largely via CYP 3A4 and is a substrate for P-glycoprotein. Prucalopride is susceptible to drug-drug interactions with ag... | null | Prucalopride – Motegrity® | Gastrointestinal Agents | null |
Halothane.nxml | Halothane | 2018-01-01 | Halothane is a potent volatile halogenated anesthetic gas that has been linked to many cases of idiosyncratic acute liver injury that are frequently severe. The potential of halothane to cause hepatotoxicity and the greater safety of newer anesthetics has led to a decrease in its use, currently limited to special situa... | Halothane (hal' oh thane) is a volatile anesthetic that was used widely in major surgery between its introduction in 1956 and falling out of favor in the mid 1990s. It is nonflammable, potent and well tolerated. Halothane is administered to produce end tidal concentrations of 0.7% to 1%. It has a somewhat slow onset of... | Prospective, serial blood testing often demonstrates minor transient elevations in serum aminotransferase levels in the 1 to 2 weeks after major surgery and anesthesia with halothane and other halogenated anesthetics. Appearance of ALT levels above 10 times the upper limit of normal, however, is uncommon and points to ... | The mechanism of halothane hepatotoxicity is suspected to be immunoallergic, caused by creation of reactive intermediates of the anesthetic. Approximately 60% to 80% of halothane is eliminated unchanged by the lungs, but a proportion is biotransformed by hepatic microsomal enzyme CYP 2E1 to a trifluoroacetic acid which... | Severity ranges from mild and transient aminotransferase elevations without symptoms or other evidence of liver injury, to a self limited symptomatic acute hepatitis-like reaction, to a severe, acute hepatic failure. The severity and prognosis may relate in part of patient age, being more severe in the elderly and both... | Halothane – Generic, Fluothane® | Anesthetics, Halogenated | null |
Lurasidone.nxml | Lurasidone | 2023-06-10 | Lurasidone is a second generation (atypical) antipsychotic agent that is used in the treatment of schizophrenia and bipolar depression. Lurasidone is associated with a low rate of serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury. | Lurasidone (loo ras' i done) is a second generation antipsychotic agent which appears to act as a dopamine type 2 (D2) and serotonin (5-HT)-2A receptor antagonist in a manner similar to risperidone. Several randomized controlled trials have shown that lurasidone improves symptoms of schizophrenia and it was approved fo... | Liver test abnormalities occur in 1% to 3% of patients on long term therapy with lurasidone, but similar rates have been reported with placebo therapy and with comparator agents. The ALT elevations are usually mild, transient and often resolve even without dose modification or drug discontinuation. There have been no p... | The mechanism by which lurasidone might cause serum ALT elevations or liver injury is not known. Lurasidone is extensively metabolized by the cytochrome P450 system (CYP 3A4) to its active metabolite and is susceptible to drug-drug interactions with agents that inhibit or induce CYP 3A4. | The serum aminotransferase elevations that occur on lurasidone therapy are usually self-limited and often do not require dose modification or discontinuation. No instances of acute liver failure, chronic hepatitis or vanishing bile duct syndrome have been attributed to lurasidone. Cross sensitivity to liver related or ... | Lurasidone – Generic, Latuda® | Antipsychotic Agents | [
{
"cas_registry_number": "367514-87-2",
"molecular_formula": "C28-H36-N4-O2-S",
"name": "Lurasidone"
},
{
"cas_registry_number": "106266-06-2",
"molecular_formula": "C23-H27-F-N4-O2",
"name": "Risperidone"
}
] |
Thalidomide.nxml | Thalidomide | 2022-08-30 | Thalidomide and its analogues lenalidomide and pomalidomide are immunomodulatory and antineoplastic agents that are used in the therapy of multiple myeloma. These three agents are associated with a low rate of serum aminotransferase elevations during therapy and have been implicated in causing rare instances of clinica... | Thalidomide (tha lid' oh mide) is a glutamic acid derivative that was introduced in Europe as a sedative in the late 1950s and subsequently withdrawn in 1961 when it was shown to be teratogenic, causing severe infant limb defects (phocomelia) when given to pregnant women. Several decades later, thalidomide was found to... | Serum enzyme elevations occur in 8% to 15% of patients taking thalidomide and are more frequent with higher doses. The enzyme abnormalities are usually mild and self-limited, and only rarely require drug discontinuation. In addition, both thalidomide and its derivatives, lenalidomide and pomalidomide, have been implica... | The mechanism of thalidomide hepatotoxicity is not clear, but it may be related to its activity in reducing TNF-α production, a potent inflammatory cytokine that activates T cells and promotes inflammation, but is also necessary for normal liver regeneration. Several of the reported cases of hepatotoxicity have occurre... | The severity of thalidomide induced liver injury ranges from transient, asymptomatic elevations in serum enzymes to acute liver injury with jaundice to severe acute liver failure and death. The liver injury usually starts to resolve within a week of stopping the medication, but prolonged jaundice with bile duct injury ... | Thalidomide – Thalidomid® | Antineoplastic Agents | [
{
"cas_registry_number": "50-35-1",
"molecular_formula": "C13-H10-N2-O4",
"name": "Thalidomide"
},
{
"cas_registry_number": "191732-72-6",
"molecular_formula": "C13-H13-N3-O3",
"name": "Lenalidomide"
},
{
"cas_registry_number": "19171-19-8",
"molecular_formula": "C13-H11-N3-O... |
XanthineDerivatives.nxml | Xanthine Derivatives | 2020-07-18 | null | null | null | null | null | null | null | null |
