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Diazoxide


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	C₈H₇Cl N₂O₂S
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.	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.

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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).

v • d • e Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents (including alpha)	centrally acting/antiadrenergics (Clonidine, Guanfacine, Methyldopa, Moxonidine, Rescinnamine, Reserpine, Rilmenidine) • ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) • peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin)
Vasodilators	Diazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine
Other antihypertensives	serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan)
Low ceiling diuretics	Thiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine
High ceiling diuretics	Loop diuretic (Bumetanide, Furosemide, Torasemide)
Potassium-sparing diuretics	ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)