Abstract
Journal of Ethnopharmacology
65 (1999) 243–256
Pharmacokinetics
of Hoasca alkaloids in healthy humans
J.C. Callaway a,*, D.J.
McKenna b, C.S. Grob c, G.S. Brito d, L.P. Raymon e,
R.E. Poland c, E.N. Andrade f, E.O. Andrade f, D.C. Mash g
a Uni6ersity of Kuopio, Department of Pharmaceutical Chemistry, POB 1627,
Kuopio FIN-70211, Finland
b Botanical Dimensions, POB 807, Occidental, CA 95465, USA
c Department of Psychiatry, Bldg. D-6, Harbor:UCLA Medical Center, 1000 West
Carson Street, Torrance, CA 90509, USA
d Centro De Estudos Medico, Da Unia˜o Do Vegetal, Caixa Postal 71505, 05020
-990 Sa˜o Paulo, Brazil
e Department of Pathology, Forensic Toxicology Laboratory, 12500 SW, 152nd
Street, Building B, Miami, FL 33177, USA
f Uni6ersity of Amazanas, Medical School, Department of Internal Medicine,
Manaus, Amazoˆnia, Brazil
g Uni6ersity of Miami School of Medicine, Department of Neurology, 1501 NW
9th A6enue, Miami, FL 33136, USA
Received 21 April 1998; received in revised form 1 September 1998; accepted
15 September 1998
Abstract
N,N-Dimethyltryptamine (DMT), harmine, harmaline and tetrahydroharmine (THH)
are the characteristic alkaloids
found in Amazonian sacraments known as hoasca, ayahuasca, and yaje`. 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 107.5932.5 min. While
DMT parameters correlated with those of harmine, THH showed a pharmacokinetic
profile relatively independent of
harmine’s. © 1999 Elsevier Science Ireland Ltd. All rights reserved.