Pharmacokinetics and Pharmacodynamics of an Innovative Psychedelic N,N-Dimethyltryptamine/Harmine Formulation in Healthy Participants

This secondary analysis of an RCT (n=31) evaluates a novel pharmaceutical formulation of DMT and harmine in healthy male volunteers. The study finds that intranasal DMT and buccal harmine (pharmahuasca) produce consistent pharmacokinetic profiles and safe, well-tolerated effects resembling ayahuasca, with subjective experiences lasting 2–3 hours. This formulation is proposed as a safer, standardised alternative for potential therapeutic use in mental health disorders.

Abstract of Pharmacokinetics and Pharmacodynamics of an Innovative Psychedelic DMT/Harmine Formulation in Healthy Participants

Background Recent interest in the clinical use of psychedelics has highlighted plant-derived medicines like ayahuasca showing rapid-acting and sustainable therapeutic effects in various psychiatric conditions. This traditional Amazonian plant decoction contains N,N-dimethyltryptamine (DMT) and β-carboline alkaloids such as harmine. However, its use is often accompanied by distressing effects like nausea, vomiting, and intense hallucinations, possibly due to complex pharmacokinetic/pharmacodynamic (PK-PD) interactions and lack of dose standardization.

Methods This study addresses these limitations by testing a novel pharmaceutical formulation containing pure forms of DMT and harmine in a double-blind, randomized, placebo-controlled trial with 31 healthy male volunteers. We evaluated PK-PD by monitoring drug and metabolite plasma levels, subjective effects, adverse events, and cardiovascular parameters. Each participant received three randomized treatments: 1) 100 mg buccal harmine with 100 mg intranasal DMT, 2) 100 mg buccal harmine with intranasal placebo, and 3) full placebo; using a repeated-intermittent dosing scheme, such that 10 mg of DMT (or placebo) was administered every 15 minutes.

Results DMT produced consistent PK profiles with Cmax values of 22.1 ng/ml and acute drug effects resembling the psychological effects of ayahuasca with a duration of 2–3 hours. Likewise, buccal harmine produced sustained-release PK profiles with Cmax values of 32.5 ng/ml, but lacked distinguishable subjective effects compared to placebo. All drug conditions were safe and well tolerated, indicating the formulation’s suitability for clinical applications.

Conclusion This study underscores the potential of a patient-oriented pharmaceutical formulation of DMT and harmine to reduce risks and improve therapeutic outcomes in treating mental health disorders.”

Authors: Michael J. Mueller, Helena D. Aicher, Dario A. Dornbierer, Laurenz Marten, Dila Suay, Daniel Meling, Claudius Elsner, Ilhui A. Wicki, Jovin Müller, Sandra N. Poetzsch, Luzia Caflisch, Alexandra Hempe, Camilla P. Steinhart, Maxim Puchkov, Jonas Kost, Hans-Peter Landolt, Erich Seifritz, Boris B. Quednow & Milan Scheidegger

Summary of Pharmacokinetics and Pharmacodynamics of an Innovative Psychedelic DMT/Harmine Formulation in Healthy Participants

The study explores the pharmacokinetics (PK) and pharmacodynamics (PD) of a novel pharmaceutical formulation combining DMT (N,N-dimethyltryptamine) and harmine. DMT is a potent psychedelic compound traditionally consumed in ayahuasca, an Amazonian brew containing harmine, which acts as a monoamine oxidase A (MAO-A) inhibitor. This combination enables DMT to bypass rapid enzymatic breakdown in the gut, prolonging its psychoactive effects. However, traditional ayahuasca is associated with distressing side effects such as nausea, vomiting, and inconsistent drug absorption.

The researchers aimed to address these limitations by developing a controlled formulation using intranasal DMT and buccal harmine tablets, ensuring standardised dosing and bypassing gastrointestinal absorption. This study assessed the PK-PD profile, subjective effects, and safety of this innovative administration method in healthy male participants.

Methods

Participants

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Pharmacokinetics and Pharmacodynamics of an Innovative Psychedelic N,N-Dimethyltryptamine/Harmine Formulation in Healthy Participants

https://doi.org/10.1093/ijnp/pyaf001

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Cite this paper (APA)

Mueller, M. J., Aicher, H. D., Dornbierer, D. A., Marten, L., Suay, D., Meling, D., ... & Scheidegger, M. (2025). Pharmacokinetics and Pharmacodynamics of an Innovative Psychedelic N, N-Dimethyltryptamine/Harmine Formulation in Healthy Participants: A Randomized Controlled Trial. International Journal of Neuropsychopharmacology, pyaf001.

Study details

Compounds studied
DMT

Topics studied
Healthy Subjects

Study characteristics
Original Re-analysis Placebo-Controlled Active Placebo Double-Blind Within-Subject Randomized Re-analysis

Participants
31 Humans

Institutes

Institutes associated with this publication

University of Zurich
Within the Department of Psychiatry, Psychotherapy and Psychosomatics at the University of Zurich, Dr Mialn Scheidegger is leading team conducting psychedelic research and therapy development.

Reconnect Labs
Reconnect Labs, a Swiss-based clinical-stage pharmaceutical company, is pioneering the development of Regenerative Therapeutics™ aimed at mental health, leveraging cutting-edge neuroscience and precision psychopharmacology.

Compound Details

The psychedelics given at which dose and how many times

DMT 100 mg | 1x

Linked Research Papers

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Potential therapeutic effects of an ayahuasca-inspired N,N-DMT and harmine formulation: a controlled trial in healthy subjects
This crossover RCT (n=31) investigates the effects of a novel ayahuasca-inspired formulation containing harmine and DMT in healthy male subjects. It finds that the combination of DMT and harmine, but not harmine alone, leads to a psychedelic experience with psychological insights, emotional breakthroughs, and low challenging experiences. The study reports positive persisting effects at 1- and 4-month follow-ups, with no changes in personality traits, psychological flexibility, general well-being, or increases in psychopathology.

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