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Research ArticleBehavioral Pharmacology

Effects of the α2-Adrenergic Agonist Clonidine on the Pharmacodynamics and Pharmacokinetics of 3,4-Methylenedioxymethamphetamine in Healthy Volunteers

Cédric M. Hysek, Robin Brugger, Linda D. Simmler, Marcel Bruggisser, Massimiliano Donzelli, Eric Grouzmann, Marius C. Hoener and Matthias E. Liechti
Journal of Pharmacology and Experimental Therapeutics February 2012, 340 (2) 286-294; DOI: https://doi.org/10.1124/jpet.111.188425
Cédric M. Hysek
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Robin Brugger
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Linda D. Simmler
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Marcel Bruggisser
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Massimiliano Donzelli
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Eric Grouzmann
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Marius C. Hoener
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Matthias E. Liechti
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Abstract

The mechanism of action of 3,4-methylenedioxymethamphetamine (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 effects 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.

Footnotes

  • This study was supported by the Swiss National Science Foundation [Grant 323230_126231]; and the Science Pool of the Department of Internal Medicine, University Hospital Basel, Basel, Switzerland.

  • Article, publication date, and citation information can be found at http://jpet.aspetjournals.org.

    http://dx.doi.org/10.1124/jpet.111.188425.

  • ABBREVIATIONS:

    MDMA
    3,4-methylenedioxymethamphetamine
    AMRS
    Adjective Mood Rating Scale
    ANOVA
    analysis of variance
    AUEC
    area under the effect-time curve
    Cmax
    maximal plasma concentration
    5D-ASC
    5-Dimensions of Altered States of Consciousness
    DBP
    diastolic blood pressure
    Emax
    maximal effect
    HPLC
    high-performance liquid chromatography
    5-HT
    5-hydroxytryptamine (serotonin)
    MAP
    mean arterial pressure
    MDA
    3,4-methylenedioxyamphetamine
    NE
    norepinephrine
    PK
    pharmacokinetic
    PD
    pharmacodynamic
    SBP
    systolic blood pressure
    STAI
    State-Trait Anxiety Inventory
    VAS
    Visual Analog Scale
    OB
    oceanic boundlessness
    AED
    anxious ego dissolution
    VR
    visionary restructuralization
    VIR
    vigilance reduction.

  • Received September 26, 2011.
  • Accepted October 26, 2011.
  • Copyright © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 340 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 340, Issue 2
1 Feb 2012
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Research ArticleBehavioral Pharmacology

Clonidine and MDMA

Cédric M. Hysek, Robin Brugger, Linda D. Simmler, Marcel Bruggisser, Massimiliano Donzelli, Eric Grouzmann, Marius C. Hoener and Matthias E. Liechti
Journal of Pharmacology and Experimental Therapeutics February 1, 2012, 340 (2) 286-294; DOI: https://doi.org/10.1124/jpet.111.188425

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Research ArticleBehavioral Pharmacology

Clonidine and MDMA

Cédric M. Hysek, Robin Brugger, Linda D. Simmler, Marcel Bruggisser, Massimiliano Donzelli, Eric Grouzmann, Marius C. Hoener and Matthias E. Liechti
Journal of Pharmacology and Experimental Therapeutics February 1, 2012, 340 (2) 286-294; DOI: https://doi.org/10.1124/jpet.111.188425
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