Diazoxide
 | |
|---|---|
| Systematic (IUPAC) name | |
| 7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide | |
| Identifiers | |
| CAS number | 364-98-7 |
| ATC code | C02DA01 V03AH01 |
| PubChem | CID 3019 |
| IUPHAR ligand | 2409 |
| DrugBank | APRD00914 |
| ChemSpider | 2911 |
| UNII | O5CB12L4FN |
| KEGG | D00294 |
| ChEMBL | CHEMBL181 |
| Chemical data | |
| Formula | C8H7ClN2O2S |
| Mol. mass | 230.672 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Protein binding | 90% |
| Metabolism | Hepatic oxidation and sulfate conjugation |
| Half-life | 21-45 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | C(AU) C(US) |
| Legal status | POM (UK) ℞-only (US) |
| Routes | Oral, intravenous |
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Diazoxide 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
It is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.
It is also used to decrease hypoglycemia due to the secretion of insulin in disease states such as insulinoma (a tumor producing insulin) or congenital hyperinsulinism.
Chemistry
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: 2067. doi:10.1126/science.133.3470.2067.
References
Retrieved from : http://en.wikipedia.org/wiki/Diazoxide
