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Zolpidem

Benzodiazepine · Hypnotic

Also known as zolpidem tartrate

BenzodiazepineHypnotic
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Avoid if possible; risk of neonatal withdrawal, hypothermia, and respiratory depression
FDA category + note
Top interactionssee all 12
  • MethylnaltrexoneSevereTextbookG&G 14e
  • NalmefeneSevereTextbookG&G 14e
  • NaloxoneSevereTextbookG&G 14e
  • NaltrexoneSevereTextbookG&G 14e

Mechanism

Zolpidem is an imidazopyridine (non-benzodiazepine) hypnotic that selectively binds to GABA-A receptors containing the α1 subunit — the predominant subtype mediating sedation and hypnosis. This α1 selectivity distinguishes it from benzodiazepines, which bind non-selectively to α1, α2, α3, and α5 subunit-containing receptors, and explains zolpidem's hypnotic effect with relatively less anxiolytic, muscle relaxant, and anticonvulsant activity. It has a short half-life (~2.5 hours) promoting sleep initiation without significant next-day sedation.

Indications

HypnoticInsomniashort-term (1–2 weeks) use in sleep onset insomniaintermittent awakenings

Dosing

Adult
10 mg at bedtime for up to 4 weeks. Debilitated patients: use elderly dose.
Renal adjustment
elimination of the drug is slower in patients with chronic renal insufficiency
Hepatic adjustment
Start with 5 mg; avoid in severe hepatic impairment
Geriatric
5 mg at bedtime for up to 4 weeks
Max dose
10 mg daily (adults); 5 mg daily (elderly)

Pharmacokinetics

Duration
Short duration of action. Minimal residual day time sedation or fading of hypnotic action on repeated nightly use.
Half-life
typically about 2 h
Bioavailability
about 70%
Protein binding
92%
Metabolism
eliminated almost entirely by conversion to inactive products in the liver, largely through oxidation of the methyl groups on the phenyl and imidazopyridine rings to the corresponding carboxylic acids
Excretion
<1%

Contraindications

  • Acute respiratory depression
  • Marked neuromuscular respiratory weakness
  • Obstructive sleep apnoea
  • Severe hepatic impairment
  • Psychotic illness

Side effects

Common
Anterograde amnesiaDizzinessHeadacheDrowsinessNauseaDiarrhoeaInfrequently produces residual daytime sedation or amnesiaMild rebound insomnia on the first night of withdrawal may occurmorning sedation (if taken late at night)prolongation of reaction-time (if taken late at night)
Serious
  • Paradoxical reactions (aggression, hallucinations)
  • Complex sleep behaviours (sleepwalking, sleep-driving)
  • Respiratory depression
  • Angioedema
  • Falls (elderly)
  • near absence of tolerance
  • low abuse potential
  • safety in overdose like BZDs
  • does not markedly depress respiration even in large doses
  • no/little rebound insomnia on discontinuation

Pregnancy & lactation

Pregnancy

Avoid if possible; risk of neonatal withdrawal, hypothermia, and respiratory depression

Drug interactions

Methylnaltrexone
Severe
Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Nalmefene
Severe
Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Naloxone
Severe
Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Naltrexone
Severe
Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Other Cns Depressants
Severe
Textbook

Typically fatal if combined in overdose.

Use with extreme caution; avoid if possible.

Source: G&G 14e

Alfentanil
Severe
Database

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Buprenorphine
Severe
Database

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: DDInter

Butorphanol
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Ciprofloxacin
Severe
Database

Drug interaction classified as: metabolism.

Source: DDInter

Codeine
Severe
Database

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: DDInter

Dextropropoxyphene
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Benzodiazepine drugs

Ask House about Zolpidem

Continue into a citation-backed clinical answer with the drug context already attached.

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