Is sertraline metabolized in the liver?
Yes, sertraline is metabolized in the liver. Multiple cytochrome P450 (CYP) isoforms are involved in the metabolism of sertraline, including CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 . These enzymes catalyze various metabolic pathways of sertraline, such as N-demethylation and deamination. CYP2C19 plays a significant role in the high-affinity N-demethylation of sertraline, while CYP2C9 contributes to the low-affinity component of this pathway . Additionally, CYP2B6 is identified as the major contributor to sertraline N-demethylation, with lesser contributions from other CYP isoforms like CYP2C19, CYP2C9, CYP3A4, and CYP2D6 . The involvement of multiple enzymes suggests that no single agent or genetic polymorphism of a drug-metabolizing enzyme can substantially alter the pharmacokinetics of sertraline .
Answers from top 5 papers
Papers (5) | Insight |
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Open access•Journal Article | Yes, Sertraline is metabolized in the liver. The paper discusses a case of hepatotoxicity induced by Sertraline, highlighting the importance of monitoring liver function in patients taking this medication. |
Yes, sertraline is metabolized in the liver. The enzymes CYP2C19 and CYP2C9 are involved in the N-demethylation of sertraline in human liver microsomes. | |
27 Citations | Yes, sertraline can cause hepatotoxicity, indicating it is metabolized in the liver. However, the exact mechanism of sertraline-induced hepatotoxicity is still debated in the literature. |
Open access•Journal Article 112 Citations | Yes, sertraline is metabolized in the liver through N-demethylation by multiple isoforms of human cytochrome P-450 enzymes, including CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. |
Yes, sertraline is metabolized in the liver by multiple enzymes, including cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases, as identified in an in vitro study on human liver microsomes. |