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AMBIEN CR® (zolpidem tartrate) Mechanism of Action
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AMBIEN CR (Zolpidem Tartrate Extended Release) Sleep Aid

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AMBIEN CR Mechanism of Action

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AMBIEN CR works by binding preferentially to the omega-1 (BZ1) receptor subtype of the GABA receptor complex. This subtype is thought to be the one most closely associated with sleep.4,6-8

AMBIEN CR is a non-benzodiazepine

AMBIEN CR is a non-benzodiazepine hypnotic agent of the imidazopyridine class. Its chemical structure differs from benzodiazepines, barbiturates, or other drugs with known hypnotic properties.4

Differences from traditional benzodiazepines

Benzodiazepines do not have a receptor preference, so they indiscriminately bind to—and activate—all omega (BZ) receptor subtypes, some of which are believed to be associated with sedative, anxiolytic, myorelaxant, and anticonvulsant activity.4,6,13

While the selective binding of AMBIEN CR to the omega-1 (BZ1) 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.4,6,13

Next: Pharmacokinetics

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* Maximum benefit is $240 off, up to $20 off each prescription (up to 12 prescriptions), depending on your out-of-pocket costs. Not valid for patients participating in Medicare, Medicaid, government (public insurance) programs, or any private payor in the state of Massachusetts and where prohibited by law.

AMBIEN CR is indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.

IMPORTANT SAFETY INFORMATION

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, as well as abnormal behaviors such as being more outgoing or aggressive than normal, confusion, agitation, and hallucinations may occur. AMBIEN CR should not be taken with alcohol as it may increase these abnormal behaviors. Discontinuation of AMBIEN CR should be strongly considered for patients reporting such complex behaviors. Angioedema may occur in patients taking AMBIEN CR and in rare cases may be fatal. Patients who develop angioedema should not be rechallenged. In primarily depressed patients, worsening of depression, including risk of suicidal thoughts or actions, including completed suicides, have been reported. 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 other hypnotic. AMBIEN CR is a Schedule IV controlled substance.

Please refer to the full prescribing information.