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

Details

Serval ID
serval:BIB_41FF2DC253FA
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
The norepinephrine transporter inhibitor reboxetine reduces stimulant effects of MDMA ("ecstasy") in humans.
Journal
Clinical Pharmacology and Therapeutics
Author(s)
Hysek C.M., Simmler L.D., Ineichen M., Grouzmann E., Hoener M.C., Brenneisen R., Huwyler J., Liechti M.E.
ISSN
1532-6535 (Electronic)
ISSN-L
0009-9236
Publication state
Published
Issued date
2011
Volume
90
Number
2
Pages
246-255
Language
english
Notes
Publication types: Journal Article ; Randomized Controlled Trial ; Research Support, Non-U.S. Gov'tPublication Status: ppublish
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.
Keywords
3,4-Methylenedioxyamphetamine/pharmacokinetics, Adrenergic Uptake Inhibitors/pharmacology, Adult, Blood Pressure/drug effects, Cross-Over Studies, Double-Blind Method, Drug Interactions, Female, Hallucinogens/pharmacology, Heart Rate/drug effects, Humans, Male, Morpholines/pharmacology, N-Methyl-3,4-methylenedioxyamphetamine/pharmacology, Norepinephrine/blood, Norepinephrine/metabolism, Norepinephrine Plasma Membrane Transport Proteins/antagonists & inhibitors, Norepinephrine Plasma Membrane Transport Proteins/metabolism, Young Adult
Pubmed
Web of science
Create date
04/10/2011 16:14
Last modification date
20/08/2019 13:43
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