source_file stringlengths 9 26 | drug_name stringlengths 4 87 | last_updated stringdate 2014-02-16 00:00:00 2025-04-25 00:00:00 | introduction stringlengths 120 6.31k ⌀ | background stringlengths 419 9.32k ⌀ | hepatotoxicity stringlengths 209 9.23k ⌀ | mechanism_of_injury stringlengths 54 1.77k ⌀ | outcome_and_management stringlengths 36 2.91k ⌀ | trade_names stringlengths 6 99 ⌀ | drug_class stringclasses 171
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|---|---|---|---|---|---|---|---|---|---|---|
Dulaglutide.nxml | Dulaglutide | 2019-04-10 | Dulaglutide is a recombinant DNA produced polypeptide analogue of human glucagon-like peptide-1 (GLP-1) which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other antidiabetic agents. There have been no published reports of hepatotoxicity attributed ... | Dulaglutide (doo" la gloo' tide) is a glucagon-like peptide-1 (GLP-1) analogue that acts like the native gastrointestinal hormone (incretin) to increase insulin secretion. Dulaglutide reproduces the activity of GLP-1, binding to specific receptors on pancreatic beta cells and increasing insulin secretion, which can lea... | In large clinical trials, serum enzyme elevations were no more common with dulaglutide therapy than with placebo or comparator agents, and no instances of clinically apparent liver injury were reported. Since licensure, there have been no published case reports of hepatotoxicity due to dulaglutide and the product label... | Dulaglutide is a polypeptide and is metabolized to amino acids by serum and tissue proteases, and is unlikely to have any direct hepatotoxic potential. Dulaglutide acts through the incretin pathway to affect glucose metabolism and, thus, is often grouped with other incretin-based antidiabetic mediations such as the DPP... | null | Dulaglutide – Trulicity® | Antidiabetic Agents | null |
Piroxicam.nxml | Piroxicam | 2020-03-20 | Piroxicam is a commonly used nonsteroidal antiinflammatory drug (NSAID) that is available by prescription only and is used in therapy of chronic arthritis. Piroxicam can cause mild serum aminotransferase elevations and, in rare instances, leads to clinically apparent acute liver injury that can be severe and even fatal... | Piroxicam (pir ox' i kam) belongs to the oxicam family, which is a class of enolic acids structurally unrelated to other NSAIDs. Piroxicam, like other NSAIDs, acts through inhibition of tissue cyclooxygenases (Cox-1 and -2) leading to a decrease in synthesis of pro-inflammatory prostaglandins, which are potent mediator... | Elevated serum aminotransferase levels have been reported in 3% to 18% of patients taking piroxicam, but symptomatic liver disease with jaundice is rare (estimated at 1 to 5 cases per 100,000 prescriptions). The latency to onset of symptoms of clinically apparent liver injury due to piroxicam is variable from a few day... | The mechanism of piroxicam induced liver injury is not known, but may be due to a toxic metabolic intermediate of piroxicam metabolism, which occurs largely in the liver. Cases with allergic manifestations (fever, rash, eosinophilia) may also have a component of hypersensitivity. | Severity of the liver injury from piroxicam ranges from asymptomatic elevations in serum aminotransferase levels to severe hepatitis with acute liver failure. Several instances of chronic vanishing bile duct syndrome have been attributed to other oxicam NSAIDs, but not specifically to piroxicam. In most instances, howe... | Piroxicam – Generic, Feldene® | Nonsteroidal Antiinflammatory Drugs | null |
Ertapenem.nxml | Ertapenem | 2017-01-17 | Ertapenem is a broad spectrum carbapenem antibiotic used primarily for the treatment of aerobic gram-negative bacterial infections. Ertapenem, like other carbapenems, is associated with transient and asymptomatic elevations in serum enzymes. The carbapenems have also been linked to rare instances of clinically apparent... | Ertapenem (er" ta pen' em) is a broad spectrum beta-lactam antibiotic used predominantly for treatment of severe aerobic gram-negative infections. Ertapenem, like other carbapenems, binds to bacterial penicillin binding proteins and interferes with bacterial cell wall integrity and synthesis. It is a broad spectrum ant... | Mild, transient, asymptomatic elevations in serum aminotransferase levels occur in about 5% of patients receiving parenteral ertapenem for 5 to 14 days. These abnormalities are usually self-limited and asymptomatic. In the limited period that it has been available, no cases of hepatitis with jaundice have been reported... | null | The liver injury due to the carbapenems is usually mild, asymptomatic and self-limited. Rarely, the carbapenems can cause a clinically apparent acute cholestatic hepatitis that is usually self-limiting and not requiring therapy or intervention. There is little information on possible cross sensitivity to liver injury a... | Ertapenem – Invanz® | Antiinfective Agents | null |
Captopril.nxml | Captopril | 2018-02-11 | Captopril is an angiotensin-converting enzyme (ACE) inhibitor used in the therapy of hypertension and heart failure. Captopril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. | Captopril (kap' toe pril) was the first 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, captopril inhibits the conversion of angiotensin I, a relatively inactive molecule, to angiotensin II which is the major me... | Captopril, 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. While rare, several dozen cases of clinically apparent liver in... | The cause of the minor serum aminotransferase associated with captopril is not known. The clinically apparent acute liver injury from captopril is likely an idiosyncratic reaction to a metabolite. Captopril is hydrolyzed by the liver to its active metabolite captoprilat and has little further hepatic metabolism. | Most instances of acute liver injury reported with captopril use have been self limited, but there have been rare reports of acute liver failure due to captopril and several reports of cholestatic hepatitis leading to prolonged jaundice. Patients with severe captopril induced acute liver injury and hypersensitivity rea... | Captopril – Generic, Capoten® | Angiotensin-Converting Enzyme Inhibitors | null |
SawPalmetto.nxml | Saw Palmetto | 2020-04-02 | Saw palmetto is a popular herbal medication and extract derived from the fruit of the low growing, small palm, Serenoa repens, which has fan shaped leaves and is native to Florida and the Southeast United States. Currently, saw palmetto is used mostly for symptoms of benign prostatic hypertrophy. Saw palmetto has been ... | Saw palmetto (saw pal met’ toe) is a widely used herbal derived from the fruit of the low growing bushy palm of the same name (Serenoa repens). Native Americans used saw palmetto fruit both as a food as well as an herbal remedy with multiple uses, including as a sedative, diuretic, sleeping aid, expectorant and cough s... | Chronic therapy with saw palmetto has not been linked to serum enzyme elevations and prospective trials found little or no evidence of liver injury from its administration. However, there have been rare case reports of clinically apparent liver injury attributed to saw palmetto, although in some instances, other possib... | Saw palmetto extracts have many components, but none of them has been shown to be particularly hepatotoxic. The rare cases of liver injury reported with saw palmetto use have had idiosyncratic features. Saw palmetto has few herb-drug interactions and is not affected by inducers or inhibitors of the cytochrome P450 enzy... | Hepatotoxicity from saw palmetto is very rare and cases have been self-limiting upon stopping the herbal. There have been no instances leading to fatalities, liver transplantation, chronic hepatitis, or vanishing bile duct syndrome. Studies of rechallenge have not been reported.\n\nOther Names: Cabbage palm, Sabal\n\nD... | Saw Palmetto – Generic | Herbal and Dietary Supplements | null |
Histrelin.nxml | Histrelin | 2023-05-28 | Histrelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of production of testosterone (in men) and estrogen (in women) and is used predominantly to treat advanced prostate cancer. Histrelin is associated with a low rate of transient serum enzyme elevations during therapy, but has not bee... | Histrelin (his trel' in) is a nonapeptide analogue of gonadotropin releasing hormone that acts on the pituitary to cause the synthesis and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH), two gonadotropins that act on the male testes to stimulate the production of testosterone and on the fema... | Histrelin has been associated with serum enzyme elevations during therapy in rates similar to those of other GnRH analogues. The serum enzyme elevations are generally mild, asymptomatic and resolve even without dose adjustment or drug discontinuation. ALT elevations above 3 times the upper limit of normal occur in less... | The cause of the minor serum enzyme elevations that can occur during histrelin therapy is unknown. Histrelin is a short peptide similar to GnRH and is metabolized locally in tissue and not by the hepatic cytochrome P450 system. Some serum enzyme elevations may be caused by nonalcoholic fatty liver arising because of we... | The serum enzyme elevations during histrelin therapy rarely require dose modification or drug discontinuation and should instead lead to investigation of other possible causes of liver injury. There is no evidence for cross sensitivity to liver injury among the various GnRH analogues, despite their similarity in chemic... | Histrelin – Supprelin® | Antineoplastic Agents | null |
Apoaequorin.nxml | Apoaequorin | 2019-12-11 | Apoaequorin is a recombinant protein used as a dietary supplement that is purported to improve memory and verbal learning. Apoaequorin has not been associated with serum enzyme elevations during therapy nor with clinically apparent liver injury. | Apoaequorin is a calcium binding protein found in luminescent jellyfish (Aequorea victoria). When the natural (apo) form of the protein is conjugated with coelenterazine, the resulting protein aequorin has natural bioluminescence when exposed to calcium. For this reason, it has been used as a research molecule to study... | Apoaequorin is considered generally safe and without major adverse effects. In the human studies that have been published there were no reports of serum enzyme elevations occurring during therapy and no mention of serious adverse events or hepatotoxicity.\n\nLikelihood score: E (unlikely cause of clinically apparent li... | null | null | Apoaequorin – Prevagen® | Herbal and Dietary Supplements | null |
Givosiran.nxml | Givosiran | 2020-02-27 | Givosiran is synthetic small interfering RNA (siRNA) molecule directed against 5-aminolevulinic acid synthase that is used to treat acute hepatic porphyria. Givosiran has been linked to mild-to-moderate ALT elevations during therapy, but has not been linked to instances of idiosyncratic acute liver injury with symptoms... | Givosiran (giv” oh sir’ an) is a synthetic double stranded, small interfering RNA (siRNA) directed against 5-aminolevulinic acid synthase 1, which results in decreases in serum delta aminolevulinic acid (ALA) and porphobilinogen (PBG), intermediates in porphyrin metabolism which accumulate in patients with acute hepati... | The acute hepatic porphyrias are rare, and the pivotal trials of givosiran were conducted in rather small numbers of patients, so the full spectrum of hepatotoxicity may not be fully known. Nevertheless, in the registration controlled trials, serum aminotransferase elevations arose in 13% of givosiran- versus 2% of pla... | The cause of hepatic injury from the givosiran and other siRNA therapeutics is unknown. One possibility is that suppression of 5-aminolevulinic acid synthase may cause cell damage in some hepatocytes. The mRNA suppression appears to lower but not completely eliminate enzyme activity, but individual hepatocytes may vary... | The liver injury associated with givosiran therapy has invariably been mild, not associated with jaundice and rapidly resolving often without discontinuation or even dose adjustment. In prelicensure clinical trials, subjects received hemin therapy for acute attacks without evidence of liver injury, and there is no reas... | Givosiran – Givlaari® | Genetic Disorder Agents | null |
Anagrelide.nxml | Anagrelide | 2017-07-05 | Anagrelide is an antithrombotic and platelet reducing agent that is used to treat the thrombocythemia associated with myeloproliferative diseases. Anagrelide has had limited clinical use, but has not been linked to significant serum enzyme elevations during therapy or to instances of clinically apparent acute liver inj... | Anagrelide (an ag' re lide) is platelet reducing agent that is used to treat thrombocytosis due to myeloproliferative diseases. Its mechanism of action is not well defined, but it appears to inhibit the maturation and differentiation of megakaryocytes, and both synthesis and release of platelets as well as subsequent p... | In preregistration studies, anagrelide was not associated with serum enzyme elevations or with episodes of clinically apparent liver injury. Since its approval, there has been a single published abstract reporting progressive, ultimately fatal cholestasis after liver transplantation and use of anagrelide, but there hav... | The mechanism by which anagrelide might cause serum aminotransferase elevations or liver injury is not known. The typical daily dose is low (1 to 10 mg), which may account for its relative lack of hepatotoxicity.\n\nDrug Class: Antithrombotic Agents\n\nOther Drugs in the Subclass (Primary Thrombocythemia): Hydroxyurea,... | null | Anagrelide – Generic, Agrylin® | Antithrombotic Agents | null |
ThrombopoietinRecept.nxml | Thrombopoietin Receptor Agonists | 2018-12-30 | The thrombopoietin receptor agonists mimic the action of thrombopoietin on its receptor and stimulate the activation, proliferation and maturation of megakaryocytes, resulting in an increase in circulating platelet counts. Thrombopoietin itself acts in this manner, but when recombinant thrombopoietins were used clinica... | null | null | null | null | Avatrombopag – Doptelet® | Hematologic Growth Factors | [
{
"cas_registry_number": "570406-98-3",
"molecular_formula": "C29-H34-Cl2-N6-O3-S2",
"name": "Avatrombopag"
},
{
"cas_registry_number": "496775-61-2",
"molecular_formula": "C25-H22-N4-O4",
"name": "Eltrombopag"
},
{
"cas_registry_number": "1110766-97-6",
"molecular_formula": ... |
Romidepsin.nxml | Romidepsin | 2020-09-25 | Romidepsin is an intravenously administered histone deacetylase inhibitor and antineoplastic agent that is approved for use in refractory or relapsed cutaneous and peripheral T cell lymphomas. Romidepsin is associated with modest rate of minor serum enzyme elevations during therapy but has not been linked to cases of c... | Romidepsin (roe" mi dep' sin) is an intravenously administered antineoplastic agent which acts by inhibition of histone deacetylases, thereby preventing removal of acetyl groups from histones. The accrual of acetyl groups on histones causes cell cycle arrest and apoptotic cell death. Malignant cells and particularly ma... | In clinical trials of romidepsin in patients with CTLC and PTLC, the rates of serum enzyme elevations during therapy ranged from 7% to 20%, but the abnormalities were usually transient and mild and did not require dose modifications. Serum ALT elevations above 5 times ULN occurred in 6% of patients. In the preregistrat... | The reason why romidepsin might cause serum enzyme elevations is not known, but may be a direct toxicity to hepatocytes caused by inhibition of histone deacetylase or other enzyme activities. Romidepsin is metabolized in the liver by cytochrome P450 system, predominantly CYP 3A4 and is susceptible to drug-drug interact... | Serum enzyme elevations during romidepsin therapy are usually mild and rarely dose limiting. Romidepsin should be held if ALT or AST values rise above 5 times the ULN and should be permanently discontinued if elevations exceed 20 times the ULN, or with the appearance of jaundice or symptoms of liver injury. There is no... | Romidepsin – Istodax® | Antineoplastic Agents | null |
Zolpidem.nxml | Zolpidem | 2018-02-20 | Zolpidem is a benzodiazepine receptor agonist that is used for the treatment of insomnia. Zolpidem has rarely been implicated in causing serum enzyme elevations and has not been reported to cause clinically apparent liver injury. | Zolpidem (zol' pi dem) is a non-benzodiazepine, benzodiazepine receptor agonist of the imidazopyridine class that acts by binding to the benzodiazepine (BZ) site on the GABA receptor complex, causing neural inhibition and helping to induce sleep. Zolpidem has selectivity for certain BZ receptor subtypes and does not ha... | In multiple premarketing randomized controlled trials, zolpidem was not associated with an increased rate of serum enzyme elevations in comparison to placebo therapy. A single instance of clinically apparent liver injury has been reported. The onset of injury was 2 days after a single dose of zolpidem and was accompani... | null | null | Zolpidem – Generic, Ambien® | Sedatives and Hypnotics | null |
