Hypnotic medication
Zolpidem Trade names Ambien and Ambien CR, others[ 1] AHFS /Drugs.com Monograph MedlinePlus a693025 License data
Pregnancy category 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 ATC code Legal status
Bioavailability 70% (by mouth) Protein binding 92%[ 9] Metabolism Liver through CYP3A4 (~60%), CYP2C9 (~20%), and CYP1A2 (~14%)[ 11] Metabolites (ZCA) zolpidem 6-carboxylic acid; (ZPCA) zolpidem phenyl-4-carboxylic acid Onset of action ≤ 30 Minutes Elimination half-life 2.0 - 3 hours[ 10] [ 9] Duration of action 3 hours Excretion Kidney (56%)fecal (34%)
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 InfoCard 100.115.604 Formula C 19 H 21 N 3 O Molar mass 307.397 g·mol−1 3D model (JSmol ) Melting point 193–197 °C (379–387 °F) [ 9]
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
N Y (what is this?) (verify)
Zolpidem , sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems .[ 10] [ 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 .[ 10]
Common side effects include daytime sleepiness , headache, nausea, and diarrhea.[ 10] 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 .[ 10] [ 16] Zolpidem is a GABAA receptor agonist of the imidazopyridine class.[ 10] It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines .[ 10] It generally has a half-life of two to three hours.[ 10] This, however, is increased in those with liver problems .[ 10]
Zolpidem was approved for medical use in the United States in 1992.[ 10] [ 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]
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^ "Zolpidem Use During Pregnancy" . Drugs.com . 30 June 2020. Retrieved 14 August 2020 .
^ Ries RK (2009). Principles of addiction medicine (4 ed.). Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins. p. 106. ISBN 978-0-7817-7477-2 . Archived from the original on 8 September 2017.
^ Victorri-Vigneau C, Gérardin M, Rousselet M, Guerlais M, Grall-Bronnec M, Jolliet P (January 2014). "An update on zolpidem abuse and dependence". Journal of Addictive Diseases . 33 (1): 15–23. doi :10.1080/10550887.2014.882725 . ISSN 1055-0887 . PMID 24467433 .
^ "Scheduling of zolpidem (Stilnox)" . Therapeutic Goods Administration (TGA) . 21 February 2008. Retrieved 15 August 2020 .
^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 3 August 2023 .
^ a b c d Matheson E, Hainer BL (July 2017). "Insomnia: Pharmacologic Therapy" . American Family Physician . 96 (1): 29–35. PMID 28671376 .
^ a b "Ambien- zolpidem tartrate tablet, film coated" . DailyMed . 29 August 2019. Retrieved 15 August 2020 .
^ a b c Salvà P, Costa J (September 1995). "Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications". Clinical Pharmacokinetics . 29 (3): 142–153. doi :10.2165/00003088-199529030-00002 . PMID 8521677 . S2CID 23391285 .
^ a b c d e f g h i j "Zolpidem (Monograph)" . The American Society of Health-System Pharmacists. 27 April 2023. Retrieved 10 March 2024 .
^ Von Moltke LL, Greenblatt DJ, Granda BW, Duan SX, Grassi JM, Venkatakrishnan K, et al. (July 1999). "Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations" . British Journal of Clinical Pharmacology . 48 (1): 89–97. doi :10.1046/j.1365-2125.1999.00953.x . PMC 2014868 . PMID 10383565 .
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^ Cite error: The named reference NICE2014
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^ Cite error: The named reference EUsleep2017
was invoked but never defined (see the help page ).
^ Cite error: The named reference ACP2016
was invoked but never defined (see the help page ).
^ a b Gunja N (June 2013). "The clinical and forensic toxicology of Z-drugs" . Journal of Medical Toxicology . 9 (2): 155–62. doi :10.1007/s13181-013-0292-0 . PMC 3657020 . PMID 23404347 .
^ "Drug Approval Package: Ambien (Zolpidem Tartrate) NDA 19908" . U.S. Food and Drug Administration (FDA) . 24 December 1999. Retrieved 15 August 2020 .
^ "FDA Approves First Generic Versions of Ambien (Zolpidem Tartrate) for the Treatment of Insomnia" . U.S. Food and Drug Administration (FDA) (Press release). Archived from the original on 6 March 2010. Retrieved 24 January 2010 .
^ "Zolpidem" . LiverTox . Archived from the original on 16 March 2018. Retrieved 15 March 2018 .
^ "Some Sleep Drugs Can Impair Driving" . U.S. Food and Drug Administration (FDA) . 13 June 2013. Retrieved 15 March 2018 .
^ "The Top 300 of 2021" . ClinCalc . Archived from the original on 15 January 2024. Retrieved 14 January 2024 .
^ "Zolpidem - Drug Usage Statistics" . ClinCalc . Retrieved 14 January 2024 .