BLACK BOX WARNING
- complex sleep behaviors including sleepwalking, sleep-driving; discontinue if complex sleep behavior occurs
zaleplon
Brand: Sonata
⚠ BBW Beers Criteria Prototype: zolpidem
Drug Class: non-benzodiazepine hypnotic (Z-drug)
Drug Family: sedative/hypnotic
Subclass: pyrazolopyrimidine GABA-A BZ1 modulator
Organ Systems: cns
Mechanism of Action
Pyrazolopyrimidine that selectively binds the BZ1 site on GABA-A receptors containing alpha1 subunits, producing sedation. Shortest-acting Z-drug — ultra-short half-life of 1 hour; minimal residual sedation.
GABA-A receptor (alpha1 subunit — BZ1 site)
Indications
- short-term treatment of insomnia (sleep onset only; not sleep maintenance)
Contraindications
- severe hepatic impairment
Adverse Effects
Common
- drowsiness
- headache
- dizziness
- memory impairment
Serious
- complex sleep behaviors (rare)
- dependence
- respiratory depression
Pharmacokinetics (ADME)
| Absorption | oral; food significantly delays absorption; avoid with heavy meal |
| Distribution | 60% protein bound |
| Metabolism | hepatic via CYP3A4 and aldehyde oxidase to inactive metabolites |
| Excretion | renal |
| Half-life | 1 hour |
| Onset | 15–30 minutes |
| Peak | 1 hour |
| Duration | 3–4 hours |
| Protein Binding | 60% |
| Vd | 1.4 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP3A4 inhibitors | increase zaleplon levels | moderate |
| cimetidine | inhibits both CYP3A4 and aldehyde oxidase; 85% increase in zaleplon AUC | major |
Nursing Considerations
- Zaleplon's 1-hour half-life allows it to be taken in the middle of the night as long as 4 hours of sleep remain; unique attribute among hypnotics.
- Avoid heavy meals before taking; food delays absorption significantly.
- Risk of dependence and complex sleep behaviors are similar to zolpidem despite shorter half-life.
- Not suitable for sleep maintenance insomnia (waking in the middle of the night); only benefits sleep onset.
Clinical Pearls
- Zaleplon's ultra-short half-life (1 hour) is its defining pharmacokinetic feature, enabling middle-of-the-night dosing without morning impairment — however, it provides no sleep maintenance benefit.
- Among Z-drugs (zaleplon, zolpidem, eszopiclone), zaleplon has the least evidence for sleep maintenance and shortest duration, but carries the same complex sleep behavior risk.
Safety Profile
Pregnancy avoid
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.