Pharmacokinetics of Hoasca alkaloids in healthy humans.
James C. Callaway, Dennis J. Mckenna, C S Grob, Glacus S. Brito, Lionel P. Raymon, Russell E. Poland, E N Andrade, E O Andrade, Deborah C. Mash
Journal of Ethnopharmacology June 1, 1999 DOI: 10.1016/s0378-8741(98)00168-8 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Observational pharmacokinetic study Peer reviewed |
|---|---|
| Sample size | 15 |
| Population | Volunteers who ingested hoasca in a ceremonial context |
| Dose | 2 ml hoasca/kg body weight |
| Topics | Ayahuasca |
| Key findings | Peak psychoactivity coincided with high alkaloid concentrations, particularly DMT which had an average Tmax of 107.5 minutes. |
Abstract
N,N-Dimethyltryptamine (DMT), harmine, harmaline and tetrahydroharmine (THH) are the characteristic alkaloids found in Amazonian sacraments known as hoasca, ayahuasca, and yajè. Such beverages are characterized by the presence of these three harmala alkaloids, where harmine and harmaline reversibly inhibit monoamine oxidase A (MAO-A) while tetrahydroharmine weakly inhibits the uptake of serotonin. Together, both actions increase central and peripheral serotonergic activity while facilitating the psychoactivity of DMT. Though the use of such 'teas' has be known to western science for over 100 years, little is known of their pharmacokinetics. In this study, hoasca was prepared and administered in a ceremonial context. All four alkaloids were measured in the tea and in the plasma of 15 volunteers, subsequent to the ingestion of 2 ml hoasca/kg body weight, using gas (GC) and high pressure liquid chromatographic (HPLC) methods. Pharmacokinetic parameters were calculated and peak times of psychoactivity coincided with high alkaloid concentrations, particularly DMT which had an average Tmax of 107.5 +/- 32.5 min. While DMT parameters correlated with those of harmine, THH showed a pharmacokinetic profile relatively independent of harmine's.
Comparable studies
Other experimental studies on ayahuasca, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Seeing with the eyes shut: Neural basis of enhanced imagery following ayahuasca ingestion Human participants (number not stated) | 2011 | Within-subjects experimental study | |
| Ayahuasca enhances creative divergent thinking while decreasing conventional convergent thinking Participants at spiritual ayahuasca workshops | 2016 | Within-subjects experimental study | n = 26 |
| Metabolism and disposition of N,N‐dimethyltryptamine and harmala alkaloids after oral administration of ayahuasca Healthy male volunteers | 2012 | Observational pharmacokinetic study | n = 10 |
| New World Tryptamine Hallucinogens and the Neuroscience of Ayahuasca. | 2018 | Review with original neuroimaging and neurophysiological data | |
| Stability Evaluation of DMT and Harmala Alkaloids in Ayahuasca Tea Samples Ayahuasca tea samples | 2020 | Experimental study |
Citations in the library
Cited by 206
- Rapid antidepressant effects of the psychedelic ayahuasca in treatment-resistant depression: a randomized placebo-controlled trial Psychological Medicine June 15, 2018
- The Psychedelic State Induced by Ayahuasca Modulates the Activity and Connectivity of the Default Mode Network PLoS One February 18, 2015
- Acute Effects of Lysergic Acid Diethylamide in Healthy Subjects Biological Psychiatry November 29, 2014
- Human Pharmacology of Ayahuasca: Subjective and Cardiovascular Effects, Monoamine Metabolite Excretion, and Pharmacokinetics Journal of Pharmacology and Experimental Therapeutics June 18, 2003
- Clinical investigations of the therapeutic potential of ayahuasca: rationale and regulatory challenges. Pharmacology & Therapeutics May 1, 2004
and 201 more in the library
Cites 8
- Dose-Response Study of N,N-Dimethyltryptamine in Humans Archives of General Psychiatry February 1, 1994
- Monoamine oxidase inhibitors in South American hallucinogenic plants: Tryptamine and β-carboline constituents of Ayahuasca Journal of Ethnopharmacology April 1, 1984
- Human Psychopharmacology of Hoasca, A Plant Hallucinogen Used in Ritual Context in Brazil The Journal of Nervous and Mental Disease February 1, 1996
- Platelet serotonin uptake sites increased in drinkers ofayahuasca Psychopharmacology November 1, 1994
- Effects of Ayahuasca on the human EEG Phytomedicine April 1, 1998
and 3 more in the library