[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Z-drug hypnotics](https://durgical.com/en/pharmacology/classes/z-drug-hypnotics/) › Zaleplon

# Zaleplon

## Z-drug hypnotics?

Z-drug hypnotics

An ultra-short-acting Z-drug that shortens the time to fall asleep without adding total sleep. It can cause complex sleep behaviours such as sleep-driving.

Updated Nov 1, 2026

## Quick facts

**Group**
[Z-drug hypnotics](https://durgical.com/en/pharmacology/classes/z-drug-hypnotics/)

**Target**
GABA-A receptor (α1-containing), benzodiazepine site

**Used for**
Short-term treatment of insomnia

**Key effects**
Headache and dizziness · Somnolence · Nausea

**Monitor**
Sleep onset and next-day alertness

**ATC**
N05CF03

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

◎**GABA-A receptor (α1-containing), benzodiazepine site**Zaleplon

ⓘ The figure shows zolpidem, another Z-drug, in the human GABA-A receptor; zaleplon acts at the same benzodiazepine site.

**Target in 3D:** GABA-A receptor (α1-containing), benzodiazepine site. PDB structure 8DD2 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8DD2) · Drag to rotate · pinch to zoom

Zaleplon is a non-benzodiazepine (a pyrazolopyrimidine) that binds the benzodiazepine site of GABA-A receptors containing the α1 subunit (the omega-1 site). It strengthens GABA's chloride current. Its very short action shortens sleep onset but does not lengthen total sleep.

- Binds α1-containing GABA-A receptors (omega-1 site)
- GABA's chloride current grows stronger
- Sleep comes sooner; the effect ends within hours

## Indications

- Short-term treatment of insomnia with difficulty falling asleep [Insomnia disorder →](https://durgical.com/en/conditions/insomnia-disorder/)

## Adverse effects

### Common

- Headache and dizziness
- Somnolence
- Nausea
- Amnesia and tingling

### Serious (rare, important)

- Complex sleep behaviours (sleep-driving, sleepwalking) while not fully awake
- Abnormal thinking and worsening depression with suicidal thoughts
- Angioedema and anaphylaxis

## Contraindications

- Hypersensitivity to zaleplon

## Key interactions

**Alcohol and other CNS depressants**
Additive sedation and impairment

**Cimetidine**
Higher zaleplon levels; lower starting dose

**Rifampin (strong CYP3A4 inducer)**
Much lower zaleplon levels

## What is monitored

- Sleep onset and next-day alertness
- Unusual night-time behaviour and mood

## Administration and safety

- Given by mouth right before bedtime, or after getting into bed and failing to fall asleep
- Not with or right after a heavy, high-fat meal
- Controlled medicine (Schedule IV in the United States)

## Pregnancy and breastfeeding

There are no studies in pregnant women and its use is not recommended; it is avoided during breastfeeding.

## Nursing care

- Check that a full night in bed is possible before giving it
- Ask about alcohol and other sedatives
- Teach to report sleep-driving or other actions done while not fully awake
- Reassess if insomnia persists after 7 to 10 days

## Pharmacokinetics

**Absorption**
About 30% bioavailable; a heavy high-fat meal delays it and lowers the peak

**Metabolism**
Mainly by aldehyde oxidase, with a smaller CYP3A4 role

**Half-life**
About 1 hour

## Memory aid

Zaleplon: «Z-one-hour» – the shortest Z-drug: helps fall asleep, not stay asleep.

## Test yourself

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

## Why does zaleplon not increase total sleep time?

Its half-life is about one hour, so it only helps with falling asleep.

## Which enzyme mainly metabolises zaleplon?

Aldehyde oxidase (CYP3A4 has a smaller role).

## Which GABA-A subunit site does it prefer?

The α1 (omega-1) benzodiazepine site.

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

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 4

- [Zolpidem](https://durgical.com/en/pharmacology/zolpidem/)
- [Eszopiclone](https://durgical.com/en/pharmacology/eszopiclone/)
- [Suvorexant](https://durgical.com/en/pharmacology/suvorexant/)
- [Flumazenil](https://durgical.com/en/pharmacology/flumazenil/)

## Related conditions 1

- [Insomnia disorder](https://durgical.com/en/conditions/insomnia-disorder/)

[← Back to the class: Z-drug hypnotics](https://durgical.com/en/pharmacology/classes/z-drug-hypnotics/)

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 - ZALEPLON capsule](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2f44db39-e1d9-451e-ba31-e4b10366a430) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N05CF03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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