Etanercept.nxml | Etanercept | 2017-02-10 | Etanercept is an antagonist of tumor necrosis factor alpha (TNFα) which has potent antiinflammatory activity and is used widely in severe forms of rheumatoid arthritis and psoriasis. Etanercept has been linked to rare instances of acute, clinically apparent liver injury. | Etanercept (ee tan' er sept) is a soluble form of the human TNFα receptor which is fused wih the Fc portion of immunoglobulin G. This recombinant fusion protein binds serum TNFα, leading to inhibition of pathways of inflammation and pain mediated by this potent, pro-inflammatory cytokine. Etanercept was approved for us... | Etanercept has been associated with low rates of serum ALT elevations during therapy that are generally asymptomatic, transient, and do not require dose modifications. There have been isolated reports of clinically apparent liver injury during etanercept therapy, but the frequency has been far less than with infliximab... | The liver injury caused by etanercept is likely due to induction of autoimmunity. While a high proportion of patients develop autoantibodies either de novo or in rising titer, only rarely do persons develop clinically apparent autoimmune conditions, such as lupus-like syndrome or autoimmune hepatitis. | The hepatotoxicity of etanercept has largely been mild and self-limiting, although sometimes requiring corticosteroid therapy. No instances of chronic hepatitis or vanishing bile duct syndrome have been reported. Patients who are to start etanercept therapy should be screened for evidence of hepatitis B, and those with... | Etanercept – Enbrel® | Antirheumatic Agents; Dermatologic Agents | null |
Pregabalin.nxml | Pregabalin | 2020-07-30 | Pregabalin is an inhibitor of neuronal activity used for therapy of painful neuropathy and as an anticonvulsant. Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare. | Pregabalin (pre gab' a lin) is a structural analogue of gamma-aminobutyric acid (GABA) but is novel in its activity, having no effects on GABA-A or GABA-B receptors. Instead, the neuronal activity of pregabalin appears to be mediated by its binding to the alpha-2-delta subunit of the presynaptic voltage-gated calcium c... | Limited data is available on the hepatotoxicity of pregabalin. In prelicensure clinical trials in diabetic neuropathy and epilepsy, therapy with pregabalin was not associated with an increased frequency of serum aminotransferase elevations or liver toxicity. Since its approval and more wide scale use, however, pregabal... | The low rate of significant hepatotoxicity from pregabalin may be due to its minimal hepatic metabolism and rapid urinary excretion. The injury is clearly idiosyncratic and either immunologic or metabolic causes are possible. | The case reports of hepatic injury due to pregabalin were followed by complete recovery without evidence of residual or chronic injury. There is no information about cross reactivity with other compounds having similar structure (gabapentin).\n\nDrug Class: Anticonvulsants | Pregabalin – Generic, Lyrica® | Anticonvulsants | null |
Erdafitinib.nxml | Erdafitinib | 2022-12-01 | Erdafitinib is an oral small molecule inhibitor of fibroblast growth factor (FGF) receptors 1 to 4 that is used in the therapy of locally advanced, unresectable or metastatic urothelial carcinoma. Erdafitinib has been associated with a high rate of serum enzyme elevations during therapy, but has not been linked to case... | Erdafitinib (er” da fi’ ti nib) is an orally available, small molecule inhibitor of fibroblast growth factor (FGF) receptors 1-4 which is used to treat advanced, unresectable or metastatic urothelial carcinoma. Fibroblast growth factors include 22 related ligands that act on cells via more than 20 different FGF recepto... | In the prelicensure clinical trials of erdafitinib in patients with urothelial carcinoma, liver test abnormalities were frequent although usually mild. Some degree of ALT elevation arose in up to 41% of erdafitinib treated patients, but were above 5 times the upper limit of normal in only 1% to 2%. In these trials that... | The cause of liver injury from erdafitinib is unknown, but a pattern of abnormalities suggests some degree of low level, direct hepatotoxicity. Some of the adverse effects of erdafitinib are due to its effects on FGF signaling (hyperphosphatemia) and others may be due to off-target effects on other kinases. Erdafitinib... | Erdafitinib is associated with a moderate rate of serum aminotransferase elevations that are generally transient and not associated with symptoms or jaundice. While regular monitoring of liver tests is not specifically recommended during erdafitinib therapy, elevations if confirmed should lead to more careful follow up... | Erdafitinib – Balversa® | Antineoplastic Agents | null |
Lomustine.nxml | Lomustine | 2019-06-03 | Lomustine is an orally administered alkylating agent used alone and in combination with other antineoplastic agents in the treatment of several malignancies including Hodgkin disease, lymphoma, and brain cancer. Lomustine therapy is associated with minor transient serum enzyme elevations and has been linked to rare cas... | Lomustine (loe mus' teen: also known as CCNU) is a nitrosourea similar to carmustine (BCNU), which acts as an alkylating agent and is used in the therapy of several forms of lymphoma and solid organ cancer. Like cyclophosphamide, lomustine requires activation in the liver to form its active intermediaries which act by ... | Mild and transient elevations in serum aminotransferase or alkaline phosphatase levels are found in a high proportion of patients treated antineoplastic regimens that include lomustine. The abnormalities are generally transient, do not cause symptoms and do not require dose modification. Clinically apparent liver injur... | The cause of idiosyncratic hepatotoxicity from lomustine is not known. Lomustine is extensively metabolized by hepatic cytochrome P450 system. | The severity of liver injury ranges from mild elevations in liver enzymes to mild and self limited cholestatic liver injury. It is not known whether patients with acute liver injury due to lomustine have cross sensitivity to hepatic injury with other alkylating agents.\n\nDrug Class: Antineoplastic Agents, Alkylating A... | Lomustine – CeeNU® | Antineoplastic Agents, Alkylating Agents | null |
