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zaleplon

Novel Benzodiazepine Receptor Site Agonist · Hypnotic

Novel Benzodiazepine Receptor Site AgonistHypnotic
CDSCO approved
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
—
not curated
Top interactionssee all 12 →
  • AlfentanilSevereDatabaseDDInter
  • BenzhydrocodoneSevereDatabaseDDInter
  • BuprenorphineSevereDatabaseDDInter
  • ButorphanolSevereDatabaseDDInter

Mechanism

Zaleplon preferentially binds to the benzodiazepine binding site on GABAA receptors containing the α1 receptor subunit, enhancing GABAA receptor function.

Indications

InsomniaSleep-onset insomniasleep-onset insomnia (use should be limited to 1–2 weeks)

Dosing

Adult
5-, 10-, or 20-mg doses

Pharmacokinetics

Duration
Shortest acting, effective only in sleep-onset insomnia. Can be taken late at night (> 4 hours before waking time) without causing morning sedation. No day-time anxiety or rebound insomnia observed. Hypnotic effect does not fade on nightly use.
Half-life
about 1 h
Bioavailability
about 30% (because of presystemic metabolism)
Metabolism
largely by aldehyde oxidase and to a lesser extent by CYP3A4

Side effects

Serious
  • tolerance and dependence is unusual

Drug interactions

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Buprenorphine
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Butorphanol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Codeine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Dextropropoxyphene
Severe
Database

Clinical effect not specified

Source: DDInter

Dezocine
Severe
Database

Clinical effect not specified

Source: DDInter

Dihydrocodeine
Severe
Database

Clinical effect not specified

Source: DDInter

Fentanyl
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Hydrocodone
Severe
Database

.

Source: DDInter

Hydromorphone
Severe
Database

Clinical effect not specified

Source: DDInter

Levacetylmethadol
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Irritable bowel syndrome
ISG · Gastroenterology · 2023
Neonatal infection
NICE · Neonatology · 2021
Status epilepticus
AAN · Neurology · 2020
Fetal growth restriction
FOGSI · Obstetrics & Gynaecology · 2018

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team