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Tranquilizer/Anxiolytics: Buspirone

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NeuroPsychopharmacotherapy

Abstract

Buspirone was developed in 1968. It is an anxiolytic agent that is a member of the azaspirodecanedione that was approved for treatment of anxiety in 1986. It is rapidly absorbed and undergoes first-pass metabolism with several active metabolites. Its use is not recommended in severe hepatic and renal disease. The proposed mechanism of action is through partial agonism of the 5-HT1A receptors, notably lacking benzodiazepine or GABA affinity. The majority of clinical trials have been completed in generalized anxiety disorder (GAD), and a recent meta-analysis found buspirone to be more efficacious at reducing symptoms of anxiety than placebo. Clinical studies found buspirone to be well tolerated with the most common side effect being dizziness and nausea. Serious life-threatening side effects can occur when taken in combination with MAO inhibitors. Overall, there appears to be less abuse potential than other anxiolytics; however, case reports do suggest that abuse should be monitored for. Drug combinations that impact CYP3A4 function require monitoring or dose adjustments.

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References

  • Barbhaiya RH, Shukla UA, Pfeffer M, Pittman KA, Shrotriya R, Laroudie C, et al. Disposition kinetics of buspirone in patients with renal or hepatic impairment after administration of single and multiple doses. Eur J Clin Pharmacol. 1994;46(1):41–7. Available from: https://doi.org/10.1007/BF00195914. Springer-Verlag

  • Blanco C, Bragdon LB, Schneier FR, Liebowitz MR. The evidence-based pharmacotherapy of social anxiety disorder [internet]. Cambridge, UK: Cambridge University Press; 2013. p. 235–49. https://doi.org/10.1017/S1461145712000119.

    Book  Google Scholar 

  • Boerner RJ et al. Kava-Kava extract LI 150 is as effective as Opipramol and Buspirone in Generalised Anxiety Disorder--an 8-week randomized, double-blind multicentre clinical trial in 129 out-patients. Phytomedicine: international journal of phytotherapy and phytopharmacology 2003;10 Suppl 4:38–49

    Google Scholar 

  • Chessick CA, Allen MH, Thase ME, Batista Miralha da Cunha AABC, Kapczinski F, Silva de Lima M, dos Santos Souza JJSS. Azapirones for generalized anxiety disorder. Cochrane Database of Systematic Reviews 2006, Issue 3. Art. No.: CD006115

    Google Scholar 

  • Chiaie RD et al. Assessment of the efficacy of buspirone in patients affected by generalized anxiety disorder, shifting to buspirone from prior treatment with lorazepam: a placebo-controlled, double-blind study. J Clin Psychopharm 1995;15(1):12–19

    Google Scholar 

  • Cohn JB, et al. Double-blind comparison of buspirone and clorazepate in anxious outpatients. The American Journal of Medicine 1986a;80(3B)

    Google Scholar 

  • Cottraux J et al. A controlled study of cognitive behaviour therapy with buspirone or placebo in panic disorder with agoraphobia. The British journal of psychiatry : the journal of mental science 1995;167(5):635–641

    Google Scholar 

  • Davidson JR, et al. Efficacy, safety, and tolerability of venlafaxine extended release and buspirone in outpatients with generalized anxiety disorder. The journal of clinical psychiatry 1999;60(8):528–535

    Google Scholar 

  • Eison AS. Azapirones: history of development. J Clin Psychopharmacol. 1990;10(3 Suppl):2S–5S. Available from: http://www.ncbi.nlm.nih.gov/pubmed/1973936

    Article  CAS  Google Scholar 

  • Eison AS, Temple DL. Buspirone: review of its pharmacology and current perspectives on its mechanism of action. Am J Med. 1986;80(3 SUPPL. 2):1–9.

    Article  CAS  Google Scholar 

  • Gammans RE, Mayol RF, Labudde JA. Metabolism and disposition of buspirone. Am J Med. 1986;80(3 SUPPL. 2):41–51. Available from: http://www.amjmed.com/article/0002934386903311/fulltext. Elsevier

    Article  CAS  Google Scholar 

  • Lader M. Long-term anxiolytic therapy: the issue of drug withdrawal. J Clin Psychiatry. 1987:12–6. Available from: http://www.ncbi.nlm.nih.gov/pubmed/2891684

  • Lader M et al. A multicentre double-blind comparison of hydroxyzine, buspirone and placebo in patients with generalized anxiety disorder. Psychopharmacology 1998;139(4):402–406

    Google Scholar 

  • Landén M, Eriksson E, Ã…gren H, Fahlén T. Effect of buspirone on sexual dysfunction in depressed patients treated with selective serotonin reuptake inhibitors. J Clin Psychopharmacol. 1999;19(3):268–71. Available from: https://pubmed.ncbi.nlm.nih.gov/10350034/

    Article  Google Scholar 

  • Lee ST et al. Efficacy of the 5-HT1A agonist, buspirone hydrochloride, in migraineurs with anxiety: a randomized, prospective, parallel group, double-blind, placebo-controlled study. Headache 2005;45(8):1004–1011

    Google Scholar 

  • Le Foll B, Payer D, Di Ciano P, Guranda M, Nakajima S, Tong J, et al. Occupancy of dopamine D3 and D2 receptors by Buspirone: A [11C]-(+)-PHNO PET study in humans; 2015;41(2):529–37. https://doi.org/10.1038/npp.2015.177. England: Springer Science and Business Media LLC.

