Back زولبيديم Arabic زولپیدم AZB Zolpidem Czech Solpidem Welsh Zolpidem German Ζολπιδέμη Greek Zolpidem Spanish زولپیدم Persian Tsolpideemi Finnish Zolpidem French

Zolpidem

Zolpidem
Clinical data
Trade namesAmbien and Ambien CR, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa693025
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 classNonbenzodiazepine, sedative-hypnotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability70% (by mouth)
Protein binding92%[9]
MetabolismLiver 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-life2.0 - 3 hours[10][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 Edit this at Wikidata
Chemical and physical data
FormulaC19H21N3O
Molar mass307.397 g·mol−1
3D model (JSmol)
Melting point193–197 °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 checkY
  • Key:ZAFYATHCZYHLPB-UHFFFAOYSA-N checkY
 ☒NcheckY (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]

  1. ^ Cite error: The named reference genericnames was invoked but never defined (see the help page).
  2. ^ "Zolpidem Use During Pregnancy". Drugs.com. 30 June 2020. Retrieved 14 August 2020.
  3. ^ 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.
  4. ^ 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.
  5. ^ "Scheduling of zolpidem (Stilnox)". Therapeutic Goods Administration (TGA). 21 February 2008. Retrieved 15 August 2020.
  6. ^ 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.
  7. ^ a b c d Matheson E, Hainer BL (July 2017). "Insomnia: Pharmacologic Therapy". American Family Physician. 96 (1): 29–35. PMID 28671376.
  8. ^ a b "Ambien- zolpidem tartrate tablet, film coated". DailyMed. 29 August 2019. Retrieved 15 August 2020.
  9. ^ 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.
  10. ^ 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.
  11. ^ 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.
  12. ^ Cite error: The named reference UKlabel was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference NICE2014 was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference EUsleep2017 was invoked but never defined (see the help page).
  15. ^ Cite error: The named reference ACP2016 was invoked but never defined (see the help page).
  16. ^ 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.
  17. ^ "Drug Approval Package: Ambien (Zolpidem Tartrate) NDA 19908". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 15 August 2020.
  18. ^ "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.
  19. ^ "Zolpidem". LiverTox. Archived from the original on 16 March 2018. Retrieved 15 March 2018.
  20. ^ "Some Sleep Drugs Can Impair Driving". U.S. Food and Drug Administration (FDA). 13 June 2013. Retrieved 15 March 2018.
  21. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  22. ^ "Zolpidem - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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