- Generic name: Buspirone
- Trade names: Buspar, Buspirex, Vanspar
- Pharmacologic category: Antianxiety, Anxiolytic, Azapirones
- Manufacturer: Bristol Myers SQUIBB
- FDA approved: September 29, 1986
- Pregnancy category: B
- Habit forming? Probably not
Medical uses
Buspirone is a psychotropic drug with anxiolytic properties which belongs chemically to the class of azaspirodecanediones. It is mainly used for mild-to-moderate generalized anxiety disorder, but not for other anxiety disorders. Buspirone may be ineffective for panic attacks and usually is not used for tension caused by the stress of everyday life.
Buspirone may help to feel less nervous and irritable, and may control symptoms such as trouble sleeping, sweating, and pounding heartbeat. This
drug has slow onset of action and works gradually over a two to four week period.
Buspirone may reduce anger and aggression and appears to be less likely than benzodiazepines to cause disinhibition.
Pharmacological characteristics
- Absorption: rapidly and almost completely absorbed from the GI tract.
- Elimination half-life: 2.4 hours (range: 2-11 hours)
- Metabolism: Hepatic via oxidation; extensive first-pass effect
- Excretion: Urine: 65%; feces: 35%; about 1% excreted unchanged
Advantages
- Buspirone is not sedative, and it does not impair cognitive or motor performance.
- Not addictive, even with long-term use
- Virtually no withdrawal symptoms, even when the drug is discontinued quickly.
- Buspirone does not intensify the effects of CNS depressants
- Well tolerated by elderly people
- Low risk for drug interactions -- buspirone does not inhibit P450 enzymes.
Disadvantages
- Slow onset of action. The main disadvantage is that 1 to 3 weeks elapse before the anxiolytic
activity becomes evident.
- Mild efficacy. Buspirone has less anxiolytic efficacy than benzodiazepines and is usually reserved as an augmenting medication to treat anxiety.
- Potential for increased blood pressure.
- Due to a relatively short plasma half-life, buspirone requires multiple daily dosing, which may result in poor treament compliance.
- Grapefruit may increase the amount of buspirone in the bloodstream.
Unlabeled uses
- Management of aggression in mental retardation and secondary mental disorders
- Depression
- Augmenting agent for antidepressants
- Premenstrual syndrome4
- ADHD 6
- Bruxism (teeth grinding) 5
Buspirone for Anxiety
Generalized Anxiety Disorder
Buspirone has been used with moderate success in the treatment of Generalized Anxiety Disorder (GAD) but has not demonstrated utility in the potentially comorbid conditions that often accompany GAD.
Buspirone works better for patients with GAD who have not previously been treated with benzodiazepines7. Patients previously treated with benzodiazepines may respond less well to buspirone.
Buspirone is less effective than benzodiazepines in the treatment of anxiety3, 8 . Compared with the benzodiazepines, buspirone has no immediate effects, works slowly, and does not cause euphoria. It must be
taken consistently for at least 2 weeks to achieve an anti-anxiety effect and therefore cannot be used on an "as-needed" basis.
Dosage for Generalized Anxiety Disorder:
Initially, 10 - 15 mg daily in 2 or 3 divided doses. Increase dosage in increments of 5 mg daily every 2–4 days according to individual response up to 15–30 mg daily in 2 or 3 divided doses.
The maximal daily dosage is 45 mg in the United Kingdom and 60 mg in the United States.
Social Anxiety
Buspirone has modest efficacy in the treatment of social anxiety disorder (social phobia)1. Research suggest that buspirone may be useful in augmenting partial response to an SSRI2.
Other Anxiety Disorders
Because buspirone has a negligible potential for abuse, it is useful in persons whose anxiety coexists with alcoholism.
Mechanism of action
Buspirone, an azpirone derivative, has a high affinity for serotonin 5-HT1A and 5-HT2 receptors, without affecting benzodiazepine-GABA receptors. It has weak dopamine D2 receptors blocking action. Buspirone has NO no antipsychotic or extrapyramidal effects.
Its distinctive mechanism of action contributes towards a superior safety profile with generally more endurable side effects. Does not substantially impair psychomotor function, and produces only minor sedation (drowsiness or fatigue). As an anxiolytic it is approximately equivalent to diazepam.
Reviews, Discussions, Forums
References
- 1. Schneier FR, Saoud JB, Campeas R, Fallon BA, Hollander E, Coplan J, Liebowitz MR. Buspirone in social phobia. J Clin Psychopharmacol. 1993 Aug;13(4):251-6.
- 2. Van Ameringen M, Mancini C, Wilson C. Buspirone augmentation of selective serotonin reuptake inhibitors (SSRIs) in social phobia. J Affect Disord. 1996;39:115–21.
- 3. Enkelmann R. Alprazolam versus buspirone in the treatment of outpatients with generalized anxiety disorder. Psychopharmacology (Berl). 1991;105(3):428-32. PubMed
- 4. Nazari H, Yari F, Jariani M, Marzban A, Birgandy M. Premenstrual syndrome. Nazari H, Yari F, Jariani M, Marzban A, Birgandy M. Arch Gynecol Obstet. 2013
- 5. Bostwick JM, Jaffee MS. Buspirone as an antidote to SSRI-induced bruxism in 4 cases. J Clin Psychiatry. 1999 Dec;60(12):857-60 PubMed
- 6. Davari-Ashtiani R, Shahrbabaki ME, Razjouyan K, Amini H, Mazhabdar H. Buspirone versus methylphenidate in the treatment of attention deficit hyperactivity disorder: a double-blind and randomized trial. Child Psychiatry Hum Dev. 2010 Dec;41(6):641-8. PubMed
- 7. Chessick CA, Allen MH, Thase M, Batista Miralha da Cunha AB, Kapczinski FF, de Lima MS, dos Santos Souza JJ. Azapirones for generalized anxiety disorder. Cochrane Database Syst Rev. 2006 Jul 19;(3):CD006115. PubMed
- 8. 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 Jul;88(1):1-11.
By HealthyStock Research Group, September 2009
Medical resources reviewed: August 2018
