Generic
Buspirone
2 brands available in the market
At a glance
Buspirone is an anxiolytic medication used in the treatment of anxiety disorder. It works by modulating serotonin receptors in the brain, reducing symptoms of anxiety such as irritability, restlessness, lack of concentration, fatigue, sweating, increased heart rate, and racing thoughts.
Description
Buspirone is an anxiolytic used for the treatment of anxiety disorder. It binds to serotonin receptors (particularly 5-HT1A) to regulate the chemicals that cause anxiety.
Buspirone exerts anxiolytic activity through high affinity for serotonin 5-HT1A and 5-HT2 receptors. It has moderate affinity for dopamine D2 receptors but no affinity for GABA receptors.
Indications
- Anxiety disorder
Therapeutic class
Anxiolytic
Pharmacological class
Azapirone (5-HT1A Receptor Agonist)
Pharmacology
Buspirone acts as a partial agonist at serotonin 5-HT1A receptors. It activates presynaptic 5-HT1A autoreceptors to regulate serotonin release and postsynaptic 5-HT1A receptors to produce anxiolytic effects. It has no direct interaction with GABA receptors, which explains its lower sedative profile compared to benzodiazepines.
Mechanism of action
Buspirone binds to serotonin 5-HT1A receptors, modulating serotonergic activity to calm anxiety pathways and reduce symptoms of anxiety.
Dosage
Adults (Anxiety Disorder): 10-15 mg/day orally, divided every 8-12 hours. Increase by 5 mg/day every 2-3 days to 15-30 mg/day. Max: 60 mg/day.
Hepatic impairment: Not recommended in severe hepatic impairment.
Renal impairment: Not recommended in severe renal impairment.
Note: Full efficacy may take 2-4 weeks.
Administration
Take as advised by your doctor. Swallow tablets whole; do not chew, crush, or break. May be taken with or without food, preferably at a fixed time each day.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common side effects: Nausea, headache, vomiting, dry mouth, sleepiness, dizziness, constipation, diarrhea, abdominal pain.
These side effects are usually mild and resolve over time.
Precautions & warnings
- Full efficacy may take 2-4 weeks to achieve.
- May cause dizziness and sleepiness; use caution while driving or doing anything requiring concentration.
- Avoid alcohol consumption (may cause excessive drowsiness).
- Do not stop abruptly without consulting your doctor.
- Avoid use in severe hepatic or renal impairment.
- Caution during pregnancy and lactation.
Contraindications
- Hypersensitivity to buspirone
- Epilepsy (seizure disorders)
- Severe renal or hepatic impairment
- Children under 18 years
- Pregnancy and lactation
Drug interactions
- Alcohol and other CNS depressants: Enhanced sedative effects.
- Haloperidol: May increase serum haloperidol levels.
- MAO inhibitors: May cause increased blood pressure (potentially fatal) – avoid concurrent use.
Food interactions
Alcohol consumption is unsafe (may cause excessive drowsiness and sedation).
Use in pregnancy
Generally considered safe during pregnancy (Category B). Animal studies have shown low or no adverse effects; limited human studies available.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Probably unsafe during breastfeeding. Limited human data suggests the drug may pass into breast milk and harm the baby.
Pediatric use
Safety and effectiveness in children under 18 years have not been established.
Geriatric use
No specific dose adjustment required for elderly, but caution advised (consider reduced hepatic and renal function).
Renal / hepatic impairment
Hepatic impairment: Use with caution; dose adjustment may be needed. Not recommended in severe hepatic impairment.
Overdose effects
Overdose symptoms: Nausea, vomiting, dizziness, drowsiness, pupillary constriction. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.
Chemical structure
Buspirone Hydrochloride (Azapirone Anxiolytic)