II. 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

III. 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

IV. 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

V. 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

VI. 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

VII. Precautions

  1. Avoid use in pregnancy and Lactation
  2. Avoid in hepatic or renal Impairment

VIII. 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

IX. Pharmacokinetics

  1. Low oral Bioavailability (<5%)
  2. Half-Life: 2 to 3 hours
  3. Peaks: 0.9 to 1.5 hours after ingestion

X. 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

XI. Management: Protocol to convert from Benzodiazepine to Buspirone

  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

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Related Studies

Cost: Medications

buspirone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
BUSPIRONE HCL 10 MG TABLET Generic $0.04 each
BUSPIRONE HCL 15 MG TABLET Generic $0.05 each
BUSPIRONE HCL 30 MG TABLET Generic $0.17 each
BUSPIRONE HCL 5 MG TABLET Generic $0.03 each
BUSPIRONE HCL 7.5 MG TABLET Generic $0.16 each

Ontology: Buspirone (C0006462)

Definition (NCI_NCI-GLOSS) A drug that is used to treat certain anxiety disorders. It belongs to the family of drugs called antianxiety agents.
Definition (NCI) An anxiolytic agent chemically and pharmacologically unrelated to benzodiazepines, barbiturates, or other sedative/hypnotic drugs. Although its exact mechanism of action is unknown, buspirone may exert its anti-anxiety effects via serotonin (5-HT1A) and dopamine receptors (D2) and may indirectly affect other neurotransmitter systems. Unlike typical benzodiazepine anxiolytics, this agent does not exert anticonvulsant or muscle relaxant effects and lacks prominent sedative effects.
Definition (MSH) An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.
Definition (CSP) 8-(4-(2-pyrimidinyl)-1-piperazinyl) butyl-8-azaspirodecane-7,9- dione; serotonergic tranquilizer frequently contrasted with benzodiazepine-type, GABAergic tranquilizers.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002065
SnomedCT 387523009, 91452003
LNC LP17859-7, MTHU024715
English Buspirone, N-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1-cyclopentanediacetamide, 8-Azaspiro(4.5)decane-7,9-dione, 8-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-, buspirone (medication), Buspirone [Chemical/Ingredient], BUSPIRONE, busPIRone, buspirone, Buspirone (product), Buspirone (substance)
Swedish Buspiron
Czech buspiron
Finnish Buspironi
Russian BUSPIRON, БУСПИРОН
Japanese ブスピロン
Polish Buspiron
Spanish buspirona (producto), buspirona (sustancia), buspirona, Buspirona
French Buspirone
German Buspiron
Italian Buspirone
Portuguese Buspirona

Ontology: Buspar (C0600122)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002065
English BuSpar, buspar, Bespar, Bristol Myers Brand of Buspirone Hydrochloride, Bristol Myers Squibb Brand of Buspirone Hydrochloride, Bristol-Myers Brand of Buspirone Hydrochloride, Bristol-Myers Squibb Brand of Buspirone Hydrochloride, Hormosan Brand of Buspirone Hydrochloride, UPSA Brand of Buspirone Hydrochloride, Buspar