The Norepinephrine Transporter Inhibitor Reboxetine Reduces Stimulant Effects of MDMA (“Ecstasy”) in Humans
Cédric M. Hysek, Linda D. Simmler, M. Ineichen, Eric Grouzmann, Marius C. Hoener, Rudolf Brenneisen, Jörg Huwyler, Matthias E. Liechti
Clinical Pharmacology & Therapeutics June 15, 2011 DOI: 10.1038/clpt.2011.78 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Randomized controlled trial Placebo-controlled Double-blind Peer reviewed |
|---|---|
| Sample size | 16 |
| Population | Healthy subjects |
| Interventions | Reboxetine MDMA |
| Topics | MDMA |
| Keywords | Stimulant Reboxetine Norepinephrine transporter Pharmacology |
| Citations | 153 |
| Key findings | Reboxetine reduced MDMA's cardiovascular and subjective stimulant effects, demonstrating that norepinephrine transporter-mediated release is critical for these effects in humans. |
Abstract
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.