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Buspar (Discontinued), Buspirone
Management of Disorders or Short-Term Relief of Symptoms:Initial: 7.5mg bidTitrate: May increase by 5mg/day at intervals of 2-3 days, prnUsual: 20-30mg/day in divided dosesMax: 60mg/day
Periodically reassess usefulness of drug if used for extended periods
Renal ImpairmentSevere: Not recommended
Hepatic ImpairmentSevere: Not recommended
Take in a consistent manner w/ regard to the timing of dosing; either always w/ or always w/o food
Tab: 5mg*, 7.5mg*, 10mg*, 15mg*, 30mg* *scored
Hypersensitivity to buspirone HCl.
May impair mental/physical abilities. Does not exhibit cross-tolerance with benzodiazepines and other common sedatives/hypnotics; before starting therapy, withdraw gradually from prior treatment, especially in patients using a CNS depressant chronically. May cause acute and chronic changes in dopamine-mediated neurological function; syndrome of restlessness, appearing shortly after initiation, reported. May interfere with urinary metanephrine/catecholamine assay; d/c therapy for at least 48 hrs prior to undergoing urine collection for catecholamines. Not recommended with severe hepatic/renal impairment.
Dizziness, nausea, headache, nervousness, lightheadedness, excitement, drowsiness, fatigue, insomnia, dry mouth.
See Dosage. Elevated BP reported with MAOI; avoid concomitant use. Avoid with alcohol. Dizziness, headache, nausea, and increased nordiazepam reported with diazepam. May increase serum concentrations of haloperidol. ALT elevations reported with trazodone. Caution with CNS-active drugs. CYP3A4 inhibitors (eg, diltiazem, ketoconazole, ritonavir) may increase concentrations; may require dose adjustment. CYP3A4 inducers (eg, dexamethasone, phenytoin, rifampin), including potent inducers, may decrease concentrations; may require dose adjustment of buspirone. Avoid with large amounts of grapefruit juice. Nefazodone may decrease concentrations of metabolite 1-pyrimidinylpiperazine (1-PP). May increase levels of nefazodone. Cimetidine may increase Cmax and Tmax. Prolonged PT reported with warfarin. May displace less firmly bound drugs like digoxin.
Category B, not for use in nursing.
Atypical anxiolytic; has not been established. Has a high affinity to 5-HT1A receptors and moderate affinity for brain D2-dopamine receptors; may have indirect effects on other neurotransmitter systems.
Absorption: Rapid. (20mg, single dose) Cmax=1-6ng/mL; Tmax=40-90 min. Distribution: Plasma protein binding (86%). Metabolism: Liver (extensive 1st-pass), primarily by oxidation via CYP3A4, and by hydroxylation; 1-PP (active metabolite). Elimination: Urine (29-63%), feces (18-38%); (10-40mg, single dose) T1/2=2-3 hrs.
Assess for hypersensitivity to drug, hepatic/renal impairment, pregnancy/nursing status, and possible drug interactions.
Monitor for CNS effects, syndrome of restlessness, and other adverse reactions. Periodically reassess usefulness of drug if used for extended periods.
Instruct to inform physician about any medications, prescription or nonprescription, alcohol, or drugs patient is taking or planning to take, and if patient is pregnant/breastfeeding, becomes pregnant, or is planning to become pregnant. Advise not to drive a car or operate potentially dangerous machinery until effects have been determined. Instruct to avoid drinking large amounts of grapefruit juice.
(5mg, 10mg, 15mg, 30mg) 20-25°C (68-77°F). (7.5mg) 25°C (77°F); excursions permitted between 15-30°C (59-86°F).