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Zolpidem, sold under the brand name Ambien, among others, is a medication primarily used for the short-term treatment of sleeping problems.[8][10] Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and behavioral changes, such as sleep hygiene, have been tried.[11][12][13] It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer.[5] It is taken by mouth and is available in conventional tablets, sublingual tablets, or oral spray.[8]

Quick facts: Clinical data, Trade names, AHFS/Drugs.com, M...
Zolpidem
Clinical data
Trade namesAmbien and Ambien CR, Stilnox, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa693025
Pregnancy
category
Dependence
liability
Moderate[3]
Routes of
administration
By mouth (tablet), sublingual, oromucosal (spray), rectal
Drug classNonbenzodiazepine, sedative-hypnotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability70% (by mouth)
Protein binding92%
MetabolismLiver through CYP3A4 (~60%), CYP2C9 (~20%), and CYP1A2 (~14%)[7]
Metabolites(ZCA) zolpidem 6-carboxylic acid; (ZPCA) zolpidem phenyl-4-carboxylic acid
Onset of action≤ 30 Minutes
Elimination half-life2.0 - 3 hours[8][9]
Duration of action3 hours
ExcretionKidney (56%)
fecal (34%)
Identifiers
  • N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide hemitartrate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.115.604
Chemical and physical data
FormulaC19H21N3O
Molar mass307.397 g·mol−1
3D model (JSmol)
  • CN(C)C(=O)Cc1c(nc2ccc(C)cn12)c3ccc(C)cc3
  • InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 Y
  • Key:ZAFYATHCZYHLPB-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)
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Common side effects include daytime sleepiness, headache, nausea, and diarrhea.[8] More severe side effects include memory problems and hallucinations.[5] 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.[14] 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.[14] While flumazenil, a GABAA–receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose.[15]

Zolpidem is a nonbenzodiazepine which acts as a sedative and hypnotic.[8][15] Zolpidem is a GABAA receptor agonist of the imidazopyridine class.[8] It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines.[8] It generally has a half-life of two to three hours.[8] This, however, is increased in those with liver problems.[8]

Zolpidem was approved for medical use in the United States in 1992.[8][16] It became available as a generic medication in 2007.[17] Zolpidem is a Schedule IV controlled substance under the Controlled Substances Act of 1970 (CSA).[5][6] 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.[18][19] In 2020, it was the 47th most commonly prescribed medication in the United States, with more than 14 million prescriptions.[20][21]

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