Indolealkylamines: Biotransformations and Potential Drug–Drug Interactions
The AAPS Journal May 3, 2008 Ai‐ming Yu 60 citations
Indolealkylamine (IAA) drugs, which are serotonin analogs, include both clinically used antimigraine triptans and substances of abuse. Understanding their metabolism and pharmacokinetics helps prevent unwanted drug-drug interactions (DDIs). For abused IAAs like lysergic acid amides, tryptamine derivatives, and beta-carbolines, a stable metabolite can serve as a biomarker for intoxication. Recent studies show that polymorphic cytochrome P450 2D6 (CYP2D6) plays an important role in IAA metabolism, meaning variations in CYP2D6 status can alter metabolism, pharmacokinetics, and toxicity, potentially increasing risk. DDIs with IAAs can also occur at both pharmacokinetic and dynamic levels, possibly leading to severe serotonin toxicity. This review describes the metabolism and potential DDIs of these therapeutic and abused IAA drugs.