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	364-98-7
ATC code	C02DA01 V03AH01
PubChem	3019
DrugBank	APRD00914
Chemical data
Formula	C8H7N2ClO2S
Mol. weight	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.	C(AU) C(US)
Legal status	POM(UK) ℞-only(US)
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) edit
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
High ceiling diuretics:	Bumetanide, Furosemide, Torasemide
Potassium-sparing diuretics:	Amiloride, Eplerenone, Spironolactone, Triamterene