Why is AMBIEN CR unique?

AMBIEN CR is a non-benzodiazepine.

AMBIEN CR is not a benzodiazepine-in fact, it's a distinct non-benzodiazepine hypnotic of the imidazopyridine class. It has a chemical structure (shown below) that is different from those of benzodiazepines, barbiturates, or other drugs with known hypnotic properties.¹

AMBIEN CR works through preferential binding

AMBIEN CR works by binding preferentially to the omega-1 (BZ-1) receptor subtype of the GABA_A receptor complex.¹ This subtype is thought to be the one most closely associated with sleep.²
In contrast, benzodiazepines do not have a receptor preference, so they bind to-and activate-all omega (BZ) receptor subtypes. Other omega (BZ) receptor subtypes are associated with anxiolytic, myorelaxant, and anticonvulsant activity.^1,2

The primary effect is sleep

Even though the selective binding of AMBIEN CR to the omega-1 (BZ-1) receptor is not absolute, it may help explain the relative absence of myorelaxant and anticonvulsant effects in animal studies, as well as the preservation of deep sleep (stages 3 and 4) in human studies of AMBIEN CR at hypnotic doses.¹

Important safety information:

AMBIEN CR is indicated for the treatment of insomnia.

In elderly or debilitated patients, or patients with hepatic insufficiency, the recommended dose is 6.25 mg and patients should be closely monitored. Due to its rapid onset of action, patients should take AMBIEN CR right before going to bed and when ready for sleep.

Patients should not take AMBIEN CR unless they are prepared to get a full night's sleep (7 to 8 hours) to avoid residual effects.

Until they know how it will affect their physical or mental performance upon awakening, patients should not drive or operate hazardous machinery after taking AMBIEN CR or any other sleep medication. Complex behaviors such as somnambulism, including driving or eating while not fully awake, with amnesia for the event, have been reported in patients who have taken a sedative hypnotic. Discontinuation of AMBIEN CR should be strongly considered for patients reporting such complex behaviors. Rare cases of angioedema have been reported in patients after taking sedative hypnotics. Patients who develop angioedema should not be rechallenged. The most commonly observed adverse effects in controlled clinical trials were headache, somnolence, and dizziness. Because individuals with a history of addiction or substance abuse are at increased risk of habituation and dependence, they should be under careful surveillance when receiving AMBIEN CR or any o ther hypnotic. AMBIEN CR is a Schedule IV controlled substance. US clinical trial experience from zolpidem does not reveal any clear evidence for withdrawal syndrome.

Please refer to the full prescribing information.

References:

1 AMBIEN CR Prescribing Information.
2 Sanger DJ, Benavides J, Perrault G, et al. Recent developments in the behavioral pharmacology of benzodiazepine ( Omega

) receptors: evidence for the functional significance of receptor subtypes. Neurosci Biobehav Rev. 1994;18:355-372.