Clinical Overview
Buspirone is a non-benzodiazepine anxiolytic indicated for generalized anxiety disorder. It offers an alternative to benzodiazepines without the risks of dependence, withdrawal, or cognitive impairment, making it particularly suitable for long-term anxiety treatment and patients with substance abuse history.
Primary Clinical Applications
Buspirone is indicated specifically for generalized anxiety disorder and is often used as first-line treatment for chronic anxiety. It may be particularly beneficial for elderly patients, those with substance abuse history, or patients who need to maintain cognitive function while treating anxiety.
Mechanism and Clinical Benefits
Buspirone acts as a partial agonist at serotonin 5-HT1A receptors and has some activity at dopamine D2 receptors. Unlike benzodiazepines, it does not enhance GABA activity, resulting in anxiolytic effects without sedation, dependence potential, or cognitive impairment.
Clinical Considerations
Buspirone has a delayed onset of action (2-4 weeks for full effect) and does not provide immediate anxiety relief like benzodiazepines. It does not prevent benzodiazepine withdrawal and cannot be used for acute anxiety episodes. The medication requires consistent daily dosing and may cause initial dizziness or nausea.
Prescribing Information
Dosing & Administration
Generalized Anxiety Disorder – Adults:
- Initial: 7.5 mg twice daily (15 mg daily)
- Titration: Increase by 5 mg daily every 2-3 days
- Range: 20-60 mg daily in divided doses
- Maximum: 60 mg daily
- Typical effective dose: 30 mg daily
Elderly:
- Initial: 5 mg twice daily
- Titrate slowly based on response and tolerance
Administration:
- Take with food to improve absorption and reduce nausea
- Divide daily dose into 2-3 administrations
- Consistent timing each day
- Consistent food intake (always with or always without food)
Indications
- Management of generalized anxiety disorder
- Short-term relief of anxiety symptoms
Contraindications
- Hypersensitivity to buspirone
- Severe hepatic or renal impairment
- Use with MAOIs
Warnings & Precautions
- Delayed onset: 2-4 weeks for full anxiolytic effect
- Not for acute anxiety: Does not provide immediate relief
- Benzodiazepine withdrawal: Does not prevent or treat withdrawal symptoms
- Dizziness: May affect ability to drive or operate machinery
- Serotonin syndrome: Risk when combined with other serotonergic drugs
Drug Interactions
- MAOIs: Contraindicated – risk of hypertensive reactions
- CYP3A4 inhibitors: Significantly increase buspirone levels
- CYP3A4 inducers: May decrease buspirone effectiveness
- Grapefruit juice: Increases buspirone levels
- Serotonergic drugs: Theoretical risk of serotonin syndrome
Adverse Reactions
Common (≥5%):
- Dizziness, nausea, headache, nervousness
- Lightheadedness, excitement
Less Common:
- Drowsiness, fatigue, insomnia, dry mouth
Advantages:
- No dependence potential, no withdrawal syndrome
- No cognitive impairment, minimal sedation
Special Populations
- Hepatic Impairment: Reduce dose by 50% for moderate impairment
- Renal Impairment: Reduce dose by 25-50% for moderate-severe impairment
- Elderly: Start with lower doses, titrate slowly
- Pregnancy: Category B – generally considered safe
- Food effects: Take consistently with regard to food