Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance
This review article (2017) investigates the metabolism of psilocybin and psilocin (to which it metabolizes via dephosphorylation).
Authors
- Dinis-Oliveira, R. J.
Published
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 the 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.
Research Summary of 'Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance'
Introduction
Hallucinogens produce dose-dependent alterations in perception, thought and mood without markedly depressing or stimulating psychomotor function; sensory distortions such as synesthesia are common but frank hallucinations are not always present. Psilocybin and its dephosphorylated form psilocin are tryptamine-based indole alkaloids present in many Psilocybe and related mushroom genera; both act primarily at serotonin (5-HT) receptors, notably 5-HT2A, and have low abuse potential compared with other classes of psychoactives. While historically used recreationally, renewed clinical interest has arisen because of preliminary therapeutic signals for anxiety, depression and certain addictions, alongside continuing forensic concerns about acute toxic effects and variable individual responses. Dinis-Oliveira set out to review the metabolic fate of psilocybin and psilocin, with particular attention to major and minor metabolites that are relevant for clinical pharmacology and forensic toxicology. The review aims to collate human and non-human metabolic data, indicate enzymatic pathways and principal urinary metabolites, and discuss implications for detection, pharmacodynamics and potential drug interactions.
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Dinis-Oliveira, R. J. (2017). Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance. Drug Metabolism Reviews, 49(1), 84-91. https://doi.org/10.1080/03602532.2016.1278228
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