User:Mr. Ibrahem/Diazepam

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Mr. Ibrahem/Diazepam
Clinical data
Pronunciation/daɪˈæzɪpæm/
Trade namesValium, Vazepam, Valtoco, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa682047
License data
Pregnancy
category
  • AU: C
Dependence
liability		High[2]
Addiction
liability		Moderate[3][4]
Routes of
administration		By mouth, IM, IV, rectal, nasal spray[5]
Legal status
Legal status
Pharmacokinetic data
Bioavailability76% (64–97%) by mouth, 81% (62–98%) rectal[7]
MetabolismLiver—CYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to desmethyldiazepam
Elimination half-life(50 hours); 20–100 hours (36–200 hours for main active metabolite desmethyldiazepam)[8][6]
ExcretionKidney
Identifiers
  • 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one[1]
Chemical and physical data
FormulaC16H13ClN2O
Molar mass284.74 g·mol−1
3D model (JSmol)
  • CN1C2=C(C(C3=CC=CC=C3)=NCC1=O)C=C(Cl)C=C2
  • InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3 checkY
  • Key:AAOVKJBEBIDNHE-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect.[11] It is commonly used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, muscle spasms, trouble sleeping, and restless legs syndrome.[11] It may also be used to cause memory loss during certain medical procedures.[12][13] It can be taken by mouth, inserted into the rectum, injected into muscle, injected into a vein or used as a nasal spray.[5][13] When given into a vein, effects begin in one to five minutes and last up to an hour.[13] By mouth, effects begin after 15 to 60 minutes.[14]

Common side effects include sleepiness and trouble with coordination.[13][8] Serious side effects are rare.[11] They include suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy.[11][13][15] Occasionally, excitement or agitation may occur.[16][17] Long term use can result in tolerance, dependence, and withdrawal symptoms on dose reduction.[11] Abrupt stopping after long-term use can be potentially dangerous.[11] After stopping, cognitive problems may persist for six months or longer.[16] It is not recommended during pregnancy or breastfeeding.[13] Its mechanism of action is by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA).[16]

Diazepam was patented in 1959 by Hoffmann-La Roche.[11][18][19] It has been one of the most frequently prescribed medications in the world since its launch in 1963.[11] In the United States it was the highest selling medication between 1968 and 1982, selling more than two billion tablets in 1978 alone.[11] In 2017, it was the 135th most commonly prescribed medication in the United States, with more than five million prescriptions.[20][21] In 1985 the patent ended, and there are now more than 500 brands available on the market.[11] It is on the World Health Organization's List of Essential Medicines as an alternative to lorazepam.[22] The wholesale cost in the developing world is about US$0.01 per dose as of 2015.[23] In the United States, it is about US$0.40 per dose.[13]

References[edit]

  1. ^ a b "National Highway Traffic Safety Administration Drugs and Human Performance Fact Sheet- Diazepam". Archived from the original on 2017-03-27. Retrieved 2017-11-13.
  2. ^ Edmunds, Marilyn; Mayhew, Maren (17 April 2013). Pharmacology for the Primary Care Provider (4th ed.). Mosby. p. 545. ISBN 9780323087902. Archived from the original on 1 August 2020. Retrieved 31 July 2020.
  3. ^ Clinical Addiction Psychiatry. Cambridge University Press. 2010. p. 156. ISBN 9781139491693. Archived from the original on 2017-09-08.
  4. ^ Ries, Richard K. (2009). Principles of addiction medicine (4 ed.). Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins. p. 106. ISBN 9780781774772. Archived from the original on 2017-09-08.
  5. ^ a b "Valtoco- diazepam spray". DailyMed. 13 January 2020. Archived from the original on 1 August 2020. Retrieved 13 February 2020.
  6. ^ a b "Diazepam Tablets BP 10mg - Summary of Product Characteristics (SmPC)". (emc). 16 September 2019. Archived from the original on 25 July 2020. Retrieved 25 July 2020.
  7. ^ Dhillon S, Oxley J, Richens A (March 1982). "Bioavailability of diazepam after intravenous, oral and rectal administration in adult epileptic patients". British Journal of Clinical Pharmacology. 13 (3): 427–32. doi:10.1111/j.1365-2125.1982.tb01397.x. PMC 1402110. PMID 7059446.
  8. ^ a b "Valium- diazepam tablet". DailyMed. 8 November 2019. Archived from the original on 28 June 2019. Retrieved 30 December 2019.
  9. ^ "DIAZEPAM emulsion - Essential drugs". medicalguidelines.msf.org. Retrieved 1 September 2020.
  10. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 28 July 2020. Retrieved 30 August 2020.
  11. ^ a b c d e f g h i j Calcaterra NE, Barrow JC (April 2014). "Classics in chemical neuroscience: diazepam (valium)". ACS Chemical Neuroscience. 5 (4): 253–60. doi:10.1021/cn5000056. PMC 3990949. PMID 24552479.
  12. ^ "Diazepam". PubChem. National Institute of Health: National Library of Medicine. 2006. Archived from the original on 2015-06-30. Retrieved 2006-03-11.
  13. ^ a b c d e f g "Diazepam". The American Society of Health-System Pharmacists. Archived from the original on 2015-06-30. Retrieved 2015-06-05.
  14. ^ Dhaliwal JS, Saadabadi A (2019). "Diazepam". StatPearls. StatPearls Publishing. PMID 30725707. Archived from the original on 8 March 2021. Retrieved 2019-10-13.
  15. ^ Dodds TJ (March 2017). "Prescribed Benzodiazepines and Suicide Risk: A Review of the Literature". The Primary Care Companion for CNS Disorders. 19 (2). doi:10.4088/PCC.16r02037. PMID 28257172.
  16. ^ a b c Riss J, Cloyd J, Gates J, Collins S (August 2008). "Benzodiazepines in epilepsy: pharmacology and pharmacokinetics". Acta Neurologica Scandinavica. 118 (2): 69–86. doi:10.1111/j.1600-0404.2008.01004.x. PMID 18384456.
  17. ^ Perkin, Ronald M. (2008). Pediatric hospital medicine : textbook of inpatient management (2nd ed.). Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins. p. 862. ISBN 9780781770323. Archived from the original on 1 August 2020. Retrieved 31 July 2020.
  18. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 535. ISBN 9783527607495. Archived from the original on 1 August 2020. Retrieved 31 July 2020.
  19. ^ US patent 3371085, Leo Henryk Sternbach & Earl Reeder, "5-ARYL-3H-1,4-BENZODIAZEPIN-2(1H)-ONES", published 1968-02-27, issued 1968-02-27, assigned to Hoffmann La Roche AG 
  20. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  21. ^ "Diazepam - Drug Usage Statistics". ClinCalc. Archived from the original on 12 April 2020. Retrieved 11 April 2020.
  22. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  23. ^ "Diazepam". International Drug Price Indicator Guide. Archived from the original on 28 March 2017. Retrieved 2 December 2015.
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