Buspirone chemical structure
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Buspirone

Buspirone (brand-names Ansial®, Ansiced®, Anxiron®, Axoren®, Bespar®, Buspar®, Buspimen®, Buspinol®, Buspisal®, Narol®) is an anxiolytic drug. more...

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It shows no potential for addiction compared to other drugs commonly prescribed for anxiety, especially benzodiazepine medications. The development of tolerance has not been noticed. Cross-tolerance to benzodiazepines, barbiturates and alcohol does not exist. Furthermore, it is non-sedating. It is thought to act by interfering with the function of the neurotransmitter serotonin in the brain, particularly by serving as a 5-HT1A receptor partial agonist. Additionally, it acts as a mixed agonist/antagonist on postsynaptic Dopamine receptors. GABA-mediated effects are lacking. Buspirone may also have indirect effects on other neurotransmitters in the brain. The action of a single dose is much longer than the short halflife of 2-3 hours indicates.

The bioavailability of Buspirone is very low and variable due to extensive first pass metabolism. The drug is quickly resorbed. Taking the drug together with food may increase the bioavailabilty. The drug is highly (95%) plasma-bound. The active metabolite 1-PP is also a 5-HT1A partial agonist with anxiolytic properties, but weaker so than the mother-drug.

Bristol-Myers Squibb gained FDA approval for Buspirone in 1986. The drug went generic in 2001.

It is also useful as an augmenting agent, for the treatment of depression, when added to SSRIs (selective serotonin reuptake inhibitors).

The main disadvantage is that 1 to 3 weeks elapse before the anxiolytic activity becomes evident. Often patients have to be initially cotreated with a benzodiazepine for immediate anxiolysis. Generally, Buspirone works less well than benzodiazepines. It is particular difficult to treat patients pretreated with benzodiazepines knowing the immediate effects of these tranqulizers.

Indications

  • Generalized anxiety disorder of mild to moderate intensity

N.B. Busprirone is definitively not effective against other types of panic disorders with or without agoraphobia and social phobia.

  • Augmention of SSRI-Treatment against Depression

Contraindications

  • Myasthenia gravis
  • Acute closed angle glaucoma
  • Severly compromised liver- and renal-function
  • Concomittant treatment with a MAO-Inhibitor (severe hypertensive crises have been seen)
  • Caution : Preexisting heart conditions (e.g. myocardial infarction)

Side-effects

Rarely, side-effects have a dangerous nature or intensity. Some tend to disappear with continued therapy, or are less frequent if the initial dose is low and increased gradually (vertigo, agitation, insomnia).

  • Most frequent: vertigo, headaches, nervousness, agitation, light-headedness, nausea;
  • Often (>1%) : drowsiness, insomnia, concentration disorders, confusion, depression, agitation, intestinal disorders, paresthesia, coordination disorders, tremors, disturbed visus, tinnitus, fatigue, weakness, Angina pectoris, sore throat, tachycardias, palpitations, dry mouth, pain in muscles and joints;
  • Seldomly: allergic reactions, subdermal bleeding, extrapyramidal symptoms, hallucinations, psychosis, ataxia, epileptic seizures, syncope, tunnel vision, urine retention, alopecia, pruritus.

The dyscognitive side-effects of benzodiazepines are lacking completely.

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Systemic absorption of amitriptyline and buspirone after oral and transdermal administration to healthy cats
From International Journal of Pharmaceutical Compounding, 11/1/04 by Foy, Elizabeth

Systemic absorption of amitriptyline and buspirone after oral and transdermal administration to healthy cats.

Mealey KL, Peck KE, Bennett BS et al. J Vet Intern Med 2004; 18(1): 43-46.

At the time of writing, the authors were affiliated with either the College of Veterinary Medicine, Washington State University, Pullman, Washington, or the Texas Veterinary Medical Diagnostic Laboratory, Texas A & M University, College Station, Texas. They state that urine spraying by cats is a serious and common behavioral problem and has successfully been treated by the use of buspirone as well as by amitriptyline. Unfortunately, veterinary formulations of many drugs are not marketed. In addition, cats are resistant to administration of oral medications including solids as well as liquids. Compounding pharmacists have been advertising transdermal gels as an alternative route of administration for cats, including transdermal buspirone and amitriptyline. The authors set out to discover if transdermal absorption of these two drugs in cats was similar to systemic absorption following oral administration. They describe the six cats used in the study, the drug formulations and the experimental protocol. Transdermal Pluronic lecithin organogels (PLOs) were obtained from a veterinary compounding pharmacy. In addition, one-month supplies of buspirone at 2.5 mg/0.1 mL and amitriptyline at 5 mg/0.1 mL were ordered for two fictitious patients being treated at the University's veterinary teaching hospital. Preparation and also administration of the drug-containing gels are briefly described. The commercial immunoassays used to detect plasma levels of buspirone and amitriptyline are described in great detail. Their results indicated thattransdermal absorption of both buspirone and amitriptyline were poor relative to oral administration of these drugs. In their discussion, the authors state, "Results of this study raise doubts about the reliability of pluronic F127 (PLO) gels as vehicles for the transdermal route of administration for buspirone and amitriptyline in cats. In the single-dose transdermal studies reported here, neither drug demonstrated predictable, consistent systemic absorption." They state that more studies are needed and conclude that, "Failure of a cat to respond to a pharmacologie trial of buspirone or amitriptyline administered transdermally may simply result from failure of the drug to reach therapeutic concentrations."

References

1. [No author listed.] U.S. Food and Drug Administration. Center for Veterinary Medicine. Animal Medicinal D rug Use Clarification Act of 1994 (AMDUCA). [U.S. Food and Drug Administration Website.l Available at: www.fda.gov.cvm/index/amduca/ amducatoc.htm. Accessed July 5, 2004.

2. Federal Register. (1996) Nov 7; 61(217): 57731. [U.S. Food and Drug Administration Website.] Extralabel drug use in animals; final rule. Available at: www/fda.gov/cvm/index/amduca/amducafr.htm. Accessed July 5, 2004.

3. [No author listed.] American Veterinary Medical Association. [American Veterinary Medical Association Website.] AVMA Position Statements. Compounding (Approved by AVMA Executive Board, November 2000). Available at: www.avma.org/policies/compounding.htm. Accessed July 5, 2004.

4. [No author listed.] American Veterinary Medical Association. [American Veterinary Medical Association Website.] Extralabel drug use (ELDU): An informational outline of the Animal Medicinal Drug Use Clarification Act (AMDUCA). 1998; Revised June 2003. Available at: www.avma.org/scienact/amduca/amducal.asp. Accessed July G, 2004.

5. [No author listed.] American Veterinary Medical Association. [American Veterinary Medical Association Website.] Extralabel drug use algorithm. Available at: www.avma.org/scienact/amduca/amduca2.asp. Accessed July 6, 2004.

Address correspondence to: Elizabeth Foy, College of Pharmacy, Dalhousie University, Halifax, NS B3H 3J5, Canada. E-mail: elizabeth.foy@dal.ca

Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2004
Provided by ProQuest Information and Learning Company. All rights Reserved

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