Midazolam
| Clinical data | |
|---|---|
| Pronunciation | /mɪˈdæzəlæm/ |
| Trade names | Versed, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a609003 |
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| Addiction liability | High |
| Routes of administration | By mouth, intramuscular, intravenous, buccal, intranasal |
| Drug class | Benzodiazepine |
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| Pharmacokinetic data | |
| Bioavailability | By mouth (variable, around 40%)[9][10] intramuscular 90%+ |
| Protein binding | 97% |
| Metabolism | Liver: CYP3A3, CYP3A4, CYP3A5 |
| Onset of action | Within 5 min (IV), 15 min (IM), 20 min (oral)[11] |
| Elimination half-life | 1.5–2.5 hours[12] |
| Duration of action | 1 to 6 hrs[11] |
| Excretion | Kidney |
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| ECHA InfoCard | 100.056.140 |
| Chemical and physical data | |
| Formula | C18H13ClFN3 |
| Molar mass | 325.77 g·mol−1 |
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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.[11] It induces sleepiness, decreases anxiety, and causes anterograde amnesia.[11]
The drug does not cause an individual to become unconscious, merely to be sedated.[11] It is also useful for the treatment of prolonged (lasting over five minutes) seizures.[13] Midazolam can be given by mouth, intravenously, by injection into a muscle, by spraying into the nose, or through the cheek.[11][13] When given intravenously, it typically begins working within five minutes; when injected into a muscle, it can take fifteen minutes to begin working;[11] when taken orally, it can take 10–20 minutes to begin working.[14]
Side effects can include a decrease in efforts to breathe, low blood pressure, and sleepiness.[11] 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.[11]
- ^ 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.
- ^ "Product information". Health Canada. 28 June 2004. Retrieved 14 April 2024.
- ^ "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.
- ^ "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.
- ^ "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.
- ^ "Seizalam- midazolam hydrochloride injection, solution". DailyMed. Archived from the original on 12 May 2021. Retrieved 1 January 2021.
- ^ "Nayzilam- midazolam spray". DailyMed. 19 January 2023. Archived from the original on 10 December 2023. Retrieved 4 July 2024.
- ^ "Buccolam EPAR". European Medicines Agency. 5 September 2011. Archived from the original on 25 February 2024. Retrieved 4 July 2024.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ Cite error: The named reference
medsafe2012was invoked but never defined (see the help page). - ^ 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.
- ^ "Midazolam, Midazolam Hydrochloride Monograph for Professionals". Drugs.com. Retrieved 3 September 2024.
- ^ 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.
- ^ a b Hamilton R (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 21. ISBN 9781284057560.
- ^ "Midazolam use while Breastfeeding". Archived from the original on 5 September 2015. Retrieved 29 August 2015.
- ^ 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.
- ^ 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.