buspirone
Buspirone is an azapirone anxiolytic approved for generalized anxiety disorder (GAD). Unlike benzodiazepines, it has no sedative, muscle-relaxant, or anticonvulsant properties and is not associated with dependence.
5mg, 7.5mg, 10mg, 15mg, 30mg (typically dosed BID-TID)
Tablets: 5mg, 7.5mg, 10mg, 15mg, 30mg (most are scored for splitting)
Category B (animal studies show no risk; human data limited)
Partial agonist at presynaptic and postsynaptic 5-HT1A serotonin receptors. Weak dopamine D2 antagonist. Onset of anxiolytic effect is delayed (2-4 weeks).
Buspirone has minimal classical withdrawal because it does not act on GABA. Most patients can discontinue with a 1-2 week stepdown. Rebound anxiety is the main concern.
Buspirone is not associated with the dependence or discontinuation syndrome seen with SSRIs or benzodiazepines. A short stepdown (e.g., halve dose for 1 week, then stop) is usually sufficient. Slower if used long-term or in combination with other anxiolytics.
Evidence-based phased reduction schedule. Always taper under medical supervision.
| Phase | Duration | Notes |
|---|---|---|
| Initial reduction | 1 week | Halve total daily dose. Most patients tolerate this step well. |
| Final reduction | 1 week | Reduce to lowest available dose, then stop. Watch for rebound anxiety. |
1-3 days after stopping
3-7 days
Typically within 1-2 weeks
Rebound anxiety may persist 2-4 weeks if the underlying anxiety condition is not addressed
Practical insights shared by members tapering BuSpar. Not medical advice — always consult your prescriber.
Toxicity
Generally low toxicity. Serotonin syndrome possible with serotonergic combinations. Dizziness, headache, nausea, and lightheadedness most common adverse effects.
Pharmacokinetics
Rapidly absorbed but extensive first-pass metabolism limits oral bioavailability to ~4%. Food increases bioavailability.
~5.3 L/kg
Extensive hepatic metabolism via CYP3A4 to multiple metabolites including the active 1-(2-pyrimidinyl)-piperazine (1-PP).
Renal (~29-63% as metabolites), fecal (~18-38%).
~95%
~28 mL/min/kg
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