Tucatinib.nxml | Tucatinib | 2023-09-08 | Tucatinib is tyrosine kinase inhibitor that targets the human epidermal growth factor receptor 2 (HER2) and is used in combination with other antineoplastic agents in the treatment of refractory, advanced or metastatic HER2 positive breast and colorectal cancer. Serum aminotransferase elevations are common during thera... | Tucatinib (too ka’ ti nib) is an orally available small molecule inhibitor of the human epidermal growth factor receptor 2 (HER2), a tyrosine kinase that is overexpressed in some cancers and leads to excessive cell growth and proliferation. HER2 is an oncogenic driver found overexpressed in 15% to 20% of cases of breas... | In the prelicensure clinical trials of tucatinib in combination with trastuzumab and capecitabine in patients with metastatic and unresectable HER2 positive breast cancer, liver test abnormalities were frequent although usually self-limited and mild. Some degree of ALT elevations arose in 46% of those receiving tucatin... | The cause of serum aminotransferase elevations from tucatinib is unknown, but the pattern of abnormalities suggests direct liver injury. Tucatinib is metabolized in the liver via the cytochrome P450 system, largely CYP 2C8 and 3A4, and is susceptible to drug-drug interactions with agents that inhibit or induce these CY... | The product label for tucatinib recommends monitoring for routine liver tests before and every 3 weeks during treatment. Serum aminotransferase elevations above 5 times ULN or bilirubin above 3 times ULN should lead to dose reduction or temporary cessation of tucatinib therapy and careful monitoring. If serum aminotran... | Tucatinib – Tukysa® | Antineoplastic Agents | null |
EmergencyContracepti.nxml | Emergency Contraceptive Agents | 2020-06-02 | Levonorgestrel is a synthetic progesterone that is used for emergency contraception. Levonorgestrel is also used alone and in combination with estrogens in conventional oral contraceptives. Use of levonorgestrel for emergency contraception has not been associated with serum enzyme elevations or clinically apparent live... | Levonorgestrel (lee" voe nor jes' trel) is a synthetic progesterone that is used as a single or as two oral doses within 2 days of unprotected intercourse or contraceptive failure as a means of emergency contraception. Levonorgestrel acts as an agonist of the progesterone receptor and is believed to act by preventing o... | In large prospective trials of levonorgestrel as emergency contraception that included laboratory testing, mean serum ALT and AST levels remained unchanged and only rare, minor elevations of serum enzymes occurred that were invariably transient, not accompanied by jaundice or symptoms and not considered related to the ... | The mechanism by which levonorgestrel used for emergency contraception might cause liver injury is uncertain. It is typically given in one or two low doses, the total amount being only 1.5 mg. Levonorgestrel is metabolized in the liver predominantly via CYP 3A4 and is susceptible to drug-drug interactions with potent i... | null | Levonorgestrel – Generic, Plan B® | Emergency Contraceptive Agents | [
{
"cas_registry_number": "797-63-7",
"molecular_formula": "C21-H28-O2",
"name": "Levonorgestrel"
},
{
"cas_registry_number": "159811-51-5",
"molecular_formula": "C28-H35-N-O3",
"name": "Ulipristal"
},
{
"cas_registry_number": "57-83-0",
"molecular_formula": "C21-H30-O2",
... |
Cetuximab.nxml | Cetuximab | 2017-10-03 | Cetuximab is a chimeric mouse-human monoclonal antibody to the human epidermal growth factor (EGF) receptor which is used in the treatment of metastatic colon and head and neck cancers. Cetuximab has been linked to mild and transient serum enzyme elevations during therapy, but has not been implicated in cases of clinic... | Cetuximab (se tux’ i mab) is a chimeric mouse-human monoclonal IgG1 kappa antibody to the human epidermal growth factor (EGF) receptor which is present on many normal cell types and is overexpressed in several forms of cancer. Cetuximab has been shown to prolong survival in patients with EGF receptor expressing and wil... | Publications on the large scale trials of cetuximab, rates of ALT elevations and clinically apparent liver injury were usually not mentioned. In a study of squamous cell carcinoma of the head and neck, some degree of ALT elevation was reported in 45% of persons receiving cetuximab and radiation therapy versus 22% of th... | The cause of the serum enzyme elevations during cetuximab therapy is not known. However, the human EGF receptor is present on many cells and some of the adverse events, including mild liver injury, may be due to a direct effect of the monoclonal antibody on cells that express EGF receptors. | The serum aminotransferase elevations that occur on cetuximab therapy are generally transient, mild and asymptomatic and do not require dose modification or delay in therapy. Elevations above 5 times the upper limit of normal should lead to more careful monitoring and discontinuation or delay in therapy until levels re... | Cetuximab – Erbitux® | Antineoplastic Agents | null |
Tolterodine.nxml | Tolterodine | 2023-07-12 | Tolterodine is an anticholinergic agent used to treat urinary incontinence and overactive bladder syndrome. Tolterodine therapy has not been associated liver enzyme elevations while only a single case report has been published of clinical apparent acute liver injury attributed to its use. | Tolterodine (tol ter' oh deen) is a synthetic anticholinergic and antispasmotic agent that inhibits muscarinic actions of acetylcholine on autonomic nerve endings, decreasing secretions and inhibiting gastrointestinal and bladder motility. Tolterodine increases bladder capacity and decreases bladder contractions and th... | In multiple randomized controlled trials of tolterodine in patients with overactive bladder syndrome, serum aminotransferase and alkaline phosphatase elevations were not common, arising in less than 1% of treated subjects and in a similar proportion of placebo recipients. In these clinical trials there were no reports ... | The mechanism by which tolterodine might cause liver injury unknown. It is metabolized in the liver by microsomal P450 enzymes, predominantly CYP 3A4 and 2D6. Despite this, drug-drug interactions are uncommon. A major reason for its safety may relate to the low daily dose.\n\nDrug Class: Anticholinergic Agents | null | Tolterodine – Generic, Detrol® | Anticholinergic Agents | null |
