BUSPIRONE

 

• A. 27.5 +/- 10.25% of an orally administered dose of buspirone was found as metabolites in feces (Mayol et al, 1985).
• 8.5 ELIMINATION HALF-LIFE
• 8.5.1 PARENT COMPOUND
• A. GENERAL
• 1. Plasma t1/2 is just over 2 hours (Mayol et al, 1985). The in vivo neuroleptic action in animals is approximately 2 to 3 hours, the anxiolytic action is longer (Wood et al, 1985).
• 2. RENAL AND HEPATIC IMPAIRMENT - Plasma concentration (max) and AUC after single and multiple doses are significantly higher in patients with renal or hepatic impairment. There is high variability between subjects, thus the authors could not recommend a definitive dosing schedule (Barbhaiya et al, 1994).
• 8.5.2 METABOLITE
• A. GENERAL
• 1. 1-PP peaks (in animal studies) at approximately 90 minutes with an apparent t1/2 of 120 minutes.
• 9.0 PHARMACOLOGY/TOXICOLOGY
• 9.1 PHARMACOLOGIC MECHANISM
• A. Buspirone is a psychotropic agent which has anxiolytic properties in humans and has blocked apomorphine-induced stereotype and emesis and disrupts conditioned avoidance behavior in animals. Buspirone does not appear to have cataleptogenic or anticonvulsant activity (Wood et al, 1983).
• B. Buspirone does not directly affect benzodiazepine receptors, or GABA receptors. It does influence dopaminergic transmission (Caccia et al, 1983).
• C. Buspirone suppresses serotonergic activity while enhancing dopaminergic and noradrenergic cell firing (Eison & Temple, 1986).
• 10.0 PHYSICOCHEMICAL
• 10.1 PHYSICAL CHARACTERISTICS
• A. The tablets have an unpleasant taste that may discourage children (Prod Info, 1985).
• 12.0 REFERENCES
• 12.2 GENERAL BIBLIOGRAPHY
• 1. AHA (American Heart Association): Guidelines for cardiopulmonary resuscitation and emergency cardiac care. JAMA 1992; 268:2171-2302.
• 2. AMA Department of Drugs: Drug Evaluation Subscription. American Medical Association, Chicago, IL, 1991.
• 3. Balster RL & Wolverton WL: Intravenous buspirone self-administration in rhesus monkeys. J Clin Psychiatry 1982; 43:34-37.
• 4. Barbhaiya RH, Shukla UA, Pfeffer M et al: Disposition kinetics of buspirone in patients with renal or hepatic impairment after administration of single and multiple doses. Eur J Clin Pharmacol 1994; 46:41-47.
• 5. Barceloux D, McGuigan M, Hartigan-Go K: Position statement: cathartics. American Academy of Clinical Toxicology; European Association of Poisons Centres and Clinical Toxicologists. Clin Toxicol 1997; 35:743-752.
• 6. Baselt RC: Disposition of Toxic Drugs and Chemicals in Man, 5th ed., Chemical Toxicology Institute, Foster City, CA, 2000.
• 7. Benitz WE & Tatro DS: The Pediatric Drug Handbook, 2nd ed. Year Book Medical Publishers, Chicago, IL, 1988.
• 8. Benitz WE & Tatro DS: The Pediatric Drug Handbook, 3rd ed. Mosby-Year Book Inc, Chicago, IL, 1995.
• 9. Brown TM, Skop BP & Mareth TR: Pathophysiology and management of the serotonin syndrome. Ann Pharmacother 1996; 30:527-533.
• 10. Caccia S, Muglia M, Mancinelli A et al: Disposition and metabolism of buspirone and its metabolite 1-2 (pyrimidinyl)-piperazine in the rat. Xenobiotica 1983; 13:147-153.
• 11. Catalano G, Catalano MC & Hanley PF: Seizures associated with buspirone overdose: case report and literature review. Clin Neuropharmacol 1998; 21:347-350.
