[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Other anxiolytics](https://durgical.com/en/pharmacology/classes/other-anxiolytics/) › Buspirone

[Pharmacology](https://durgical.com/en/pharmacology/) · [Other anxiolytics](https://durgical.com/en/pharmacology/classes/other-anxiolytics/)

# Buspirone

A non-sedating anxiety medicine that acts on serotonin 5-HT1A receptors. It causes no dependence, but does not work at once or on panic attacks.

Updated 2026-11-01

- Class: [Other anxiolytics](https://durgical.com/en/pharmacology/classes/other-anxiolytics/)
- Receptor: Serotonin 5-HT1A receptor
- ATC code: N05BE01

◎**Serotonin 5-HT1A receptor**Buspirone

ⓘ The figure shows buspirone itself bound to the human 5-HT1A receptor coupled to its Gi protein.

**Target in 3D:** Serotonin 5-HT1A receptor. PDB structure 8FYX (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8FYX) · Drag to rotate · pinch to zoom

## Mechanism of action

Buspirone binds serotonin 5-HT1A receptors with high affinity and dopamine D2 receptors moderately. How this relieves anxiety is not fully known. It has no affinity for the benzodiazepine site and does not change GABA binding, so it lacks anticonvulsant, muscle-relaxant and marked sedative effects.

- Binds serotonin 5-HT1A receptors
- Serotonin signalling adapts over weeks
- Anxiety slowly eases, without sedation

## Pharmacokinetics

**Absorption**
Absorbed by mouth with extensive first-pass metabolism; food increases absorption, so it is taken the same way each time

**Metabolism**
Mainly by CYP3A4

**Half-life**
About 2 to 3 hours

## Indications

- Anxiety disorders, mainly generalized anxiety disorder [Generalized anxiety disorder →](https://durgical.com/en/conditions/generalized-anxiety-disorder/)

## Adverse effects

### Common

- Dizziness and light-headedness
- Nausea
- Headache
- Nervousness and excitement

### Serious (rare, important)

- Serotonin syndrome and raised blood pressure with MAO inhibitors

## Contraindications

- Hypersensitivity to buspirone
- MAO inhibitors, or within 14 days of stopping one; linezolid or IV methylene blue

## Key interactions

**MAO inhibitors**
High blood pressure and serotonin syndrome

**CYP3A4 inhibitors (diltiazem, verapamil, erythromycin, itraconazole, nefazodone) and grapefruit juice**
Higher buspirone levels

**Rifampin (CYP3A4 inducer)**
Lower buspirone levels

## What is monitored

- Anxiety symptoms over the following weeks; the need for treatment is reviewed periodically
- Dizziness

## Administration and safety

- Given by mouth, always with food or always without it
- Not a controlled substance
- A benzodiazepine is tapered gradually before switching; buspirone does not cover withdrawal

## Nursing care

- Teach that relief builds over weeks and that it is not taken «as needed» for panic
- Ask about MAO inhibitors and other serotonergic drugs
- Teach to avoid large amounts of grapefruit juice
- Check for dizziness before walking

## Pregnancy and breastfeeding

Human data are limited; the benefit is weighed against unknown risk.

## Memory aid

Buspirone: «BUS-pirone takes the slow bus» – weeks to work, no sedation, no dependence, 5-HT1A.

## Test yourself

Think of the answer, then tap the question to see it.

## Can buspirone be used for an acute panic attack?

No; its anxiolytic effect builds over weeks.

## Why must a long-term benzodiazepine user be tapered before starting buspirone?

Buspirone has no cross-tolerance and will not block benzodiazepine withdrawal.

## Which drink raises buspirone levels?

Grapefruit juice (CYP3A4 inhibition).

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/buspirone/)

## Related drugs

- [Alprazolam](https://durgical.com/en/pharmacology/alprazolam/)
- [Diazepam](https://durgical.com/en/pharmacology/diazepam/)

## Related conditions

- [Generalized anxiety disorder](https://durgical.com/en/conditions/generalized-anxiety-disorder/)

[← Back to the class: Other anxiolytics](https://durgical.com/en/pharmacology/classes/other-anxiolytics/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - BUSPIRONE HYDROCHLORIDE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8dc1ee33-e5aa-4462-8fb9-9bbdf5463488) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N05BE01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [8FYX: Buspirone-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex](https://www.rcsb.org/structure/8FYX) (RCSB Protein Data Bank, 2024).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/buspirone/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/buspirone/