Diazoxide
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| Clinical data | |
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| Trade names | Proglycem |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Oral, intravenous |
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| Pharmacokinetic data | |
| Protein binding | 90% |
| Metabolism | Hepatic oxidation and sulfate conjugation |
| Elimination half-life | 21-45 hours |
| Excretion | Renal |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.006.063 |
| Chemical and physical data | |
| Formula | C8H7ClN2O2S |
| Molar mass | 230.672 g/mol g·mol−1 |
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Diazoxide (INN; brand name Proglycem[1]) is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.
Uses
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[2]
Diazoxide also inhibits the secretion of insulin from the pancreas, thus it is used to counter hypoglycemia in disease states such as insulinoma (a tumor producing insulin)[3] or congenital hyperinsulinism.
Chemistry
Diazoxide can be prepared from dichloronitrobenzene:[4]
References
- ^ Diazoxide, drugs.com
- ^ van Hamersvelt HW, Kloke HJ, de Jong DJ, Koene RA, Huysmans FT (1996). "Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?". J. Hypertens. 14 (8): 1041–5. PMID 8884561.
{{cite journal}}: Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ Huang Q, Bu S, Yu Y; et al. (2007). "Diazoxide prevents diabetes through inhibiting pancreatic beta-cells from apoptosis via Bcl-2/Bax rate and p38-beta mitogen-activated protein kinase". Endocrinology. 148 (1): 81–91. doi:10.1210/en.2006-0738. PMID 17053028.
{{cite journal}}: Explicit use of et al. in:|author=(help); Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ Rubin, A. A.; Roth, F. E.; Winbury, M. M.; Topliss, J. G.; Sherlock, M. H.; Sperber, N.; Black, J. (1961). "New Class of Antihypertensive Agents". Science. 133 (3470): 2067. doi:10.1126/science.133.3470.2067.