Romosozumab.nxml | Romosozumab | 2021-06-07 | Romosozumab is a humanized monoclonal antibody to sclerostin which is used to treat osteoporosis. Romosozumab is generally well tolerated and has not been associated with serum aminotransferase elevations during therapy or with instances of clinically apparent liver injury. | Romosozumab (roe’ moe soz’ ue mab) is a humanized monoclonal IgG2 antibody directed against sclerostin, an osteocyte-derived glycoprotein that inhibits bone formation via interruption of Wnt/beta-catenin signaling which results in an inhibition of osteoblast activity. Romosozumab is used to treat osteoporosis and is on... | Mild-to-moderate serum aminotransferase elevations arise a small percentage of treated patients, but are generally asymptomatic and transient and rarely necessitate discontinuation of romosozumab injections. In registration trials of romosozumab there were no instances clinically apparent liver injury or severe hepatic... | The possible mechanisms of liver injury due to romosozumab are unclear. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids.\n\nDrug Class: Monoclonal Antibodies, Osteoporosis Agents | null | Romosozumab – Evenity® | Osteoporosis Agents | null |
Pexidartinib.nxml | Pexidartinib | 2019-10-10 | Pexidartinib is an orally available small molecule multi-kinase inhibitor that is used as an antineoplastic agent in the treatment of tenosynovial giant cell tumors. Pexidartinib is associated with a high rates of serum aminotransferase and alkaline phosphatase elevations during therapy and has been implicated in sever... | Pexidartinib (pex” i dar’ ti nib) is a potent small molecule inhibitor of several kinase receptors, including colony stimulating factor 1 (CSF1) receptor, FMS-like tyrosine kinase 3 receptor (FLT3) and the proto-oncogene c-kit. These kinase receptors activate intracellular signaling cascades that can promote unregulate... | Elevations in serum aminotransferase levels are common during pexidartinib therapy, occurring in 50% to 90% of patients and rising above 5 times the upper limit of the normal range in 12% to 20%. In addition, elevations in alkaline phosphatase levels occur in up to 20% of treated persons. In registration trials, clinic... | The cause of the cholestatic liver injury due to pexidartinib is not known. Pexidartinib is metabolized in the liver largely by the cytochrome P450 system (largely CYP 3A4) and is susceptible to drug-drug interactions with inhibitors or inducers of the microsomal CYPs. | Pexidartinib therapy has been associated with transient serum aminotransferase elevations during therapy in at least half of subjects and with several instances of acute liver injury with jaundice and symptoms. Severe progressive cholestasis leading to liver transplantation or death has been described in several patien... | Pexidartinib – Turalio® | Antineoplastic Agents | null |
Paroxetine.nxml | Paroxetine | 2020-04-08 | Paroxetine is a selective serotonin reuptake inhibitor (SSRI) used in the therapy of depression, anxiety disorders and obsessive-compulsive disorder. Paroxetine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent ... | Paroxetine (pa rox' e teen) 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. Paroxetine was approved for use in the United States in 1992 and it remai... | Liver test abnormalities have been reported to occur in up to 1% of patients on paroxetine, but 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 without jaundi... | The mechanism by which paroxetine causes liver injury is not known. Paroxetine is metabolized at least in part by the liver, mainly via the cytochrome P450 system, and hepatotoxicity may be mediated by toxic intermediates of its metabolism. | The serum aminotransferase elevations that occur on paroxetine therapy are usually self-limited and do not require dose modification or discontinuation of therapy. Acute liver failure has been reported, but is very rare with paroxetine induced liver injury as is chronic liver injury. Persons with intolerance to paroxet... | Paroxetine – Generic, Paxil® | Antidepressant Agents | null |
Benzbromarone.nxml | Benzbromarone | 2017-09-05 | Benzbromarone is a nonpurine xanthine oxidase inhibitor used for the treatment of gout, but never approved for use in the United States because of concerns over reports of acute liver injury and deaths with its use. | Benzbromarone (benz broe' ma rone) is a nonpurine inhibitor of xanthine oxidase that shares no structural homology to allopurinol or to hypoxanthine, but rather is a structural homologue of amiodarone and dronedarone. Therapy leads to lowering of serum uric acid levels within a few weeks, and chronic therapy has been s... | Liver test abnormalities have been reported to occur rarely during benzbromarone therapy, in only 0.1% of patients in clinical trials. Furthermore, it was used widely for many years without reports of hepatotoxicity until the late 1980s, after which several cases of acute liver injury and acute liver failure during ben... | The mechanism of benzbromarone hepatotoxicity is believed to be due to its hepatic metabolism by CYP 2C9 and possible effects of the parent compound or its metabolites on mitochondrial function. Benzbromarone is a benzofuran and shares structural similarities with benzarone and amiodarone, all three of which affect mit... | Acute cases of benzbromarone and benzarone hepatotoxicity have varied in severity, but a high proportion of cases developed acute liver failure leading to death or emergency liver transplantation. Chronic liver injury and vanishing bile duct syndrome related to these agents have not been reported. Recurrence is common ... | null | null | [
{
"cas_registry_number": "3562-84-3",
"molecular_formula": "C17-H12-Br2-O3",
"name": "Benzbromarone"
},
{
"cas_registry_number": "1951-25-3",
"molecular_formula": "C25-H29-12-N-O3",
"name": "Amiodarone"
},
{
"cas_registry_number": "1477-19-6",
"molecular_formula": "C17-H14-O3... |
