Comparative Pharmacology
Head-to-head clinical analysis: AMBIEN CR versus EQUANIL.
Head-to-head clinical analysis: AMBIEN CR versus EQUANIL.
AMBIEN CR vs EQUANIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Gamma-aminobutyric acid (GABA) receptor positive allosteric modulator; increases frequency of chloride channel opening, potentiating inhibitory neurotransmission.
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.
400 mg orally 3-4 times daily; maximum 2400 mg/day. Alternatively, 200 mg orally 3-4 times daily for mild anxiety.
None Documented
None Documented
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.
Terminal elimination half-life is 6-20 hours (mean 10 hours). In hepatic cirrhosis, half-life may be prolonged to 24-36 hours due to impaired clearance.
Primarily renal (80% as metabolites, <5% unchanged), minor fecal (<10%)
Primarily renal excretion of conjugated metabolites (inactive); approximately 90% of a dose is excreted in urine, with less than 10% in feces. Less than 5% is excreted unchanged.
Category C
Category C
Sedative-Hypnotic
Sedative-Hypnotic