Diazoxide
From Wikipedia, the free encyclopedia
|
Diazoxide
|
|
| Systematic (IUPAC) name | |
| 7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide | |
| Identifiers | |
| CAS number | |
| ATC code | C02 V03AH01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C8H7ClN2O2S |
| Mol. mass | 230.672 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 90% |
| Metabolism | Hepatic oxidation and sulfate conjugation |
| Half life | 21-45 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral, intravenous |
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.
It is used as a vasodilator in the treatment of acute hypertension, and also to decrease the secretion of insulin in disease states such as insulinoma (a tumor producing insulin).
| Antihypertensives (C02) and diuretics (C03) | |
|---|---|
| Antiadrenergic agents (including alpha) | Clonidine, Doxazosin, Guanethidine, Guanfacine, Lofexidine,Mecamylamine, Methyldopa, Moxonidine, Prazosin, Rescinnamine, Reserpine |
| Vasodilators | Diazoxide, Hydralazine, Minoxidil, Nitroprusside, Phentolamine |
| Other antihypertensives | Bosentan, Ketanserin |
| Low ceiling diuretics | Bendroflumethiazide, Chlorothiazide, Chlortalidone, Hydrochlorothiazide, Indapamide, Quinethazone, Mersalyl, Metolazone, Theobromine, Cicletanine |
| High ceiling diuretics | Bumetanide, Furosemide, Torasemide |
| Potassium-sparing diuretics | Amiloride, Eplerenone, Spironolactone, Triamterene |