pubmed.ncbi.nlm.nih.gov

Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic Repercussions - PubMed

Review

Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic Repercussions

Ricardo Jorge Dinis-Oliveira et al. Curr Mol Pharmacol. 2019.

Abstract

Background: Mescaline (3,4,5-trimethoxyphenethylamine), mainly found in the Peyote cactus (Lophophora williamsii), is one of the oldest known hallucinogenic agents that influence human and animal behavior, but its psychoactive mechanisms remain poorly understood.

Objectives: This article aims to fully review pharmacokinetics and pharmacodynamics of mescaline, focusing on the in vivo and in vitro metabolic profile of the drug and its implications for the variability of response.

Methods: Mescaline pharmacokinetic and pharmacodynamic aspects were searched in books and in PubMed (U.S. National Library of Medicine) without a limiting period. Biological effects of other compounds found in peyote were also reviewed.

Results: Although its illicit administration is less common, in comparison with cocaine and Cannabis, it has been extensively described in adolescents and young adults, and licit consumption often occurs in religious and therapeutic rituals practiced by the Native American Church. Its pharmacodynamic mechanisms of action are primarily attributed to the interaction with the serotonergic 5-HT2A-C receptors, and therefore clinical effects are similar to those elicited by other psychoactive substances, such as lysergic acid diethylamide (LSD) and psilocybin, which include euphoria, hallucinations, depersonalization and psychoses. Moreover, as a phenethylamine derivative, signs and symptoms are consistent with a sympathomimetic effect. Mescaline is mainly metabolized into trimethoxyphenylacetic acid by oxidative deamination but several minor metabolites with possible clinical and forensic repercussions have also been reported.

Conclusion: Most reports concerning mescaline were presented in a complete absence of exposure confirmation, since toxicological analysis is not widely available. Addiction and dependence are practically absent and it is clear that most intoxications appear to be mild and are unlikely to produce lifethreatening symptoms, which favors the contemporary interest in the therapeutic potential of the drugs of the class.

Keywords: Mescaline; metabolism; peyote; pharmacodynamics; pharmacokinetics; toxicity..

Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

PubMed Disclaimer

Figures

Fig. (1)
Fig. (1)

Cactaceae plant family containing mescaline. A and B - Lophophora williamsii; C and D - Echinopsis pachanoi; E - Echinopsis peruviana; F - Echinopsis lageniformis; G - Pereskia aculeate.

Fig. (2)
Fig. (2)

A - Agave angustifolia, the mescal plant; B - Dermatophyllum secundiflorum.

Fig. (3)
Fig. (3)

Main alkaloids found in the peyote cactus.

Fig. (4)
Fig. (4)

Mescaline pharmacodynamics at the serotonergic terminal is mediated through 5-HT2A-C receptors. 5-HIAA, 5-hydroxyindoleacetic acid; MAO, monoamine oxidase; IP3, inositol 1,4,5-triphosphate.

Fig. (5)
Fig. (5)

Major and minor metabolic routes of mescaline. MAO, monoamine oxidase; DAO, diamine oxidase.

Similar articles

Cited by

References

    1. Bogenschutz M.P., Johnson M.W. Classic hallucinogens in the treatment of addictions. Prog. Neuropsychopharmacol. Biol. Psychiatry. 2016;64:250–258. - PubMed
    1. Nichols D.E. Hallucinogens. Pharmacol. Ther. 2004;101:131–181. - PubMed
    1. Olive M.F., Triggle D.J. Drugs the straight facts: Peyote and mescaline. New York: Chelsea House; 2007.
    1. Lopez-Gimenez J.F., Gonzalez-Maeso J. Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathways. Curr. Top. Behav. Neurosci. 2018;36:45–73. - PMC - PubMed
    1. Dinis-Oliveira R.J. Metabolism of psilocybin and psilocin: Clinical and forensic toxicological relevance. Drug Metab. Rev. 2017;49:84–91. - PubMed

Publication types

MeSH terms

Substances