Cyclobenzaprine.nxml | Cyclobenzaprine | 2017-01-30 | Cyclobenzaprine is a centrally acting muscle relaxant closely related to the tricyclic antidepressants. Despite its similarity to tricyclic antidepressants, there is little evidence that cyclobenzaprine causes liver injury. | Cyclobenzaprine (sye" kloe ben' za preen) is a tricyclic antidepressant derivative that relaxes skeletal muscle by an unknown mechanism of action. Cyclobenzaprine is also a central nervous system depressant, and its efficacy may be related to its sedative effects. Cyclobenzaprine is used for the treatment of painful mu... | The product insert for cyclobenzaprine mentions that abnormal liver function, hepatitis, jaundice, and cholestasis occur in <1% of patients. Details about these cases are not available and no convincing case reports of cyclobenzaprine hepatotoxicity have been published.\n\nLikelihood score: E* (Unproven but suspected c... | Because cyclobenzaprine is a tricyclic antidepressant derivative, it is unclear why it is not associated with hepatotoxicity similar to that attributed to the tricyclic antidepressants. Cyclobenzaprine is metabolized by the liver and has an enterohepatic circulation and half-life of several days. | The minor ALT elevations associated with chronic cyclobenzaprine use are usually asymptomatic and transient. Any elevation of greater than 10 times the upper limit of normal or persistence of abnormalities greater than 5 times the upper limit of normal should lead to discontinuation. Rechallenge is not recommended unle... | Cyclobenzaprine – Generic, Flexeril® | Autonomic Agents: Muscle Relaxants, Central | null |
Promethazine.nxml | Promethazine | 2017-01-16 | Promethazine is first generation antihistamine that belongs to the phenothiazine class and is used predominantly as an antiemetic to treat nausea and vomiting and prevent motion sickness. Despite its phenothiazine structure, promethazine has not been linked to instances of clinically apparent acute liver injury. | Promethazine (proe meth' a zeen) is a first generation antihistamine that is used widely to treat and prevent nausea and to a lesser extent to treat allergy symptoms and as a mild sedative. Promethazine belongs to the phenothiazine class of antihistamines and is a potent antiemetic. Because of its sedating effects, pro... | Despite widespread use and similarity to phenothiazines, promethazine has not been clearly linked to liver test abnormalities or to clinically apparent liver injury. The reason for its safety may relate to low daily dose and limited duration of use.\n\nLikelihood score: E (unlikely to be a cause of clinically apparent ... | null | null | Promethazine – Generic, Phenergan® | Antihistamines | null |
Enalapril.nxml | Enalapril | 2018-02-11 | Enalapril is an angiotensin-converting enzyme (ACE) inhibitor widely used in the therapy of hypertension and heart failure. Enalapril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. | Enalapril (en al' a pril) was the second ACE inhibitor to be approved for use in the United States and is still widely used for therapy of hypertension and heart failure. Like other ACE inhibitors, enalapril inhibits the conversion of angiotensin I, a relatively inactive molecule, to angiotensin II which is the major m... | Enalapril, 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. In addition, more than a dozen instances of clinically apparent... | The cause of the minor serum aminotransferase elevations associated with enalapril is not known. The clinically apparent cases of hepatotoxicity due to enalapril are clearly idiosyncratic and likely due to a reaction to a metabolite. The instances of enalapril associated liver injury associated with a long latency may ... | Most instances of acute liver injury reported with enalapril use have been self limited, but severe and fatal instances have been reported as have cases of vanishing bile duct syndrome. Patients with severe enalapril induced acute liver injury should avoid use of other ACE inhibitors, although cross sensitivity to live... | Enalapril – Generic, Vasotec® | Angiotensin-Converting Enzyme Inhibitors | null |
Voxelotor.nxml | Voxelotor | 2021-07-12 | Voxelotor is an oral inhibitor of hemoglobin S polymerase that is used in the therapy of sickle cell disease. Voxelotor has been associated with rare instances of mild-to-moderate serum enzyme elevations during therapy, but has not been linked to instances of idiosyncratic acute liver injury. | Voxelotor (vox el’ oh tor) is an orally available, small molecule inhibitor of hemoglobin S polymerase, an enzyme which promotes the aggregation of deoxygenated hemoglobin S. Inhibition of this enzyme decreases sickling of red blood cells. Sickle cell disease is caused by an inherited mutation in the β globin gene that... | In clinical trials of voxelotor in patients with sickle cell disease, serum aminotransferase elevations occurred in 1% to 2% of patients during therapy, but the elevations were usually asymptomatic, self-limited in course and mild-to-moderate in degree. Patients with sickle cell disease frequently have liver test abnor... | The mechanism by which voxelotor might cause liver injury is unknown, but may be due to an intermediate product of its metabolism. Voxelotor is metabolized in the liver largely by the CYP 3A4 and is susceptible to drug-drug interactions with inhibitors or inducers of this enzyme reactivity and with other CYP 3A4 substr... | Liver injury due to voxelotor is generally mild and asymptomatic. Elucidating the cause of liver test abnormalities in patients with sickle cell disease is difficult as they are susceptible to several forms of liver injury including acute viral hepatitis, iron overload, gallstone disease, congestive hepatopathy from pu... | Voxelotor – Oxbryta® | Sickle Cell Disease Agents | null |
Oxybate.nxml | Oxybate | 2021-08-18 | Oxybate is a small, neuroactive molecule (gamma-hydroxybutyrate) that is used to treat catalepsy and daytime sleepiness in patients with narcolepsy. Oxybate has been reported to cause serum enzyme elevations during therapy, but has not been implicated in instances of clinically apparent acute liver injury. | Oxybate (ox' i bate) is a simple amino acid-like molecule (sodium 4-hydroxybutyrate) that has mild neuroactivity which acts to induce normal sleep patterns. Its mechanism of action is unclear, but it is a derivative of gamma-aminobutyric acid (GABA) and appears to be an agonist at the GABA-B receptor. In prospective, r... | In preregistration clinical trials, serum enzyme elevations were reported in small numbers of treated patients, but no instance of clinically apparent liver injury was reported. Since the approval and more widespread use of oxybate, there have been no published cases of liver injury due to oxybate, and in postmarketing... | The mechanism by which oxybate might cause liver injury is not known. Hydroxybutyrate is an endogenous derivative of GABA and thus is unlikely to be inherently hepatotoxic or immunogenic.\n\nDrug Class: CNS Stimulants, Narcolepsy Agents\n\nOther Drugs in the Subclass, Narcolepsy Agents: Amphetamines, Armodafinil, Dextr... | null | Sodium Oxybate – Xyrem® | Narcolepsy Agents | [
