Midazolam

Midazolam
Clinical data
Pronunciation/mɪˈdæzəlæm/
Trade namesVersed, others
AHFS/Drugs.comMonograph
MedlinePlusa609003
License data
Pregnancy
category
  • AU: C
Addiction
liability		Moderate[1] - with higher abuse potential[2][3]
Routes of
administration		By mouth, intramuscular, intravenous, buccal, intranasal
Drug classBenzodiazepine
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class B1 (Psychoactive drugs)[4]
  • CA: Schedule IV[5][6]
  • DE: Prescription only (Anlage III for higher doses)
  • NZ: Class C
  • UK: POM (Prescription only)[7][8]
  • US: Schedule IV[9][10]
  • EU: Rx-only[11]
Pharmacokinetic data
BioavailabilityBy mouth (variable, around 40%)[12][13]
intramuscular 90%+
Protein binding97%
MetabolismLiver: CYP3A3, CYP3A4, CYP3A5
Onset of actionWithin 5 min (IV), 15 min (IM), 20 min (oral)[14]
Elimination half-life1.5–2.5 hours[15]
Duration of action1 to 6 hrs[14]
ExcretionKidney
Identifiers
IUPAC name
  • 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a] [1,4]benzodiazepine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.056.140
Chemical and physical data
FormulaC18H13ClFN3
Molar mass325.77 g·mol−1
3D model (JSmol)
SMILES
  • ClC1=CC=C2C(C(C3=CC=CC=C3F)=NCC4=CN=C(C)N42)=C1
  • InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3 Y
  • Key:DDLIGBOFAVUZHB-UHFFFAOYSA-N Y
  (verify)

Midazolam, sold under the brand name Versed among others, is a benzodiazepine medication used for anesthesia, premedication before surgical anesthesia, and procedural sedation, and to treat severe agitation.[14] It induces sleepiness, decreases anxiety, and causes anterograde amnesia.[14]

The drug does not cause an individual to become unconscious, merely to be sedated.[14] It is also useful for the treatment of prolonged (lasting over five minutes) seizures.[16] Midazolam can be given by mouth, intravenously, by injection into a muscle, by spraying into the nose, or through the cheek.[14][16] When given intravenously, it typically begins working within five minutes; when injected into a muscle, it can take fifteen minutes to begin working;[14] when taken orally, it can take 10–20 minutes to begin working.[17]

Side effects can include a decrease in efforts to breathe, low blood pressure, and sleepiness.[14] Tolerance to its effects and withdrawal syndrome may occur following long-term use.[18] Paradoxical effects, such as increased activity, can occur especially in children and older people.[18] There is evidence of risk when used during pregnancy but no evidence of harm with a single dose during breastfeeding.[19][20]

Midazolam was patented in 1974 and came into medical use in 1982.[21] It is on the World Health Organization's List of Essential Medicines.[22] Midazolam is available as a generic medication.[19] In many countries, it is a controlled substance.[14]

  1. ^ Brazos Valley Rehab (24 February 2023). "What Is Midazolam Addiction?". Promises Behavioral Health. College Station, Texas: © Promises Brazos Valley. Retrieved 14 August 2025.
  2. ^ Ries RK (2009). "2" (Hardcover). In Fiellin DA, Miller SC, Saitz R (eds.). Principles of Addiction Medicine (Fourth ed.). Philadelphia, PA: Lippincott Williams & Wilkins. pp. 105–106. ISBN 9780781774772. Retrieved 14 August 2025.
  3. ^ Kerr T, Kiatying-Angsulee N, Fairbairn N, Hayashi K, Suwannawong P, Kaplan K, et al. (March 2010). "High rates of midazolam injection among drug users in Bangkok, Thailand". Harm Reduction Journal. 7 (1). BioMed Central: 7. doi:10.1186/1477-7517-7-7. PMC 2855558. PMID 20338062.{{cite journal}}: CS1 maint: overridden setting (link)
  4. ^ 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 16 August 2023.
  5. ^ "Product information". Health Canada. 28 June 2004. Retrieved 14 April 2024.
  6. ^ "Health product highlights 2021: Annexes of products approved in 2021". Health Canada. 3 August 2022. Archived from the original on 25 March 2024. Retrieved 25 March 2024.
  7. ^ "Buccolam 10 mg oromucosal solution - Summary of Product Characteristics (SmPC)". (emc). 7 June 2022. Archived from the original on 4 July 2024. Retrieved 16 June 2022.
  8. ^ "Hypnovel 10mg in 2ml - Summary of Product Characteristics (SmPC)". (emc). 16 February 2022. Archived from the original on 4 July 2024. Retrieved 16 June 2022.
  9. ^ "Seizalam- midazolam hydrochloride injection, solution". DailyMed. Archived from the original on 12 May 2021. Retrieved 1 January 2021.
  10. ^ "Nayzilam- midazolam spray". DailyMed. 19 January 2023. Archived from the original on 10 December 2023. Retrieved 4 July 2024.
  11. ^ "Buccolam EPAR". European Medicines Agency. 5 September 2011. Archived from the original on 25 February 2024. Retrieved 4 July 2024.
  12. ^ Heizmann P, Eckert M, Ziegler WH (2012). "Pharmacokinetics and bioavailability of midazolam in man". British Journal of Clinical Pharmacology. 16 (Suppl 1): 43S – 49S. doi:10.1111/j.1365-2125.1983.tb02270.x. PMC 1428091. PMID 6138080.
  13. ^ Johnson TN, Rostami-Hodjegan A, Goddard JM, Tanner MS, Tucker GT (September 2002). "Contribution of midazolam and its 1-hydroxy metabolite to preoperative sedation in children: a pharmacokinetic-pharmacodynamic analysis". British Journal of Anaesthesia. 89 (3): 428–437. doi:10.1093/bja/aef213. PMID 12402721.
  14. ^ a b c d e f g h i "Midazolam Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 5 September 2015. Retrieved 1 August 2015.
  15. ^ Cite error: The named reference medsafe2012 was invoked but never defined (see the help page).
  16. ^ a b Brigo F, Nardone R, Tezzon F, Trinka E (August 2015). "Nonintravenous midazolam versus intravenous or rectal diazepam for the treatment of early status epilepticus: A systematic review with meta-analysis". Epilepsy & Behavior. 49: 325–336. doi:10.1016/j.yebeh.2015.02.030. PMID 25817929. S2CID 33207030.
  17. ^ "Midazolam, Midazolam Hydrochloride Monograph for Professionals". Drugs.com. Retrieved 3 September 2024.
  18. ^ a b 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.
  19. ^ a b Hamilton R (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 21. ISBN 9781284057560.
  20. ^ "Midazolam use while Breastfeeding". Archived from the original on 5 September 2015. Retrieved 29 August 2015.
  21. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 539. ISBN 9783527607495. Archived from the original on 30 November 2021. Retrieved 24 August 2020.
  22. ^ 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.
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