Carvedilol inhibits the cardiostimulant and thermogenic effects of MDMA in humans
British Journal of Pharmacology – March 08, 2012
Source: OpenAlex
Summary
Carvedilol, an adrenoceptor antagonist, significantly reduced heart rate and blood pressure increases caused by MDMA (125 mg) in a crossover study involving 16 healthy participants. Specifically, carvedilol (50 mg) lowered MDMA-induced elevations in heart rate and body temperature without altering the subjective experience of ecstasy, such as feelings of euphoria or stimulation. This suggests that carvedilol could be a promising option for addressing cardiovascular and hyperthermic issues linked to ecstasy use while leaving its psychoactive effects intact.
Abstract
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.