Drug Guide
Buspirone Hydrochloride
Classification
Therapeutic: Anxiolytic
Pharmacological: Serotonergic agent
FDA Approved Indications
- Generalized Anxiety Disorder (GAD)
Mechanism of Action
Buspirone acts as a partial agonist at 5-HT1A serotonergic receptors, leading to anxiolytic effects without significant sedation or dependence.
Dosage and Administration
Adult: Start with 15 mg per day in two or three divided doses. Dose may be increased by 5 mg at intervals of 2 or more days, up to a maximum of 60 mg/day. Adjustments should be made based on clinical response and tolerability.
Pediatric: Safety and effectiveness in pediatric patients have not been established.
Geriatric: Start with lower doses (e.g., 7.5 mg twice daily). Monitor closely due to potential for increased sensitivity.
Renal Impairment: Adjust dosage as needed; no specific guidelines established. Evaluate renal function regularly.
Hepatic Impairment: Use with caution; start with lower doses and titrate carefully.
Pharmacokinetics
Absorption: Rapidly absorbed with peak plasma concentrations in about 1 hour.
Distribution: Widely distributed; low protein binding (~7%).
Metabolism: Primarily hepatic via CYP3A4 to inactive metabolites.
Excretion: Renal excretion of unchanged drug and metabolites.
Half Life: Approximately 2-3 hours.
Contraindications
- Hypersensitivity to buspirone
- Use with monoamine oxidase inhibitors (MAOIs) within 14 days.
Precautions
- Use with caution in patients with hepatic or renal impairment. Monitor for serotonin syndrome, especially if used with other serotonergic agents. Avoid grapefruit juice, which can increase buspirone levels.
Adverse Reactions - Common
- Dizziness (Common)
- Nausea (Common)
- Headache (Common)
- Nervousness (Common)
Adverse Reactions - Serious
- Serotonin syndrome (including agitation, hallucinations, coma) (Rare)
- Extrapyramidal symptoms (Rare)
- Priapism (Very rare)
Drug-Drug Interactions
- Concomitant use with SSRIs, MAOIs, or other serotonergic agents increases risk of serotonin syndrome.
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) can increase buspirone levels.
Drug-Food Interactions
- Grapefruit juice may increase plasma concentrations of buspirone.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for effectiveness in reducing anxiety symptoms and for adverse effects.
Diagnoses:
- Risk for falls due to dizziness
- Anxiety related to underlying condition or medication side effects.
Implementation: Administer consistently, avoid sudden discontinuation, and educate patients on limitations of use, including that it may take several weeks for full therapeutic effect.
Evaluation: Assess reduction in anxiety symptoms and monitor for adverse reactions.
Patient/Family Teaching
- Take medication regularly as prescribed.
- Do not suddenly stop medication without consulting a healthcare provider.
- Report any signs of serotonin syndrome, unusual mood changes, or worsening symptoms.
- Limit grapefruit juice during treatment.
Special Considerations
Black Box Warnings: N/A
Genetic Factors: No specific genetic considerations noted.
Lab Test Interference: No significant interference reported.
Overdose Management
Signs/Symptoms: Dizziness, drowsiness, confusion, agitation.
Treatment: Supportive care; no specific antagonist. Activated charcoal may be considered if ingestion is recent. Cite medical attention immediately.
Storage and Handling
Storage: Store at room temperature, away from moisture, heat, and light.
Stability: Stable for at least 2 years when properly stored.