• 12. Chamberlain JM, Altieri MA, Futterman C et al; A prospective, randomized study comparing intramuscular midazolam with intravenous diazepam for the treatment of seizures in children. Ped Emerg Care, 1997; 13:92-94.
• 13. Chyka PA & Seger D: Position statement: single-dose activated charcoal. American Academy of Clinical Toxicology; European Association of Poisons Centres and Clinical Toxicologists. Clin Toxicol 1997; 35:721-736.
• 14. Coates NE: Priapism associated with Buspar (letter). South Med J 1990; 83:983.
• 15. Dougherty RJ & Gates RR: The role of buspirone in the management of alcohol withdrawal: a preliminary investigation. J Subst Abuse Treat 1990; 7:189-192.
• 16. Dursun SM, Burke JG, Nielsen F et al: SSRI-related toxic serotonin syndrome: improvement of discontinuation of treatment and propranolol. Eur Psychiatr 1997; 12:321-323.
• 17. Eison AS & Temple DL Jr: Buspirone: review of its pharmacology and current perspectives on its mechanism of action. Am J Med 1986; 80(Suppl 3B):1-9.
• 18. FDA: Poison treatment drug product for over-the-counter human use; tentative final monograph. Fed Register 1985; 50:2244-2262.
• 19. Fuller RW: Buspirone metabolite and panic attacks (letter). Lancet 1990; 335:470.
• 20. Gammans RE, Mayol RF, LaBuddle JA et al: Metabolic fate of 14C/15N-buspirone in man. Fed Proceed 1982; 39:752.
• 21. Giang DW & McBride MC: Lorazepam versus diazepam for the treatment of status elipticus. Pediatr Neurol 1988; 4:358-361.
• 22. Gillman PK: Ecstasy, serotonin syndrome and the treatment of hyperpyrexia (letter). MJA 1997; 167:109-111.
• 23. Goetz CM, Krenzelok EP, Lopez G et al: Buspirone toxicity: a prospective study (Abstract 167). Vet Hum Toxicol 1989; 31:371.
• 24. Goldberg RJ & Huk M: Serotonin syndrome from trazodone and buspirone (letter). Psychosomatics 1992; 33:235-236.
• 25. Graham PM: Successful treatment of the toxic serotonin syndrome with chlorpromazine (letter). Med J Australia 1997; 166:166-167.
• 26. Guze BH & Baxter LR Jr: The serotonin syndrome: case responsive to propranolol (letter). J Clin Psychopharmacol 1986; 6:119-120.
• 27. Hoes MJAJM: Mirtazapine as treatment for serotonin syndrome. Pharmacopsychiatry 1996; 29:81.
• 28. Kastenholz KV & Crismon ML: Buspirone, a novel nonbenzodiazepine anxiolytic. Clin Pharm 1984; 3:600-607.
• 29. Kline SS, Mauro LS, Scala-Barnett DM et al: Serotonin syndrome versus neuroleptic malignant syndrome as a cause of death. Clin Pharmac 1989; 8:510-514.
• 30. Lader M: Can buspirone induce rebound, dependence or abuse? Br J Psyc 1991; 159 (suppl. 12):45-51.
• 31. Lahat E, Goldman M, Barr J et al: Comparison of intranasal midazolam with intravenous diazepam for treating febrile seizures in children: prospective randomized study. BMJ 2000; 321:83-86.
• 32. Langlois RP & Paquette D: Sustained bradycardia during fluvoxamine and buspirone intoxication. Can J Psyc 1994; 39:126-127.
• 33. LeWitt PA, Walters A, Hening W et al: Persistent movement disorders induced by buspirone. Movement Disorders 1993; 8:331-334.
• 34. Mayol RF, Adamson DS, Gammans RE et al: Pharmacokinetics and disposition of 14C-buspirone HCl after intravenous and oral dosing in man. Clin Pharmacol Ther 1985; 37:210.
• 35. Mayol RF, Gammans RE & MacKenthun AV: Effect of food on the bioavailability of buspirone HCl. Clin Research 1983; 31:631A.
