Toxicokinetics and Toxicodynamics of Ayahuasca Alkaloids N , N -Dimethyltryptamine (DMT), Harmine, Harmaline and Tetrahydroharmine: Clinical and Forensic Impact.
Level 5 - mechanism / opinion, no new human data
Narrative review without systematic search or primary data
PubMed 33114119 · doi:10.3390/ph13110334
What was done
Narrative review summarizing published literature on the toxicokinetics, toxicodynamics, and physiological effects of ayahuasca and its primary constituents (DMT, harmine, harmaline, tetrahydroharmine), with focus on pharmacological synergy, adverse effects, forensic aspects, and psychiatric applications.
What was found
The abstract reports qualitative mechanisms and findings with no quantitative numbers. Harmala alkaloids inhibit MAO-A, blocking first-pass degradation of DMT into 3-indole-acetic acid and permitting central nervous system access. DMT acts primarily via 5-HT2A receptors alongside other targets. Adverse effects range from mild to rarely severe, with reported lack of dependence or tolerance. Potential benefits were identified for depression, anxiety, and substance abuse disorders.
Why it matters
Explains the essential synergistic pharmacokinetic mechanism underlying oral DMT bioavailability and contextualizes the therapeutic and toxicological profile of ayahuasca.
Limits
As a narrative review, it lacks a systematic search protocol, quality assessment of included studies, and original experimental data. The abstract reports no quantitative pharmacokinetic values, risk estimates, or effect sizes.
Cited by
- supports Ayahuasca combines dimethyltryptamine (DMT) with a monoamine oxidase (MAO) inhibitor, which prevents rapid metabolism in the gut and prolongs its duration of action.