Pronunciation: byoo-SPY-rone HIGH-droe-KLOR-ide
Class: Antianxiety agent
- Tablets 5 mg
- Tablets 7.5 mg
- Tablets 10 mg
- Tablets 15 mg
- Tablets 30 mg
CO Buspirone (Canada)
Mechanism unknown; does not exert anticonvulsant or muscle relaxant effects.
Rapidly absorbed. C max is 1 to 6 mg/mL. T max is 40 to 90 min.
About 86% bound to plasma proteins.
Extensive first-pass metabolism. Primarily metabolized by oxidation (which is mediated by CYP3A4) to active metabolite.
Within 24 h, 29% to 63% excreted in urine, primarily as metabolites; 18% to 38% is excreted in feces. The t ½ is about 2 to 3 h.
Special PopulationsRenal Function Impairment
AUC increased 4-fold.Hepatic Function Impairment
AUC increased 13-fold.
Indications and Usage
Treatment of anxiety disorders; short-term relief of anxiety symptoms.
Reduction of symptoms of PMS.
Dosage and AdministrationAdults Initial dose
PO 7.5 mg twice daily; may increase by 5 mg/day every 2 to 3 days as needed (max, 60 mg/day in divided doses).
Store tablets below 86°F.
Dizziness, headache, and nausea can occur.Fluoxetine
Buspirone effects may be decreased. Paradoxical worsening of obsessive-compulsive disorder (OCD) may occur.Haloperidol
Buspirone may increase haloperidol plasma levels.Inducers of CYP3A4 (eg, carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin)
May reduce buspirone plasma levels, decreasing the therapeutic effect.Inhibitors of CYP3A4 (eg, diltiazem, erythromycin, grapefruit juice, itraconazole, ketoconazole, nefazodone, ritonavir, verapamil)
May elevate buspirone plasma levels, increasing the pharmacologic and adverse effects.MAOIs (eg, isocarboxazid)
Risk of elevated BP may be increased. Do not administer buspirone with or within 14 days of MAOI administration.Nefazodone
If used with buspirone, a low dose (eg, 2.5 mg/day) is recommended.Trazodone
ALT may be elevated.
Laboratory Test Interactions
None well documented.
Chest pain (at least 1%); tachycardia/palpitations (1%).
Dizziness (12%); drowsiness (10%); headache (6%); nervousness (5%); lightheadedness (3%); excitement, numbness, anger/hostility, confusion, weakness (2%); paresthesia, incoordination, tremor (1%); dream disturbances (at least 1%); cogwheel rigidity, dizziness, dystonic reactions, ataxia, extrapyramidal effects, dyskinesias (acute and tardive), emotional lability, serotonin syndrome, difficulty in recall (postmarketing).
Skin rash, sweating/clamminess (1%); ecchymosis (postmarketing).
Blurred vision (2%); tinnitus, sore throat, nasal congestion (at least 1%); visual changes (postmarketing).
Nausea (8%); diarrhea (2%).
Urinary retention (postmarketing).
Allergic reactions (including urticaria), angioedema (postmarketing).
Category B .
Undetermined. Breast-feeding should be avoided.
The safety and efficacy of buspirone were evaluated in 2 placebo-controlled, 6-wk trials involving a total of 559 pediatric patients (ranging from 6 to 17 yr of age) with generalized anxiety disorder (GAD). Doses studied were 7.5 to 30 mg twice daily (15 to 60 mg/day). There were no significant differences between buspirone and placebo with regard to the symptoms of GAD following doses recommended for the treatment of GAD in adults. Pharmacokinetic studies have shown that, for identical doses, plasma exposure to buspirone and its active metabolite, 1-PP, are equal to or higher in pediatric patients than adults. No unexpected safety findings were associated with buspirone in these trials. There are no long-term safety or efficacy data in this population.
Administration of buspirone not recommended.
Administration of buspirone not recommended.
Nausea, vomiting, dizziness, drowsiness, miosis, gastric distress.
- Advise patient or caregiver to read the patient information leaflet before starting therapy and with each refill.
- Advise patient that medication is usually started at a low dose and then gradually increased until max benefit is obtained.
- Advise patient that medication must be taken daily as prescribed in order to obtain max benefit and not to use on an as needed basis.
- Advise patient to take each dose consistently either with or without food.
- Caution patient to avoid grapefruit and grapefruit juice while taking this medication.
- Caution patient to take as prescribed and not to stop taking or change the dose unless advised by health care provider.
- Advise patient that if a dose is missed to skip that dose and take the next dose at the regularly scheduled time. Caution patient to never take 2 doses at the same time.
- Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
- Instruct patient to contact health care provider if symptoms do not appear to be getting better, are getting worse, or if bothersome side effects (eg, drowsiness, dizziness) occur.
- Advise patient that drug may cause drowsiness or dizziness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
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