The norepinephrine transporter inhibitor reboxetine reduces stimulant effects of MDMA ("ecstasy") in humans.
Author(s): Hysek CM, Simmler LD, Ineichen M, Grouzmann E, Hoener MC, Brenneisen R, Huwyler J, Liechti ME
Affiliation(s): Psychopharmacology Research Group, Division of Clinical Pharmacology and Toxicology, Department of Biomedicine and Department of Internal Medicine, University Hospital and University of Basel, Basel, Switzerland.
Publication date & source: 2011-08, Clin Pharmacol Ther., 90(2):246-55. Epub 2011 Jun 15.
Publication type: Randomized Controlled Trial; Research Support, Non-U.S. Gov't
This study assessed the pharmacodynamic and pharmacokinetic effects of the interaction between the selective norepinephrine (NE) transporter inhibitor reboxetine and 3,4-methylenedioxymethamphetamine (MDMA, "ecstasy") in 16 healthy subjects. The study used a double-blind, placebo-controlled crossover design. Reboxetine reduced the effects of MDMA including elevations in plasma levels of NE, increases in blood pressure and heart rate, subjective drug high, stimulation, and emotional excitation. These effects were evident despite an increase in the concentrations of MDMA and its active metabolite 3,4-methylenedioxyamphetamine (MDA) in plasma. The results demonstrate that transporter-mediated NE release has a critical role in the cardiovascular and stimulant-like effects of MDMA in humans.