{
"cas_registry_number": "502-85-2",
"molecular_formula": "C4-H7-Na-O3",
"name": "Sodium Oxybate"
},
{
"cas_registry_number": "6610-05-5",
"molecular_formula": "C4-H9-N-O2.Na",
"name": "Sodium gamma-Aminobutyrate"
}
] |
Metronidazole.nxml | Metronidazole | 2020-02-20 | Metronidazole is a nitroimidazole derivative bactericidal agent widely used in the treatment of many anaerobic and certain protozoan and parasitic infections. Metronidazole has been linked to rare instances of acute, clinically apparent liver injury. | Metronidazole (met" roe nid' a zole) is a nitroimidazole antibiotic that is activated by reduction of its nitro group by susceptible organisms. The activated form of metronidazole is a highly reactive radical anion which targets and damages large protein molecules and DNA. Mammalian cells do not ordinarily activate met... | Despite the wide use of metronidazole, only rare cases of hepatotoxicity have been reported, and metronidazole is not listed among causes of drug induced liver injury and acute liver failure in large case series. High doses of metronidazole given parenterally or in an overdose can cause elevations in serum aminotransfe... | The cause of acute liver injury due to metronidazole is probably immunoallergic, given the short latency period and recurrence with rechallenge. However, the frequency of severe hepatotoxicity in children with Cockayne syndrome suggests a direct toxic effect, probably involving breaks in double stranded DNA. Metronidaz... | The liver injury from metronidazole is rare, but can result in liver failure and death. In typical cases, recovery is expected in 1 to 3 months. Rechallenge results in prompt recurrence and should be avoided. Patients with Cockayne syndrome should not receive metronidazole and should best avoid other nitroimidazole ant... | Metronidazole – Generic, Flagyl® | Antiinfective Agents | null |
ClinicalCourse.nxml | Clinical Course and Diagnosis of Drug Induced Liver Disease | 2019-05-04 | null | null | null | null | null | null | null | null |
Tremelimumab.nxml | Tremelimumab | 2023-01-15 | Tremelimumab is a monoclonal antibody check point inhibitor that is used in combination with durvalumab, a second check point inhibitor, in the therapy of unresectable hepatocellular carcinoma (HCC) and non-small cell lung cancer (NSCLC). The combination of tremelimumab and durvalumab is associated with a relatively hi... | Tremelimumab (tre” me lim’ ue mab) is an IgG2 monoclonal antibody to the cytotoxic T lymphocyte antigen-4 (CTLA-4) which is used in combination with durvalumab, a monoclonal antibody to the programmed cell death receptor ligand-1 (PD-L1), as immune therapy of HCC and NSCLC. Both tremelimumab and durvalumab are check po... | Serum enzyme elevations occur in 41% to 56% of patients taking the combination of tremelimumab and durvalumab and rise to above 5 times the upper limit of normal (ULN) in 8% to 18% of patients. Immune mediated reactions are reported to occur in up to 36% of patients, which are liver related in 7.5% of patients with HCC... | The mechanism of tremelimumab immune mediated organ damage is due to inhibition of checkpoint proteins that results in breaking tolerance to self-antigens and T cell activation. Off target T cell activation leads to immune-relayed adverse events such as hepatitis. Liver related immune reactions usually respond to immun... | The severity of tremelimumab and durvalumab induced liver injury ranges from transient, asymptomatic elevations in serum enzymes to acute liver injury with jaundice to severe acute liver failure and death. Guidelines for management of patients receiving the combination of tremelimumab and durvalumab recommend monitorin... | Tremelimumab – Imjudo® | Antineoplastic Agents | null |
Amifampridine.nxml | Amifampridine | 2019-05-15 | Amifampridine is an orally available potassium channel blocker that increases acetylcholine in synaptic clefts of peripheral nerve endings and is used to treat the Lambert-Eaton myasthenic syndrome. Amifampridine is associated with a low rate of transient serum enzyme elevations during therapy but has not been linked w... | Amifampridine (am" i fam' pri deen) is a diaminopyridine that acts on peripheral potassium channels and is used to treat the Lambert-Eaton myasthenic syndrome, a rare form of myasthenia suspected to be autoimmune in nature. The inhibition of the potassium channel on neuromuscular junctions causes depolarization of the ... | Amifampridine has had limited clinical use, but adverse events have been largely neurologic and gastrointestinal. Serum ALT elevations were not reported in the prelicensure studies of amifampridine but were reported as occurring in a small proportion of patients in safety reviews by the Food and Drug Administration. Ne... | The mechanism by which amifampridine might cause liver injury is not known. It is extensively metabolized by the liver largely by N-acetyltransferase (NAT) to an inactive metabolite. The NAT gene is highly polymorphic and activity rates range from slow to fast. Persons who are slow acetylators have 3- to 5-fold higher ... | null | Amifampridine – Generic, Firdapse®, Ruzurgi® | Myasthenia Agents | null |
