No

Antianxiety Agent, Miscellaneous

Management of anxiety disorders (GAD)

B

Hypersensitivity to buspirone or any component

Safety and efficacy not established in children <18 years of age; use in hepatic or renal impairment is not recommended; does not prevent or treat withdrawal from benzodiazepines. Low potential for cognitive or motor impairment. Use with monoamine oxidase inhibitors may result in hypertensive reactions.

>10%: Central nervous system: Dizziness

1% to 10%:

Central nervous system: Drowsiness, EPS, serotonin syndrome, confusion, nervousness, lightheadedness, excitement, anger, hostility, headache

Dermatologic: Rash

Gastrointestinal: Diarrhea, nausea

Neuromuscular & skeletal: Muscle weakness, numbness, paresthesia, incoordination, tremor

Ocular: Blurred vision, tunnel vision

Miscellaneous: Diaphoresis, allergic reactions

Symptoms of overdose include dizziness, drowsiness, pinpoint pupils, nausea, vomiting

There is no known antidote for buspirone, treatment is supportive

CYP3A3/4 enzyme substrate

Erythromycin, clarithromycin, itraconazole, ketoconazole, and grapefruit juice may result in large increases in buspirone concentrations (dizziness, sedation)

Enzyme inducers (carbamazepine, rifampin) may reduce serum concentrations of buspirone resulting in loss of efficacy

Buspirone should not be used concurrently with an MAO inhibitor due to reports of increased blood pressure

Diltiazem and verapamil may increase serum concentrations of buspirone; consider a dihydropyridine calcium channel blocker

The mechanism of action of buspirone is unknown. Buspirone has a high affinity for serotonin 5HT1a and 5HT2 receptors, without affecting benzodiazepine-GABA receptors; buspirone has moderate affinity for dopamine D₂ receptors

Peak serum concentration: Within 1 hour

Protein binding: 86%

Metabolism: In the liver by oxidation and undergoes extensive first-pass metabolism

Half-life: 2-3 hours

Time to peak serum concentration: Oral: Within 40-60 minutes

Adults: Oral: 15 mg/day (7.5 mg twice daily); may increase in increments of 5 mg/day every 2-4 days to a maximum of 60 mg/day; target dose for most people is 30 mg/day (15 mg twice daily)

Food may decrease the absorption of buspirone, but it may also decrease the first-pass metabolism, thereby increasing the bioavailability of buspirone

Mental status, symptoms of anxiety; monitor for benzodiazepine withdrawal

AST, ALT, growth hormone(s), prolactin (S)

No information available to require special precautions

No effects or complications reported

Take only as directed; do not increase dose or take more often than prescribed. May take 2-3 weeks to see full effect; do not discontinue without consulting prescriber. Do not use excessive alcohol or other prescription or OTC medications (especially pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, lightheadedness, impaired coordination, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or upset stomach, nausea (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report persistent vomiting, chest pain or rapid heartbeat, persistent CNS effects (eg, confusion, restlessness, anxiety, insomnia, excitation, headache, dizziness, fatigue, impaired coordination), or worsening of condition. Breast-feeding precautions: Breast-feeding is not recommended.

Monitor mental status

Tablet, as hydrochloride: 5 mg, 7.5 mg, 10 mg, 15 mg

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