Diazepam
| Clinical data | |
|---|---|
| Pronunciation | Endrika:IPAc-en |
| Trade names | Valium, Vazepam, Valtoco, others[1] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682047 |
| [[Regulation of therapeutic goods |Endrika:Engvar data]] | |
| Pregnancy category |
|
| Dependence liability | High[2] |
| Addiction liability | Moderate[3][4] |
| Routes of administration | By mouth, IM, IV, rectal, nasal spray[5] |
| Sata ara-dalàna | |
| Sata ara-dalàna |
|
| Pharmacokinetic data | |
| Bioavailability | 76% (64–97%) by mouth, 81% (62–98%) rectal[7] |
| Metabolism | Liver—CYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to desmethyldiazepam |
| Elimination half-life | (50 hours); 20–100 hours (36–200 hours for main active metabolite desmethyldiazepam)[8][6] |
| Excretion | Kidney |
| Identifiers | |
| |
| Angon-drakitra simika sy ara-batana | |
| Raikipohy | C16H13ClN2O |
| Molar mass | 28474 g·mol−1 |
| Modely 3D (JSmol) | |
| |
| |
| | |
Diazepam, izay namidy voalohany tamin'ny anarana hoe Valium, dia fanafody avy amin'ny fianakaviana benzodiazepine izay mazàna miteraka fiantraikany mampitony.[9] Matetika izy io no ampiasaina hitsaboana aretina isan-karazany, anisan'izany ny tebiteby, ny androbe, ny aretin'ny fihemorana vokatry ny alikaola, ny aretin'ny fihemorana vokatry ny benzodiazepine, ny fihenjanana hozatra, ny olana amin'ny torimaso, ary ny aretin'ny tongotra tsy mety sasatra.[9] Mety hampiasaina hiteraka fahaverezan'ny fitadidiana mandritra ny fitsaboana sasany ihany koa izy io.[10][11] Azo raisina am-bava izy io, ampidirina ao amin'ny lava-pitombenana, tsindrona ao amin'ny hozatra, tsindrona ao amin'ny lalan-drà na ampiasaina ho toy ny famafazana orona.[11] Rehefa ampidirina amin'ny lalan-drà dia manomboka miasa ao anatin'ny iray ka hatramin'ny dimy minitra ary maharitra hatramin'ny adiny iray.[11] Rehefa avy ampiasaina amin'ny vava, dia manomboka miasa aorian'ny 15 ka hatramin'ny 60 minitra.[12]
Anisan'ny voka-dratsiny mahazatra ny fahatsapana ho rendremana sy ny olana amin'ny fandrindrana ny fihetsika.[11][8] Mahalana vao misy voka-dratsy lehibe.[9] Anisan'izany ny famonoan-tena, ny fihenan'ny fifohana rivotra, ary ny fitomboan'ny mety hisian'ny androbe raha ampiasaina matetika loatra amin'ireo voan'ny androbe.[9][11][13] Indraindray, mety hitranga ny fientanentanana na ny tebiteby.[14][15] Ny fampiasana maharitra dia mety hiteraka fandeferana, fiankinan-doha ary soritr'aretina fisintahana amin'ny fampihenana ny fatra.[9] Mety hampidi-doza ny fijanonana tampoka aorian'ny fampiasana maharitra.[9] Rehefa mijanona ny fampiasana azy dia mety haharitra enim-bolana na mihoatra ny olana ara-tsaina.[14] Tsy soso-kevitra ny hampiasana azy mandritra ny fitondrana vohoka na ny fampinonoana.[11] Ny fomba fiasany dia amin'ny fampitomboana ny fiantraikan'ny neurotransmitter <i id="mwlg">gamma</i> -aminobutyric acid (GABA).[14]
Nahazo patanty tamin'ny 1959 avy amin'i Hoffmann-La Roche ny Diazepam.[9][16] Iray amin'ireo fanafody matetika indrindra omena eran-tany izy io hatramin'ny nanombohany tamin'ny 1963.[9] Tany Etazonia, io no fanafody be mpividy indrindra teo anelanelan'ny taona 1968 sy 1982, izay nivarotra takelaka mihoatra ny roa lavitrisa tamin'ny taona 1978 fotsiny.[9] Tamin'ny taona 2017, io no fanafody faha-135 be mpampiasa indrindra any Etazonia, miaraka amin'ny fanafody mihoatra ny dimy tapitrisa.[17][18] Tamin'ny 1985 no nifarana ny patanty, ary ankehitriny dia misy marika maherin'ny 500 azo alaina eny an-tsena.[9] Ao amin'ny Lisitry ny Fanafody Tena Ilaina ao amin'ny Fikambanana Iraisam-pirenena Momba ny Fahasalamana izy io ho solon'ny lorazepam.[19] Eo amin'ny 0.01 dolara amerikana isaky ny fatra ny vidin'ny ambongadiny any amin'ny firenena an-dalam-pandrosoana as of 2015[update] [20] Any Etazonia, eo amin'ny 0.40 dolara amerikana eo ho eo isaky ny fatra izany.[11]
References
[hanova | hanova ny fango]- 1 2 "National Highway Traffic Safety Administration Drugs and Human Performance Fact Sheet- Diazepam". Archived from the original on 2017-03-27. Retrieved 2017-11-13.
