buspirone (BuSpar)
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Introduction
Tradename: BuSpar.
Indications
- generally considered drug of choice in the initial treatment of anxiety
- especially useful for patients with history of chemical dependence - little potential for abuse
- not for acute anxiety
Contraindications
- avoid use in patient with hepatic or renal impairment
Caution:
- safety not established in children < 18 years of age
- avoid driving when initiating therapy until certain than buspirone does not adversely effect mental status
- not for PRN use
- does not prevent benzodiazepine withdrawals Report: changes in senses (smelling, hearing, vision)
Advantages
- well tolerated
- does not interact with alcohol or benzodiazepines
- does not cause drug dependency
Disadvantages
- very slow to work (2-4 weeks)
- not always effective
- adverse effects
Dosage
- start 5 mg PO TID (after meals)
- increase by 5 mg every 2-3 days
- max 60 mg/day
- most patients respond to 15-30 mg QD
Tabs: 5 & 10 mg.
Pharmacokinetics
- anxiolytics effects may take several weeks
- extensive 1st pass metabolism in the liver
- administration after meals increases absorption
- age & gender do NOT affect pharmacokinetics
elimination via liver
elimination via kidney
protein binding = >95 %
elimination by hemodialysis = -
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- chest pain, confusion, muscle weakness, tachycardia, blurred vision, dry mouth, tinnitus, insomnia, nightmares, weakness, sedation, disorientation, excitement, fever, ataxia, rash, urticaria, vomiting, diarrhea, flatulence, leukopenia, eosinophilia
- other
- increased serum transaminases
Drug interactions
- MAO inhibitors in combination may cause hypertensive crisis
- cimetidine
- alcohol
- highly protein-bound drugs
- haloperidol
- any drug that inhibits cyt P450 3A4 may increase levels of buspirone
- any drug that induces cyt P450 3A4 may diminish levels of buspirone
Laboratory
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 1120
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995