Tofacitinib.nxml | Tofacitinib | 2022-08-30 | Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis, psoriatic arthritis and inflammatory bowel disease. Tofacitinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy, but has yet to be lin... | Tofacitinib (tow" fa sye' ti nib) is an orally available, specific inhibitor of Janus-associated kinases (mainly JAK1 and JAK3) that is used to treat moderate-to-severe rheumatoid arthritis, psoriatic arthritis and inflammatory bowel disease. The Janus kinases are critical steps in immune activation as well as in hemat... | In large registration clinical trials, serum aminotransferase elevations occurred in 28% to 34% of tofacitinib treated subjects compared to 25% in comparator arms and 10% in placebo recipients. These elevations were typically mild and transient, but values above 3 times the upper limit of normal (ULN) occurred in 1% to... | The causes of serum enzyme elevations during tofacitinib therapy are not known. Tofacitinib is metabolized in the liver largely through the CYP 3A4 pathway and liver injury may be related to production of a toxic or immunogenic intermediate. Because it is a substrate for CYP 3A4, tofacitinib is susceptible to drug-drug... | Monitoring of serum aminotransferase levels is recommended for patients starting tofacitinib. 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 to suggest ... | Tofacitinib – Xeljanz® | Antirheumatic Agents | [
{
"cas_registry_number": "941678-49-5",
"molecular_formula": "C17-H18-N6",
"name": "Ruxolitinib"
},
{
"cas_registry_number": "477600-75-2",
"molecular_formula": "C16-H20-N6-O",
"name": "Tofacitinib"
}
] |
Acalabrutinib.nxml | Acalabrutinib | 2021-03-21 | Acalabrutinib is an oral inhibitor of Bruton’s tyrosine kinase that is used in the therapy of B cell malignancies including refractory mantle cell lymphoma and chronic lymphocytic leukemia. Acalabrutinib has been associated with mild-to-moderate serum enzyme elevations during therapy but has not been linked to instance... | Acalabrutinib (a kal" a broo' ti nib) is an orally available, small molecule inhibitor of Bruton’s tyrosine kinase (BTK), which is an essential component in the B cell receptor signaling pathway. Inhibition of this pathway prevents B cell activation, differentiation and proliferation. Deficiency of BTK is the cause of ... | In open label clinical trials of acalabrutinib in patients with CLL and mantle cell lymphoma, serum aminotransferase elevations occurred in 19% to 23% of patients during therapy and rose to above 5 times ULN in 2% to 3%. These elevations were transient and resolved spontaneously but occasionally led to early drug disco... | The mechanism by which acalabrutinib might cause liver injury is unknown but may be due to off-target inhibition of tyrosine kinases. Acalabrutinib 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. Reactivation of hepat... | Liver injury due to acalabrutinib is generally mild and asymptomatic. Reactivation of hepatitis B, however, can result in severe hepatitis and even acute hepatic failure. Patients who are to receive B cell inhibitors such as acalabrutinib, ibrutinib, rituximab and usteokinumab should be screened for serologic markers o... | Acalabrutinib – Calquence® | Antineoplastic Agents | [
{
"cas_registry_number": "1420477-60-6",
"molecular_formula": "C26-H23-N7-O2",
"name": "Acalabrutinib"
},
{
"cas_registry_number": "936563-96-1",
"molecular_formula": "C25-H24-N6-O2",
"name": "Ibrutinib"
}
] |
Selegiline.nxml | Selegiline | 2017-07-21 | Selegiline is an inhibitor of monamine oxidase used in the treatment of depression and as adjunctive therapy in combination with levodopa and carbidopa in the therapy of Parkinson disease. Selegiline has been associated with a low rate of serum enzyme elevations during treatment, but has not been linked to instances of... | Selegiline (se le' ji leen) is a specific inhibitor of monamine oxidase (MAO) type B, which is a major enzyme in the pathway of dopamine and levodopa metabolism. As a result, selegiline results in an increase in the bioavailability of levodopa, enhancing and increasing the duration of its effects in Parkinson disease. ... | Selegiline has been reported to cause serum enzyme elevations in up to 40% of patients treated long term. Although the abnormalities were usually mild and self-limiting, they were persistent with continuation of treatment in some patients, ultimately requiring drug discointuation. Selegiline has not been implicated in ... | Selegiline is extensively removed from the blood by the liver (first pass metabolism) and undergoes hepatic conjugation and elimination. The pathways of selegiline metabolism have not been well defined. | The only liver abnormalities that have attributed to selegiline have been mild and self-limiting elevations in serum enzymes. No instances of acute hepatitis, acute liver failure, chronic hepatitis or vanishing bile duct syndrome have been linked to selegiline use.\n\nDrug Class: Antiparkinson Agents\n\nOther Drugs in ... | Selegiline – Generic, Atapryl®, Eldepryl® | Antiparkinson Agents | null |
Chlorzoxazone.nxml | Chlorzoxazone | 2017-01-30 | Chlorzoxazone is a centrally acting muscle relaxant commonly used for low back pain. Chlorzoxazone has been linked to rare instances of acute liver injury, a few of which have been fatal. | Chlorzoxazone (klor zox' a zone) acts centrally rather than directly on muscles to relieve muscle spasms, either through its sedative effects or other unknown mechanisms. Chlorzoxazone is indicated for therapy of low back pain and muscle spasms, although its overall efficacy is considered only fair. Chlorzoxazone was a... | There have been no adequate prospective studies demonstrating the rates of ALT or AST elevations on chlorzoxazone therapy. Rare instances of clinical apparent liver disease possibly attributable to chlorzoxazone have appeared, including fatal cases. Such cases must be very rare, as this agent is widely used. While case... | The cause of acute hepatic injury from chlorzoxazone is unknown, but is clearly idiosyncratic and likely due to hypersensitivity. | The idiosyncratic liver injury due to chlorzoxazone ranges from mild, self-limited hepatitis to severe, protracted liver injury leading to death or need for liver transplantation. Rechallenge leads to rapid return of hepatic injury and should be avoided. No cross reactivity with other muscle relaxants has been identifi... | Chlorzoxazone – Generic, Parafon Forte® | Autonomic Agents: Muscle Relaxants, Central | null |
SerotoninRcptAgonist.nxml | Serotonin Receptor Agonists (Triptans) | 2018-02-10 | The triptans are a group of serotonin receptor agonists that are useful in the therapy of vascular headaches and migraine. The triptans are generally used in low doses for a limited period of time and have not been associated with serum enzyme elevations, but some have been implicated in rare instances of clinically ap... | The triptans (trip' tans) are synthetic serotonin receptor agonists that are used in the therapy of migraine and vascular headache. Serotonin (5-hydroxytryptamine or 5-HT) is a monoamine that has multiple actions, acting as a neurotransmitter and bioactive amine. The diversity of actions of serotonin is partially due t... | In large prospective controlled trials, the different triptans have not been associated with serum enzyme elevations or hepatotoxicity; however, the frequency of monitoring in most studies was limited and rates of ALT elevations not reported. There have been rare individual reports of cholestatic hepatitis after the us... | The cause of idiosyncratic liver injury after triptan use is not known, but is likely due to a toxic metabolite causing an acute, cholestatic hepatitis-like injury. An intriguing hypothesis is that the serotonin agonist activity causes biliary dyskinesis and functional obstruction. | null | Almotriptan – Generic, Almogran®, Axert® | Migraine Headache Agents | [
{
"cas_registry_number": "154323-57-6",
"molecular_formula": "C17-H25-N3-O2-S",
"name": "Almotriptan"
},
{
"cas_registry_number": "177834-92-3",
"molecular_formula": "C22-H26-N2-O2-S.Br-H",
"name": "Eletriptan"
},
{
"cas_registry_number": "158930-17-7",
"molecular_formula": "... |
Thioguanine.nxml | Thioguanine | 2017-08-17 | Thioguanine (also referred to as 6-thioguanine and as tioguanine) is a purine analogue that is used in the therapy of acute and chronic myelogenous leukemias. Thioguanine therapy is associated with minor, usually transient and asymptomatic elevations in serum aminotransferase levels and has also been linked to rare ins... | Thioguanine (thye" oh gwa' neen) is a thiopurine, a purine analogue and antimetabolite. It is a derivative of mercaptopurine (2-amino-6-mercaptopurine) and, like its parent molecule, inhibits purine metabolism, thus blocking DNA, RNA and subsequent protein synthesis. Thioguanine also has antiinflammatory activity. Thio... | As with other thiopurines, thioguanine has been associated with several forms of hepatotoxicity, including mild, transient and asymptomatic rises in serum aminotransferase levels, an acute hepatic injury developing during the first year of starting therapy, and a chronic hepatic injury marked by variable degrees of pel... | The mechanism by which thioguanine causes idiosyncratic acute liver injury is not known, but is likely due to an immunological response to a metabolic byproduct of its metabolism. Thioguanine undergoes extensive hepatic metabolism to 6-mercaptopurine and thereafter to other thiopurines via three different pathways. Pat... | The serum aminotransferase elevations that occur during thioguanine therapy may improve spontaneously or with dose reduction and generally resolve rapidly with discontinuation. In patients who have aberrant metabolism of thiopurines to 6-methylmercaptopurine (6-MMP) as shown by elevated plasma levels, lowering the dose... | Thioguanine – Generic, Tabloid® | Antineoplastic Agents | null |
disclaimer.nxml | Disclaimer | 2019-09-03 | null | null | null | null | null | null | null | null |
Famotidine.nxml | Famotidine | 2018-01-25 | Famotidine is a histamine type 2 receptor antagonist (H2 blocker) which is commonly used for treatment of acid-peptic disease and heartburn. Famotidine has been linked to rare instances of clinically apparent acute liver injury. | Famotidine (fam oh' ti deen) was the third 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. The H2 blockers are specific antagonists of the histamine type 2 receptor, which is found on the baso... | Chronic therapy with famotidine 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 ap... | Famotidine is metabolized by the microsomal P450 drug metabolizing enzymes and injury may be the result of its activation to a toxic intermediate. | The hepatic injury caused by famotidine is usually rapidly reversible with stopping the medication (Case 1). Famotidine has not been definitively linked to cases of acute liver failure, chronic hepatitis, prolonged cholestasis or vanishing bile duct syndrome. The results of rechallenge have not been reported. There app... | Famotidine – Generic, Pepcid® | Antiulcer Agents | null |
Oliceridine.nxml | Oliceridine | 2024-07-05 | Oliceridine is an intravenously administered, synthetic opioid that is used to treat moderate-to-severe pain not responsive to nonsteroidal antiinflammatory agents. Oliceridine is associated with a low rate of serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent l... | Oliceridine (oh” li ser’ i deen) is an intravenously administered, synthetic opioid approved for use in moderate-to-severe acute pain in adults after surgery or painful procedures. Oliceridine is an agonist of the μ-opioid receptor with a potency similar to that of morphine, but with post-receptor actions that are bias... | Serum ALT elevations developed in 1% to 3% of patients receiving oliceridine and in a similar proportion (2.4%) receiving morphine after abdominal surgery. However, the aminotransferase elevations were not associated with jaundice and were usually considered unrelated to therapy. Since approval of oliceridine, there ha... | Oliceridine like other opioid analgesics has not been associated with significant liver injury. The reasons for its lack of hepatotoxicity may relate to the short duration of therapy and the low doses used. Oliceridine is metabolized in the liver predominantly by cytochrome P450 enzymes (CYP 2D6 and 3A4). | The product label for oliceridine does not recommend screening or monitoring for routine liver tests before or during therapy.\n\nDrug Class: Opioids, Opioid Antagonists\n\nOther Drugs in this Class: Alfentanil, Fentanyl, Morphine, Remifentanil, Sufentanil | Oliceridine – Olinvyk® | Opioids | null |
Eplerenone.nxml | Eplerenone | 2021-10-13 | Eplerenone is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease. | Eplerenone (e pler' e none) is a competitive antagonist of aldosterone at the mineralocorticoid receptor. The aldosterone receptor in the late distal tubules and collecting ducts of the kidneys induces sodium reabsorption and potassium excretion in the distal tubule. Inhibition of this receptor promotes a sodium diures... | Eplerenone therapy has been associated with a low rate of serum aminotransferase elevations which are typically mild and transient. ALT elevations of greater than 3 times the ULN occurred in 0.7% and greater than 5 times in 0.2% of eplerenone treated compared to 0.3% and 0.3% of placebo treated subjects. Idiosyncratic,... | Eplerenone is metabolized in the liver by the cytochrome P450 system (CYP 3A4) and hepatic reactions may be generated by intermediates in its metabolism. | The mild serum aminotransferase elevations that have been reported with eplerenone resolved rapidly on discontinuation and in some instances resolved even with drug continuation. While yet unproven, cross reactivity to the liver injury that can occur with spironolactone should be assumed.\n\nDrug Class: Diuretics, Pota... | Eplerenone – Generic, Inspra® | Diuretics | null |
LoopDiuretics.nxml | Loop Diuretics | 2021-10-13 | The loop diuretics are potent and widely used agents in the therapy of edematous states and congestive heart failure and less commonly for hypertension. Clinically apparent acute liver injury due to the loop diuretics is exceeding rare, if it occurs at all. | The loop diuretics act by inhibition of the sodium-potassium-chloride symporter present in the thick ascending limb of the loop of Henle causing an inhibition of sodium reuptake. The increase in delivery of sodium to the distal convoluted loop overwhelms its capacity for sodium reabsorption and a brisk sodium diuresis ... | Use of the loop diuretics has not been associated with an increased rate of serum aminotransferase elevations. There have been only rare, reported cases of clinically apparent liver injury associated with loop diuretics and most of these reports were not very convincing. Interestingly, furosemide causes a direct hepato... | The cause of the rare occurrence of clinically apparent liver injury associated with the loop diuretics is not known. These agents are metabolized minimally by the liver and generally have rapid renal excretion. | Cases of clinically apparent liver injury due to the loop diuretics have been too few to characterize their severity and course. There have been no published instances of acute liver failure or chronic liver injury attributed to any of the loop diuretics. Cross reactivity among the four agents is unlikely because of th... | Bumetanide – Generic, Bumex® | Diuretics | [
{
"cas_registry_number": "28395-03-1",
"molecular_formula": "C17-H20-N2-O5-S",
"name": "Bumetanide"
},
{
"cas_registry_number": "58-54-8",
"molecular_formula": "C13-H12-Cl2-O4",
"name": "Ethacrynic Acid"
},
{
"cas_registry_number": "54-31-9",
"molecular_formula": "C12-H11-Cl-... |
Apalutamide.nxml | Apalutamide | 2023-03-15 | Apalutamide is a third generation, oral nonsteroidal antiandrogen used to treat nonmetastatic castration-resistant prostate cancer. Apalutamide is associated with a low rate of serum enzyme elevation during therapy but has not been linked to cases of clinically apparent liver injury with jaundice. | Apalutamide (a pa lut' a mide) is a small molecule androgen receptor antagonist which binds to the intracellular receptor and prevents its translocation to the nucleus and subsequent DNA binding, thereby blocking its activity. Therapy with apalutamide lowers residual testosterone levels after surgical castration in men... | In prelicensure controlled trials of apalutamide, serum aminotransferase elevations were uncommon and generally transient and mild, not requiring dose modification. Clinically apparent liver injury with jaundice attributable to apalutamide was not reported in the preregistration trials and is not mentioned as an advers... | The possible cause of liver injury due to apalutamide therapy is unknown. While first and second generation antiandrogens have been implicated in causing liver injury, the more potent third general factors have not. Apalutamide is extensively metabolized in the liver predominantly by CYP 2C8 and 3A and is an inducer of... | The liver injury linked to apalutamide therapy has been generally mild, consisting of transient and asymptomatic elevations in serum aminotransferase levels and rarely requiring dose modification or discontinuation. Apalutamide has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duc... | Apalutamide – Erleada® | Antineoplastic Agents | null |