Pimavanserin.nxml | Pimavanserin | 2023-06-10 | Pimavanserin is an atypical antipsychotic used in the treatment of hallucinations and delusions in patients with Parkinson disease and psychosis. Use of pimavanserin is associated with a low rate of serum enzyme elevations during therapy but it has not been linked to instances of clinically apparent acute liver injury. | Pimavanserin (pim" a van' ser in) is non-dopaminergic atypical antipsychotic agent that appears to act as a selective inverse agonist of the serotonin (5-HT) 2A receptor. It has little or no activity against the 5-HT2B and 2C receptors which may account for its relative lack of adverse effects. The absence of dopamine ... | Liver test abnormalities are uncommon (<1%) in patients taking pimavanserin, and the frequency of elevations appears to be similar to the rate that occurs with placebo therapy. No liver related serious adverse events or cases of clinically apparent liver injury were reported in the preregistration trials of pimavanseri... | The potential mechanism by which pimavanserin might cause liver injury is not apparent. Pimavanserin is metabolized in the liver, primarily via CYP 3A and is susceptible to drug-drug interactions with agents that are potent inducers or inhibitors of CYP 3A activity. | Liver test abnormalities during pimavanserin therapy are uncommon and typically transient, mild and not associated with symptoms or jaundice. There have been no reports of hepatitis, acute liver failure, chronic hepatitis or vanishing bile duct syndrome attributed to pimavanserin. It is unlikely that there is cross sen... | Pimavanserin – Nuplazid® | Antipsychotic Agents | null |
Olanzapine.nxml | Olanzapine | 2023-06-05 | Olanzapine is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness. Olanzapine is not infrequently associated with serum aminotransferase elevations during therapy and there have been rare instances of clinically apparent acute liver injury linked to its use. | Olanzapine (oh lan' za peen) is a thienobenzodiazepine derivative which appears to act as a dopamine (D1-4) and serotonic (5-HT2A/2C and 5-HT6) receptor antagonist. Olanzapine was approved for use in schizophrenia in the United States in 1996 and continues to be used for this indication. Olanzapine is also used in mood... | Liver test abnormalities have been reported to occur in 10% to 50% of patients on long term therapy with olanzapine. These abnormalities are usually mild, asymptomatic and transient, and can reverse even with continuation of medication. In addition, instances of more marked elevations in serum aminotransferase levels a... | The mechanism by which olanzapine causes serum aminotransferase elevations is not known. Some instances of ALT elevations occurring on olanzapine therapy may be due to nonalcoholic fatty liver disease caused by weight gain that occurs in at least one-quarter of treated patients generally during the first 1 to 2 years o... | The serum aminotransferase elevations that occur on olanzapine therapy are usually self-limited and rarely require dose modification or discontinuation of therapy. No instances of chronic liver disease or vanishing bile duct syndrome have been attributed to olanzapine. Switching to other atypical antipsychotics is occa... | Olanzapine – Generic, Zyprexa® | Antipsychotic Agents | null |
Duloxetine.nxml | Duloxetine | 2018-01-08 | Duloxetine is a selective serotonin and norepinephrine reuptake inhibitor widely used as an antidepressant and for neuropathic pain. Duloxetine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injur... | Duloxetine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) that is used as an antidepressant and for neuropathic pain. By blocking the reuptake of serotonin and norepinephrine in CNS synaptic clefts, the brain levels of these neurotransmitters are increased, which is associated with an antidepress... | Liver test abnormalities with ALT elevations above 3 times the upper limit of normal have been reported to occur in ~1% of patients on duloxetine, but elevations were usually self-limited and did not require dose modification or discontinuation. Rare instances of acute, clinically apparent episodes of liver injury with... | The mechanism by which duloxetine causes liver injury is not known, but is likely due to a metabolic byproduct. Duloxetine is metabolized by the liver, mainly via the cytochrome P450 system (CYP1A2 and 2D6) and is susceptible to drug-drug interactions with agents that alter activity of those microsomal enzymes (such as... | The serum aminotransferase elevations that occur on duloxetine 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 duloxetine therapy. Persons with intolerance to duloxetine may have simi... | Duloxetine – Cymbalta® | Antidepressant Agents | null |
Trimipramine.nxml | Trimipramine | 2020-04-05 | Trimipramine is a tricyclic antidepressant used in the therapy of major (endogenous) as well as reactive (exogenous) depression. In clinical trials, trimipramine therapy was not associated with an increased rate of elevations in serum aminotransferase levels, and it has yet to be linked to instances of clinically appar... | Trimipramine (trye mip' ra meen) is a tricyclic antidepressant that is believed to act by enhancing serotonergic and dopaminergic neurotransmission. Like most tricyclic antidepressants, trimipramine is a weak inhibitor of serotonin, norepinephrine and dopamine reuptake, but also has direct antagonist activity for some ... | In clinical trials, liver test abnormalities were uncommon in patients taking trimipramine (<1%) and generally no more frequent than in placebo or comparator arm recipients. No instances of acute, clinically apparent liver injury attributed to trimipramine have been reported. Most other tricyclic antidepressants in cli... | The mechanism by which trimipramine might cause liver injury is not known. Trimipramine is metabolized at least in part by the liver, but it has not been linked to significant drug-drug interactions. | The serum aminotransferase elevations that occur on amoxapine therapy are usually self-limited and do not require dose modification or discontinuation of therapy. No instances of acute liver failure or vanishing bile duct syndrome due to trimipramine have been reported. There is no information on cross sensitivity to l... | Trimipramine – Generic, Surmontil® | Antidepressant Agents | null |
