Hydralazine

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]

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Mechanism

Hydralazine works through a cGMP-mediated mechanism, resulting in smooth muscle relaxation.^[2]

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.^[2]

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.

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. ^ ^{a b} Bhushan, Vikas, Tao T. Lee, and Ali Ozturk. First Aid for the USMLE Step 1. New York: McGraw-Hill Medical, 2007. 251.