Temozolomide.nxml | Temozolomide | 2020-09-02 | Temozolomide is an orally administered alkylating agent used largely in the therapy of malignant brain tumors including glioblastoma and astrocytoma. Temozolomide has been associated with a low rate of serum enzyme elevations during treatment and with rare instances of clinically apparent cholestatic liver injury. | Temozolomide (tem" oh zol' oh mide) is an imidazotetrazine derivative similar to dacarbazine (DTIC), which acts as an alkylating agent disrupting DNA replication, causing modification and cross linking of DNA, thus inhibiting DNA, RNA and protein synthesis and causing programmed cell death (apoptosis) in rapidly dividi... | Serum aminotransferase elevations occur during temozolomide therapy in up to 12% of patients, but these elevations are usually mild and self-limited, not requiring dose adjustment or drug discontinuation. An instance of serum aminotransferase elevation with jaundice was reported in the registration trials of temozolomi... | Temozolomide is hydrolyzed to the active intermediate at physiological pH and does not require hepatic metabolism or affect the cytochrome P450 (CYP) system to a major degree, perhaps accounting for its relative lack of direct hepatotoxicity. The cases of acute cholestatic liver injury have resembled idiosyncratic drug... | The severity of liver injury caused by temozolomide ranges from minor transient elevations in serum enzymes to severe cholestatic hepatitis that can be prolonged. Temozolomide has not been reported to cause acute liver failure but has been linked to instances of chronic liver injury and paucity of bile ducts on liver b... | Temozolomide – Generic, Temodar® | Antineoplastic Agents, Alkylating Agents | null |
Teplizumab.nxml | Teplizumab | 2023-01-15 | Teplizumab is a humanized monoclonal antibody to CD3 which is used to delay the onset of clinically significant type 1 diabetes (stage 3 diabetes) in a patient at high risk as shown by the presence of anti-pancreatic islet cell autoantibodies and dysglycemia (stage2 diabetes). Teplizumab is given intravenously once dai... | Teplizumab (tep liz’ ue mab) is a humanized monoclonal IgG1 antibody directed against CD3, which results in inhibition of cytotoxic T cell activation and proliferation. Because type 1 diabetes is thought to be caused by cytotoxic T cell destruction of pancreatic islet beta cells that produce insulin, teplizumab was eva... | Mild-to-moderate serum aminotransferase elevations arise in up to 25% of patients treated with teplizumab, usually during the 14 days of therapy and often associated with evidence of mild-to-moderate cytokine release syndrome. The ALT and AST elevations are usually mild, transient and asymptomatic, rising to above 3 ti... | The possible mechanisms of liver injury due to teplizumab are unclear, but probably relate to cytokine release induced by the binding of the monoclonal antibody to activated T cells that then release cytokines into the circulation that can cause transient liver injury. There is no evidence that the cytokine release ind... | Drug Class: Monoclonal Antibodies, Antidiabetic Agents | Teplizumab – Tzield® | Antidiabetic Agents | null |
Acetaminophen.nxml | Acetaminophen | 2016-01-28 | Acetaminophen is a widely used nonprescription analgesic and antipyretic medication for mild-to-moderate pain and fever. Harmless at low doses, acetaminophen has direct hepatotoxic potential when taken as an overdose and can cause acute liver injury and death from acute liver failure. Even in therapeutic doses, acetami... | Acetaminophen (a seet" a min' oh fen), which is known as paracetamol in Europe, is an aminophenol that is believed to act centrally as an analgesic and antipyretic agent. While technically a nonsteroidal antiinflammatory drug (NSAID), acetaminophen unlike typical NSAIDs (ibuprofen, naproxen, indomethacin) has only mino... | Chronic therapy with acetaminophen in doses of 4 grams daily has been found to lead to transient elevations in serum aminotransferase levels in a proportion of subjects, generally starting after 3 to 7 days, and with peak values rising above 3-fold elevated in 39% of persons. These elevations are generally asymptomatic... | The mechanism of acetaminophen hepatotoxicity has been extensively analyzed in humans and in animal models. Acetaminophen is largely converted to nontoxic glucuronate or sulfate conjugates and secreted in the urine. A minor amount of acetaminophen is metabolized via the cytochrome P450 system to intermediates that can ... | The minor aminotransferase elevations that occur during chronic therapy with acetaminophen are rarely symptomatic, generally go undetected, resolve rapidly with discontinuation of acetaminophen and sometimes even with continuation at the same dose. Such transient aminotransferase elevations do not appear to have lastin... | Acetaminophen – Generic, Various Trade Names | Nonsteroidal Antiinflammatory Drugs | null |
Lonafarnib.nxml | Lonafarnib | 2021-01-07 | Lonafarnib is an oral, small molecule inhibitor of farnesyltransferase that is used to treat Hutchison-Gilford progeria syndrome and is under investigation as therapy of chronic hepatitis D. Lonafarnib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy, but has not ... | Lonafarnib (loe” na far’ nib) is an orally available, specific inhibitor of farnesyltransferase and is approved for the treatment of Hutchinson-Gilford progeria syndrome (HGPS), a rare autosomal dominant form of accelerated aging (arising in 1 in 4 million live births). Persons with HGPS develop cardiovascular disease ... | In the small prelicensure clinical trials conducted in children with progeria, serum aminotransferase elevations occurred in 35% of lonafarnib treated subjects but were usually mild and self-limited, rising to above 3 times the upper limit of normal (ULN) in only 5%. There were no liver related serious adverse events a... | The causes of serum enzyme elevations during lonafarnib therapy are not known. Lonafarnib 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, lona... | Monitoring of laboratory tests including routine liver tests is recommended for patients treated with lonafarnib. 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... | Lonafarnib – Zokinvy® | Genetic Disease Agents, Small Molecule Enzyme Inhibitors | null |
Phenotypes_acutehepa.nxml | Acute Hepatitis | 2019-05-04 | null | null | null | null | null | null | null | null |
Umbralisib.nxml | Umbralisib | 2023-10-10 | Umbralisib is an oral kinase inhibitor that is was given accelerated approved for use in adults with relapsed or refractory marginal zone and follicular lymphoma in 2021, but the approval was withdrawn a year later because of data from a trial showing excess mortality with its use. Umbralisib was associated with a mode... | Umbralisib (um" bra lis' ib) is an orally available, small molecule inhibitor of multiple kinases that play a role in B cell malignant cellular pathways and that was used in the therapy of refractory cases of marginal zone and follicular lymphoma. The kinases inhibited by umbralisib include phosphatidylinositol 3-kinas... | In clinical trials of umbralisib in adults with lymphoma, the rates of serum enzyme elevations during therapy ranged from 15% to 35% and were above 5 times the ULN in 5% to 8% and occasionally above 20 times ULN (<1%). The aminotransferase elevations arose within 4 to 12 weeks of starting therapy in most instances and ... | The reason why umbralisib causes serum enzyme elevations is not known, but may be a direct toxicity to hepatocytes caused by inhibition of PI3K activity or the result of change in B cell activity and caused by induction of autoimmunity. Umbralisib is metabolized primarily by aldehyde oxidase which is present in many ti... | Serum enzyme elevations were not uncommon during chemotherapy with umbralisib and were often dose limiting. The product label recommended that umbralisib not be used with other agents with hepatotoxic potential. Furthermore, regular monitoring of liver tests every 2 to 4 weeks was recommended during the first six month... | Umbralisib – Ukoniq® [On June 1, 2022, FDA approval was withdrawn due to safety concerns.] | Antineoplastic Agents | null |
Troglitazone.nxml | Troglitazone | 2018-06-06 | Troglitazone was the first thiazolidinedione approved for use in the United States and was licensed for use in type 2 diabetes in 1997, but withdrawn 3 years later because of the frequency of liver injury including acute liver failure associated with its use. | Troglitazone (troe gli' ta zone) is an insulin sensitizing agent thought to act by engagement of PPAR-γ receptors which induce multiple genes involved in glucose and fatty acid metabolism. In clinical trials, troglitazone was found to lower blood glucose and HbA1c levels and had additive effects with the sulfonylureas ... | Large prospective studies showed that significant elevations in serum aminotransferase levels (equal to or greater than 3 times the upper limit of the normal range [ULN]) occurred in 1.9% of patients with diabetes treated with troglitazone for 24 to 48 weeks, compared to only 0.6% in placebo recipients. These enzyme el... | The mechanism of liver injury due to troglitazone is unknown. Signs and symptoms of allergic and immune reactivity are rare and a metabolic defect in its metabolism is suspected to be the cause. Troglitazone is a potent inducer of CYP 3A4 and has a distinctive alpha tocopherol (vitamin E-like) side chain which can be m... | The liver injury from troglitazone can be severe and even fatal. In several cases there was incomplete recovery at the time of the last follow up evaluation, suggesting that the injury can become chronic in some instances. Prednisone has been reported to have a beneficial effect, but only in anecdotal reports. While se... | Troglitazone – Rezulin® (Withdrawn from U.S. Market) | Hypoglycemic Agents | null |
Acarbose.nxml | Acarbose | 2021-01-10 | Acarbose is an alpha glucosidase inhibitor which decreases intestinal absorption of carbohydrates and is used as an adjunctive therapy in the management of type 2 diabetes. Acarbose has been linked to rare instances of clinically apparent acute liver injury. | Acarbose (ay' kar bose) is an inhibitor of intestinal alpha glucosidase, an enzyme responsible for digestion and absorption of starch, disaccharides and dextrin. Acarbose is a complex oligosaccharide produced in bacteria that has activity against glucoamylase, sucrase, maltase and isomaltase, intestinal brush border gl... | In several large clinical trials, serum enzyme elevations above 3 times the upper limit of normal were more common with acarbose therapy (2% to 5%) than with placebo, but all elevations were asymptomatic and resolved rapidly with stopping therapy. These studies reported no instances of clinically apparent liver injury.... | The cause of liver injury during acarbose therapy is not known. Acarbose is an oligosaccharide of microbial origin and is minimally absorbed (0.5% to 1.7%), so that systemic toxicity and liver injury were not expected and remain unexplained. Liver injury from acarbose is clearly idiosyncratic and may relate to an immun... | The liver injury caused by acarbose has generally been mild and self-limited with the injury resolving rapidly once acarbose is discontinued. Cross sensitivity with other hypoglycemic agents has not been described. Furthermore, liver injury has not been described in patients taking the other currently available alpha g... | Acarbose – Generic, Precose® | Antidiabetic Agents | null |
Phenobarbital.nxml | Phenobarbital | 2020-07-30 | Phenobarbital is a barbiturate that is widely used as a sedative and an antiseizure medication. Phenobarbital has been linked to rare instances of idiosyncratic liver injury that can be severe and even fatal. | Phenobarbital (fee" noe bar' bi tal) is a barbiturate and is believed to act as a nonselective depressant. Phenobarbital also has anticonvulsant activity and is thought to act by suppressing spread of seizure activity by enhancing the effect of gamma aminobutyric acid (GABA), raising the seizure threshold. Phenobarbita... | Prospective studies suggest that less than 1% of subjects develop elevations in serum aminotransferase levels during long term phenobarbital therapy. Clinically apparent hepatotoxicity from phenobarbital is rare but can be abrupt in onset, severe and even fatal. Phenobarbital hepatotoxicity typically occurs in the sett... | The mechanism of phenobarbital hepatotoxicity is thought to be hypersensitivity or an immunological response to a metabolically generated drug-protein complex. | Phenobarbital hepatotoxicity is usually rapidly reversible with improvements beginning within 5 to 7 days of stopping the drug and being complete within 1 to 2 months. In cases of severe injury, progression to acute liver failure and death can occur. Corticosteroids have been used but with uncertain effectiveness. Prol... | Phenobarbital – Generic, Luminal® Sodium | Anticonvulsants | null |
Quinupristin-Dalfopr.nxml | Quinupristin-Dalfopristin | 2018-05-21 | Quinupristin and dalfopristin are intravenously administered, streptogramin antibiotics used in fixed combination to treat severe bacterial infections due to susceptible organisms including methicillin resistant Staphylococcus aureus (MRSA). The fixed combination of quinupristin and dalfopristin is associated with a lo... | Quinupristin (kwin" ue pris' tin) and dalfopristin (dal” foe pris’ tin) are streptogramin antibiotics that were initially isolated from Streptomyces pristinaspiralis. Quinupristin, a derivative of pristamycin IA, and dalfopristin, a derivative of pristamycin IIA, are synergistic in activity and are used in a fixed dose... | Elevations in serum aminotransferase levels occur in a proportion of patients receiving quinupristin and dalfopristin, but rates 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 ... | The cause of the mild-to-moderate serum aminotransferase elevations that occur during quinupristin and dalfopristin therapy is unknown. Both are extensively metabolized in the liver, largely via the cytochrome P450 system (CYP 3A4) and the combination is susceptible to drug-drug interactions with agents that are substr... | null | Quinupristin-Dalfopristin – Synercid® | Antiinfective Agents | [
{
"cas_registry_number": "120138-50-3",
"molecular_formula": "C53-H67-N9-O10-S",
"name": "Quinupristin"
},
{
"cas_registry_number": "112362-50-2",
"molecular_formula": "C34-H50-N4-O9-S",
"name": "Dalfopristin"
}
] |
Brexanolone.nxml | Brexanolone | 2019-04-12 | Brexanolone is a unique, intravenously administered, neuroactive steroidal antidepressant used in the therapy of moderate-to-severe postpartum depression. In prelicensure clinical trials, brexanolone therapy was not associated with an increased rate of serum aminotransferase elevations, and it has not been linked to in... | Brexanolone (brex an' oh lone) is allopregnanolone an active metabolite of progesterone which is found in high concentrations during pregnancy and falls precipitously at the time of delivery, shortly before the usual time of onset of postpartum depression. When given intravenously in doses that achieve plasma levels ty... | In premarketing studies, liver test abnormalities were uncommon in patients receiving brexanolone (<1%) and no more frequent than in placebo recipients. No instances of acute, clinically apparent liver injury attributed to brexanolone have been reported. However, general clinical experience with brexanolone has been li... | The mechanism by which brexanolone might cause liver injury is not known. Brexanolone is metabolized largely via non-cytochrome P450 pathways, predominantly by keto-reduction, glucuronidation and sulfation. It has few significant drug-drug interactions. Concurrent use of other antidepressants may lead to excess sedatio... | null | Brexanolone – Zulresso® | Antidepressant Agents | null |
PKEnhancers.nxml | Pharmacokinetic Enhancers | 2017-08-17 | null | null | null | null | null | null | null | null |
Elvitegravir_Cobicis.nxml | Elvitegravir | 2018-01-30 | Elvitegravir is a human immunodeficiency virus (HIV) integrase inhibitor which is used largely in a four drug combination with cobicistat, emtricitabine and tenofovir as therapy of HIV infection. Therapy with this elvitegravir based regimen is often associated with transient serum aminotransferase elevations during the... | Elvitegravir (el" vi teg' ra vir) is a 4-quinolone-3-glyoxylic acid and antiretroviral agent that acts by inhibition of viral DNA strand transfer by the HIV integrase, a necessary step in HIV replication. Elvitegravir has been shown to lower serum levels of HIV RNA and to raise CD4 counts. In multiple prospective clini... | In premarketing clinical trials, serum ALT elevations greater than 5 times the upper limit of normal occurred in 15% of patients treated with elvitegravir combined with cobicistat, emtricitabine and tenofovir. This rate was somewhat lower than what occurred in comparator arms. Most serum enzyme elevations with elvitegr... | The possible mechanism of liver injury due to elvitegravir is unknown. Elvitegravir is extensively metabolized in the liver via the cytochrome P450 system (predominantly CYP 3A4), and production of a toxic or immunogenic intermediate may trigger liver injury. | null | Elvitegravir – Vitekta® | Antiviral Agents | [
