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zolpidem

Brand: Ambien, Ambien CR, Intermezzo, Edluar, Zolpimist

⚠ BBW Beers Criteria Prototype Drug
Drug Class: sedative-hypnotic
Drug Family: sedative/hypnotic
Subclass: non-benzodiazepine GABA-A agonist (Z-drug) / imidazopyridine
Organ Systems: cns

Mechanism of Action

Selectively binds the BZ1 (omega-1) subtype of GABA-A receptors containing alpha-1 subunits, producing sedation and hypnosis with reduced anxiolytic, muscle relaxant, and anticonvulsant effects compared to benzodiazepines; selectivity is dose-dependent.

GABA-A receptor (BZ1/omega-1 subtype selective)

Indications

  • insomnia (sleep onset; CR formulation for maintenance)

Contraindications

  • severe hepatic impairment
  • complex sleep behaviors from prior zolpidem use

Adverse Effects

Common

  • daytime drowsiness
  • dizziness
  • headache
  • anterograde amnesia
  • ataxia

Serious

  • complex sleep behaviors (sleepwalking, sleep-driving, preparing and eating food while asleep — may be fatal)
  • dependency
  • respiratory depression with CNS depressants
  • worsening depression/suicidal ideation

Pharmacokinetics (ADME)

Absorption Rapid absorption; bioavailability ~70%; food delays absorption
Distribution Protein binding 92%; Vd 0.54 L/kg
Metabolism CYP3A4 (primary), CYP2C9, CYP1A2 to inactive metabolites
Excretion Renal (~56%) and fecal (~37%)
Half-life 1.5–2.4 hours (IR); 2.8 hours (CR); prolonged in elderly and hepatic impairment
Onset 15–30 minutes
Peak 1.6 hours
Duration 4–6 hours (IR); 6–8 hours (CR)
Protein Binding 92%
Vd 0.54 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
CNS depressants/alcohol additive CNS depression; respiratory depression major
CYP3A4 inhibitors increase zolpidem levels moderate
rifampin CYP3A4 induction reduces zolpidem efficacy moderate

Nursing Considerations

  1. Counsel patients to take only when able to devote 7–8 hours to sleep; taking with less sleep time available increases morning drowsiness and impaired driving — particularly dangerous the morning after taking the CR formulation
  2. FDA-recommended doses for women are half those for men (lower CYP3A4 metabolism rate in women); women: 5 mg IR or 6.25 mg CR; men: 10 mg IR or 12.5 mg CR
  3. Assess for complex sleep behaviors at every follow-up; instruct patient and household members to report any activity occurring during apparent sleep — discontinue immediately if such behavior occurs
  4. Beers Criteria drug in elderly — significantly increased fall and fracture risk; cognitive impairment; recommend non-pharmacological sleep interventions as first-line

Clinical Pearls

  • Zolpidem's selectivity for alpha-1-containing GABA-A receptors (BZ1 subtype) theoretically reduces tolerance and dependence compared to benzodiazepines, but clinical practice shows similar dependence patterns with prolonged use
  • Morning 'hangover' impairment is significant enough that the FDA requires women to take half the dose of men due to demonstrably slower clearance — a rare example of sex-based dosing

Safety Profile

Pregnancy use-with-caution
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.

Insomnia (sleep Onset; CR Formulation For Maintenance) Sedative-hypnotic
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