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Midazolam

"Versed" redirects here. For the book of poetry, see Versed (poetry collection).

Midazolam
Clinical data
Pronunciation/mɪˈdæzəlæm/
Trade namesVersed, others
AHFS/Drugs.comMonograph
MedlinePlusa609003
License data
Pregnancy
category
  • AU: C
Addiction
liability		High[citation needed]
Routes of
administration		By mouth, intramuscular, intravenous, buccal, intranasal
Drug classBenzodiazepine
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityBy mouth (variable, around 40%)[10][11]
intramuscular 90%+
Protein binding97%
MetabolismLiver: CYP3A3, CYP3A4, CYP3A5
Onset of actionWithin 5 min (IV), 15 min (IM), 20 min (oral)[12]
Elimination half-life1.5–2.5 hours[13]
Duration of action1 to 6 hrs[12]
ExcretionKidney
Identifiers
  • 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 Edit this at Wikidata
Chemical and physical data
FormulaC18H13ClFN3
Molar mass325.77 g·mol−1
3D model (JSmol)
  • 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 checkY
  • Key:DDLIGBOFAVUZHB-UHFFFAOYSA-N checkY
  (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.[12] It induces sleepiness, decreases anxiety, and causes anterograde amnesia.[12]

The drug does not cause an individual to become unconscious, merely to be sedated.[12] It is also useful for the treatment of prolonged (lasting over five minutes) seizures.[14] Midazolam can be given by mouth, intravenously, by injection into a muscle, by spraying into the nose, or through the cheek.[12][14] When given intravenously, it typically begins working within five minutes; when injected into a muscle, it can take fifteen minutes to begin working.[12]

Side effects can include a decrease in efforts to breathe, low blood pressure, and sleepiness.[12] Tolerance to its effects and withdrawal syndrome may occur following long-term use.[15] Paradoxical effects, such as increased activity, can occur especially in children and older people.[15] There is evidence of risk when used during pregnancy but no evidence of harm with a single dose during breastfeeding.[16][17]

Midazolam was patented in 1974 and came into medical use in 1982.[18] It is on the World Health Organization's List of Essential Medicines.[19] Midazolam is available as a generic medication.[16] In many countries, it is a controlled substance.[12]

  1. ^ "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.
  2. ^ 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.
  3. ^ "Product information". Health Canada. 28 June 2004. Retrieved 14 April 2024.
  4. ^ "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.
  5. ^ "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.
  6. ^ "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.
  7. ^ "Seizalam- midazolam hydrochloride injection, solution". DailyMed. Archived from the original on 12 May 2021. Retrieved 1 January 2021.
  8. ^ "Nayzilam- midazolam spray". DailyMed. 19 January 2023. Archived from the original on 10 December 2023. Retrieved 4 July 2024.
  9. ^ "Buccolam EPAR". European Medicines Agency. 5 September 2011. Archived from the original on 25 February 2024. Retrieved 4 July 2024.
  10. ^ 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.
  11. ^ 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.
  12. ^ 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.
  13. ^ Cite error: The named reference medsafe2012 was invoked but never defined (see the help page).
  14. ^ 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.
  15. ^ 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.
  16. ^ a b Hamilton R (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 21. ISBN 9781284057560.
  17. ^ "Midazolam use while Breastfeeding". Archived from the original on 5 September 2015. Retrieved 29 August 2015.
  18. ^ 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.
  19. ^ 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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