{
"cas_registry_number": "697761-98-1",
"molecular_formula": "C23-H23-Cl-F-N-O5",
"name": "Elvitegravir"
},
{
"cas_registry_number": "1004316-88-4",
"molecular_formula": "C40-H53-N7-O5-S2",
"name": "Cobicistat"
}
] |
Eszopiclone.nxml | Eszopiclone | 2018-02-20 | Eszopiclone is a benzodiazepine receptor agonist that is used for the treatment of insomnia. Eszopiclone has not been implicated in causing serum enzyme elevations or clinically apparent liver injury. | Eszopiclone (es zoe' pi klone) is a non-benzodiazepine, benzodiazepine receptor agonist of the cyclopyrrolone class that acts by binding to the benzodiazepine (BZ) site on the GABA receptor complex, causing neural inhibition and helping to induce sleep. Eszopiclone has selectivity for certain BZ receptor subtypes, and ... | In multiple premarketing randomized controlled trials, eszopiclone was not associated with an increased rate of serum enzyme elevations in comparison to placebo therapy, and no instance of clinically apparent liver injury was reported. Since its approval and widescale use, eszopiclone has not been implicated in causing... | null | null | Eszopiclone – Generic, Lunesta® | Sedatives and Hypnotics | null |
Ponesimod.nxml | Ponesimod | 2021-07-15 | Ponesimod is an orally available immunomodulatory drug used to treat relapsing forms of multiple sclerosis. Ponesimod is associated with transient serum enzyme elevations during therapy but has not been linked to instances of clinically apparent liver injury with jaundice, although experience with its use has been limi... | Ponesimod (poe nes’ i mod) is an immunomodulatory agent used in the treatment of multiple sclerosis that is believed to act by modulating sphingosine-1-phosphate (S1P) receptors. Ponesimod is an analogue of sphingosine and related in structure to fingolimod, the first S1P receptor modulator approved for use in multiple... | In preregistration trials of ponesimod, serum ALT elevations were common (in up to 23% of recipients) but were typically mild and asymptomatic, returning to baseline values even with continuation of therapy or within a few months of stopping. In one prospective, carefully monitored trial, serum aminotransferase elevati... | The mechanism by which ponesimod might cause liver injury is not known. It is extensively metabolized by liver via multiple enzymes in the cytochrome P450 system, predominantly CYP 3A4, and drug-drug interactions with agents that induce or inhibit these enzymes are likely to occur. Serum enzyme elevations have been fre... | While chronic therapy with ponesimod can be associated with mild-to-moderate serum aminotransferase elevations, it has not been linked to any cases of clinically apparent liver injury. Because of the frequency of enzyme elevations detected during therapy, the product label for ponesimod recommends obtaining baseline li... | Ponesimod – Ponvory® | Multiple Sclerosis Agents | null |
Hydroxyzine.nxml | Hydroxyzine | 2017-01-16 | Hydroxyzine is a first generation antihistamine that is used largely for symptoms of itching, nausea, anxiety and tension. Hydroxyzine has not been linked to instances of clinically apparent acute liver injury. | Hydroxyzine (hye drox' i zeen) is a first generation antihistamine that is used mostly to treat itching and nausea. Because of its sedating effects, hydroxyzine is also used for anxiety, tension and as a mild sleeping aid. Hydroxyzine belongs to the piperazine class of antihistamines (with cyclizine and meclizine) whic... | Despite widespread use, hydroxyzine has not been linked to liver test abnormalities or to clinically apparent liver injury. Indeed, hydroxyzine is commonly used for the pruritus associated with liver disease. The reason for its safety may relate to low daily dose and limited duration of use.\n\nLikelihood score: E (unl... | null | null | Hydroxyzine – Generic, Atarax®, Vistaril® | Antihistamines | null |
Bacopa.nxml | Bacopa monnieri | 2024-04-24 | Bacopa is an herbal extract made from the leaves of Bacopa monnieri, a herbaceous plant native to the Indian subcontinent which has been used in Ayurvedic medicine for centuries to treat anxiety, insomnia, and epilepsy and to improve memory and cognitive function. Bacopa has not been linked to liver enzyme elevations d... | Bacopa is an herbal extract made from the fresh or dried leaves of Bacopa monnieri, a creeping, herbaceous plant native to the Indian subcontinent that has been used for centuries in Ayurvedic medicine to treat anxiety, depression, memory loss, and epilepsy. Currently it is widely used to boost memory and improve cogni... | Bacopa extract has not been linked to serum enzyme elevations during therapy, although there have been few prospective studies in humans that have reported on laboratory test results during treatment. Importantly, despite widespread use, bacopa has not been implicated in cases of clinically apparent liver disease.\n\nL... | null | null | Bacopa – Generic | Herbal and Dietary Supplements | null |
Causality.nxml | Causality | 2019-11-20 | null | null | null | null | null | null | null | null |
Riociguat.nxml | Riociguat | 2018-06-04 | Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension. Riociguat has not been linked to significant serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury. | Riociguat (rye" oh sig' ue at) is small molecular weight stimulator of soluble guanylate cyclase, an enzyme responsible for synthesis of cyclic guanine monophosphate (cyclic GMP), an important mediator of endothelial cell relaxation. By stimulating cyclic GMP, riociguat leads to relaxation of vascular smooth muscle cel... | In preregistration studies, riociguat was not associated with serum enzyme elevations or with episodes of clinically apparent liver injury. Since approval of riociguat, there have been no published reports of hepatotoxicity, and the product label does not mention liver injury as an adverse event.\n\nLikelihood score: E... | The mechanism by which riociguat might cause serum aminotransferase elevations or liver injury is not known. It is metabolized by the hepatic cytochrome P450 system (predomination 3A4 and is susceptible to drug-drug interactions. The absence of significant hepatotoxicity from riociguat may related to the relatively low... | The serum enzyme elevations associated with riociguat use have been rare, mild-to-moderate and self-limited in course, usually resolving despite drug continuation. Clinically apparent liver injury from riociguat has not been described. There is no information on cross sensitivity to hepatic injury among the various age... | Riociguat – Adempas® | Pulmonary Arterial Hypertension Agents | null |
Risankizumab.nxml | Risankizumab | 2021-06-09 | Risankizumab is a humanized monoclonal antibody to IL-23 which is used to treat moderate-to-severe plaque psoriasis. Risankizumab is generally well tolerated and is associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent liver injury. | Risankizumab (ris” an kiz’ ue mab) is a humanized monoclonal IgG1 antibody directed against the p19 subunit of IL-23, which results in inhibition of IL-23 signaling and decrease in synthesis of proinflammatory cytokines such as IL-17. Risankizumab has been evaluated as therapy of several immune and inflammatory conditi... | Mild-to-moderate serum aminotransferase elevations arise in up to 10% of patients treated with risankizumab, but the abnormalities are generally transient and asymptomatic, rarely necessitating drug discontinuation. In large, preregistration trials there were no instances clinically apparent liver injury or severe hepa... | The possible mechanisms of liver injury due to risankizumab are unclear. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids. There is no evidence to suggest that inhibition of IL23 signaling would trigger liver injury or autoimmune liver co... | null | Risankizumab – Skyrizi® | Psoriasis Agents | null |
Resveratrol.nxml | Resveratrol | 2024-11-30 | Resveratrol is a plant polyphenol found in high concentrations in red grapes that has been proposed as a treatment for hyperlipidemia and to prevent fatty liver, diabetes, atherosclerosis and aging. Resveratrol use has been associated with rare instances of serum enzyme elevations during therapy but has not been convin... | Resveratrol is a natural plant polyphenol (3,5,4’-trihydroxystilbene) that is found in highest concentrations in the skin of red grapes and other fruits (mulberries, blueberries, blackberries). In cell culture, resveratrol has antiinflammatory, cytoprotective, and antineoplastic properties which can be reproduced in se... | There have been multiple trials of resveratrol in human subjects, but the dose regimen and duration of therapy has varied greatly and many trials lacked information on adverse events, ALT elevations, and hepatotoxicity. Nevertheless, in most studies there was no mention of serum ALT elevations or only rare and mild-to-... | null | null | Resveratrol – Generic | Herbal and Dietary Supplements | null |
Omega3FattyAcids.nxml | Omega-3 Fatty Acids | 2017-04-08 | Omega-3 fatty acids are essential polyunsaturated fatty acids that have diverse functions in normal metabolism and health and are used as nutritional supplements for general health and for disease prevention and as prescription drugs for treatment of hypertriglyceridemia. The omega-3 fatty acids are generally safe and ... | The omega-3 fatty acids are essential fatty acids that serve several important functions in normal metabolism and health. Omega-3 refers to their common structural feature of an unsaturated double bond at the third carbon bond from the “omega” end of the long chain fatty acid (n-3). There are three essential omega-3 fa... | In the many, large, randomized controlled trials of the omega-3 fatty acids, side effects have been minimal. Use of omega-3 fatty acids even in high doses has not been linked convincingly to serum enzyme elevations or to instances of clinically apparent liver injury. At high doses used to treat hypertriglyceridemia, mi... | Omega-3 fatty acids are metabolized in the liver by beta-oxidation and broken down locally, usually into short chain fatty acids. They have little effect on hepatic cytochrome P450 or drug transporter activity. Their effects on triglyceride metabolism are more likely to be beneficial than harmful to hepatocytes. | null | Omega-3 Fatty Acids – Generic® | Herbal and Botanical Supplements | [
{
"cas_registry_number": "463-40-1",
"molecular_formula": "C18-H30-O2",
"name": "ALA"
},
{
"cas_registry_number": "1553-41-9",
"molecular_formula": "C20-H30-O2",
"name": "EPA"
},
{
"cas_registry_number": "25167-62-8",
"molecular_formula": "C22-H32-O2",
"name": "DHA"
}
] |
Eculizumab.nxml | Eculizumab | 2017-03-25 | Eculizumab is a humanized monoclonal antibody to complement factor 5 which acts to block complement activation and is used to treat paroxysmal nocturnal hemoglobinuria and hemolytic uremic syndrome. Eculizumab has been linked to several instances of serum enzyme elevations after repeated infusions and to rare instances... | Eculizumab (e" kue liz' ue mab) is a recombinant, humanized IgG monoclonal antibody to complement factor 5, which inhibits its enzymatic cleavage and activation. Activated complement is an important mediator of immune damage including hemolysis of red blood cells and plays an essential role in the hemolysis and tissue ... | In clinical trials of eculizumab in patients with PNH and atypical HUS, serum enzyme levels were rarely mentioned and laboratory test results were described as being stable or unremarkable. In preregistration studies of eculizumab there were no reports of clinically apparent liver injury with jaundice. Indeed, in many ... | The mechanism by which eculizumab might cause liver injury is unknown. Eculizumab is a monoclonal antibody and, like other proteins, is metabolized into amino acids and is unlikely to have intrinsic toxicity. Because it blocks the activation of complement, it might predispose to conditions that depend on complement act... | Eculizumab therapy has been linked to rare instances of mild, transient serum enzyme elevations during therapy, typically arising 1 to 3 weeks after an initial or early infusion of the monoclonal antibody. Instances of jaundice and symptoms from liver injury with eculizumab therapy are rare and not well described, but ... | Eculizumab – Soliris® | Hematologic Agents | null |
Lanreotide.nxml | Lanreotide | 2017-04-11 | Lanreotide is a synthetic polypeptide analogue of somatostatin that resembles the native hormone in its ability to suppress levels and activity of growth hormone, insulin, glucagon and many other gastrointestinal peptides. Because its half-life is longer than somatostatin, lanreotide can be used clinically to treat neu... | Lanreotide (lan ree' oh tide) is a synthetic octapeptide and analogue of somatostatin that is used for its ability to suppress levels and activities of hormones (growth hormone, insulin, gastrin, secretin, glucagon) or active neuropeptides (serotonin, vasoactive intestinal polypeptide [VIP]). Natural somatostatin is pr... | In preregistration studies of lanreotide, serum enzyme levels did not change appreciably and there were no reports of clinically apparent acute liver injury. Pooled analyses reported that there were no overall changes in serum ALT, AST or alkaline phosphatase levels during therapy or instances of clinically meaningful ... | Lanreotide, like somatostatin, decreases cholecystokinin secretion, gall bladder contractility and bile secretion, perhaps accounting for the high rate of gall bladder sludge and stone formation with long term use. How lanreotide might cause acute liver injury independent of its effect on bile flow and gall bladder fun... | The liver injury due to the lanreotide is generally due to its effects on the gallbladder and bile flow. Patients with hepatobiliary complications of lanreotide therapy are likely to have recurrence with restarting and have similar response to other somatostatin analogues such as octreotide and pasireotide.\n\nDrug Cla... | Lanreotide – Somatuline Depot® | Hormonal Agents | [
{
"cas_registry_number": "108736-35-2",
"molecular_formula": "C54-H69-N11-O10-S2",
"name": "Lanreotide"
},
{
"cas_registry_number": "83150-76-9",
"molecular_formula": "C49-H66-N10-O10-S2",
"name": "Octreotide"
},
{
"cas_registry_number": "396091-73-9",
"molecular_formula": "C... |
Thiotepa.nxml | Thiotepa | 2020-09-12 | Thiotepa is an intravenously or locally applied alkylating agent which is currently used in the therapy of breast, ovarian and bladder cancer. Thiotepa therapy has been associated with low rates of serum enzyme elevations during therapy and rare instances of acute, clinically apparent injury. | Thiotepa (thye' oh tep' a) is an ethylenimine similar in structure and activity to altretamine and is believed to act as an alkylating agent. The alkylating agents act by causing modification and cross linking of DNA, thus inhibiting DNA, RNA and protein synthesis and causing programmed cell death (apoptosis) in rapidl... | Thiotepa is associated with an appreciable rate of serum enzyme elevations during therapy, but these are generally mild and self-limited, not requiring dose adjustment. Rare instances of clinically apparent acute liver injury attributed to thiotepa have been reported, particularly with high doses. In most instances, th... | The potential mechanism of hepatotoxicity from thiotepa is probably similar to that of other alkylating agents, a direct cytotoxic injury to rapidly dividing cells. High doses are likely to injure other cells such as sinusoidal endothelial cells and hepatocytes. The cause of the idiosyncratic liver injury associated wi... | Liver injury is not uncommon with high doses of thiotepa. The severity of injury in reported cases has generally been mild-to-moderate and self-limited in course, although fatalities attributed to hepatotoxicity have been reported. The sinusoidal obstruction syndrome associated with thiotepa and other alkylating agents... | Thiotepa – Generic, Thioplex® | Antineoplastic Agents, Alkylating Agents | null |
