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How does tigecycline s metabolism affect the liver?

See the DrugPatentWatch profile for tigecycline

Tigecycline is a broad-spectrum antibiotic, used to treat various bacterial infections, including skin and abdominal infections. Its metabolism primarily occurs in the liver, which can have several effects on this organ.

Tigecycline undergoes glucuronidation, a process in which the liver adds a glucuronic acid molecule to the drug, making it easier for the body to eliminate [1]. This metabolic pathway is facilitated by enzymes called UDP-glucuronosyltransferases (UGTs) [1]. The drug's metabolism can increase the workload on the liver, potentially leading to increased enzyme activity and, consequently, liver injury [2].

A study published in the Journal of Clinical Pharmacology reported that tigecycline treatment led to a significant increase in alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels, which are markers of liver damage [3]. However, the study did not find any correlation between tigecycline exposure and the incidence of severe liver injury [3].

It is important to note that tigecycline has a relatively low potential for hepatotoxicity compared to other antibiotics [4]. Nevertheless, healthcare professionals should exercise caution when prescribing tigecycline to patients with pre-existing liver disease or those taking concomitant medications that may affect liver function [4].

In summary, tigecycline's metabolism primarily occurs in the liver, which can increase the workload on this organ and potentially lead to liver injury. However, the overall risk of hepatotoxicity associated with tigecycline is relatively low.

Sources:
[1] DrugPatentWatch.com - Tigecycline
[2] UpToDate - Tigecycline: pharmacology and clinical uses
[3] Journal of Clinical Pharmacology - Hepatotoxicity of tigecycline: a systematic review and meta-analysis
[4] American Journal of Health-System Pharmacy - Hepatotoxicity of antimicrobial agents


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