Buspirone (Buspar) Flashcards

Study Notes

Drug Class

Buspirone is classified as an antianxiety medication.

Route of Administration

Administered orally.

Dosing Information

Anxiety:
- Initial dose: 7.5 mg taken orally twice daily.
- Titration: Increase by 5 mg/day every 2 to 3 days as needed.
- Typical dose range: 20 to 30 mg daily, in 2 to 3 divided doses.
- Maximum allowed dose: 60 mg/day.
Depression:
- Starting dose: 5 mg orally three times daily, increasing by 5 to 10 mg every 2 to 3 days up to 90 mg/day (40 mg/day frequently associated with response).
- Geriatric dosing: Start with 10 mg orally twice a day; adjust as tolerated to a maximum of 60 mg/day.

Renal Failure Dosage Adjustments

Severe renal impairment: Not recommended to use.
Anuric patients: Reduce dose by 25% to 50%.
Mild to moderate impairment: No dose adjustment necessary.

Primary Uses

Indicated for the treatment of anxiety.

Administration Guidelines

Consistent oral intake with or without food is necessary.
Store Ambien at room temperature (25°C or 77°F) with acceptable range between 15 and 30°C (59 and 86°F).

Precautions

Avoid use with alcohol, MAO inhibitors, or excessive grapefruit juice.
Not recommended for those with severe hepatic impairment.
Gradual withdrawal of CNS-depressant drugs is advisable before starting buspirone.
Severe renal impairment is a contraindication for use.

Common Adverse Effects

May cause dizziness, nausea, headache, nervousness, lightheadedness, drowsiness, blurred vision, restlessness, dry mouth, upset stomach, stuffy nose, sore throat, tinnitus, excitement, and insomnia.

Drug Interactions

Contraindicated with MAO inhibitors if taken within the last 14 days; can lead to dangerous interactions.

Monitoring Efficacy

Improvement in anxiety symptoms suggests drug efficacy.
Continuous evaluation is recommended with extended use beyond 3 to 4 weeks.

Mechanism of Action

Buspirone’s exact mechanism is unknown; however, it has high affinity for serotonin (5-HT1A) receptors and moderate affinity for D2-dopamine receptors without affecting benzodiazepine receptors or GABA binding.

Pharmacokinetics

Absorption: Peak concentration is reached in 40 to 90 minutes; bioavailability around 90%.
Effects of Food: Food can increase AUC and Cmax significantly.
Distribution: Approximately 86% protein bound.
Metabolism: Hepatically metabolized (CYP3A4) with extensive first-pass effects; produces an active metabolite known as 1-pyrimidinylpiperazine (1-PP).
Excretion: 18% to 38% excreted in feces; 29% to 63% excreted renally mainly as metabolites.
Elimination Half-Life: Ranges from 2 to 3 hours; prolonged in cases of hepatic or renal dysfunction.

Medication Counseling

Advise patients to avoid activities requiring alertness until drug effects are known.
Educate about side effects such as dizziness, confusion, and blurred vision.
Consistent dosing with or without food is essential, along with avoiding alcohol and excessive grapefruit juice.
Emphasize the importance of consulting healthcare professionals before taking new medications, including over-the-counter and herbal options.

Description

Test your knowledge about Buspirone, an antianxiety medication. These flashcards cover essential information including drug class, administration routes, and dosing recommendations. Perfect for students and healthcare professionals alike!