• 36. McIvor RJ & Sinanan K: Buspirone-induced mania (letter). Br J Psychiatry 1991; 158:136-137.
• 37. Mills KC: Serotonin syndrome: a clinical update. Med Toxicol 1997; 13:763-783.
• 38. Moskowitz H & Smiley A: Effects of chronically administered buspirone and diazepam on driving-related skills performance. J Clin Psychiatry 1982; 43(Sect 2):45-55.
• 39. Personal Communication: Dr Cashkin, Miles Incorporated, Pharmaceuticals Division, West Haven, CT, July 1990.
• 40. Product Information Ativan(R), 1999, Wyeth-Ayerst Co, Philadelphia, PA
• 41. Product Information: Ativan(R), lorazepam. Wyeth, Philadelphia, PA, 1991.
• 42. Product Information: BUSPAR(R), Mead Johnson Pharmaceuticals, Evansville, IN, 1988.
• 43. Product Information: DE Gamble, M.D., Mead Johnson Pharmaceutical Group, May 3, 1985.
• 44. Riblet LA, Allen LE, Hyslay DK et al: Pharmacologic activity of buspirone, a novel non-benzodiazepine antianxiety agent. Fed Proceed 1980; 39:752.
• 45. Riblet LA, Tylor DP, Eison MS et al: Pharmacology and neurochemistry of buspirone. J Clin Psychiatry 1982; 43:11-18.
• 46. Ritchie EC, Bridenbaugh RH & Jabbari B: Acute generalized myoclonus following buspirone administration. J Clin Psychiatry 1988; 49:242-243.
• 47. Robinson D, Napoliello MJ & Schenk J: The safety and usefulness of buspirone as an anxiolytic in elderly versus young patients. Clin Ther 1988; 10:740-746.
• 48. Scott R, Besag FMC, Neville BGR: Buccal midazolam and rectal diazepam for treatment of prolonged seizures in childhood and adolescence: a randomized trial. Lancet 1999; 353:623-626.
• 49. Soni P & Weintraub AL: Buspirone-associated mental status changes. J Am Acad Child Adolesc Psychiatry 1992; 31:1098-1099.
• 50. Sternbach H: The serotonin syndrome. Am J Psychiatr 1992; 149:1410-1411.
• 51. Tiller JWG, Burrows GD & O'Sullivan BT: Buspirone overdose (letter). Med J Aust 1989; 150:54-55.
• 52. Trachman SB: Buspirone-induced psychosis in a human immunodeficiency virus-infected man. Psychosomatics 1992; 33:332-335.
• 53. Uhlenhuth EH: Discussant presentation: Buspirone: a clinical review of a new, non-benzodiazepine anxiolytic. J Clin Psychiatry 1982; 43:109-116.
• 54. USP DI Volume I Drug information for the health care professional. 20th edition, 2000; Micromedex Inc, World Color Book Services, Taunton, MA.
• 55. USPDI: Drug Information for the Health Care Professional, Volume 1, 19th ed., Micromedex Inc., Englewood, CO, 1999.
• 56. Vale JA: Position Statement: gastric lavage. American Academy of Clinical Toxicology/European Association of Poisons Centres and Clinical Toxicologists. Clin Toxicol 1997; 35:711-719.
• 57. WHO: Buspirone: central nervous system and extrapyramidal effects. WHO Drug Information 1988; 2:149.
• 13.0 AUTHOR INFORMATION
• 13.1 CONTRIBUTOR(S) TO THIS DOCUMENT
• A. Original publication: 05/85
• B. Most recent revision: 01/01
• C. List of contributors:

§               1. Katherine M Hurlbut, MD

§               2. Suman Wason, MD

§               3. Barry H Rumack, MD

§               4. POISINDEX(R) Editorial Staff

• D. Specialty Board: PSYCHOACTIVE DRUGS
• Refer to the POISINDEX EDITORIAL BOARD section for more information. (MG0456)

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