Zolpidem
Hypnotic medication / From Wikipedia, the free encyclopedia
Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems.[11][12] Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and after behavioral changes, such as sleep hygiene, have been tried.[13][14][15] It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer.[7] It is taken by mouth and is available in conventional tablets, sublingual tablets, or oral spray.[11]
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Trade names | Ambien and Ambien CR, others[1] |
AHFS/Drugs.com | Monograph |
MedlinePlus | a693025 |
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Dependence liability | Physical: High Psychological: Moderate[3] |
Addiction liability | High[4] |
Routes of administration | By mouth, sublingual, oromucosal (spray), rectal |
Drug class | Nonbenzodiazepine, sedative-hypnotic |
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Bioavailability | 70% (by mouth) |
Protein binding | 92%[9] |
Metabolism | Liver through CYP3A4 (~60%), CYP2C9 (~20%), and CYP1A2 (~14%)[10] |
Metabolites | (ZCA) zolpidem 6-carboxylic acid; (ZPCA) zolpidem phenyl-4-carboxylic acid |
Onset of action | ≤ 30 Minutes |
Elimination half-life | 2.0 - 3 hours[11][9] |
Duration of action | 3 hours |
Excretion | Kidney (56%) fecal (34%) |
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ECHA InfoCard | 100.115.604 |
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Formula | C19H21N3O |
Molar mass | 307.397 g·mol−1 |
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Melting point | 193–197 °C (379–387 °F) [9] |
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Common side effects include daytime sleepiness, headache, nausea, and diarrhea.[11] More severe side effects include memory problems and hallucinations.[7] While flumazenil, a GABAA–receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose.[16]
Zolpidem is a nonbenzodiazepine or Z-drug which acts as a sedative and hypnotic.[11][16] Zolpidem is a GABAA receptor agonist of the imidazopyridine class.[11] It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines.[11] It generally has a half-life of two to three hours.[11] This, however, is increased in those with liver problems.[11]
Zolpidem was approved for medical use in the United States in 1992.[11][17] It became available as a generic medication in 2007.[18] Zolpidem is a Schedule IV controlled substance under the Controlled Substances Act of 1970 (CSA).[7][8] 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.[19][20] In 2021, it was the 63rd most commonly prescribed medication in the United States, with more than 10 million prescriptions.[21][22]