Global InformationDiazepam information
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| Pronunciation | /daɪˈæzɪpæm/ dy-AZ-ip-am |
| Trade names | Valium, Vazepam, Valtoco, others[1] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682047 |
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| Dependence liability | High[3] |
| Addiction liability | Moderate[4][5] |
| Routes of administration | oral, intramuscular, intravenous, rectal, nasal,[6] buccal film |
| Drug class | Benzodiazepine |
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| Pharmacokinetic data | |
| Bioavailability | 76% (64–97%) oral, 81% (62–98%) rectal[11] |
| Metabolism | Liver – CYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to temazepam |
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| Elimination half-life | (50 h); 20–100 h (32–200 h for main active metabolite desmethyldiazepam)[10][8][9] |
| Excretion | Kidney |
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| ECHA InfoCard | 100.006.476 |
| Chemical and physical data | |
| Formula | C16H13ClN2O |
| Molar mass | 284.74 g·mol−1 |
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Diazepam, sold under the brand name Valium among others, is a medicine of the benzodiazepine family that acts as an anxiolytic.[13] It is used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, muscle spasms, insomnia, and restless legs syndrome.[13] It may also be used to cause memory loss during certain medical procedures.[14][15] It can be taken orally (by mouth), as a suppository inserted into the rectum, intramuscularly (injected into muscle), intravenously (injection into a vein) or used as a nasal spray.[6][15] When injected intravenously, effects begin in one to five minutes and last up to an hour.[15] When taken by mouth, effects begin after 15 to 60 minutes.[16]
Common side effects include sleepiness and trouble with coordination.[10][15] Serious side effects are rare.[13] They include increased risk of suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy.[13][15][17] Occasionally, excitement or agitation may occur.[18][19] Long-term use can result in tolerance, dependence, and withdrawal symptoms on dose reduction.[13] Abrupt stopping after long-term use can be potentially dangerous.[13] After stopping, cognitive problems may persist for six months or longer.[18] It is not recommended during pregnancy or breastfeeding.[15] Its mechanism of action works by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA).[18]
Diazepam was patented in 1959 by Hoffmann-La Roche.[13][20][21] It has been one of the most frequently prescribed medications in the world since its launch in 1963.[13] In the United States it was the best-selling medication between 1968 and 1982, selling more than 2 billion tablets in 1978 alone.[13] In 2021, it was the 149th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[22][23] In 1985, the patent ended, and there are more than 500 brands available on the market.[13] It is on the World Health Organization's List of Essential Medicines.[24]
- ^ a b Cite error: The named reference
autowas invoked but never defined (see the help page). - ^ a b "Valium". NPS MedicineWise. 31 January 2020. Archived from the original on 29 July 2020. Retrieved 9 January 2023.
- ^ 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.
- ^ Clinical Addiction Psychiatry. Cambridge University Press. 2010. p. 156. ISBN 978-1-139-49169-3. Archived from the original on 8 September 2017.
- ^ 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.
- ^ a b "Valtoco – diazepam spray". DailyMed. 13 January 2020. Archived from the original on 1 August 2020. Retrieved 13 February 2020.
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
- ^ a b "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.
- ^ a b "Diazepam Injection BP Summary of Product Characteristics (SmPC)". emc. 17 January 2022. Archived from the original on 25 January 2023. Retrieved 11 February 2024.
- ^ a b c "Valium – diazepam tablet". DailyMed. 8 November 2019. Archived from the original on 28 June 2019. Retrieved 30 December 2019.
- ^ 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.
- ^ Goodkin HP (2010). "Diazepam". In Panayiotopoulos CP (ed.). Atlas of Epilepsies. London: Springer. doi:10.1007/978-1-84882-128-6_263. ISBN 978-1-84882-128-6.
- ^ 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.
- ^ Cite error: The named reference
PubChemwas invoked but never defined (see the help page). - ^ a b c d e f "Diazepam". The American Society of Health-System Pharmacists. Archived from the original on 30 June 2015. Retrieved 5 June 2015.
- ^ Dhaliwal JS, Saadabadi A (September 2022). "Diazepam". StatPearls [Internet]. StatPearls Publishing. PMID 30725707. Archived from the original on 8 March 2021. Retrieved 13 October 2019.
- ^ 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.
- ^ 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. S2CID 24453988.
- ^ Perkin RM (2008). Pediatric hospital medicine : textbook of inpatient management (2nd ed.). Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins. p. 862. ISBN 978-0-7817-7032-3.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 535. ISBN 978-3-527-60749-5. Archived from the original on 14 January 2023. Retrieved 5 June 2020.
- ^ US patent 3371085, Sternbach LH, Reeder E, "5-ARYL-3H-1,4-BENZODIAZEPIN-2(1H)-ONES", published 1968-02-27, issued 1968-02-27, assigned to Hoffmann La Roche AG
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Diazepam - Drug Usage Statistics". ClinCalc. Archived from the original on 4 January 2024. Retrieved 14 January 2024.
- ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.