Betaine.nxml | Betaine | 2017-09-26 | Betaine is a modified amino acid consisting of glycine with three methyl groups that serves as a methyl donor in several metabolic pathways and is used to treat the rare genetic causes of homocystinuria. Betaine has had only limited clinical use, but has not been linked to instances of serum enzyme elevations during th... | Betaine (bee' ta een) is a naturally occurring modified amino acid that is used therapeutically to treat genetic homocystinuria. Homocystinuria can be caused by several inherited defects in sulfur amino acid metabolism, the most common of which are cystathionine β-synthase deficiency (CβS) and 5,10-methylenetetrahydrof... | In small, open label trials of betaine therapy for homocystinuria as well as in small controlled trials of betaine in other conditions (Alzheimer disease, nonalcoholic steatohepatitis), serum enzyme elevations and clinically apparent liver injury were not reported. Indeed, in some studies, betaine has been associated w... | Betaine is a naturally occurring modified form of glycine that aids in the transsulfuration pathways converting homocysteine to methionine. Administration of betaine even in high doses (6 to 20 grams daily) has not been linked to hepatotoxicity.\n\nDrug Class: Genetic Disorder Agents | null | Betaine – Cystadane® | Genetic Disorder Agents | [
{
"cas_registry_number": "107-43-7",
"molecular_formula": "C5-H11-N-O2",
"name": "Betaine"
},
{
"cas_registry_number": "56-40-6",
"molecular_formula": "C2-H5-N-O2",
"name": "Glycine"
}
] |
Nelarabine.nxml | Nelarabine | 2020-05-01 | Nelarabine is a purine analogue and antineoplastic agent used in the therapy of T cell lymphoblastic leukemia or lymphoma. Nelarabine is associated with a low rate of transient serum enzyme elevations during therapy and has been linked to rare instances of clinically apparent acute liver injury with jaundice. | Nelarabine (ne lar' a been) is a purine analogue that is used in the treatment of T cell leukemia or lymphoma. Nelarabine is arabinosyl derivative of deoxyguanosine (2-amino-9-beta-D-arabinofuranosyl-6-methoxy-9-H-guanine) that, after removal of the methoxy group by adenosine deaminase in serum, is taken up and convert... | In clinical trials, serum enzymes elevations occurred in a small proportion of patients treated with nelarabine when given as sole therapy for refractory or relapsed acute leukemia. These elevations are generally mild-to-moderate, transient and asymptomatic. Elevations of aminotransferase levels above 5 times the upper... | Hepatotoxicity from nelarabine is likely due to direct toxicity as is typical for other purine analogues. | The severity of the liver injury linked to nelarabine therapy is generally self-limited and mild and resolves with stopping therapy. There is little evidence of cross sensitivity to liver injury among the various antineoplastic or antiviral purine analogues.\n\nDrug Class: Antineoplastic Agents, Antimetabolites\n\nOthe... | Nelarabine – Generic, Arranon® | Antineoplastic Agents | null |
ErgotAlkaloids.nxml | Ergot Alkaloids | 2018-02-10 | Ergot alkaloids are widely used for therapy of acute migraine headaches and include ergotamine and dihydroergotamine, both of which act by causing vasoconstriction of the carotid artery beds. Ergot alkaloids have multiple side effects, but have little effect on the liver and have not been clearly linked to instances of... | Ergotamine (er got' a meen) and dihydroergotamine are ergot alkaloids that act as vasoconstrictors, probably by stimulating alpha adrenergic receptors particularly in the carotid artery bed. The ergotamines may also have serotoninergic effects which may also be beneficial in migraine. The ergotamines were first reporte... | Neither ergotamine nor dihydroergotamine have been implicated in causing liver enzyme elevations, but they are generally used in limited amounts for short and intermittent periods of time. Ergotamine abuse can lead to arterial or venous spastic episodes, and at least one case of portal and splenic vein thrombosis with ... | Ergotamine is extensively metabolized by the liver, but it is given in low doses, and intermediates of its metabolism, even if potentially toxic, are likely conjugated and excreted rapidly and without hepatic injury. The vasospastic actions of ergotamines can cause arterial and venous spasms and potentially thromboses ... | null | Dihydroergotamine – Generic, Migranal® | Migraine Headache Agents | [
{
"cas_registry_number": "511-12-6",
"molecular_formula": "C33-H37-N5-O5",
"name": "Dihydroergotamine"
},
{
"cas_registry_number": "113-15-5",
"molecular_formula": "C33-H35-N5-O5",
"name": "Ergotamine"
}
] |
Amlodipine.nxml | Amlodipine | 2016-03-01 | Amlodipine besylate is a second generation calcium channel blocker that is used in the therapy of hypertension and angina pectoris. Amlodipine has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury. | Amlodipine (am loe' di peen) belongs to the dihydropyridine class of calcium channel blockers and is used in the treatment of both hypertension and angina pectoris. Like other calcium channel blockers, amlodipine acts by blocking the influx of calcium ions into vascular smooth muscle and cardiac muscle cells during mem... | Chronic therapy with amlodipine is associated with a low rate of serum enzyme elevations at rates that are similar to matched control populations. The enzyme elevations are usually mild, transient and asymptomatic and may resolve even during continued therapy. Clinically apparent liver injury from amlodipine is rare an... | The mechanism of amlodipine hepatotoxicity is not known, but liver injury is probably due to production of a toxic intermediate in its metabolism. | The severity of liver injury from amlodipine ranges from mild and transient serum enzyme elevations to self-limited jaundice. Complete recovery is expected after stopping the drug and recovery is usually rapid (4 to 8 weeks). Cases with chronic or fulminant liver injury due to amlodipine have not been reported. Little ... | Amlodipine – Generic, Norvasc® | Cardiovascular Agents | null |
Golimumab.nxml | Golimumab | 2017-02-10 | Golimumab is a human monoclonal antibody to tumor necrosis factor (TNF) alpha that is used in the treatment of rheumatoid arthritis and ulcerative colitis. Golimumab has been linked to a low rate of serum enzyme elevations during therapy, but has not been linked to cases of idiosyncratic, clinically apparent liver inju... | Golimumab (goe lim’ ue mab) is a human monoclonal immunoglobulin antibody to tumor necrosis factor (TNF) alpha, a proinflammatory cytokine that plays a role in cell injury, inflammation and tissue damage in inflammatory, autoimmune diseases. Golimumab is one of several monoclonal antibody inhibitors of TNF and has been... | In prelicensure controlled trials, serum ALT elevations occurred in up to 8% of golimumab vs 1% to 3% of placebo treated subjects. The elevations were usually mild-to-moderate in severity, asymptomatic, not accompanied by jaundice and self-limited in course. ALT elevations above 5 times the upper limit of normal (ULN) ... | The mechanism of liver injury in reactivation of hepatitis B appears to be a brisk immunological response to newly expressed viral antigens. Injury generally arises after anti-TNF therapy has stopped or between courses of treatment. | Guidelines for management of patients who are to receive golimumab recommend routine screening for hepatitis B before starting treatment. Screening should include tests for HBsAg and anti-HBc (and perhaps also anti-HBs as this may help in management). Prophylaxis with a potent oral, antiviral agent effective against he... | Golimumab – Simponi® | Antirheumatic Agents | null |
AnthraxAntitoxins.nxml | Anthrax Antitoxins | 2017-03-27 | High titers of antibody to infectious bacteria and viruses can be used to both prevent and treat infectious diseases. In particular, antitoxins have been shown to be beneficial in several forms of severe acute infections such as diphtheria, rabies and anthrax. The recent use of active anthrax spores as a bioweapon, par... | Obiltoxaximab (oh" bil tox ax i mab) is a human-mouse chimeric monoclonal antibody to the Bacillus anthrax protective antigen that is the major immunogenic antigen produced by the bacterial infection. The binding of obiltoxaximab to the anthrax protective antigen blocks the binding of the bacterial toxin to host cells.... | In human volunteer studies, obiltoxaximab was associated with local infusion and general hypersensitivity reactions, but clinical laboratory results were said to be unchanged over time. There have been no reports of hepatotoxicity associated with administration of obiltoxaximab.\n\nLikelihood score: E (unlikely cause o... | Obiltoxaximab is a monoclonal antibody and is unlikely to be inherently hepatotoxic. Recombinant proteins are often metabolized in the cells on which they act but are also metabolized in the liver, largely to small peptides and amino acids which may be reused to synthesize proteins and are unlikely to be toxic or immun... | null | Obiltoxaximab – Anthim® | Antiinfective Agents | [
{
"cas_registry_number": "1351337-07-9",
"molecular_formula": "Monoclonal Antibody",
"name": "Obiltoxaximab"
},
{
"cas_registry_number": "565451-13-0",
"molecular_formula": "Monoclonal Antibody",
"name": "Raxibacumab"
}
] |
Crizanlizumab.nxml | Crizanlizumab | 2021-07-12 | Crizanlizumab is a humanized monoclonal antibody to P-selectin which is used to prevent painful crises in sickle cell disease. Crizanlizumab is generally well tolerated and has not been associated with serum aminotransferase elevations during therapy or with instances of clinically apparent liver injury. | Crizanlizumab (kriz an liz ue mab) is a humanized monoclonal IgG2 antibody directed against P-selectin, which is used to prevent painful, vaso-occlusive crises in patients with sickle cell disease. Sickle cell disease is caused by an inherited mutation in the β globin gene that creates hemoglobin S, which is prone to a... | Mild-to-moderate serum aminotransferase elevations arise a small percentage of treated patients, but are generally asymptomatic and transient and rarely necessitate discontinuation of crizanlizumab injections. In registration trials of crizanlizumab there were no reported instances clinically apparent liver injury or s... | Possible mechanisms of liver injury due to crizanlizumab are not known. Monoclonal antibodies and immunoglobulins are generally taken up and metabolized intracellularly to short peptides and amino acids. | Drug Class: Genetic Disorder Agents, Monoclonal Antibodies, Sickle Cell Disease Agents | Crizanlizumab – Adakveo® | Sickle Cell Disease Agents | null |
resource.nxml | DILI Information Resources | 2021-04-01 | null | null | null | null | null | null | null | null |
Delafloxacin.nxml | Delafloxacin | 2020-03-10 | Delafloxacin is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria as well as atypical pathogens. Delafloxacin has been linked to mild ALT elevations during therapy, but has yet to be linked to instances of idiosyncratic acute liver injury with symptoms and jaundice as have been d... | Delafloxacin (del" a 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, delafloxacin is active against a wide range of aerobic gram-positive and gram-negative organisms.... | Delafloxacin, like other fluoroquinolones, is associated with a low rate (3% to 4%) of serum enzyme elevations during therapy. These abnormalities are generally mild, asymptomatic and transient, resolving even with continuation of therapy. ALT elevations above 5 times the upper limit of normal occur in 1% or less of su... | The cause of hepatic injury from the fluoroquinolones is unknown but appears to be hypersensitivity. | Mild-to-moderate injury from fluoroquinolone induced hepatitis should be followed by full recovery within 4 to 8 weeks. Cases of acute liver failure with death or need for liver transplantation have been reported, nor have chronic cases with bile duct loss. Cross reactivity of the hepatic injury between different fluor... | Delafloxacin – Baxdela® | Antiinfective Agents | null |
Dostarlimab.nxml | Dostarlimab | 2022-06-08 | Dostarlimab is a human monoclonal antibody to the programmed cell death receptor 1 (PD-1) and a checkpoint inhibitor used in the immunotherapy of cancer. Dostarlimab therapy has many adverse effects and particularly immune related conditions including acute hepatitis, which can be serious and even life threatening. | Dostarlimab (dos tar’ li mab) is a human recombinant monoclonal IgG4 antibody to the programmed cell death receptor 1 (PD-1) and is a checkpoint inhibitor used in cancer immunotherapy. PD-1 is an important checkpoint protein that is expressed on activated T and B cells and macrophages. Binding of the monoclonal antibod... | Mild-to-moderate serum aminotransferase and alkaline phosphatase elevations are common (15% to 25%) during dostarlimab therapy, but are usually self-limited and resolve even with continuing cyclic therapy. Serum ALT elevations above 5 times the upper limit of normal (ULN) occur in 2% to 3% of patients. In addition, a p... | The liver injury due to dostarlimab is likely to be immunologically mediated, and many cases of checkpoint inhibitor-related hepatitis appear to respond to corticosteroid or other immunosuppressive agents allowing continuation or restarting of therapy. | Guidelines for management of patients receiving dostarlimab 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 i... | Dostarlimab – Jemperli® | Antineoplastic Agents | null |
Temazepam.nxml | Temazepam | 2023-06-22 | Temazepam is an orally available benzodiazepine used in the therapy of insomnia. As with most benzodiazepines, temazepam has not been associated with serum aminotransferase or alkaline phosphatase elevations during therapy, and clinically apparent liver injury from temazepam has not been reported and must be very rare,... | Temazepam (tem az' e pam) is a benzodiazepine that is used as a sleeping aid in the therapy of insomnia. The soporific activity of the benzodiazepines is mediated by their ability to enhance gamma-aminobutyric acid (GABA) mediated inhibition of synaptic transmission through binding to the GABA A receptor. Temazepam was... | Temazepam, like other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from temazepam is extremely rare, if it occurs at all. There have been no case reports of symptomatic, acute liver injury from temazepam. Isolated single cases of clinically apparent liver injury ... | Temazepam is metabolized by the liver to inactive metabolites. Liver injury from benzodiazepines is probably due to the toxic effects of a rarely produced intermediate metabolite. | The case reports of hepatic injury due to benzodiazepines were followed by prompt and complete recovery upon stopping the medication, without evidence of residual or chronic injury. No cases of acute liver failure or chronic liver injury due to temazepam have been described. There is no information about cross reactivi... | Temazepam – Generic, Restoril® | Sedatives and Hypnotics | null |
ImmuneFeatures.nxml | Immunological Features | 2019-05-04 | null | null | null | null | null | null | null | null |
Pergolide.nxml | Pergolide | 2017-07-20 | Pergolide is an oral dopamine receptor agonist used predominantly in the therapy of Parkinson disease. Pergolide therapy is associated with low rate of transient serum enzyme elevations during treatment and has been implicated in rare cases of acute liver injury. | Pergolide (per' goe lide) is an ergot derivative similar to bromocriptine which acts as a dopamine receptor agonist. Pergolide, unlike bromocriptine, has agonist activity on both D1 and D2 dopamine receptors and acts directly on the substantia nigra. Pergolide was approved for use in the United States in 1988 and has b... | Pergolide has been reported to cause serum aminotransferase elevations in a small proportion of patients, but these abnormalities are usually mild, asymptomatic and self-limiting even without dose adjustment. In addition, pergolide has been implicated in a small number of cases of clinically apparent, acute liver injur... | Pergolide is metabolized extensively by the liver and metabolic byproducts excreted rapidly in the urine. | Most instances of suspected hepatotoxicity of pergolide have been mild and self-limited. There have been no published reports of acute liver failure or chronic hepatitis due to pergolide. There is likely cross sensitivity to hypersensitivity reactions among the different ergot alkaloids, such as bromocriptine.\n\nDrug ... | Pergolide – Generic, Permax® | Antiparkinson Agents | null |
Panitumumab.nxml | Panitumumab | 2020-04-15 | Panitumumab is a human monoclonal antibody to the epidermal growth factor (EGF) receptor, which is used in the treatment of refractory metastatic colorectal cancer. Panitumumab has been linked to minor serum enzyme elevations during therapy, but has not been implicated in cases of clinically apparent liver injury. | Panitumumab (pan” i toom’ ue mab) is a human monoclonal IgG2 antibody to the epidermal growth factor receptor (EGFR, HER1), which is used to treat EGFR-expressing metastatic colorectal cancer. Panitumumab has been shown to induce objective responses in metastatic colorectal cancer and to improve progression free surviv... | The rates of serum aminotransferase elevations during panitumumab therapy have not been reported in any detail from clinical trials, but nor has the absence of such elevations. In the FDA review of panitumumab, ALT elevations above 5 times the upper limit of normal (ULN) were reported to be 6% and not greater than with... | The cause of the transient enzyme elevations during monoclonal antibody therapies is generally unknown, but may relate to direct effects of the antibody reactivity to cell surface markers that may be over-expressed on cancer cells, but are also present in lower density on normal epithelial cells.\n\nDrug Class: Antineo... | null | Panitumumab – Vectibix® | Antineoplastic Agents | null |
