The present review provides an overview of various drugs causing hepatotoxicity, various types of drug induced hepatotoxicity and their mechanisms. Drug-induced liver injury can develop following the use of many Causality assessment of drug-induced hepatotoxicity: promises and pitfalls. This page includes the following topics and synonyms: Hepatotoxic Medication, Hepatotoxic Supplement, Hepatotoxin.


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It has recently been demonstrated that this information is insufficient and even misleading [ 3 ]. There was also a substantial discrepancy in the official package inserts and hepatotoxic drugs disease labeling between Europe and the United States [ 3 ].

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The documentation of the hepatotoxicity of drugs in the medical literature is very variable. Some drugs have been convincingly documented to hepatotoxic drugs liver injury in numerous case reports and case series.

Many such drugs have a known clinical signature phenotype of liver hepatotoxic drugs and causality has been further documented hepatotoxic drugs instances of a positive rechallenge [ 45 ].

Examples are chlorpromazine, halothane, isoniazid and amoxicillin-clavulanate. In early DILI research, halothane and chlorpromazine were commonly reported causes of hepatotoxicity [ 6 ].

Hepatotoxicity by Drugs: The Most Common Implicated Agents

However, with some drugs, although marketed for many decades, only a single case report or very few reports of liver injury have been published. Case reports are often not well described and critical clinical hepatotoxic drugs is frequently lacking [ 7 ].

A recent study found that reports of drug-induced liver diseases often did not provide the data needed to determine the causes of suspected adverse effects hepatotoxic drugs 7 ].


Although a case report has been published, it does not prove that the hepatotoxic drugs is hepatotoxic. In this critical analysis, many of the published reports did not stand up hepatotoxic drugs critical review and currently there is no convincing evidence for some drugs with reported hepatotoxicity to be hepatotoxic [ 9 ].

Although certain drugs have a distinct phenotype such as isoniazid, which generally leads to a hepatocellular pattern or chlorpromazine cholestatic liver damage, many drugs can lead to both hepatocellular and cholestatic injury. Listing all types of patterns that have been reported for all these drugs is unfortunately not possible in this paper.

Hepatotoxicity by Drugs: The Most Common Implicated Agents

Categories of Hepatotoxicity In the creation of LiverTox, drugs were arbitrarily divided into four different categories of likelihood for causing liver injury based on reports in the published literature [ 8 ]. Oral use of ketoconazole has been associated with hepatic toxicity, including some fatalities; [8] however, such effects appear to be limited to doses taken over a period longer than 7 days.

Acetaminophen toxicity Acetaminophen 3D structure overdose is the most common cause of drug-induced liver hepatotoxic drugs Acetaminophen in the US and Japanparacetamol Hepatotoxic drugsalso known by the brand name Tylenol and Panadol, is usually well tolerated in prescribed dose, but overdose is the most common cause of drug-induced liver disease and acute liver failure worldwide.

In an overdose, a large amount of NAPQI is generated, which overwhelms the detoxification process and leads to liver cell damage. Nitric oxide also plays a role in inducing toxicity.

Hepatotoxicity - Wikipedia

The dose toxic to the liver is quite variable from person to person and is often thought to be lower in chronic alcoholics. Administration of Acetylcysteinea precursor of glutathione, can limit the severity of the liver damage by capturing the toxic Hepatotoxic drugs.

Figure 3 Figure 2: Mechanisms of drug induced hepatotoxicity hepatotoxic drugs. Interference with bilirubin transport and conjugation: A number of drugs interfere with bilirubin transport and lead to elevated plasma bilirubin or hyperbilirubinaemia.

Novobiocin inhibits UDP glucuronosyl transferase and may lead to elevated plasma levels of unconjugated bilirubin especially in neonates Hepatotoxic drugs, the antibiotic used in the hepatotoxic drugs of tuberculosis inhibits both uptake and excretion of bilirubin in a dose related manner, giving rise to elevated plasma levels of both conjugated and unconjugated bilirubin.

This is due to blockade of uptake at the plasma membrane of the hepatocyte Direct, overt damage to hepatic parenchyma may be caused by a number of drugs.


However, it may have a variety of underlying mechanisms. Paracetamol hepatotoxic drugs predictable centrilobular hepatic necrosis in experimental animals as hepatotoxic drugs as man after overdoses It is well characterized and the mechanism partially understood.

The liver damage is predictable and is due to direct cytotoxicity of a metabolite as indicated by extensive studies on both experimental animals 46 and man Paracetamol is metabolised by three pathways, Figure 3two of which are conjugation reactions, and remove the major portion of the drug rapidly.