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A systematic review of the pharmacokinetics of classical serotonergic psychedelic compounds in healthy adult subjects.

Elliot Hampsey, Kirsty Martin, Michail Kalfas, Louis Benson, Sirid Wihlborg, Luke Jelen, Allan H Young, James Rucker

Journal of psychopharmacology (Oxford, England) May 29, 2026 Peer reviewed DOI: 10.1177/02698811261453938 via PubMed

Summary

The systematic review analyzed the pharmacokinetic properties of classical psychedelics, including LSD, psilocybin, DMT, mescaline, and 5-MEO-DMT, based on data from 32 trials involving healthy adult volunteers. LSD was the most studied compound, followed by DMT and psilocybin. The review found that both LSD and psilocybin exhibited dose proportional Cmax values, and noted clinically significant differences between oral and IV formulations of DMT. Variations in absorption, distribution, and elimination among these compounds were highlighted.

Study at a glance

Design systematic review
Sample size 32
Population healthy adult volunteers
Key finding Key findings include dose proportional Cmax values for LSD and psilocybin, alongside clinically significant differences between oral and IV formulations of DMT.

Abstract

Despite renewed investigations into classical psychedelic compounds, their pharmacokinetic profiles remain incompletely understood. This systematic review collated data from healthy adult volunteers on the pharmacokinetic properties of lysergic acid diethylamide (LSD), psilocybin, dimethyltryptamine (DMT), mescaline, and 5-methoxy-N,N-dimethyltryptamine (5-MEO-DMT). We identified 32 eligible trials. LSD was the most studied compound, followed by DMT, split between intravenous (IV) and oral formulations. Psilocybin was also frequently studied. Mescaline was reported in two trials, with IV LSD, IV psilocybin, inhalation 5-MEO-DMT, and intranasal 5-MEO-DMT reported in single studies. Key findings include dose proportional Cmax values for LSD and psilocybin, alongside differences between oral and IV formulations of DMT that may be clinically significant. This systematic review highlights key variations in absorption, distribution, and elimination between the studied compounds that may have important implications in both clinical and research settings.

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