Buspirone
Buspirone
Buspar (US brand discontinued; generic widely available)
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Summary
Common uses
Generalized anxiety disorder (FDA)0, Depression adjunct to SSRI/SNRI (off-label)0, SSRI-induced sexual dysfunction (off-label adjunct, weak evidence)0, Sleep-related bruxism (off-label)0
Pharmacy
Starting dose
5 mg PO TID or 7.5 mg PO BID; titrate by 5 mg every 2-3 days to clinical effect, commonly 30-60 mg/day divided BID-TID
Preparations
Tablets 5, 7.5, 10, 15, 30 mg (the 15 and 30 mg tablets are scored for halving and quartering)
US FDA Max
60 mg/day
Pharmacology
Routes
Oral
Onset
Anxiolytic effect emerges over 2-4 weeks — buspirone does NOT work for acute anxiety, which is the central teaching point and the most common cause of treatment failure
Duration
~8 hours (TID dosing)
Half-life
Buspirone 2-3 hours; 1-PP active metabolite 4-6 hours[1]
Bioavailability
~4% (extensive first-pass metabolism)[1]
Pregnancy
Limited human data; older agent with substantial use experience and no clear teratogenic signal.[citation needed]
Legal status
Purported mechanism
Serotonin 5-HT1A receptor partial agonist (acts at both presynaptic autoreceptors and postsynaptic sites) with weak dopamine D2 receptor antagonism. No GABA receptor activity, so buspirone has no sedation, no muscle relaxation, no tolerance to anxiolytic effect, no withdrawal syndrome, no dependence liability, and no controlled-substance status, distinguishing it sharply from the benzodiazepines.0 Strong CYP3A4 substrate: grapefruit juice, ketoconazole, erythromycin, and clarithromycin substantially raise plasma exposure; rifampin and St. John's wort lower it. The 2-4 week onset means buspirone is appropriate for chronic GAD-style anxiety but not acute anxiety[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Buspar (buspirone hydrochloride), Bristol-Myers Squibb/various, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf