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

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), psilocybi

Authors
Hampsey E, Martin K, Kalfas M, Benson L, Wihlborg S, Jelen L, Young AH, Rucker J
Journal
Journal of psychopharmacology (Oxford, England)
Published
2026-08-01
DOI
10.1177/02698811261453938
PMID
42212869
Content type
Review
Authority
Academic

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.

Citation

Hampsey E, Martin K, Kalfas M, Benson L, Wihlborg S, Jelen L, Young AH, Rucker J (2026) A systematic review of the pharmacokinetics of classical serotonergic psychedelic compounds in healthy adult subjects.. Journal of psychopharmacology (Oxford, England). doi:10.1177/02698811261453938

View source

DOI: 10.1177/02698811261453938

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