- ↑ (17 April 2013) Pharmacology for the Primary Care Provider, 4th, Mosby.
- ↑ (2010) Clinical Addiction Psychiatry. Cambridge University Press.
- ↑ (2009) Principles of addiction medicine., 4, Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins.
- ↑ "Valtoco- diazepam spray". DailyMed. 13 January 2020. Archived from the original on 1 August 2020. Retrieved 13 February 2020.
- 1 2 "Diazepam Tablets BP 10mg - Summary of Product Characteristics (SmPC)". (emc). 16 September 2019. Archived from the original on 25 July 2020. Retrieved 25 July 2020.
- ↑ "Bioavailability of diazepam after intravenous, oral and rectal administration in adult epileptic patients". British Journal of Clinical Pharmacology 13 (3): 427–32. March 1982. doi:10.1111/j.1365-2125.1982.tb01397.x. PMC 1402110. PMID 7059446. https://archive.org/details/sim_british-journal-of-clinical-pharmacology_1982-03_13_3/page/427.
- 1 2 "Valium- diazepam tablet". DailyMed. 8 November 2019. Archived from the original on 28 June 2019. Retrieved 30 December 2019.
- 1 2 3 4 5 6 7 8 9 10 "Classics in chemical neuroscience: diazepam (valium)". ACS Chemical Neuroscience 5 (4): 253–60. April 2014. doi:10.1021/cn5000056. PMC 3990949. PMID 24552479. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=3990949.
- ↑ "Diazepam". PubChem. National Institute of Health: National Library of Medicine. 2006. Archived from the original on 2015-06-30. Retrieved 2006-03-11.
- 1 2 3 4 5 6 7 "Diazepam". The American Society of Health-System Pharmacists. Archived from the original on 2015-06-30. Retrieved 2015-06-05.
- ↑ (2019) “Diazepam”, StatPearls. StatPearls Publishing.
- ↑ "Prescribed Benzodiazepines and Suicide Risk: A Review of the Literature". The Primary Care Companion for CNS Disorders 19 (2). March 2017. doi:10.4088/PCC.16r02037. PMID 28257172.
- 1 2 3 "Benzodiazepines in epilepsy: pharmacology and pharmacokinetics". Acta Neurologica Scandinavica 118 (2): 69–86. August 2008. doi:10.1111/j.1600-0404.2008.01004.x. PMID 18384456.
- ↑ Perkin, Ronald M. (2008). Pediatric hospital medicine : textbook of inpatient management, 2nd, Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins.
- ↑ Fischer, Jnos (2006). Analogue-based Drug Discovery. John Wiley & Sons.
- ↑ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
- ↑ "Diazepam - Drug Usage Statistics". ClinCalc. Archived from the original on 12 April 2020. Retrieved 11 April 2020.
- ↑ (2019) World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ↑ "Diazepam". International Drug Price Indicator Guide. Archived from the original on 28 March 2017. Retrieved 2 December 2015.
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