The Norepinephrine Transporter Inhibitor Reboxetine Reduces Stimulant Effects of MDMA (“Ecstasy”) in Humans
C.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 via OpenAlex
Summary
AI-generated from the abstractBlocking the norepinephrine transporter with reboxetine reduces the cardiovascular and subjective stimulant effects of MDMA (ecstasy) in humans, even though MDMA and its active metabolite reach higher concentrations in the blood. In a double-blind, placebo-controlled crossover study with 16 healthy adults, reboxetine lowered MDMA-induced increases in plasma norepinephrine, blood pressure, heart rate, drug high, stimulation, and emotional excitement. The findings indicate that transporter-mediated norepinephrine release is essential for MDMA's cardiovascular and stimulant-like effects.
Study at a glance
| Characteristics | Randomized controlled trial Placebo-controlled Double-blind Peer reviewed |
|---|---|
| Sample size | 16 |
| Population | Healthy subjects |
| Topics | MDMA |
| Keywords | Stimulant Reboxetine Norepinephrine transporter |
| Citations | 153 |
| Key finding | 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.