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BusPIRone


Pronunciation

 (byoo SPYE rone)


U.S. Brand Names

 BuSpar®


Synonyms

 Buspirone Hydrochloride


Generic Available

 Yes


Canadian Brand Names

 Apo-Buspirone®; BuSpar®; Buspirex; Gen-Buspirone; Lin-Buspirone; Novo-Buspirone; Nu-Buspirone; PMS-Buspirone


Use

 Management of generalized anxiety disorder (GAD)


Use - Unlabeled/Investigational

 Management of aggression in mental retardation and secondary mental disorders; major depression; potential augmenting agent for antidepressants; premenstrual syndrome


Pregnancy Risk Factor

 B


Lactation

 Excretion in breast milk unknown/not recommended


Contraindications

 Hypersensitivity to buspirone or any component of the formulation


Warnings/Precautions

 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 MAO inhibitors may result in hypertensive reactions.


Adverse 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


Overdosage/Toxicology

 Symptoms of overdose include dizziness, drowsiness, pinpoint pupils, nausea, and vomiting. There is no known antidote for buspirone. Treatment is supportive.


Drug Interactions

 Substrate of CYP2D6 (minor), 3A4 (major)

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

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of buspirone. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of buspirone. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

MAO inhibitors: Buspirone should not be used concurrently with an MAO inhibitor due to reports of increased blood pressure; includes classic MAO inhibitors and linezolid (due to ability to inhibit MAO)

Nefazodone: Concurrent use may increase risk of CNS adverse events. Limit buspirone initial dose (eg, 2.5 mg/day).

Selegiline: Theoretically, risk of interaction with selective MAO type B inhibitor would be less than with nonselective inhibitors; however, this combination is generally best avoided

SSRIs: Concurrent use of buspirone with SSRIs may cause serotonin syndrome. Some SSRIs may increase buspirone serum concentrations (see CYP3A4 inhibitors). Buspirone may increase the efficacy of fluoxetine in some patients; however, the anxiolytic activity of buspirone may be lost when combined with SSRIs (fluoxetine).

Trazodone: Concurrent use of buspirone with trazodone may cause serotonin syndrome


Ethanol/Nutrition/Herb Interactions

Ethanol: Ethanol (may increase CNS depression).

Food: Food may decrease the absorption of buspirone, but it may also decrease the first-pass metabolism, thereby increasing the bioavailability of buspirone. Grapefruit juice may cause increased buspirone concentrations; avoid concurrent use.

Herb/Nutraceutical: St John's wort may decrease buspirone levels or increase CNS depression. Avoid valerian, gotu kola, kava kava (may increase CNS depression).


Mechanism of Action

 The mechanism of action of buspirone is unknown. Buspirone has a high affinity for serotonin 5-HT1A and 5-HT2 receptors, without affecting benzodiazepine-GABA receptors; buspirone has moderate affinity for dopamine D2 receptors


Pharmacodynamics/Kinetics

Absorption: Oral: ~100%

Distribution: Vd: 5.3 L/kg

Protein binding: 95%

Metabolism: Hepatic via oxidation; extensive first-pass effect

Bioavailability: ~4%

Half-life elimination: Mean: 2.4 hours (range: 2-11 hours)

Time to peak, serum: Within 0.7-1.5 hours

Excretion: Urine: 65%; feces: 35%; ~1% dose excreted unchanged


Dosage

 Oral:

Generalized anxiety disorder:

Children and Adolescents: Initial: 5 mg daily; increase in increments of 5 mg/day at weekly intervals as needed, to a maximum dose of 60 mg/day divided into 2-3 doses

Adults: 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)

Dosing adjustment in renal or hepatic impairment: Buspirone is metabolized by the liver and excreted by the kidneys. Patients with impaired hepatic or renal function demonstrated increased plasma levels and a prolonged half-life of buspirone. Therefore, use in patients with severe hepatic or renal impairment cannot be recommended.


Monitoring Parameters

 Mental status, symptoms of anxiety


Patient Education

 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 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 precaution: Breast-feeding is not recommended.


Additional Information

 Has shown little potential for abuse; needs continuous use. Because of slow onset, not appropriate for "as needed" (prn) use or for brief, situational anxiety. Ineffective for treatment of benzodiazepine or ethanol withdrawal.


