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Effects of the α2-adrenergic agonist clonidine on the pharmacodynamics and pharmacokinetics of 3,4 methylenedioxymehtamphetamine in healthy volunteers.
MedLine Citation:
PMID:  22034656     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The mechanism of action of 3,4-methylenedioximethamphetamine (MDMA, ecstasy) involves the carrier-mediated and potentially vesicular release of monoamines. We assessed the effects of the sympatholytic α2-adrenergic receptor agonist clonidine (150 µg, p.o.), which inhibits the neuronal vesicular release of norepinephrine, on the cardiovascular and psychotropic response to MDMA (125 mg, p.o.) in 16 healthy subjects. The study used a randomized, double-blind, placebo-controlled crossover design with four experimental sessions. The administration of clonidine 1 h before MDMA reduced the MDMA-induced increases in plasma norepinephrine concentrations and blood pressure but only to the extent that clonidine lowered norepinephrine levels and blood pressure compared with placebo. Thus, no interaction was found between the cardiovascular effects of the two drugs. Clonidine did not affect the psychotropic or pharmacokinetics of MDMA. The lack of an interaction of the effects of clonidine and MDMA indicates that vesicular release of norepinephrine, which is inhibited by clonidine, does not critically contribute to the effects of MDMA in humans. Although clonidine may be used in the treatment of stimulant-induced hypertensive reactions, the present findings do not support a role for α2-adrenergic receptor agonists in the prevention of psychostimulant dependence.
Authors:
Cedric M Hysek; Robin Brugger; Linda D Simmler; Marcel Bruggisser; Massimiliano Donzelli; Eric Grouzmann; Marius C Hoener; Matthias E Liechti
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-10-27
Journal Detail:
Title:  The Journal of pharmacology and experimental therapeutics     Volume:  -     ISSN:  1521-0103     ISO Abbreviation:  -     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-10-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376362     Medline TA:  J Pharmacol Exp Ther     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
1 University Hospital Basel;
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