  • Lexicomp. Buspirone (Lexi-Drugs).

    Google Scholar 

  • Loane C, Politis M. Buspirone: what is it all about? [Internet]. Brain Res. 2012:111–8. Available from: https://pubmed.ncbi.nlm.nih.gov/22608068/

  • Mezher AW, McKnight CA, Caplan JP. Buspirone abuse: No safe haven [Internet]. Elsevier Inc.; 2019. p. 534–5. Available from: https://pubmed.ncbi.nlm.nih.gov/30685117/

  • Mokhber N et al. Randomized, single-blind, trial of sertraline and buspirone for treatment of elderly patients with generalized anxiety disorder. Psychiatry and Clinical Neurosciences 2010;64(2):128–133

    Google Scholar 

  • Monograph. Product monograph: Buspirone (Buspirone Hydrochloride) [Internet]. Sollentuna: Orion Pharma; 2015. Available from: http://libris.kb.se/resource/bib/10002850

  • National Center for Biotechnology Information. PubChem Database. Buspirone, CID=2477. https://pubchem.ncbi.nlm.nih.gov/compound/Buspirone#section=Depositor-Supplied-Synonyms. Accessed on June 26, 2020.

  • Sheehan DV et al The relative efficacy of buspirone, imipramine and placebo in panic disorder: a preliminary report. Pharmacology, biochemistry, and behavior 1988;29(4):815–817

    Google Scholar 

  • Sheehan DV, Raj AB, Harnett-Sheehan K, Soto S, Knapp E. The relative efficacy of high-dose buspirone and alprazolam in the treatment of panic disorder: a double-blind placebo-controlled study. Acta Psychiatr Scand; 1993 [cited 2020 Aug 10];88(1). Available from: https://pubmed-ncbi-nlm-nih-gov.myaccess.library.utoronto.ca/8372689/

  • Slee A, Nazareth I, Bondaronek P, Liu Y, Cheng Z, Freemantle N. Pharmacological treatments for generalised anxiety disorder: a systematic review and network meta-analysis. Lancet. 2019;393(10173):768–77. Available from: http://www.thelancet.com/article/S0140673618317938/fulltext. Lancet Publishing Group.

    Article  CAS  Google Scholar 

  • Toothaker RD, Welling PG. The effect of food on drug bioavailability. Ann Rev. 1980;20(1):173–99. Available from: https://pubmed.ncbi.nlm.nih.gov/6992698/

    CAS  Google Scholar 

  • Tunnicliff G. Molecular basis of Buspirone’s anxiolytic action. Pharmacol Toxicol. 1991;69(3):149–56. Available from: https://pubmed.ncbi.nlm.nih.gov/1796057/

    Article  CAS  Google Scholar 

  • Velosa JF, Riddle MA. Pharmacologic treatment of anxiety disorders in children and adolescents. Child Adolesc Psychiatr Clin N Am; 2000 [cited 2020 Aug 10];9(1). Available from: https://pubmed-ncbi-nlm-nih-gov.myaccess.library.utoronto.ca/10674193/

  • Wilson TK, Tripp J. StatPearls [internet]. Treasure Island: StatPearls Publishing; 2020.

    Google Scholar 

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Authors and Affiliations

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

    Brett D. M. Jones

  2. Department of Psychiatry, Centre for Addiction and Mental Health, University of Toronto, Toronto, ON, Canada

    M. Ishrat Husain

Authors
  1. Brett D. M. Jones
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  2. M. Ishrat Husain
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Correspondence to Brett D. M. Jones .

Editor information

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

    Toshiharu Nagatsu

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

    Weidong Le

  5. Würzburg, Bayern, Germany

    Christian Riederer

Section Editor information

  1. Department of Psychiatry, Centre for Addiction and Mental Health, University of Toronto, Toronto, ON, Canada

    Stefan Kloiber

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Jones, B.D.M., Husain, M.I. (2021). Tranquilizer/Anxiolytics: Buspirone. In: Riederer, P., Laux, G., Nagatsu, T., Le, W., Riederer, C. (eds) NeuroPsychopharmacotherapy. Springer, Cham. https://doi.org/10.1007/978-3-319-56015-1_160-1

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  • DOI: https://doi.org/10.1007/978-3-319-56015-1_160-1

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-56015-1

  • Online ISBN: 978-3-319-56015-1

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