Carvedilol inhibits the cardiostimulant and thermogenic effects of MDMA in humans.

Hysek C, Schmid Y, Rickli A, Simmler LD, Donzelli M, Grouzmann E, Liechti ME
Br J Pharmacol. 2012 166 (8): 2277-88

PMID: 22404145 · PMCID: PMC3448893 · DOI:10.1111/j.1476-5381.2012.01936.x

BACKGROUND AND PURPOSE - The use of ± 3,4-methylenedioxymethamphetamine (MDMA, 'ecstasy') is associated with cardiovascular complications and hyperthermia.

EXPERIMENTAL APPROACH - We assessed the effects of the α(1) - and β-adrenoceptor antagonist carvedilol on the cardiostimulant, thermogenic and subjective responses to MDMA in 16 healthy subjects. Carvedilol (50 mg) or placebo was administered 1 h before MDMA (125 mg) or placebo using a randomized, double-blind, placebo-controlled, four-period crossover design. KEY RESULTS Carvedilol reduced MDMA-induced elevations in blood pressure, heart rate and body temperature. Carvedilol did not affect the subjective effects of MDMA including MDMA-induced good drug effects, drug high, drug liking, stimulation or adverse effects. Carvedilol did not alter the plasma exposure to MDMA.

CONCLUSIONS AND IMPLICATIONS - α(1) - and β-Adrenoceptors contribute to the cardiostimulant and thermogenic effects of MDMA in humans but not to its psychotropic effects. Carvedilol could be useful in the treatment of cardiovascular and hyperthermic complications associated with ecstasy use.

© 2012 The Authors. British Journal of Pharmacology © 2012 The British Pharmacological Society.

MeSH Terms (16)

Adrenergic Antagonists Adult Area Under Curve Body Temperature Carbazoles Carvedilol Catecholamines Cross-Over Studies Drug Interactions Female Heart Rate Humans Male N-Methyl-3,4-methylenedioxyamphetamine Propanolamines Young Adult

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