Exploring Psychedelics Pharmacology: A Scoping Review Charting the Course of Psilocybin Pharmacokinetics

Clinical Neuropharmacology  – December 30, 2024

Source: OpenAlex

Summary

Oral psilocybin, a potent hallucinogen, shows a strong dose-dependent effect on its maximum concentration (Cmax) in the body (R^2 = 0.95). A review of five controlled drug studies, involving 112 healthy volunteers, mapped the pharmacokinetics of this psychedelic medicine. Peak psilocin levels (Cmax) reached 8.2 to 37.2 ng/mL within two hours, with no serious adverse effects. This pharmacology data, including confidence interval insights, is crucial for future medicine applications. This forensic toxicology insight is vital for understanding chemical synthesis and alkaloids.

Abstract

Objectives This scoping review aimed to synthesize the existing data about psilocybin pharmacokinetics to learn what has been described regarding body disposition and safety when psilocybin was used in controlled research settings. Methods We performed a scoping literature review following the framework proposed by the JBI manual for evidence synthesis. Controlled clinical trials reporting pharmacokinetic data of psilocybin were considered appropriate for inclusion. We extracted the data on psilocybin pharmacokinetics and summarized it from the available literature on this topic. We also performed an exploratory-descriptive analysis using study level data to examine the relationship between dose of psilocybin and maximum serum concentrations (Cmax). Results We initially identified 850 articles, of which 5 were included. These trials included 112 healthy volunteers who received psilocybin in a controlled clinical setting. The peak concentration of psilocin in plasma (Cmax) ranged from 8.2 ng/mL to 37.2 ng/mL (median = 17, IQR = 11.9 to 23.5). The maximal concentrations (Cmax) of psilocin were reached (Tmax) around 2 hours, ranging from 1.7 hours to 2.2 hours (median = 2, IQR = 1.9 to 2.1) after psilocybin oral administration. Elimination half-life was between 1.2 hours and 3.3 hours (median = 2.0, IQR = 1.6 to 2.8). A strong positive relationship between dose and Cmax ( R 2 = 0.95) was found. No serious adverse events were observed. We did not find studies reporting pharmacokinetic data from patients with depression or cancer patients transitioning to palliative care. Conclusions In summary, this review unveils oral psilocybin pharmacokinetics in healthy adults, revealing gaps in its application to target populations like those with depression or in palliative care.

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