The norepinephrine transporter inhibitor reboxetine reduces stimulant effects of MDMA ("ecstasy") in humans.

Hysek CM, Simmler LD, Ineichen M, Grouzmann E, Hoener MC, Brenneisen R, Huwyler J, Liechti ME
Clin Pharmacol Ther. 2011 90 (2): 246-55

PMID: 21677639 · DOI:10.1038/clpt.2011.78

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.

MeSH Terms (18)

3,4-Methylenedioxyamphetamine Adrenergic Uptake Inhibitors Adult Blood Pressure Cross-Over Studies Double-Blind Method Drug Interactions Female Hallucinogens Heart Rate Humans Male Morpholines N-Methyl-3,4-methylenedioxyamphetamine Norepinephrine Norepinephrine Plasma Membrane Transport Proteins Reboxetine Young Adult

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