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Diazepam

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Diazepam
Clinical data
Pronunciation/daɪˈæzɪpæm/ dy-AZ-ip-am
Trade namesValium, Vazepam, Valtoco, others[6]
AHFS/Drugs.comMonograph
MedlinePlusa682047
License data
Pregnancy
category
Dependence
liability		High[1]
Addiction
liability		Moderate[2][3]
Routes of
administration		oral, intramuscular, intravenous, rectal, nasal,[5] buccal film
Drug classBenzodiazepine
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability76% (64–97%) oral, 81% (62–98%) rectal[11]
MetabolismLiver – CYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to temazepam
Metabolites
Elimination half-life(50 h); 20–100 h (32–200 h for main active metabolite desmethyldiazepam)[9][7][8]
ExcretionKidney
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.006.476 Edit this at Wikidata
 ☒NcheckY (what is this?)  (verify)

Diazepam (brand names: Valium, Dialar, Diazemuls, Diazepam Desitin, Diazepam RecTubes, Stesolid and Tensium) is a benzodiazepine. It acts to reduce anxiety (as an anxiolytic medication).[13]

It is made mostly to treat anxiety,[14] certain forms of epilepsy,[14] muscle spasms (seizures[14]), fits,[14] and sleeping problems[verification needed]. It can also be taken to help people relax before an operation or other medical or dental treatments. This is known as a pre-med.[14] Compared to similar medications, its half-life is on the longer end.

It works by increasing the levels of a calming chemical in the brain called GABA (gamma-aminobutyric acid). Like with other benzodiazepines, there is a risk of addiction if it is used for long periods of time. For this reason the drug used for 2-4 weeks maximum to avoid dependence.[14]

Diazepam was patented in 1959 by Hoffmann-La Roche.[15][16][17] It has been one of the most prescribed medications in the world since 1963[15] many times. In 1985, the patent ended. There are now 500 or more brands available on the market.[15] It is on the World Health Organization's List of Essential Medicines.[18]

Prescribing

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It has been the most prescribed medicine in the United States many times. It was the best-selling medication between 1968 and 1982 in America.[15] There, it sold more than 2 billion tablets in 1978 alone.[15] In 2022, it was the 169th most popular medication in the United States, with more than 3 million prescriptions.[19][20]

Use

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It is sometimes used recreationally to cause a calming effect. Diazepam has caused huge problems in Scotland in the past.[21]

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References

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  1. ↑ Edmunds M, Mayhew M (2013). Pharmacology for the Primary Care Provider (4th ed.). Mosby. p. 545. ISBN 978-0-323-08790-2. Archived from the original on 14 January 2023. Retrieved 13 July 2020.
  2. ↑ Clinical Addiction Psychiatry. Cambridge University Press. 2010. p. 156. ISBN 978-1-139-49169-3. Archived from the original on 8 September 2017.
  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. ↑ 4.0 4.1 "Valium". NPS MedicineWise. 31 January 2020. Archived from the original on 29 July 2020. Retrieved 9 January 2023.
  5. ↑ "Valtoco – diazepam spray". DailyMed. 13 January 2020. Archived from the original on 1 August 2020. Retrieved 13 February 2020.
  6. ↑ "National Highway Traffic Safety Administration Drugs and Human Performance Fact Sheet- Diazepam". Archived from the original on 27 March 2017. Retrieved 13 November 2017.
  7. ↑ 7.0 7.1 "Diazepam Tablets BP 10 mg – Summary of Product Characteristics (SmPC)". (emc). 16 September 2019. Archived from the original on 25 July 2020. Retrieved 25 July 2020.
  8. ↑ 8.0 8.1 "Diazepam Injection BP Summary of Product Characteristics (SmPC)". emc. 17 January 2022. Archived from the original on 25 January 2023. Retrieved 11 February 2024.
  9. ↑ 9.0 9.1 "Valium – diazepam tablet". DailyMed. 8 November 2019. Archived from the original on 28 June 2019. Retrieved 30 December 2019.
  10. ↑ "Libervant- diazepam film". DailyMed. 27 April 2024. Retrieved 18 May 2024.
  11. ↑ 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.
  12. ↑ Goodkin HP (2010). "Diazepam". In Panayiotopoulos CP (ed.). Atlas of Epilepsies. London: Springer. pp. 1727–1731. doi:10.1007/978-1-84882-128-6_263. ISBN 978-1-84882-128-6.
  13. ↑ Calcaterra, Nicholas E.; Barrow, James C. (2014-04-16). "Classics in Chemical Neuroscience: Diazepam (Valium)". ACS Chemical Neuroscience. 5 (4): 253–260. doi:10.1021/cn5000056. PMC 3990949. PMID 24552479.
  14. ↑ 14.0 14.1 14.2 14.3 14.4 14.5 "Diazepam: medicine for anxiety, muscle spasms and seizures". nhs.uk. 2022-02-07. Retrieved 2024-05-31.
  15. ↑ 15.0 15.1 15.2 15.3 15.4 Calcaterra, Nicholas E.; Barrow, James C. (2014-04-16). "Classics in Chemical Neuroscience: Diazepam (Valium)". ACS Chemical Neuroscience. 5 (4): 253–260. doi:10.1021/cn5000056. PMC 3990949. PMID 24552479.
  16. ↑ Ganellin, C. Robin; Fischer, János, eds. (2006). Analogue-based drug discovery. Weinheim: Wiley-VCH. ISBN 978-3-527-60749-5.
  17. ↑ US3371085A, Reeder, Earl & Sternbach, Leo Henryk, "5-aryl-3h-1,4-benzodiazepin-2(1h)-ones", issued 1968-02-27 
  18. ↑ Organization, World Health (2023). "The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023)". {{cite journal}}: Cite journal requires |journal= (help)
  19. ↑ "The Top 300 of 2022". clincalc.com. Retrieved 2025-04-05.
  20. ↑ "Diazepam - Drug Usage Statistics, ClinCalc DrugStats Database". clincalc.com. Retrieved 2025-04-05.
  21. ↑ "Street valium blamed for 'unprecedented' spike in drugs deaths". BBC News. 2019-01-28. Retrieved 2024-06-01.


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