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.
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 [edit]
Diazoxide can be prepared from dichloronitrobenzene:[4]
Side effects [edit]
Diazoxide interferes with insulin release through its action on potassium channels.[citation needed] The efflux of potassium, as an effect of Diazoxide, will lead to hyperpolarization of cell membrane that leads to decrease calcium influx. The low calcium will decrease the release of insulin. Therefore this medicine is not given to non-insulin dependent diabetic patients.
References [edit]
- ^ Diazoxide, drugs.com
- ^ van Hamersvelt HW, Kloke HJ, de Jong DJ, Koene RA, Huysmans FT (August 1996). "Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?". J. Hypertens. 14 (8): 1041–5. PMID 8884561.
- ^ Huang Q, Bu S, Yu Y, et al. (January 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.
- ^ 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.
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