Comparative Pharmacology
Head-to-head clinical analysis: AMBIEN versus AMBIEN CR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMBIEN versus AMBIEN CR.
AMBIEN vs AMBIEN CR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Positive allosteric modulator of GABA-A receptors, enhancing the inhibitory effects of GABA. Binds selectively to the alpha-1 subunit, producing sedative, hypnotic, and anxiolytic effects.
AMBIEN CR's active ingredient is zolpidem, a non-benzodiazepine hypnotic that binds selectively to the benzodiazepine-1 (BZ1) receptor subtype on the GABA-A receptor complex, potentiating GABAergic inhibition and promoting sleep.
5-10 mg orally once daily at bedtime, maximum 10 mg/day.
12.5 mg orally once daily immediately before bedtime; lower dose of 6.25 mg may be considered. Not to exceed 12.5 mg per day.
None Documented
None Documented
Terminal elimination half-life is approximately 2.6 hours (range 1.4–4.5 hours). In elderly patients, half-life may be prolonged to about 2.9 hours. In patients with hepatic cirrhosis, half-life is significantly increased (up to 9.8 hours).
Zolpidem immediate-release: ~2.5 h (range 1.4–3.8 h); modified-release (Ambien CR): ~2.8 h (range 1.6–4.5 h). Clinical note: Half-life increased in hepatic impairment and elderly.
Primarily renal excretion: approximately 56% of the dose is recovered in urine as metabolites (including 5% unchanged drug). Fecal excretion accounts for about 34% of the dose. Small amounts are excreted in bile.
Primarily renal (80% as metabolites, <5% unchanged), minor fecal (<10%)
Category C
Category C
Sedative-Hypnotic
Sedative-Hypnotic