Hydralazine

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Hydralazine
Systematic (IUPAC) name
1-hydrazinophthalazine
Identifiers
CAS number	86-54-4
ATC code	C02DB02
PubChem	3637
Chemical data
Formula	C8H8N4
Mol. mass	160.176 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half life	2-4 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	Oral, intravenous

Hydralazine hydrochloride (1-hydrazinophthalazine monohydrochloride; Apresoline) is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles. By relaxing vascular smooth muscle, vasodilators act to decrease peripheral resistance, thereby lowering blood pressure.^[1]

Contents 1 Mechanism 2 Clinical Use 3 Side effects 4 References

[edit] Mechanism

The mechanism of action of hydralazine is not well known. It interferes with the action the second messenger inositol triphosphate, limiting calcium release from the sarcoplasmic reticulum of smooth muscle. This results in an arterial and arteriolar relaxation.^[2]

An exam revision source declares that hydralazine works through a cGMP-mediated mechanism, resulting in smooth muscle relaxation.^[3]

[edit] Clinical Use

Hydralazine is not used as a primary drug for treating hypertension because it elicits a reflex sympathetic stimulation of the heart (the baroreceptor reflex). The sympathetic stimulation may increase heart rate and cardiac output, and may cause angina pectoris or myocardial infarction.^[1] Hydralazine may also increase plasma renin concentration, resulting in fluid retention. In order to prevent these undesirable side effects, hydralazine is generally prescribed in combination with a beta-blocker (e.g., propranolol) and a diuretic.^[1]

Hydralazine is used to treat severe hypertension, but again, it is not a first line therapy for essential hypertension. However, hydralazine is the first line therapy for hypertension in pregnancy, with methyldopa.^[3]

[edit] Side effects

Common side effects include:

• Diarrhea
• Compensatory tachycardia due to baroreceptor reflex
• Headache
• Loss of appetite
• Nausea or vomiting
• Pounding heartbeat
• Drug-Induced Lupus Erythematosus

Patients given hydralazine over a peroid of six months may develop a lupus-like syndrome or other immune related diseases that generally are reversible with withdrawal.^[1] Hydralazine is differentially acetylated by fast and slow acetylator phenotypes thus incidence of lupus-like disease in slow acetylators.

[edit] References

1. ^ ^{a b c d} Harvey, Richard A., Pamela A. Harvey, and Mark J. Mycek. Lippincott's Illustrated Reviews: Pharmacology. 2nd ed. Philadelphia: Lipincott, Williams & Wilkins, 2000. 190.
2. ^ Rang, Dale, Ritter and Flower. Pharmacology. 6th Ed, 2007.
3. ^ ^{a b} Bhushan, Vikas, Tao T. Lee, and Ali Ozturk. First Aid for the USMLE Step 1. New York: McGraw-Hill Medical, 2007. 251.

v • d • e Antihypertensives (C02) and diuretics (C03) Sympatholytic agents (including alpha) centrally acting/antiadrenergics: Clonidine • Guanfacine • Methyldopa • Moxonidine • Rilmenidine • adrenergic uptake inhibitor (Rescinnamine, Reserpine) 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)