Estrogens.nxml | Estrogens and Oral Contraceptives | 2020-05-28 | Estrogens and oral contraceptives are both associated with several liver related complications including intrahepatic cholestasis, sinusoidal dilatation, peliosis hepatis, hepatic adenomas, hepatocellular carcinoma, hepatic venous thrombosis and an increased risk of gallstones. These side effects are more common with h... | Synthetic estrogens for regulation of menstrual cycles and hormonal replacement therapy were developed in the early 1950s and came into increasing use in thereafter. Oral contraceptives (OCCs) were approved for use in the United States in 1960 and became widely used. Initial OCCs (first generation) used somewhat high d... | While early formulations of OCCs were associated with frequent serum enzyme elevations, current formulations and hormonal replacement therapy have not been linked to ALT or alkaline phosphatase elevations at rates any higher than occur with placebo. Estrogens and OCCs can cause mild inhibition of bilirubin excretion, l... | Cholestasis due to estrogens and OCCs appears to be related to inhibition of bilirubin and bile acid secretion related to effects of estrogens on the orphan nuclear receptors that modulate bile acid and bilirubin metabolism. Women with cholestasis caused by OCCs often have a history of cholestasis of pregnancy (with ja... | The cholestasis associated with OCCs is typically mild and resolves rapidly with stopping. Some cases, however, are protracted and associated with severe pruritus with or without marked jaundice. The efficacy of ursodiol in treating the cholestasis of pregnancy makes this approach appropriate in women who develop chole... | null | Hormones and Synthetic Substitutes: | null |
Clotrimazole.nxml | Clotrimazole | 2019-04-15 | Clotrimazole is an imidazole antifungal agent used primarily in the treatment of skin, oral and vaginal candida infections. Clotrimazole is typically given topically or as oral or vaginal troches and has only modest systemic absorption. Nevertheless, clotrimazole given orally or as troches has been associated with tran... | Clotrimazole (kloe trim' a zole) is a synthetic imidazole that has broad spectrum activity against Candida albicans and other yeast species. The azoles are believed to act by disruption of the fungal cell wall membrane. Clotrimazole is typically given topically or as oral or vaginal troches. When given as an oral troch... | Transient elevations in serum aminotransferase levels occur in up to 15% of patients treated with clotrimazole orally. The elevations are generally mild-to-moderate in degree and resolve spontaneously with or without discontinuation. Despite decades of widespread use, clotrimazole has not been linked to instances of cl... | The cause of the serum enzyme elevations during clotrimazole therapy is unknown, but many of the antifungal azoles have been implicated in causing liver injury. Because there is minimal systemic absorption, clotrimazole concentrations may not reach levels that could cause significant liver injury. Clotrimazole is metab... | The serum enzyme elevations attributed to clotrimazole therapy are usually mild and transient and rarely require dose adjustment or discontinuation. Nevertheless, the product labels for clotrimazole mention hepatotoxicity and recommend "periodic assessment of hepatic function", particularly in patients with preexisting... | Clotrimazole – Generic, Lotrimin®, Mycelex® (Troche) | Antifungal Agents | null |
Nilotinib.nxml | Nilotinib | 2020-05-10 | Nilotinib is a selective tyrosine kinase receptor inhibitor used in the therapy of chronic myelogenous leukemia. Nilotinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury. | Nilotinib (nye loe' ti nib) is a selective inhibitor of the abnormal tyrosine kinase receptor known as BCR-ABL, formed by the reciprocal translocation between chromosome 9 and 22, which creates the Philadelphia chromosome that is associated with chronic myelogenous leukemia (CML). The BCR-ABL tyrosine kinase receptor i... | Elevations in serum aminotransferase levels are common during nilotinib therapy, occurring in up to 70% of patients, but rising to greater than 5 times the upper limit of normal (ULN) in only 4% to 9% of recipients. These abnormalities are usually asymptomatic. If levels are markedly elevated (ALT or AST persistently g... | The cause of the liver injury due to nilotinib is unknown. Nilotinib is metabolized in the liver largely by the cytochrome P450 system, and liver injury may be due to accumulation of a toxic intermediate or from a drug-drug interaction with other medications. | Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to dose reduction or temporary cessation. Cross reactivity of the hepatic injury with other tyrosine kinase inhibitors is not common, but can occur. In using this medication, other potentially hepatotoxic agents should ... | Nilotinib – Tasigna® | Antineoplastic Agents | null |
Sarecycline.nxml | Sarecycline | 2019-04-10 | Sarecycline is an oral, once daily, narrow spectrum tetracycline used to treat moderate-to-severe acne. Oral sarecycline use has been rarely linked to serum enzyme elevations during therapy and, although suspected of causing liver injury, it has yet to be linked to clinically apparent acute hepatic injury. | Sarecycline (sar" e sye' kleen) is an oral, narrow spectrum tetracycline antibiotic with potent activity against Propionbacterium acnes, a gram-positive organism that plays an important role in the inflammatory lesions of acne vulgaris. The tetracyclines act by inhibition of protein synthesis by binding to the 30S subu... | In preclinical clinical trials of sarecycline in facial acne, serum aminotransferase elevations were mild and no more frequent than with placebo or comparator arms. There were no instances of clinically apparent liver injury. Nevertheless, other tetracycline antibiotics, even when used in low doses, are well known caus... | The mechanism by which sarecycline might cause liver injury is unknown. It has minimal hepatic metabolism and is not associated with significant drug-drug interactions. Minocycline associated liver injury and has been shown to have an association with carriage of the rare HLA allele B*35:02. | Patients on long term sarecycline who develop serum aminotransferase elevations should be monitored more carefully and, if ALT or AST rise above 5 times the upper limit of normal or are accompanied by jaundice or symptoms (including arthralgias and rash), sarecycline should be discontinued. Whether there is cross sensi... | Sarecycline – Seysara® | Antiinfective Agents | null |
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