Journal of Psychoactive Drugs
September 10, 2024
Nilubon Thaoboonruang, Manupat Lohitnavy, Ornrat Lohitnavy
11 citations
Psilocybin, the main psychoactive compound in magic mushrooms, acts as a prodrug that is rapidly converted in the body to its active form, psilocin. After ingestion, psilocin levels in blood and brain peak quickly and depend on the dose given. Psilocin is broken down through multiple metabolic pathways and has a short half-life of 2–3 hours. This review of 20 studies highlights that while basic pharmacokinetics are understood, important gaps remain—such as incomplete information on metabolism and limitations in study design—that future research should address to improve dosing and treatment optimization for conditions like major depressive disorder.
F1000Research
March 15, 2021
Prinya Musikaphongsakul, Kimheang Ya, Pakpoom Subsoontorn et al.
6 citations
A physiologically based pharmacokinetic model predicts concentrations of psilocin, the active metabolite of psilocybin, in plasma and brain after intravenous and oral administration in rats and humans. The model, built from three published studies, uses seven organ compartments and shows good overall agreement with observed data, though oral doses are under-predicted and intravenous doses over-predicted. This tool may help design safer dosing regimens for therapeutic use.
Scientific reports
April 21, 2025
Nilubon Thaoboonruang, Ornrat Lohitnavy, Kimheang Ya et al.
4 citations
A physiologically based pharmacokinetic (PBPK) model was developed to describe how psilocybin and its active metabolite psilocin distribute through the body in mice, rats, and humans. Psilocybin is assumed to convert completely to psilocin before entering systemic circulation. The model accurately characterizes concentration-time profiles across different doses and routes of administration. It can help guide therapeutic strategies and improve clinical trial designs for using psilocybin to treat major depressive disorder.
Toxicological sciences : an official journal of the Society of Toxicology
November 1, 2025
Naphat Wittayakarn, Yu-Mei Tan, Pattanachai Choomalaiwong et al.
Ayahuasca, a traditional Amazonian brew containing DMT from Psychotria viridis and harmine from Banisteriopsis caapi, produces psychoactive effects because harmine inhibits monoamine oxidase-A, preventing DMT's metabolism and increasing its systemic bioavailability. The brew shows potential therapeutic benefits for depression, anxiety, and substance use disorders. Researchers developed physiologically based pharmacokinetic (PBPK) models for DMT and harmine in rats and humans, accounting for multiple administration routes and harmine's inhibition of DMT metabolism in the liver and lungs. The models reasonably predicted plasma concentrations across dosing conditions. Simulations suggest that maintaining plasma concentration above a threshold may be more relevant for therapeutic effects than peak levels, offering a framework for safer dosing.