Anesthesia and Critical Care Concerns/Other Considerations

 Takes 2-3 weeks for full effect. Because of slow onset, not appropriate for "as needed" (prn) use or for brief, situational anxiety; not effective for severe anxiety; does not show cross-tolerance with benzodiazepines or other sedatives; less sedating than other anxiolytics; has shown little potential for abuse; needs continuous use; ineffective for benzodiazepine or ethanol withdrawal


Dental Health: Effects on Dental Treatment

 Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

 No information available to require special precautions


Mental Health: Child/Adolescent Considerations

 Anxiety disorders: One pilot study of 15 children, 6-14 years of age (mean: 10 years), with mixed anxiety disorders, used initial doses of 5 mg/day; doses were individualized with increases in increments of 5 mg/day weekly as needed, to a maximum dose of 20 mg/day divided into 2 doses (mean dose required: 18.6 mg/day). Some authors (Carrey, 1996 and Kutcher, 1992), based on their clinical experience, recommend higher doses. Open-label study in 25 prepubertal inpatients (mean age: 8 years) with anxiety symptoms and moderately-aggressive behavior utilized a mean optimal dose of 28 mg/day (Pfeffer, 1997). Dosages ranging from 15-45 mg/day were utilized in children 6-17 years of age with pervasive developmental disorders (Buitelaar, 1998). The safety and efficacy of buspirone were evaluated in two placebo-controlled 6-week trials involving a total of 559 pediatric patients (6-17 years of age) with generalized anxiety disorder (GAD). Doses studied were 7.5-30 mg twice daily (15-60 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 (Bristol-Myers Squibb, BuSpar® package labeling, July 2001).

Buitelaar JK, van der Gaag RJ, and van der Hoeven J, "Buspirone in the Management of Anxiety and Irritability in Children With Pervasive Developmental Disorders: Results of an Open-Label Study," J Clin Psychiatry , 1998, 59(2):56-9.

Carrey NJ, Wiggins DM, and Milin RP, "Pharmacological Treatment of Psychiatric Disorders in Children and Adolescents," Drugs , 1996, 51(5):750-9.

Kutcher SP, Reiter S, Gardner DM, et al, "The Pharmacotherapy of Anxiety Disorders in Children and Adolescents," Psychiatr Clin North Am , 1992, 15(1):41-67.

Pfeffer CR, Jiang H, and Domeshek LJ, "Buspirone Treatment of Psychiatrically Hospitalized Prepubertal Children With Symptoms of Anxiety and Moderately Severe Aggression," J Child Adolesc Psychopharmacol , 1997, 7(3):145-55.


Dosage Forms

 Tablet, as hydrochloride: 5 mg, 7.5 mg, 10 mg, 15 mg, 30 mg

BuSpar®: 5 mg, 10 mg, 15 mg, 30 mg


References

Buitelaar JK, van der Gaag RJ, and van der Hoeven J, "Buspirone in the Management of Anxiety and Irritability in Children With Pervasive Developmental Disorders: Results of an Open-Label Study," J Clin Psychiatry , 1998, 59(2):56-9.

Carrey NJ, Wiggins DM, and Milin RP, "Pharmacological Treatment of Psychiatric Disorders in Children and Adolescents," Drugs , 1996, 51(5):750-9.

Fanciullacci M, Sicuteri R, Alessandri M, et al, "Buspirone, But Not Sumatriptan, Induces Miosis in Humans: Relevance for a Serotoninergic Pupil Control," Clin Pharmacol Ther , 1995, 57(3):349-55.

Gammans RE, Westrick ML, Shea JP, et al, "Pharmacokinetics of Buspirone in Elderly Subjects," J Clin Pharmacol , 1989, 29(1):72-8.

Goetz CM, Krenzelok EP, Lopez G, et al, "Buspirone Toxicity: A Prospective Study," Vet Hum Toxicol , 1989, 31:371.

Green WH, Child and Adolescent Clinical Psychopharmacology , 3rd ed, Philadelphia, PA: Lippincott Williams & Wilkins, 2001.

