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 |
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