Mepenzolate.nxml | Mepenzolate | 2017-07-07 | Mepenzolate is an anticholinergic agent used to treat gastrointestinal conditions such as acid peptic disease and irritable bowel syndrome. Mepenzolate has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. | Mepenzolate (me pen' zoe late) is a synthetic quaternary ammonium anticholinergic agent which inhibits the muscarinic actions of acetylcholine on autonomic nerve endings, decreasing gastrointestinal secretions and intestinal motility. Mepenzolate has broad activity against muscarinic acetylcholine receptors, but its hi... | Like other anticholinergic agents, mepenzolate has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. The metabolism of mepenzolate is not well defined, but it is likely metabolized by the liver.\n\nReferences on the safety and potential hepatotoxicity of anticholinergics are gi... | null | null | Mepenzolate – Cantil® | Anticholinergic Agents | null |
Azacitidine.nxml | Azacitidine | 2023-07-27 | Azacitidine is a cytosine analogue and antineoplastic agent used in the therapy of myelodysplastic syndromes. Azacitidine is associated with a low rate of transient serum enzyme elevations during therapy and has not been convincingly implicated in cases of clinically apparent acute liver injury with jaundice. | Azacitidine (ay" za sye' ti deen: also spelled azacytidine) is a pyrimidine analogue (5-azacytidine) which is converted intracellularly to a triphosphate which becomes incorporated into RNA and DNA. While azacitidine has anticancer effects, it proved to have limited usefulness in solid tumors and lymphomas. In low dose... | In clinical trials, serum enzyme elevations occurred in up to 16% of patients on azacitidine therapy for cancer or myelodysplasia who had concurrent, underlying liver disease or liver metastases, but rarely in persons without a preexisting hepatic illness. In subsequent studies, liver adverse reactions attributed to az... | Hepatotoxicity from azacitidine appears to be rare and confined mostly to patients with underlying liver disease. For these reasons, the liver injury is likely due to direct toxicity. | The severity of the liver injury linked to azacitidine therapy is usually mild-to-moderate in severity occurring in patients with preexisting liver disease. Azacitidine has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. There is no information on cross sensitivity to... | Azacitidine (powder for solution) – Vidaza® | Antineoplastic Agents | null |
Phenotypes_chol.nxml | Cholestatic Hepatitis | 2019-05-04 | null | null | null | null | null | null | null | null |
Lorcaserin.nxml | Lorcaserin | 2020-06-05 | Lorcaserin is a selective serotonin agonist that was used as a weight loss agent. Lorcaserin was in clinical use for eight years when it was withdrawn because of concerns regarding an excess in cancer risk after long term use. In prelicensure studies and while in clinical use, lorcaserin was not found to be associated ... | Lorcaserin (lor ka' ser in) is a serotonin agonist that is relatively selective for the serotonin 2C (5-HT2C) receptor, that is located almost exclusively in the brain. Activation of this receptor activates pathways important in hunger and satiety, including those that induce proopiomelanocortin which decreases appetit... | In premarketing clinical trials, serum aminotransferase elevations were no more common among patients receiving lorcaserin than placebo. Clinically apparent liver injury due to lorcaserin has not been reported, but the numbers of patients treated has been limited.\n\nLikelihood score: E (unlikely cause of clinically ap... | null | No instances of acute liver failure or chronic liver injury have been linked to lorcaserin, but it has had limited general clinical use and now has been withdrawn because of an increased risk for cancer with long term use.\n\nDrug Class: Weight Loss Agents | Lorcaserin – Belviq® | Weight Loss Agents | null |
Dacarbazine.nxml | Dacarbazine | 2017-11-10 | Dacarbazine (also known as DTIC) is an intravenously administered alkylating agent used in the therapy of Hodgkin disease and malignant melanoma. Dacarbazine therapy has been associated with serum enzyme elevations during therapy and occasional cases of severe and distinctive acute hepatic failure, probably caused by a... | Dacarbazine (da kar' ba zeen) is a triazene analogue of 5-aminoimidazole-4-carboxamide, a precursor in purine biosynthesis. Its mechanism of action in cancer chemotherapy is unclear. Dacarbazine may act as a purine analogue and antimetabolite. In addition, it is extensively metabolized in the liver and produces interme... | Mild and transient elevations in serum aminotransferase levels are not uncommon during courses of systemic combination chemotherapy and the role of dacarbazine in these abnormalities is not clear. However, dose modification for serum enzyme elevations is rarely necessary. More importantly, dacarbazine is associated wit... | The mechanism of hepatotoxicity from dacarbazine is not known; however, clinical and pathologic features suggest direct injury to sinusoidal endothelial cells causing their death and extrusion into sinusoids with subsequent obstruction. The injury may be immunologically mediated as it usually occurs with the second or ... | The severity of sinusoidal obstruction syndrome varies considerably, but most published cases have been severe and rapidly fatal. Anecdotal reports suggest that corticosteroids may be beneficial, but many cases have demonstrated fatal hepatic injury by the time of recognition. Rechallenge should not be done. Defibrotid... | Dacarbazine – Generic, DTIC,® DTIC-Dome® | Antineoplastic Agents, Alkylating Agents | null |
Ipilimumab.nxml | Ipilimumab | 2022-06-23 | Ipilimumab is a human monoclonal antibody to the cytotoxic T lymphocyte antigen-4, which acts as an immune checkpoint inhibitor and is used in immunotherapy of several forms of advanced or metastatic cancer. Ipilimumab like other checkpoint inhibitors has major side effects and particularly immune related conditions, i... | Ipilimumab (ip” i lim’ ue mab) is a human recombinant monoclonal immunoglobulin G1 antibody to the cytotoxic T lymphocyte antigen-4 (CTLA-4), which has distinctive immunomodulatory activity and is used as a checkpoint inhibitor in cancer immunotherapy. The CTLA-4 antigen is an important checkpoint molecule that modulat... | Mild-to-moderate serum aminotransferase elevations are not uncommon (10% to 30%) during ipilimumab therapy, but are usually self-limited and resolve even with continuing cyclic therapy. Serum ALT elevations above 5 times the upper limit of normal (ULN) occur in 1% to 4% of patients and generally lead to temporary disco... | The mechanism of liver injury due to ipilimumab is likely to be immunologically mediated, and most cases appear to respond at least in part to corticosteroid or immunosuppressive therapy. Liver biopsies in cases of hepatocellular injury and bile duct epithelial cell biopsies in cholangiopathic injury demonstrate necros... | Guidelines for management of patients receiving ipilimumab recommend monitoring of liver tests and interrupting therapy for patients who develop serum aminotransferase elevations above 3 times the upper limit of normal (ULN) and discontinuing treatment for values above 5 times the ULN in patients without preexisting ab... | Ipilimumab – Yervoy® | Antineoplastic Agents | null |
Ethambutol.nxml | Ethambutol | 2020-12-24 | Ethambutol is a first line but adjunctive antituberculosis medication which is used only in combination with other agents such as isoniazid and rifampin. Ethambutol therapy has been associated with minor, transient and asymptomatic elevations in serum aminotransferase levels, and is a reported but rare cause of clinica... | Ethambutol (eth am' bue tol) is a semisynthetic antibiotic which is bacteriostatic against Mycobacterium tuberculosis. Ethambutol interferes with the incorporation of mycolic acid into the mycobacterial cell wall, thus inhibiting its cell wall synthesis. Ethambutol has a broader spectrum of activity against mycobacteri... | Because ethambutol is almost always used in combination with isoniazid, rifampin or other antituberculosis agents, the frequency of serum aminotransferase elevations attributable to ethambutol alone cannot be estimated with any confidence. The addition of ethambutol to isoniazid, rifampin or pyrazinamide does not appea... | The cause of liver injury due to ethambutol is not known, but is likely due to hypersensitivity. | Ethambutol is one of the few antituberculosis medications that is generally safe in the setting of liver disease. In the unlikely event of clinically apparent liver injury or allergic reaction to ethambutol, rechallenge, if necessary, should be done with caution. There does not appear to be cross sensitivity to liver i... | Ethambutol – Generic, Myambutol® | Antituberculosis Agents | null |
Abacavir.nxml | Abacavir | 2016-01-04 | Abacavir sulfate is a nucleoside analogue and reverse transcriptase inhibitor which is used in combination with other agents in the therapy of the human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Abacavir is a rare cause of clinically apparent drug induced liver injury. | Abacavir (a bak' a vir) (cyclopropylaminopurinylcyclopentene: ABC) is a structural analogue of guanosine and acts by competing with naturally occurring nucleosides for incorporation into the HIV DNA strand during viral replication, causing inhibition of the viral polymerase and chain termination. Abacavir is indicated ... | Elevations in serum aminotransferase levels above 5 times the upper limit of normal occur in up to 6% of patients on abacavir. These elevations are usually mild, transient and do not require dose adjustment. Clinically apparent hepatotoxicity is rare, but isolated cases [usually anicteric] have been published. The live... | The cause of the clinically apparent hepatotoxicity from abacavir is hypersensitivity in some cases and is typically associated with the HLA-B*57:01 haplotype. Abacavir binds to the antigen-binding cleft of the HLA-B*57:01 molecule and alters its peptide binding repertoire. Testing for this allele is available in the U... | Most cases of liver injury associated with abacavir have been mild and anicteric and resolved rapidly within 4 weeks of discontinuation. There have been no convincing published cases of acute liver failure or vanishing bile duct syndrome due to abacavir. Patients with hepatotoxicity due to abacavir can generally tolera... | Abacavir – Ziagen® | Antiviral Agents | null |
Osimertinib.nxml | Osimertinib | 2017-06-01 | Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC). Osimertinib is associated with a moderate rate of serum aminotransferase elevations during therapy and rare instances of clinically ap... | Osimertinib (oh" sim er' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against the epidermal growth factor receptor (EGFR) that is rearranged and mutated in selected cancers including approximately 5% of non-small cell lung cancer (NSCLC). The mutated, rearranged EGFR promotes unre... | Elevations in serum aminotransferase levels are uncommon during osimertinib therapy occurring in 4% to 5% of patients and rising above 5 times the upper limit of the normal range in only 1% or less. In preregistration trials, there was a single incidence of clinically apparent liver injury attributed to osimertinib the... | The mechanism by which osimertinib might cause liver injury is not known. Osimertinib is metabolized by the liver predominantly by CYP 3A4 and is susceptible to drug-drug interactions with agents that induce or inhibit FYP 3A4. | Serum enzyme elevations during osimertinib therapy are uncommon, but elevations above 5 times the upper limit of normal (if confirmed) should lead to temporary discontinuation, which should be permanent if laboratory values do not improve significantly or resolve within a few weeks or if symptoms or jaundice arises. Th... | Osimertinib – Tagrisso® | Antineoplastic Agents | null |
Neratinib.nxml | Neratinib | 2018-10-20 | Neratinib is an orally available tyrosine kinase receptor inhibitor that is used in the extended adjuvant therapy of early stage breast cancer. Neratinib is associated with a low rate of transient elevations in serum aminotransferase levels during therapy, but has not been convincingly linked to cases of clinically app... | Neratinib (ne ra' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against human epidermal growth factor receptor 2 (HER2 or ErbB2). These tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation. This mutation ... | Elevations in serum aminotransferase levels are not uncommon during neratinib therapy occurring in up to 10% of patients, but rising above 5 times the upper limit of the normal range in only 1% to 2%. In prelicensure studies, there were no instances of neratinib related clinically apparent liver injury and serum enzyme... | The abrupt and severe nature of the clinically apparent liver injury attributed to EGF receptor inhibitors suggests that it is immunologically mediated. On the other hand, the transient serum enzyme elevations that are not uncommon during therapy suggest a direct, intrinsic hepatotoxicity, perhaps caused by inhibition ... | Liver injury due to neratinib has largely been in the form of asymptomatic, transient serum enzyme elevations. Monitoring of liver tests during neratinib therapy is recommended before treatment, monthly for the first 3 months and every 3 months thereafter or as clinically indicated. Serum aminotransferase elevations ab... | Neratinib – Nerlynx® | Antineoplastic Agents | null |
Voriconazole.nxml | Voriconazole | 2017-05-17 | Voriconazole is a triazole antifungal agent used primarily in the treatment or prevention of aspergillosis and candidal infections. Voriconazole therapy is associated with transient, asymptomatic serum aminotransferase elevations and is a known cause of clinically apparent acute drug induced liver injury. | Voriconazole (vor" i kon' a zole) is a synthetic triazole and a derivative of fluconazole, which is believed to act through inhibition of the fungal 14α-ergosterol demethylase that is responsible for converting lanosterol to ergosterol, which blocks cell membrane synthesis. Voriconazole has a broad spectrum of activity... | Transient elevations in serum aminotransferase levels occur in 11% to 19% of patients on voriconazole. These elevations are usually asymptomatic and self-limited, but approximately 1% of patients require discontinuation of voriconazole because of ALT elevations. Clinically apparent hepatotoxicity is uncommon, but may b... | The cause of clinically apparent hepatotoxicity from voriconazole is unknown; however, it may have some correlation to the ability of voriconazole to alter human sterol synthesis. Because voriconazole is a substrate for several P450 enzymes (CYP 2C19, 2C9, 3A4), it has the potential to cause significant drug-drug inter... | The severity of the liver injury from voriconazole ranges from mild and transient enzyme elevations to symptomatic or severe hepatitis leading to liver transplantation or death. Cases of acute liver failure have been described due to voriconazole, but not chronic liver injury or vanishing bile duct syndrome. Most cases... | Voriconazole – Generic, Vfend® | Antifungal Agents | null |
Sulfonylureas.nxml | Sulfonylureas | 2018-03-16 | null | null | null | null | null | null | null | null |
Terbinafine.nxml | Terbinafine | 2018-01-01 | Terbinafine is an orally and topically active allylamine fungicidal agent which is used to treat superficial fungal infections of the skin and nails. Terbinafine has been clearly linked to rare instances of acute liver injury that can be severe and sometimes fatal. | Terbinafine (ter' bin a feen) is a synthetic allylamine derivative that has potent activity against many dermatophytes that affect skin and nails, including Epidermophyton floccosum, Trichophyton mentagrophytes and Trichophyton rubrum. The antifungal activity of terbinafine is believed to be due to the selective inhibi... | Drug induced liver injury due to terbinafine was identified shortly after its introduction into medical use. Oral therapy with terbinafine is associated with elevations in serum aminotransferases in less than 1% of patients and the elevations are generally asymptomatic and resolve without stopping therapy. The estimate... | The acute hepatotoxicity caused by terbinafine appears to be part of a hypersensitivity reaction, although the mechanism has not been defined. Genome-wide association studies identified polymorphisms within the HLA region of chromosome six to be linked to cholestatic cases of drug induced liver injury, and particularly... | Most cases of acute hepatic injury from terbinafine resolve within 3 to 6 months of stopping the medication. In some instances, however, the injury is severe and unremitting, leading to acute liver failure and either death or need for liver transplantation. A severe outcome is more likely if terbinafine is continued af... | Terbinafine – Generic, Lamisil® | Antifungal Agents | null |
