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Clinical pharmacokinetics

ISSN 1179-1926

3 papers in the library · 11 citations · publishing 2025

Papers

Clinical Pharmacokinetics of N,N-Dimethyltryptamine (DMT): A Systematic Review and Post-hoc Analysis.

Clinical pharmacokinetics February 1, 2025 K V van der Heijden, M E Otto, J W Schoones et al. 7 citations

A systematic review of 13 publications covering eight datasets found that the pharmacokinetics of DMT in humans have been characterized only to a limited extent. All studies administered DMT intravenously except one intramuscular injection. DMT is rapidly metabolized to indole-3-acetic acid (IAA), with a half-life of 4.8–19.0 minutes and clearance of 8.1–46.8 L/min. It shows extensive tissue redistribution, indicated by a high terminal volume of distribution (123–1084 L). High variability in dose-normalized exposure and differences between bolus and infusion administration were observed. Publications often lack details on demographics, absolute doses, and pharmacokinetic parameters, highlighting the need for further studies.

Pharmacokinetics, Pharmacodynamics, and Urinary Recovery of Oral Mescaline Hydrochloride in Healthy Participants.

Clinical pharmacokinetics July 14, 2025 Lorenz Mueller, Aaron Klaiber, Laura Ley et al. 4 citations

Mescaline, a classic psychedelic, shows dose-proportional increases in blood concentration and effects after oral administration. Peak levels occur within about 2 hours, with a half-life of 3.5 hours. Effects begin around 1 hour after dosing, with intensity and duration increasing from 13% and 2.8 hours at 100 mg to 89% and 15 hours at 800 mg. About 53% of the dose is excreted unchanged in urine, and 31% as a main metabolite. Oral bioavailability is at least 53%, limited by first-pass metabolism, with renal elimination as the primary clearance route.

Modeling Whole-Body Dynamic PET Microdosing Data to Predict the Whole-Body Pharmacokinetics of Glyburide in Humans.

Clinical pharmacokinetics November 1, 2025 Léa Comin, Solène Marie, Moreno Ursino et al.

A pharmacokinetic model built from whole-body dynamic PET scans after a microdose of radiolabeled glyburide in 16 healthy people describes the drug's biodistribution and yields parameters consistent with standard blood-based studies. The model included seven compartments, with two each for liver and kidneys. Rifampicin, a drug that can cause interactions, decreased liver distribution by 261%. The estimated central volume of distribution (3.6 L) and elimination rate (0.8 h-1) matched known glyburide pharmacokinetics, suggesting microdose PET data can be used to study whole-body drug distribution.