Pharmacology · Z-drug hypnotics
Zolpidem !
A short-acting Z-drug for trouble falling asleep. It can cause sleep-driving and next-morning impairment, more so in women and older adults.
Updated 2026-11-01
The figure shows zolpidem itself bound to the human GABA-A receptor (α1β2γ2) together with GABA.
Mechanism of action
Zolpidem is a positive modulator of the GABA-A receptor at the benzodiazepine site. It binds receptors with the α1 subunit more strongly than α2 or α3 and hardly binds α5, so it mainly brings on sleep with little anxiolytic or muscle-relaxant effect.
- Binds α1-containing GABA-A receptors at the benzodiazepine site
- GABA's chloride current grows stronger
- Sleep comes sooner; effect fades within hours
Pharmacokinetics
- Metabolism
- In the liver, mainly by CYP3A4, to inactive products
- Elimination
- Mainly in the urine
- Half-life
- About 2.5 hours on average
Indications
- Short-term treatment of insomnia with difficulty falling asleep Insomnia disorder →
Adverse effects
Common
- Drowsiness and dizziness
- Headache
- Next-day sleepiness
Contraindications
- Previous complex sleep behaviour after zolpidem
- Hypersensitivity to zolpidem
Key interactions
- Alcohol, opioids, benzodiazepines and other central nervous system depressants
- Additive sedation and impaired breathing and driving
- Rifampin and St John's wort
- Lower zolpidem levels
- Ketoconazole
- Higher zolpidem levels
What is monitored
- Next-morning alertness and driving
- Falls in older adults
- Unusual night-time behaviours
Administration and safety
- Given by mouth right before bed, only when a full night in bed is possible
- Lower starting dose for women and older adults
- Controlled medicine
Nursing care
- Check how the person slept, next-morning alertness and falls
- Ask about alcohol and other sedatives
- Teach to take it only when a full night in bed is possible and not to drive the next morning if drowsy
- Teach to report sleepwalking, sleep-driving or other actions done while not fully awake
Pregnancy and breastfeeding
Use late in the third trimester can cause breathing depression and sedation in the newborn.
Test yourself
Think of the answer, then tap the question to see it.
Which GABA-A subunit does zolpidem prefer, and what follows?
α1, which mediates sedation, so zolpidem has weak anxiolytic and muscle-relaxant effects.
Why do women start on a lower zolpidem dose?
They clear it more slowly and have higher levels, with more next-morning impairment.
What must happen after an episode of sleep-driving on zolpidem?
The drug is stopped; a previous complex sleep behaviour contraindicates it.
Related drugs
Related conditions
← Back to the class: 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 - ZOLPIDEM TARTRATE tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); 8DD2: Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus Zolpidem (RCSB Protein Data Bank, 2022).
Spotted a mistake?We are always improving for the community. Tell us what is wrong and our team will review it.Report a mistake
Representative model, for educational purposes only.