Phenotypes_chron.nxml | Chronic Hepatitis | 2019-05-04 | null | null | null | null | null | null | null | null |
Cisplatin.nxml | Cisplatin | 2020-09-15 | Cisplatin is the prototype platinum coordination complex classified as an alkylating agent and used intravenously in the treatment of several forms of cancer. Cisplatin has been associated with a low rate of serum enzyme elevations and with rare cases of clinically apparent, acute liver injury. | Cisplatin (sis pla' tin) was the first chemotherapeutic agent of its subclass to be discovered. It is an inorganic, water soluble complex containing a central platinum atom surrounded by 2 chlorine atoms and ammonia moieties in the cis position in the horizontal plane. Cisplatin forms irreversible covalent links with D... | The platinum compounds generally are not considered to be hepatotoxic, but cisplatin has been associated with a low rate of serum enzyme elevations during therapy. These elevations are usually mild, self-limited and asymptomatic, rarely requiring dose modification. There have been only rare case reports of clinically a... | The cause of hepatotoxicity from cisplatin is not known. There have been extremely few cases of cisplatin induced hepatotoxicity described and generally, the platinum coordination complexes have not been considered to be hepatotoxic. Recently however, oxaliplatin when given in multiple courses has been linked to develo... | Liver injury from cisplatin is rare and when it does occur, the severity in published cases was generally mild and the outcome benign. There is likely to be cross sensitivity to liver toxicities of the various platinum coordination complexes and rechallenge should be avoided.\n\nDrug Class: Antineoplastic Agents, Alkyl... | Cisplatin – Generic, Platinol® | Antineoplastic Agents, Alkylating Agents | null |
Delavirdine.nxml | Delavirdine | 2017-12-27 | Delavirdine is a nonnucleoside reverse transcriptase inhibitor used in combination with other agents in the therapy of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Delavirdine is associated with a low rate of transient serum aminotransferase elevations during therapy a... | Delavirdine (del a' vir deen) is an antiretroviral agent that acts by noncompetitive binding to and inhibition of the HIV reverse transcriptase. Delavirdine is a nonnucleoside reverse transcriptase inhibitor and is similar to nevirapine, efavirenz, etravirine and rilpivirine in its mechanism of action, but shares minim... | Serum aminotransferase elevations occur in 25% or more of patients on delavirdine therapy, but rise above 5 times the upper limit of normal in 4% or less; this rate is higher in patients who have chronic hepatitis C coinfection. Clinically apparent hepatotoxicity due to delavirdine must be rare, as individual case repo... | Hepatotoxicity from delavirdine is rare, but is likely due to hypersensitivity. Delavirdine is a substrate for and an inhibitor of the cytochrome P450 enzyme, CYP 3A4 and can cause significant drug-drug interactions. | The severity of the liver injury due to delavirdine can range from mild and transient enzyme elevations to acute hepatitis with jaundice. Description of cases with acute liver failure leading to liver transplantation or death have not been reported in association with delavirdine. In immunoallergic forms of acute liver... | Delavirdine – Rescriptor® | Antiviral Agents | null |
Avanafil.nxml | Avanafil | 2017-08-02 | Avanafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction. Avanafil is a relatively new medication and has yet to be linked to instances of serum enzyme elevations or with clinically apparent acute liver injury. | Avanafil (a van' a fil) is a selective inhibitor of phosphodiesterase type 5 (PDE5) which 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 phosphodiesterase is found. Avanafil is ... | Avanafil has had limited general use, but in premarketing studies it was not associated with cases of clinically apparent liver injury and serum enzyme elevations were not reported. The related PDE5 inhibitors, sildenafil and tadalafil, have been linked to isolated, rare instances of acute liver injury and jaundice. Th... | While avanafil 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. Avanafil, like the other PDE5 inhibitors, is metabolized in the liver via the cytochrome P450 system (CYP 3A4). | There is no known cross sensitivity between avanafil and the other PDE5 inhibitors currently in use in the United States. However, switching to another PDE5 inhibitor after an episode of clinically apparent liver injury should be done with caution.\n\nReferences to the safety and potential hepatotoxicity of avanafil ar... | Avanafil – Stendra ® | PDE5 Inhibitors | null |
SGLT-2_Inhibitors.nxml | Sodium-Glucose Cotransporter-2 (SGLT2) Inhibitors | 2023-02-10 | The sodium-glucose cotransporter-2 (SGLT2) inhibitors are diabetic agents that act by inhibiting the reabsorption of glucose in the proximal renal tubule, resulting in loss of glucose in the urine and reduction in serum levels. SGLT2 is the major enzyme responsible for glucose reabsorption in the kidney and its inhibit... | Bexagliflozin (bex’ a gli floe' zin) is a specific SGLT2 inhibitor that in clinical trials was shown to result in a reduction in serum HbA1c levels and better glycemic control in type 2 diabetes, both as monotherapy (in patients who failed to achieve adequate control on diet and exercise) or in combination with insulin... | In multiple large randomized controlled trials, canagliflozin, dapagliflozin, empagliflozin and ertugliflozin were not associated with serum enzyme elevations during therapy. Indeed, in retrospective analyses, therapy with SGLT2 inhibitors was associated with improvements in ALT levels, probably as a result of concurre... | The relative lack of hepatotoxicity of the SGLT2 inhibitors may relate to their minimal hepatic metabolism which is largely via UDP-glucuronylsyltransferase (UGT-1A9 and 2B4 among others). | Liver injury from the SGLT2 inhibitors is rare, and they have not been associated with acute liver failure, vanishing bile duct syndrome or chronic hepatitis. The similarity of structure and function of the SGLT2 inhibitors suggests that there may be some degree of cross sensitivity to their adverse events.\n\nDrug Cla... | Bexagliflozin – Brenzavvy® | Antidiabetic Agents | [
{
"cas_registry_number": "1118567-05-7",
"molecular_formula": "C24-H29-Cl-O7",
"name": "Bexagliflozin"
},
{
"cas_registry_number": "928672-86-0",
"molecular_formula": "C24-H25-F-O5-S.1/2H2-O",
"name": "Canagliflozin"
},
{
"cas_registry_number": "461432-26-8",
"molecular_formu... |
Methyldopa.nxml | Methyldopa | 2020-01-10 | Methyldopa (alpha-methyldopa or α-methyldopa) is a centrally active sympatholytic agent that has been used for more than 50 years for the treatment of hypertension. Methyldopa has been clearly linked to instances of acute and chronic liver injury that can be severe and even fatal. | Methyldopa (meth" il doe' pa) is a centrally active sympatholytic agent that reduces sympathic drive to the heart and peripheral circulation, leading to decreased cardiac output and lowered peripheral arterial resistance. Introduced in 1960, methyldopa rapidly became a leading antihypertensive agent, but in the last tw... | Drug induced liver injury due to methyldopa was identified shortly after its introduction into medical use in the 1960’s. Chronic use of methyldopa is associated with mild and transient elevations in serum aminotransferase levels in 5% to 35% of patients, these elevations often resolving despite continuation of the med... | null | Both the acute and the chronic forms of liver injury from methyldopa can be severe, particularly if the medication is continued despite appearance of clinically significant injury. Recovery usually occurs within 6 to 8 weeks, but patients with chronic hepatitis can be left with inactive cirrhosis. Methyldopa ranks as o... | Methyldopa – Generic, Aldomet® (Currently discontinued) | Antihypertensive Agents | null |
Ixabepilone.nxml | Ixabepilone | 2017-01-05 | Ixabepilone is a semisynthetic epothilone analogue that acts to stabilize microtubules thereby preventing mitosis and causing growth arrest in cancer cells. Ixabepilone is approved for use in refractory cases of advanced breast cancer. Its use is associated with a low rate of serum enzyme elevation, but ixabepilone has... | Ixabepilone (ix" a bep' i lone) is semisynthetic analogue of epothilone B, epothilones being cytotoxic macrolides that cause cell growth arrest by binding to microtubules and preventing mitosis. Ixabepilone is similar in activity to taxanes, but differs structurally and is not affected by taxane resistance. Therapy wit... | In preregistration controlled trials, serum aminotransferase elevations and other liver test abnormalities were rarely mentioned. A high proportion of patients treated had mild-to-moderate serum enzyme elevations at the time of starting ixabepilone, probably because of hepatic metastases and the use of other antineopla... | The cause of the liver enzyme elevations that occur during enzalutamide therapy is unknown. Ixabepilone is extensively metabolized in the liver predominantly by CYP 3A4 and 2D6 and is a strong inducer of CYP 3A4 and a moderate inducer of 2D6. Ixabepilone is susceptible to drug-drug interactions with inhibitors, inducer... | The liver injury linked to ixabepilone therapy has been generally mild, consisting of transient and asymptomatic elevations in serum aminotransferase levels. Ixabepilone has not been linked to cases of acute liver failure, chronic hepatitis or vanishing bile duct syndrome. There is no information on cross sensitivity t... | Ixabepilone – Ixempra® | Antineoplastic Agents | null |
Hydroxyurea.nxml | Hydroxyurea | 2021-07-12 | Hydroxyurea is an antimetabolite that is used in the treatment of cancer and to stimulate fetal hemoglobin production in sickle cell disease. Hydroxyurea is associated with a low rate of transient serum enzyme and bilirubin elevations during therapy, and has been implicated in rare cases of clinically apparent acute li... | Hydroxyurea (hye drox” ee ure ee’ a) is a hydroxylated analogue of urea and an antimetabolite which inhibits the enzyme ribonucleotide reductase, which is necessary for DNA synthesis and cell cycle replication. Blocking the enzyme results in cell cycle arrest in the S phase, but does not interfere with RNA or protein s... | Serum aminotransferase and bilirubin elevations occur in a small proportion of patients on conventional doses of hydroxyurea and a greater proportion at higher doses. However, the serum enzyme elevations are rarely associated with symptoms and are generally self-limited and resolve rapidly, rarely requiring dose modifi... | The syndrome of fever and acute hepatitis arising within 1 to 3 weeks of starting hydroxyurea is probably due to hypersensitivity. The cause of acute liver failure attributed to hydroxyurea is unknown, but may be related to drug-drug interactions with other potentially hepatotoxic agents. Hydroxyurea is metabolized in ... | The severity of the liver injury linked to hydroxyurea therapy is usually mild and self-limited. It has not been linked to cases of chronic hepatitis or vanishing bile duct syndrome. There is no information to suggest that there is cross sensitivity to hepatic injury between hydroxyurea and other antimetabolites or ant... | Hydroxyurea – Generic, Hydrea® (for cancer), Droxia® (for sickle cell disease) | Antineoplastic Agents; Sickle Cell Disease Agents | null |
Inebilizumab.nxml | Inebilizumab | 2024-05-14 | Inebilizumab is a monoclonal antibody to CD19 that is used to treat adults with neuromyelitis optica spectrum disorder accompanied by an autoantibody to aquaporin-4. Inebilizumab therapy is associated with an increased risk of infections and possibly reactivation of hepatitis B and tuberculosis, but it has not been ass... | Inebilizumab (in eb” i liz’ ue mab) is a humanized, cytolytic monoclonal antibody to CD19 that is used to treat adults with neuromyelitis optica spectrum disorder (NMOSD), a severe neurologic disease marked by bilateral optic neuritis and transverse myelitis that is accompanied by a distinctive autoantibody to aquapori... | In registration controlled trials, serum ALT elevations occurred in 21% of inebilizumab vs 23% of placebo recipients and were above 3 times the upper limit of normal (ULN) in 5 of 161 (3.1%) on inebilizumab vs only 1 of 51 (2%) on placebo. One patient receiving inebilizumab developed acute cholangitis with ALT and AST ... | The causes of the mild liver test abnormalities during inebilizumab therapy are not clearly known but appear to be related to the underlying condition or comorbidities such as nonalcoholic fatty liver disease or gallstone disease. Inebilizumab can cause hypersensitivity reactions including urticaria and rash, and liver... | The product label for inebilizumab does not recommend monitoring of routine liver tests during therapy but does recommend screening for hepatitis B before starting therapy and obtaining advice from a hepatologist regarding prophylaxis. Nevertheless, de novo elevations of serum aminotransferase levels above 5 times the ... | Inebilizumab – Uplizna® | Neurological Disease Agents | null |
UsnicAcid.nxml | Usnic Acid | 2018-04-25 | Usnic acid is a furandione found uniquely in lichen that is used widely in cosmetics, deodorants, toothpaste and medicinal creams as well as some herbal products. Taken orally, usnic acid can be toxic and has been linked to instances of clinically apparent, acute liver injury. | Usnic acid is a dibenzo-furandione which is uniquely found in lichen (Usnea) species, which are distributed worldwide. In vitro usnic acid has antibacterial, antifungal and antiviral activities, and lichen extracts containing usnic acid have been used in folk medicine externally for wound healing and athlete’s foot and... | Several cases of clinically apparent acute liver injury have been attributed to commercial dietary supplements that contain usnic acid. “LipoKinetix” was one such supplement advertised as a weight loss and body building supplement. Each tablet contained sodium usniate (100 mg), norephedrine (25 mg), diiodothyronine (10... | The hepatotoxicity of usnic acid is probably caused by uncoupling of oxidative phosphorylation in the liver, which can produce hepatocyte lysis and apoptosis and induces acute liver injury in animal models. | Hepatotoxicity attributed usnic acid and products such as LipoKinetix is often clinically apparent, but is usually reversible with prompt discontinuation of the nutritional supplement. Usnic acid is a direct hepatotoxin and thus is unlikely to share cross sensitivity to liver injury with other agents.\n\nDrug Class: He... | Usnic Acid – Generic | Herbal and Dietary Supplements | null |
Olaratumab.nxml | Olaratumab | 2017-05-29 | Olaratumab is a human monoclonal antibody to the platelet-derived growth factor (PDGF) receptor alpha and an antineoplastic agent used in the therapy of advanced soft tissue sarcoma. Olaratumab has not been linked to serum enzyme elevations during therapy or to idiosyncratic acute liver injury. | Olaratumab (oh" lar at' ue mab) is a recombinant human monoclonal IgG1 antibody to the platelet-derived growth factor receptor alpha. Signaling through PDGF receptors promotes cell proliferation and angiogenesis. Inhibition of the PDGF signaling decreases formation of new blood vessels, which plays an important role in... | In preregistration clinical trials, serum aminotransferase elevations were no more frequent in patients receiving olaratumab and doxorubicin than in those receiving doxorubicin alone (17.5% vs 16.1%), and no patient developed elevations above 5 times ULN or required dose modification or discontinuation for liver test a... | The possible mechanism of liver injury caused by olaratumab is not known. It is a recombinant protein and unlikely to be inherently hepatoxic. Proteins are metabolized to small polypeptides and amino acids in many cells including hepatocytes and do not alter the activity of drug metabolizing enzymes or hepatic transpor... | null | Olaratumab – Lartruvo® | Antineoplastic Agents | null |
