Pharm

Buspirone

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Buspirone, Buspar

  • See Also
  1. Anxiety Disorder
  2. Buspirone Toxicity
  • Indications
  1. Anxiety Disorders
    1. Generalized Anxiety Disorder
    2. Chronic Anxiety Disorder
    3. Anxiety in the elderly
  2. Aggression in developmentally disabled
  3. Agitated Dementia
  4. Emotional behavioral problems in brain injury
  5. Geriatric Depression
  6. Adjunctive use with SSRI in Major Depression
    1. Mixed anxiety and depression
    2. Enhance Major Depression response to SSRI
    3. Antidepressant Induced Sexual Dysfunction
  7. Alcohol Withdrawal
    1. Reduces anxiety of "needing" a drink
  8. Obsessive Compulsive depression
    1. Use Buspar with Prozac
  9. Decreases Neuroleptic adverse effects
    1. Reduces Tardive Dyskinesia
    2. Reduces Akathisia
    3. Reduces Parkinsonism
  • Mechanism
  1. Buspirone is an azapirone that modulates Serotonin transmission
  2. Partial 5-HT1A Serotonin receptor Agonist
    1. Risk of Serotonin Syndrome
  3. Partial D2 Dopamine Receptor
    1. Risk of Akathisia
  • Dosing
  1. Start: 7.5 mg PO bid (or 5 mg PO tid)
  2. Effective dose: 20 to 30 mg per day
  3. Maximum: 60 mg per day
  • Advantages (compared with Benzodiazepines)
  1. Non-addictive
  2. Less Sedation
  3. No associated memory Impairment
  4. No significant withdrawal syndrome
  5. Minimal Overdose potential
  6. No Anticholinergic Toxicity
  7. Well tolerated by elderly patients
  8. Does not affect GABA levels
  • Disadvantages (compared with Benzodiazepines)
  1. Slow onset of action (takes 2-4 weeks until effect)
  2. Not useful in Panic Attacks
  3. No Sedative effect
  4. Requires repeat dosing 2-3 times per day
  • Precautions
  1. Avoid use in pregnancy and Lactation
  2. Avoid in hepatic or renal Impairment
  • Adverse Effects
  1. Dizziness or Light Headedness
    1. Onset within 30 minutes of ingestion
    2. Duration less than 20 minutes
  2. Mild Headache
  3. Nausea
  4. Nervousness
  5. Insomnia
  • Pharmacokinetics
  1. Low oral Bioavailability (<5%)
  2. Half-Life: 2 to 3 hours
  3. Peaks: 0.9 to 1.5 hours after ingestion
  • Drug Interactions
  1. Metabolized by CYP3A4
  2. MAO Inhibitors
  3. Haloperidol (Haldol)
  4. Cyclosporine (Sandimmune)
  5. Disulfiram (Antabuse)
  6. Erythromycin and Itraconazole suppresses p450
    1. Results in Buspirone levels 5-13 times normal
  1. Convert short-acting Benzodiazepine to long-acting
    1. Example: Alprazolam to Clonazepam
  2. Start Buspirone at above doses
  3. Taper long-acting Benzodiazepine over 60 to 90 days
  • Resources
  1. Buspirone Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0eefdd8d-7745-47ae-a204-f35687f3db11
  • References
  1. Wilson (2023) Buspirone, StatPearls, Treasure Island, FL
    1. https://www.ncbi.nlm.nih.gov/books/NBK531477/
  2. (1997) Clin Pharmacol Ther, 32:348 [PubMed]
  3. Cadieux (1996) Am Fam Physician 53(7): 2349-53 [PubMed]