zolpidem AMBIEN
Class: Nonbenzodiazepine/ImidazopyridineFDA Indications: Short-term Treatment Of Insomnia
Off-Label Use: Jet Lag, Analgesia
Prescribing
FDA Schedule IVForms: 5, 10mg tablet; 6.25, 12.5mg CR tablet; 1.75, 3.5mg sublingual tab (Intermezzo)
Dose Range: 10-20 mg/day
Starting: 10 mg qhs; recommend start at 5 mg for women, elderly, patients with lower body weight. PDR lists maximum dose of 10 mg, but in practice many patients require and tolerate 20 mg QHS dosing.
Stopping: Taper to avoid rebound insomnia
Precautions
Contraindications: None, other than patients with known hypersensitivity to zolpidemSerious Side Effects: Anterograde amnesia; somnambulism (0.3-1%), sleep related eating and sleep-driving
Side Effects: daytime somnolence, dizziness, amnesia, amnesia, nausea
Pharmacodynamics
1° MOA: GABAAR α1 subunit agonistTarget: GABAA α1
Pharmacokinetics
t½: 2.5 (1.4-4.5)° TMAX: 1.5°Absorption Rate: Rapid
Substrate of: 3A4, 2C9; 1A2
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - caution with other CNS-depressants
- - 3A4 inhibitors can ↑ levels
Misc
- - preserves normal sleep architecture
- - preferential binding of GABAAR α1 subunits > α2/α3 subunits → sedation > anxiolysis
Special Populations
Category C—Crosses the placenta. No studies in pregnant women.
RID 4.7-19.1%; ∅ AE's have been reported in exposed infants
Start at 5mg to ↓ chances of motor and/or cognitive impairment
2019 BEE℞S Recommendation: Avoid. Nonbenzodiazepine benzodiazepine receptor agonist hypnotics (ie, Z drugs) have adverse events similar to those of benzodiazepines in older adults (eg, delirium, falls, fractures); increased emergency room visits/ hospitalizations; motor vehicle crashes; minimal improvement in sleep latency and duration.
No dosage adjustment necessary.
↓ dose to 5 mg qhs for hepatically impaired
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