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Agents for Treatment of Withdrawal and Dependency: Varenicline

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Abstract

Varenicline exhibits a receptor-dependent mode of action, acting as a low-efficacy partial agonist to the α4β2, α3β2, α3β4, and α6/α3β2β3 chimeric neuronal nicotinic acetylcholine receptors (nAChRs) and a high-efficacy full agonist to the α7 neuronal nAChR. There is extensive evidence that varenicline reduces nicotine craving and withdrawal symptoms by relatively selectively modulating dopaminergic function at α4β2* nAChRs (the asterisk indicates the possible presence of other nicotinic subunits in the receptor complex).

Varenicline is the most efficacious monotherapy for increasing smoking abstinence rates, with proven superiority over sustained-release bupropion, nicotine replacement therapy, and placebo. Repeated reports of neuropsychiatric and cardiovascular safety concerns against varenicline have not been confirmed by meta-analytic findings.

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Authors and Affiliations

  1. Clinic for Psychiatry and Psychotherapy, medius KLINIK Kirchheim, Kirchheim unter Teck, Germany

    Christian Jacob

  2. Department of Psychiatry, Psychosomatics and Psychotherapy, University Clinic Würzburg, Würzburg, Germany

    Thomas Polak

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Correspondence to Christian Jacob .

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Editors and Affiliations

  1. Dept Psychiatry , Psychosomatics & Psychotherapy, University of Würzburg, Medical School Clinical Neurochemistry, Würzburg, Germany

    Peter Riederer

  2. Inst für Psychologische Medizin, Haag, Bayern, Germany

    Gerd Laux

  3. Department of Psychiatry, University of Toronto Department of Psychiatry, Toronto, ON, Canada

    Benoit Mulsant

  4. Center Translational Res Neurol Diseases, Dalian Med Uni Shanghai Inst Health Sc Center Translational Res Neurol Diseases, Dalian, China

    Weidong Le

  5. Fujita Health University School Medicine, Toyoake, Aichi, Japan

    Toshiharu Nagatsu

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  1. The International College of Neuropsychopharmacology, East Kilbride, Scotland

    Toshikazu Saito

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Jacob, C., Polak, T. (2020). Agents for Treatment of Withdrawal and Dependency: Varenicline. In: Riederer, P., Laux, G., Mulsant, B., Le, W., Nagatsu, T. (eds) NeuroPsychopharmacotherapy. Springer, Cham. https://doi.org/10.1007/978-3-319-56015-1_350-1

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