Buspirone (BuSpar)
Non-benzodiazepine anxiolytic (5-HT1A partial agonist) for generalized anxiety disorder. Takes 2-4 weeks for full effect. Metabolized by CYP3A4 to active metabolite 1-PP (alpha-2 adrenergic antagonist). No sedation, dependence, or withdrawal. Not effective PRN for acute anxiety.
Projected serum levels — 10 mg, twice daily
Maintenance schedule: 10 mg twice daily (oral).
Modeled steady state after ~1 days: peak ≈ 0.32 mg, trough ≈ 0.016 mg body load. Population-based estimate over 15 days for a 10 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Anxiolytic
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 2.5 h
- Common dose
- 10 mg
- Suggested maximum
- 60 mg/day
- Reference dose range
- 5–60 mg (single dose)
- Suggested cadence
- twice daily
- Validated against
- 10 mg oral — Cmax 0.002 mg/L at 0.75 h
Documented interactions
-
contraindicated
Carbamazepine (Tegretol) + Buspirone (BuSpar)
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~0.20x
-
contraindicated
Clarithromycin (Biaxin) + Buspirone (BuSpar)
Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~10.00x
-
contraindicated
Dasatinib (Sprycel) + Buspirone (BuSpar)
Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~5.00x
-
contraindicated
Diltiazem + Buspirone (BuSpar)
Diltiazem mechanism_based of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~10.00x
-
contraindicated
Efavirenz (Sustiva) + Buspirone (BuSpar)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~0.12x
-
contraindicated
Grapefruit (whole fruit) + Buspirone (BuSpar)
Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Buspirone (BuSpar) AUC by ~10.00x
Serum checks 172 modeled interaction pairings for buspirone (buspar) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
-
Use of buspirone in patients with generalized anxiety disorder and coexisting depressive symptoms: a meta-analysis of eight randomized controlled studies
Meta-analysis of 8 RCTs (520 GAD patients) showing buspirone significantly improved HAM-A anxiety scores and global improvement compared to placebo, with concurrent improvement in depressive symptoms.
-
Assessment of the efficacy of buspirone in patients affected by generalized anxiety disorder, shifting from prior lorazepam: a placebo-controlled, double-blind study
Double-blind RCT demonstrating buspirone was more effective than placebo and comparable to lorazepam for GAD, without rebound anxiety or withdrawal syndrome upon discontinuation.
-
Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug
Comprehensive PK/PD review establishing buspirone half-life of 2-3 hours, extensive CYP3A4 metabolism, active metabolite 1-PP with alpha-2 antagonist activity, and high interindividual variability.
3 published studies referenced in the app, each with a plain-language summary.