buspirone BUSPAR
Class: 5HT1A AgonistFDA Indications: GAD
Off-Label Use: Cannabis Dependence, Smoking Cessation, Hypoactive Sexual Desire Disorder, ADHD, Treatment Resistant Depression
Prescribing
Forms: 5, 10, 15, 30mg tabletDose Range: 20-60 mg/day
Starting: 15 mg bid, increase by 5 mg increments until desired efficacy achieved
Stopping: Taper generally not necessary
Precautions
Serious Side Effects: Infrequent syncope, hypotension and hypertension. Rare cardiovascular adverse events include CVAs, CHF, MI, CMP, and bradycardiaSide Effects: xerostomia, constipation, nausea, weight loss, anorexia, myalgia, insomnia, dizziness, headache, agitation, anxiety, tremor, tremor, hyperhidrosis, tinnitus
Pharmacodynamics
1° MOA: Preferential full agonist of presynaptic 5-HT1A receptors, which are inhibitory autoreceptors2° MOA: Partial agonist of postsynaptic 5-HT1A receptors
Target:
- Presynaptic 5HT1A agonist
- Postsynaptic 5HT1A partial agonist
Pharmacokinetics
t½: 2.8° TMAX: 1°Substrate of: 3A4
Inhibits: ∅ ; Induces: ∅
Active Metabolites: 1-PP
DDIs
- - DO NOT CO-PRESCRIBE WITH MAOIs; 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
- - patients who are benzodiazepine naive respond better than those who are switched from a benzodiazepine
- - ∅ sexual dysfunction; ∅ weight gain
- - ∅ dependence or withdrawal
- - may reduce sexual dysfunction associated with GAD and/or with SSRIs
Special Populations
Category B—Although no drug-induced congenital malformations have been observed after 1st-trimester exposure to buspirone, the data are too limited to assess the safety of the drug in human pregnancy.
Because of the potential for CNS impairment in a nursing infant, maternal use of the drug, especially for prolonged periods, should be undertaken cautiously, if at all.
There were no effects of age on the pharmacokinetics of buspirone
Caution in severe impairment
Caution in severe impairment
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