Buspirone
Non-benzodiazepine azapirone anxiolytic, a 5-HT1A partial agonist that is non-sedating and non-addictive.
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Pharmacology
Contents
WHAT IS BUSPIRONE?
Detailed overview
Buspirone is an azapirone-class prescription anxiolytic approved primarily for generalized anxiety disorder (GAD). Unlike benzodiazepines it is a partial agonist at the serotonin 5-HT1A receptor with negligible GABA activity: it causes no sedation, muscle relaxation, cognitive blunting or physical dependence, and has no euphoric potential. Despite a short 2 to 3 hour half-life, its anxiolytic effect builds gradually over 2 to 4 weeks, because desensitization of presynaptic autoreceptors raises serotonergic transmission over time. For this reason it is not suitable for the immediate relief of acute, episodic anxiety.
Mechanism
5-HT1A partial agonist (non-GABAergic)
Onset
Gradual, 2 to 4 weeks
Legal status
Prescription medicine (FDA 1986)
Receptor profile
- 5-HT1A receptor (partial agonist)Strong
- Presynaptic 5-HT1A autoreceptorModerate
- Dopamine D2 receptorWeak
- Alpha-2 adrenergic receptor (1-PP metabolite)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Dizziness, lightheadedness and drowsiness, especially in the first days of treatment
- Headache and nausea
- Nervousness, restlessness or agitation
- Rarely fast heartbeat, chest tightness or paresthesia
- Unlike benzodiazepines it does not cause significant sedation, muscle relaxation or dependence
Contraindications · 4
- Contraindicated with MAO inhibitors: risk of hypertensive crisis and serotonin syndrome (14-day washout required)
- Severe hepatic or renal impairment: plasma levels may rise substantially
- Strong CYP3A4 inhibitors (e.g. ketoconazole, erythromycin) and grapefruit juice raise its levels; CYP3A4 inducers lower them
- Pregnancy and breastfeeding: only under clear indication and medical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Azapirones for generalized anxiety disorder
Chessick CA, Allen MH, Thase M, Batista Miralha da Cunha AB, Kapczinski FF, de Lima MS, dos Santos Souza JJ
Pharmacological treatments for generalised anxiety disorder: a systematic review and network meta-analysis
Slee A, Nazareth I, Bondaronek P, Liu Y, Cheng Z, Freemantle N
Azapirones versus placebo for panic disorder in adults
Imai H, Tajika A, Chen P, Pompoli A, Furukawa TA
Pharmacological treatments for social anxiety disorder in adults: a systematic review and network meta-analysis
Williams T, Hattingh CJ, Kariuki CM, Tromp SA, van Balkom AJ, Ipser JC, Stein DJ
Buspirone in Autism Spectrum Disorder: A Systematic Review
Gupta N, Gupta M
FAQ
FAQ
Non-benzodiazepine azapirone anxiolytic, a 5-HT1A partial agonist that is non-sedating and non-addictive.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.