Diazepam

Diazepam
Clinical data
Pronunciation/daɪˈæzɪpæm/ dy-AZ-ip-am
Trade namesValium, Vazepam, Valtoco, others
AHFS/Drugs.comMonograph
MedlinePlusa682047
License data
Pregnancy
category
  • AU: C
Dependence
liability		High
Addiction
liability		Moderate
Routes of
administration		oral, intramuscular, intravenous, rectal, nasal, buccal film
Drug classBenzodiazepine
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability76% (64–97%) oral, 81% (62–98%) rectal
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)
ExcretionKidney
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.006.476 Edit this at Wikidata
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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).

It is made mostly to treat anxiety, certain forms of epilepsy, muscle spasms (seizures), fits, 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. 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.

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

Prescribing

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. There, it sold more than 2 billion tablets in 1978 alone. In 2022, it was the 169th most popular medication in the United States, with more than 3 million prescriptions.

Use

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

References

  1. ↑ "National Highway Traffic Safety Administration Drugs and Human Performance Fact Sheet- Diazepam". Archived from the original on 27 March 2017. Retrieved 13 November 2017.
  2. 1 2 "Valium". NPS MedicineWise. 31 January 2020. Archived from the original on 29 July 2020. Retrieved 9 January 2023.
  3. ↑ 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.
  4. ↑ Clinical Addiction Psychiatry. Cambridge University Press. 2010. p. 156. ISBN 978-1-139-49169-3. Archived from the original on 8 September 2017.
  5. ↑ 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.
  6. ↑ "Valtoco – diazepam spray". DailyMed. 13 January 2020. Archived from the original on 1 August 2020. Retrieved 13 February 2020.
  7. 1 2 "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. 1 2 "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. 1 2 "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. 1 2 3 4 5 6 "Diazepam: medicine for anxiety, muscle spasms and seizures". nhs.uk. 2022-02-07. Retrieved 2024-05-31.
  15. 1 2 3 4 5 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)". Archived from the original on 2025-05-05. Retrieved 2025-04-05. {{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.