Zolpidem, sold under the brand name Ambien, among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and behavioral changes, such as sleep hygiene, have been tried. It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer. It is taken by mouth and is available in conventional tablets, sublingual tablets, or oral spray.
|Trade names||Ambien and Ambien CR, Stilnox, others|
|By mouth (tablet), sublingual, oromucosal (spray), rectal|
|Drug class||Nonbenzodiazepine, sedative-hypnotic|
|Bioavailability||70% (by mouth)|
|Metabolism||Liver through CYP3A4 (~60%), CYP2C9 (~20%), and CYP1A2 (~14%)|
|Metabolites||(ZCA) zolpidem 6-carboxylic acid; (ZPCA) zolpidem phenyl-4-carboxylic acid|
|Onset of action||≤ 30 Minutes|
|Elimination half-life||2.0 - 3 hours|
|Duration of action||3 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||307.397 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. The previously recommended dose was decreased in 2013, by the US Food and Drug Administration (FDA), to the immediate-release 10 mg for men, and 5 mg for women, in an attempt to reduce next-day somnolence. Newer extended-release formulations include the 6.25 mg for women, and 12.5 mg or 6.25 mg for men, which also cause next-day somnolence when used in higher doses.[medical citation needed] Additionally, driving the next morning is not recommended with either higher doses or the long-acting formulation. While flumazenil, a GABAA–receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose.
Zolpidem is a nonbenzodiazepine which acts as a sedative and hypnotic. Zolpidem is a GABAA receptor agonist of the imidazopyridine class. It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines. It generally has a half-life of two to three hours. This, however, is increased in those with liver problems.
Zolpidem was approved for medical use in the United States in 1992. It became available as a generic medication in 2007. Zolpidem is a Schedule IV controlled substance under the Controlled Substances Act of 1970 (CSA). More than ten million prescriptions are filled each year in the United States, making it one of the most commonly used treatments for sleeping problems. In 2020, it was the 47th most commonly prescribed medication in the United States, with more than 14 million prescriptions.
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