Hanna GL, Feibusch EL, and Albright KJ, "Buspirone Treatment of Anxiety, Associated With Pharyngeal Dysphagia in a Four-Year Old," J Child Adolesc Psychopharmacol , 1997, 7(2):137-43.

Kivisto KT, Lamberg TS, and Kantola T, "Plasma Buspirone Concentrations Are Greatly Increased by Erythromycin and Itraconazole," Clin Pharmacol Ther , 1997, 62(3):348-54.

Kunik ME, Yudofsky SC, Silver JM, et al, "Pharmacologic Approach to Management of Agitation Associated With Dementia," J Clin Psychiatry , 1994, 55(Suppl 2):13-7.

Kutcher SP, Reiter S, Gardner DM, et al, "The Pharmacotherapy of Anxiety Disorders in Children and Adolescents," Psychiatr Clin North Am , 1992, 15(1):41-67.

Lejoyeux M, et al, "Serotonin Syndrome: Incidence, Symptoms, and Treatment," CNS Drugs , 1994, 2:132-43.

McIvor RJ and Sinanan K, "Buspirone-Induced Mania," Br J Psychiatry , 1991, 158:136-7.

Norden MJ, "Buspirone Treatment of Sexual Dysfunction Associated With Selective Serotonin Re-Uptake Inhibitors," Depression , 1994, 2:109-12.

Pfeffer CR, Jiang H, and Domeshek LJ, "Buspirone Treatment of Psychiatrically Hospitalized Prepubertal Children With Symptoms of Anxiety and Moderately Severe Aggression," J Child Adolesc Psychopharmacol , 1997, 7(3):145-55.

Preskorn SH, "Recent Pharmacologic Advances in Antidepressant Therapy for the Elderly," Am J Med , 1993, 94(5A):2S-12S.

Schweizer E and Rickels K, "New and Emerging Clinical Uses for Buspirone," J Clin Psychiatry Monograph , 1994, 12(1):46-54.

Simeon JG, Knott VJ, DuBois C, et al, "Buspirone Therapy of Mixed Anxiety Disorders in Childhood and Adolescence: A Pilot Study," J Child Adolesc Psychopharmacol , 1994, 4(3):159-70.

Soni P and Weintraub AL, "Buspirone-Associated Mental Status Changes," J Am Acad Child Adolesc Psychiatry , 1992, 31(6):1098-9.

Sussman N, "The Usage of Buspirone in Psychiatry," J Clin Psychiatry Monograph , 1994, 12(1):3-19.

Tiller JW, Burrows GD, and O'Sullivan BT, "Buspirone Overdose," Med J Aust , 1989, 150(1):54-5.

Weis KJ, "Management of Anxiety and Depression Syndromes in Elderly," J Clin Psychiatry , 1994, 55(Suppl 2):5-12.


International Brand Names

 Ansial® (AR); Ansitec® (BR); Anxiolan® (TH); Anxiron® (CZ, HU, YU); Anxut® (DE); Apo-Buspirone® (CA); Axoren® (IT); Bespar® (DE); Busansil® (PT); Buscalma® (PT); Buscalm® (IN); Buspanil® (BR); Buspar® (AT, AU, BE, BR); BuSpar® (CA); Buspar® (CH, CN, DK, ES, FI, FR, GB, HR, ID, IE, IT, LU, NL, NO, NZ, PT, RO, SE, ZA); Busp® (DE); Buspirex (CA); Buspirol® (IL); Buspirona® (CR); Buspiron Alpharma® (DK, FI, SE); Buspiron® (CZ, NO); Buspirone® (CY, NZ, PL); Buspirone Hydrochloride® (GB); Buspiron NM Pharma® (SE); Buspon® (TR); Buxal® (PL); Effiplen® (ES); Gen-Buspirone (CA); Lin-Buspirone (CA); Mabuson® (PL); Neurosine® (MX); Novo-Buspirone (CA); Nu-Buspirone (CA); Pacific Buspirone® (NZ); Pasrin-10® (ZA); Paxon® (CL); PMS-Buspirone (CA); Relax® (DO, EC); Sorbon® (IL); Spamilan® (PL); Spitomin® (HU, RO); Stressigal® (RO); Tensispes® (RO); Tran-Q® (ID); Xiety® (ID)


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