Bisoprolol.nxml | Bisoprolol | 2017-01-15 | Bisoprolol is a cardioselective beta-blocker used in the treatment of hypertension. Bisoprolol has not been linked to instances of clinically apparent drug induced liver injury. | Bisoprolol (bis" oh proe' lol) is considered a “selective” beta-adrenergic receptor blocker in that it has potent activity against beta-1 adrenergic receptors which are found in cardiac muscle, but has little or no activity against beta-2 adrenergic receptors found on bronchial and vascular smooth muscle. Bisoprolol wa... | Bisoprolol therapy has been associated with a low rate of mild-to-moderate elevations of serum aminotransferase levels which are usually asymptomatic and transient and resolve even with continuation of therapy. There have been no well documented cases of clinically apparent, acute liver injury attributable to bisoprolo... | The mechanism of drug induced liver injury from beta-blockers such as bisoprolol is not known. Bisoprolol is extensively metabolized by the liver and excreted as inactive metabolites. The few rare cases reported were likely idiosyncratic. | The severity of liver injury due to beta-blockers ranges from mild serum aminotransferase elevations to acute hepatitis with jaundice. In large case series of drug induced liver injury and acute liver failure due to medications, bisoprolol has not been listed as a potential cause. There is little information about cros... | Bisoprolol – Generic, Zebeta® | Beta-Adrenergic Receptor Antagonists | null |
Midostaurin.nxml | Midostaurin | 2019-04-10 | Midostaurin is an orally available small molecule inhibitor of FMS-like tyrosine kinase 3 (FLT3) which is used as an antineoplastic agent in the treatment of acute myeloid leukemia with FLT3 mutations. Midostaurin is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected to... | Midostaurin (mye" doe staw' rin) is a potent small molecule multi-kinase inhibitor with specific activity against FLT3 (FMS-like tyrosine kinase 3), a tyrosine kinase receptor that is mutated in to up one-third of patients with acute myeloid leukemia (AML). The mutated FLT3 activates an intracellular signaling cascade ... | Elevations in serum aminotransferase levels are common during midostaurin therapy occurring in up to 71% of patients with AML also receiving standard induction therapy and rising above 5 times the upper limit of the normal range in 20%. In patients with systemic mastocytosis receiving midostaurin monotherapy, ALT eleva... | The possible cause of the liver injury due to midostaurin is not known. Midostaurin is metabolized in the liver largely by the cytochrome P450 system (largely CYP 3A4) and is susceptible to drug-drug interactions with inhibitors or inducers of the microsomal enzyme system, and strong modulators of CYP 3A4 should be avo... | Midostaurin therapy has been associated with transient serum aminotransferase elevations during therapy but has not been linked to instances of acute liver injury with jaundice or symptoms. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) should lead to temporary discontinuation,... | Midostaurin – Rydapt® | Antineoplastic Agents | null |
ModafinilArmodafinil.nxml | Modafinil | 2021-08-18 | Modafinil and its R-enantiomer armodafinil are central nervous system stimulants used to improve wakefulness in patients with excessive sleepiness. Both modafinil and armodafinil are associated with a low rate of serum aminotransferase elevations during therapy, but they have not been implicated in cases of clinically ... | Modafinil (moe daf' i nil) is a non-amphetamine central nervous system (CNS) stimulant whose mechanism of action is not entirely clear. Modafinil is structurally unrelated to the amphetamines, and it does not appear to affect release of CNS norepinephrine or dopamine. Modafinil is a racemic mixture of S and R enantiome... | In clinical trials, modafinil and armodafinil were associated with a low rate of serum aminotransferase and alkaline phosphatase elevations (<1%). Furthermore, despite widescale use, there have not been reports of clinically apparent liver injury due to modafinil or armodafinil. Rare instances of hypersensitivity react... | The mechanism by which modafinil and armodafinil might cause liver injury is unknown. Modafinil and armodafinil are extensively metabolized in the liver largely by CYP 3A4 and 2C91 and are susceptible to drug-drug interactions with agents that are substrates for these microsomal enzymes.\n\nDrug Class: CNS Stimulants, ... | null | Armodafinil – Generic, Nuvigil® | Central Nervous System Stimulants | [
{
"cas_registry_number": "112111-43-0",
"molecular_formula": "C15-H15-N-O2-S",
"name": "Armodafinil"
},
{
"cas_registry_number": "68693-11-8",
"molecular_formula": "C15-H15-N-O2-S",
"name": "Modafinil"
}
] |
Ritlecitinib.nxml | Ritlecitinib | 2024-03-25 | Ritlecitinib is an orally available small molecule inhibitor of Janus kinase 3 (JAK3) that is used to treat severe alopecia areata. Ritlecitinib is associated with a low rate of transient and usually mild elevations in serum aminotransferase levels during therapy but has yet to be linked to cases of clinically apparent... | Ritlecitinib (rit" le sye' ti nib) is an orally available, specific inhibitor Janus-associated kinases (mainly irreversible inhibition of JAK3) that is used to treat moderate-to-severe alopecia areata. Alopecia areata is an autoimmune disorder that is characterized by hair loss resulting in patches and even complete ba... | In the prelicensure clinical trials in alopecia areata, serum aminotransferase elevations occurred in 1% to 3% of ritlecitinib treated subjects, but similar rates were found in placebo recipients. The elevations were typically mild and transient, and values above 5 times the upper limit of normal (ULN) occurred in less... | The cause of mild serum enzyme elevations during ritlecitinib therapy is not known. Ritlecitinib is metabolized in the liver largely via CYP 3A4 and coadministration with strong inducers of CYP 3A4 should be avoided. Ritlecitinib is also an inhibitor of CYP 3A and 1A2 and can result in increases in serum levels of subs... | Serum aminotransferase elevations are uncommon during ritlecitinib therapy, but routine monitoring of liver tests is recommended in the product label “according to routine patient management.” Aminotransferase elevations above 5 times the upper limit of normal (ULN) should lead to at least temporary interruption of the... | Ritlecitinib – Litfulo® | Dermatologic Agents | null |
Nitrofurantoin.nxml | Nitrofurantoin | 2020-05-01 | Nitrofurantoin is an oral antibiotic widely used either short term to treat acute urinary tract infections or long term as chronic prophylaxis against recurrent infections. Nitrofurantoin is one of the most common causes of drug induced liver disease and can cause either an acute or a chronic hepatitis-like syndrome th... | Structurally, nitrofurantoin (nye" troe fure an' toyn) is a nitrated 5-member furan ring with a side chain of hydantoin. Nitrofurantoin inhibits several bacterial enzyme systems and has broad antibacterial activity. Its precise mechanism of action is not known. Importantly, antibacterial resistance to nitrofurantoin is... | Nitrofurantoin is currently one of the most common causes of drug induced liver injury. Liver injury from nitrofurantoin can cause either an acute or chronic hepatitis-like syndrome. The acute form is typically associated with a 1 or 2 week course of treatment with nitrofurantoin and is rare (~0.3 cases per 100,000 pre... | The mechanism of nitrofurantoin hepatotoxicity is not well known. Its nitro-reductive metabolism produces injurious oxidative free radicals which can damage hepatocytes. Many cases demonstrate evidence an autoimmune etiology and some studies have shown a linkage with HLA-DR6 and DR2. | The severity of nitrofurantoin induced liver injury ranges from mildly symptomatic elevations in serum aminotransferase levels (Cases 1 and 2), hepatitis with jaundice (Case 3) to fulminant liver failure and death (Case 4). Complete recovery is expected after stopping the drug, but recovery may be slow (2 to 6 months).... | Nitrofurantoin – Generic (Various), Furadantin®, Macrodantin® | Antiinfective Agents, Urinary (Nitrofuran Derivative) | null |
Aztreonam.nxml | Aztreonam | 2017-08-02 | Aztreonam is a parenterally administered, synthetic monobactam antibiotic that is specifically active against aerobic gram-negative bacilli is resistant to many beta-lactamases. Aztreonam therapy is often accompanied by mild, asymptomatic elevations in serum aminotransferase levels, but it has not been reported to caus... | Aztreonam (az tree' oh nam) is a monocyclic beta-lactam compound (monobactam) that was originally isolated from Chromobacterium violaceum. It acts by binding to penicillin binding proteins inhibiting cell wall synthesis and decreasing bacterial growth. Aztreonam is active mostly against gram negative organisms and more... | Aztreonam has systemic toxicities that are similar to those of other beta lactam antibiotics, but it is unclear whether it can cause hepatic injury similar to that of the penicillins or cephalosporins. Asymptomatic serum aminotransferase elevations are common during high dose, intravenous aztreonam therapy (10% to 38%)... | null | In the majority of cases, aztreonam induced liver injury appears to be transient, mild and asymptomatic, being marked by serum enzyme elevations only. Full recovery is expected after stopping the medication.\n\nDrug Class: Antiinfective Agents | Aztreonam – Azactam® | Antiinfective Agents | null |
Lazertinib.nxml | Lazertinib | 2025-03-23 | Lazertinib is a small molecule inhibitor of the epidermal growth factor (EGF) receptor that is used in combination with amivantamab to treat adults with locally advanced or metastatic non-small cell lung cancer that harbors EGF receptor mutations. The combination of lazertinib and amivantamab is associated with transie... | Lazertinib (laz’ er tin ib) is an orally available, specific inhibitor of the epidermal growth factor (EGF) receptor that is used in combination with amivantamab in the therapy of advanced or metastatic non-small cell lung cancer (NSCLC) with EGF receptor mutations. EGF receptors are frequently mutated in lung cancer a... | In the prelicensure trial of the combination of lazertinib and amivantamab, liver test abnormalities were frequent, with elevations in ALT of 65%, AST 65%, and GGT 39% but without bilirubin elevations. The enzyme elevations were usually transient, mild-to-moderate in severity and not associated with symptoms or jaundic... | The causes of serum enzyme elevations or liver injury from lazertinib therapy are probably the result of direct toxicity of the multi-kinase receptor inhibition. Lazertinib is metabolized in the liver largely via the CYP 3A4 pathway, and liver injury might also be caused by production of a toxic or immunogenic intermed... | The product label for lazertinib recommends monitoring of liver tests before initiating therapy and frequently during treatment. Serum aminotransferase elevations above 5 times the upper limit of normal (if confirmed) or any elevations accompanied by jaundice or symptoms should lead to at least temporary cessation. The... | Lazertinib – Lazcluze® | Antineoplastic Agents | null |
Phenotypes_enzy.nxml | Enzyme Elevations Without Jaundice | 2019-05-04 | null | null | null | null | null | null | null | null |
Brivaracetam.nxml | Brivaracetam | 2017-10-02 | Brivaracetam is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Brivaracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and is suspected of causing rare cases o... | Brivaracetam (briv" a ra' se tam) is a pyrrolidine derivative related in structure to levetiracetam. Its mechanism of action is not known, but it, like levetiracetam, binds to the synaptic vesicle protein 2A (SV2A) in the brain and appears to act by preventing secondary spread of focal seizure activity and decreasing s... | Prospective studies reported that chronic brivaracetam therapy was not accompanied by significant elevations in serum aminotransferase levels and clinically apparent liver injury was not observed. Brivaracetam has had limited general use, but has not been linked to instances of clinically apparent liver injury. Levetir... | The mechanism by which brivaracetam might cause liver injury is unknown, but is likely to be hypersensitivity. Brivaracetam is metabolized by hydrolysis followed by hydroxylation that is mediated by the cytochrome P450 system, predominantly CYP 2C19. Inhibitors of CYP 2C19 (such as carbamazepine and phenytoin) may incr... | Minor serum enzyme elevations during brivaracetam therapy rarely require dose modification or discontinuation, but elevations above 5 times the ULN should lead to dose modification and search for other possible causes. Acute liver failure, chronic hepatitis and vanishing bile duct syndrome have not been reported with b... | Brivaracetam – Briviact® | Anticonvulsants | [
{
"cas_registry_number": "357336-20-0",
"molecular_formula": "C11-H20-N2-O2",
"name": "Brivaracetam"
},
{
"cas_registry_number": "102767-28-2",
"molecular_formula": "C8-H14-N2-O2",
"name": "Levetiracetam"
}
] |
Selexipag.nxml | Selexipag | 2016-11-10 | Selexipag is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH). Selexipag has been associated with a low rate of serum enzyme elevations during therapy, but has yet to be implicated in cases of clinically apparent acute li... | Selexipag (se lex' i pag) is a selective prostacyclin receptor agonist that is used to treat pulmonary arterial hypertension (PAH). Inhibition of the prostaglandin receptors disrupts the intracellular pathways that lead to vasoconstriction, thus causing vasodilation. Because these receptors are found in highest concent... | Selexipag is associated with a low rate of serum aminotransferase elevations (0% to 3%) that in clinical trials was similar to the rate among placebo recipients. These elevations were usually mild (rarely above 3 times ULN), transient and not associated with symptoms. There were no cases of serum enzyme elevations with... | The mechanism by which selexipag might cause liver injury is not known. Selexipag is metabolized by the cytochrome P450 system (CYP 2C9 and 3A4), which may lead to production of a toxic intermediate and can also cause drug-drug interactions, particularly with cyclosporine A. One reason for its lack of hepatotoxicity ma... | The serum enzyme elevations associated with selexipag use have been mild-to-moderate and self-limited in course, often resolving despite drug continuation. There is no reason to believe that there is cross sensitivity to liver injury among the various therapies for PAH.\n\nDrug Class: Pulmonary Arterial Hypertension Ag... | Selexipag – Uptravi® | Pulmonary Arterial Hypertension Agents | null |
EndothelinRcptAntag.nxml | Endothelin Receptor Antagonists | 2017-09-30 | null | null | null | null | null | null | null | null |
Cimetidine.nxml | Cimetidine | 2018-01-25 | Cimetidine is a histamine type 2 receptor antagonist (H2 blocker) which is widely used for treatment of acid-peptic disease and heartburn. Cimetidine has been linked to rare instances of clinically apparent acute liver injury. | Cimetidine (sye met' i deen) was the first 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 cimetidine 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 were usually asymptomatic and transient and usually resolved even without dose modification. Several instances of ... | Cimetidine is metabolized by and inhibits the function of the microsomal P450 drug metabolizing enzymes, 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 cimetidine is usually rapidly reversible with stopping the medication (Case 1). Cimetidine has not been definitively linked to cases of acute liver failure, but there has been at least one case of prolonged cholestasis with probable vanishing bile duct syndrome after an episode of cholestat... | Cimetidine – Generic, Tagamet® | Antiulcer Agents | null |
Anifrolumab.nxml | Anifrolumab | 2023-09-20 | Anifrolumab is a human monoclonal antibody to the type 1 interferon receptor which is used in the therapy of moderate-to-severe systemic lupus erythematous. Anifrolumab has been linked to a low incidence of transient serum enzyme elevations during therapy and has not been linked to instances of clinically apparent live... | Anifrolumab (an” i frol’ ue mab) is a human monoclonal IgG1 antibody to the type 1 interferon (IFN) receptor subunit 1 which is used to treat adults with moderate-to-severe systemic lupus erythematosus (SLE). Anifrolumab binds to type 1 interferon receptors blocking their activation and induction of interferon related ... | In preregistration controlled trials, elevations in serum aminotransferase levels were uncommon (less than 1%) and no more frequent during anifrolumab than with placebo therapy. Elevations in aminotransferase levels above 5 times the ULN were less common on anifrolumab than placebo therapy, and there were no reports of... | There is little evidence that anifrolumab is a cause of liver injury, and mechanisms by which it occurs is not clear but might result from immune modulation. | The serum aminotransferase elevations that have been reported during anifrolumab therapy were generally transient, mild and asymptomatic and did not require dose modification or delay in therapy. Elevations above 5 times the upper limit of normal should lead to more careful monitoring and suspension of further infusion... | Anifrolumab – Saphnelo® | Immunosuppressive Agents | null |
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