Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance
Drug Metabolism Reviews – January 02, 2017
Source: OpenAlex
Summary
Psilocybin, a potent hallucinogen, is gaining therapeutic interest despite being a controlled substance. Its pharmacology involves conversion from a pro-drug to active psilocin through a crucial chemical transformation. This metabolism shows significant individual variability, impacting dose-response in Psychedelics and Drug Studies. Understanding these alkaloids is vital for precise clinical application. For Forensic Toxicology and Drug Analysis, identifying metabolites like psilocin-O-glucuronide is key. The chemistry of these compounds underscores their complex physiological effects, highlighting the need for careful consideration in therapeutic settings.
Abstract
Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic relevance but considerable physiological variability between individuals that can influence dose-response and toxicological profile has been reported. This review aims to discuss metabolism of psilocybin and psilocin, by presenting all major and minor psychoactive metabolites. Psilocybin is primarily a pro-drug that is dephosphorylated by alkaline phosphatase to active metabolite psilocin. This last is then further metabolized, psilocin-O-glucuronide being the main urinary metabolite with clinical and forensic relevance in diagnosis.