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Zolpidem (Ambien)
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our most widely used hypnotic, is approved only for short-term management of insomnia. However, although approval is limited to short-term use, many patients have taken the drug long term with no apparent tolerance or increase in adverse effects. All zolpidem formulations have a rapid onset, and hence can help people who have difficulty falling asleep. In addition, the extended-release formulation—Ambien CR—can help people who have difficulty maintaining sleep.
Although structurally unrelated to the benzodiazepines, zolpidem binds to the benzodiazepine receptor site on the GABA receptor-chloride channel complex and shares some properties of the benzodiazepines. Like the benzodiazepines, zolpidem can reduce sleep latency and awakenings and can prolong sleep duration. The drug does not significantly reduce time in rapid-eye-movement (REM) sleep and causes little or no rebound insomnia when therapy is discontinued. In contrast to the benzodiazepines, zolpidem lacks anxiolytic, muscle relaxant, and anticonvulsant actions. Why? Because zolpidem doesn't bind with all benzodiazepine receptors. Rather, binding is limited to the benzodiazepine1 subtype of benzodiazepine receptors.
Zolpidem is rapidly absorbed following oral administration. Plasma levels peak in 2 hours. The drug is widely distributed, although levels in the brain remain low. Zolpidem is extensively metabolized to inactive compounds that are excreted in the bile, urine, and feces. The elimination half-life is 2.4 hours.
Zolpidem has a side effect profile like that of the benzodiazepines. Daytime drowsiness and dizziness are most common, and these occur in only 1% to 2% of patients. Like the benzodiazepines, zolpidem has been associated with sleep driving and other sleep-related complex behaviors. At therapeutic doses, zolpidem causes little or no respiratory depression. Safety in pregnancy has not been established. According to the FDA, zolpidem may pose a small risk of anaphylaxis and angioedema.
Short-term treatment is not associated with significant tolerance or physical dependence. Withdrawal symptoms are minimal or absent. Similarly, the abuse liability of zolpidem is low. Accordingly, the drug is classified under Schedule IV of the Controlled Substances Act.
Like other sedative-hypnotics, zolpidem can intensify the effects of other CNS depressants. Accordingly, patients should be warned against combining zolpidem with alcohol and all other drugs that depress CNS function.
Although structurally unrelated to the benzodiazepines, zolpidem binds to the benzodiazepine receptor site on the GABA receptor-chloride channel complex and shares some properties of the benzodiazepines. Like the benzodiazepines, zolpidem can reduce sleep latency and awakenings and can prolong sleep duration. The drug does not significantly reduce time in rapid-eye-movement (REM) sleep and causes little or no rebound insomnia when therapy is discontinued. In contrast to the benzodiazepines, zolpidem lacks anxiolytic, muscle relaxant, and anticonvulsant actions. Why? Because zolpidem doesn't bind with all benzodiazepine receptors. Rather, binding is limited to the benzodiazepine1 subtype of benzodiazepine receptors.
Zolpidem is rapidly absorbed following oral administration. Plasma levels peak in 2 hours. The drug is widely distributed, although levels in the brain remain low. Zolpidem is extensively metabolized to inactive compounds that are excreted in the bile, urine, and feces. The elimination half-life is 2.4 hours.
Zolpidem has a side effect profile like that of the benzodiazepines. Daytime drowsiness and dizziness are most common, and these occur in only 1% to 2% of patients. Like the benzodiazepines, zolpidem has been associated with sleep driving and other sleep-related complex behaviors. At therapeutic doses, zolpidem causes little or no respiratory depression. Safety in pregnancy has not been established. According to the FDA, zolpidem may pose a small risk of anaphylaxis and angioedema.
Short-term treatment is not associated with significant tolerance or physical dependence. Withdrawal symptoms are minimal or absent. Similarly, the abuse liability of zolpidem is low. Accordingly, the drug is classified under Schedule IV of the Controlled Substances Act.
Like other sedative-hypnotics, zolpidem can intensify the effects of other CNS depressants. Accordingly, patients should be warned against combining zolpidem with alcohol and all other drugs that depress CNS function.