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108 PART III Cardiovascular Drugs

DRUG SUMMARY TABLE: Drugs Used in Hypertension
Mechanism Clinical Toxicities,
Subclass of Action Applications Pharmacokinetics Interactions

Diuretics (see also Chapter 15)
Hydrochlorothiazide, Block Na/Cl transporter in Hypertension, mild Oral Hypokalemia,
chlorthalidone distal convoluted tubule edema Duration: 8–12 h hyperglycemia,
Furosemide Block Na/K/2Cl transporter in Hypertension, heart Oral, parenteral Hypokalemia,
thick ascending limb failure, edema, Duration: 2–3 h hypovolemia,
hypercalcemia ototoxicity

Centrally acting
Clonidine Agonist at α2 receptors • in Hypertension Oral and transdermal Sedation, danger of
CNS this results in decreased Oral duration: 2–3 days • severe rebound
SANS outflow transdermal 1 wk hypertension if suddenly
Methyldopa Prodrug converted to Hypertension Oral Sedation, induces
methylnorepinephrine in CNS, Duration: 12–24 h hemolytic antibodies
with result like clonidine

Ganglion blockers
Hexamethonium Obsolete prototype nicotinic None Oral, parenteral Severe orthostatic
acetylcholine (ACh) receptor hypotension,
blocker in ganglia • blocks all constipation, blurred
ANS transmission vision, sexual
Trimethaphan: IV, rarely used short-acting ganglion blocker for hypertensive emergencies, controlled hypotension
Mecamylamine: oral ganglion blocker, several hours’ duration, experimental use in smoking cessation

Postganglionic neuron blockers
Reserpine Blocks vesicular pump (VMAT) Obsolete in Oral Sedation • severe
in adrenergic neurons hypertension, Duration: 5 days psychiatric depression
Huntington’s disease (high doses)
Guanadrel: blocks reuptake of norepinephrine (NET) and depletes stores; oral, long duration; severe orthostatic hypotension (guanethidine, a
similar drug, was withdrawn in the United States)

Alpha blockers
Prazosin Selective α1 blocker • reduces Mild hypertension, Oral First dose orthostatic
peripheral vascular resistance • benign prostatic Duration: 6–8 h hypotension
prostatic smooth muscle tone hyperplasia
Doxazosin, terazosin: similar to prazosin but longer duration of action

Beta blockers
Propranolol Prototype nonselective β Hypertension • many Oral, parenteral Bronchospasm in
blocker • reduces cardiac other applications (see Duration: 6–8 h (extended asthmatics • excessive
output • possible secondary Chapter 10) release forms available) cardiac depression,
reduction in renin release sexual dysfunction,
sedation, sleep
Atenolol, metoprolol: like propranolol but β1-selective; fewer adverse effects
Labetalol, carvedilol: combined α and β blockade; oral and parenteral


sulfate metabolite Severe hypertension • Oral. parenteral Excessive cardiac channel blockers • combine arrhythmias Duration: 6–8 h depression • constipation moderate vascular effect with strong cardiac effect Nifedipine. lisinopril. muscle. CNS. heart Half-life: 2. sympathetic autonomic nervous system. secretory cells emergencies oral for insulinoma excessive hypotension • hypoglycemia due to insulin-secreting tumors Fenoldopam D1 agonist • causes arteriolar Hypertensive Parenteral only. greater vasodilator than cardiodepressant effects Older oral vasodilators Hydralazine Probably causes release of Hypertension (also Oral Tachycardia. Hyperglycemia • edema. causes male-pattern baldness Duration: 6–8 h and water retention • arteriolar smooth muscle hirsutism hyperpolarization and vasodilation Vasodilators. enalapril. irbesartan.2 h but large • cough failure doses provide duration of 12 h Benazepril. Oral. topical Marked tachycardia. CHAPTER 11 Drugs Used in Hypertension 109 DRUG SUMMARY TABLE: Drugs Used in Hypertension (Continued) Mechanism Clinical Toxicities. oral Calcium channel blockers Verapamil. renal angiotensin I synthesis Duration: 12 h impairment Angiotensin antagonists ACE inhibitors Captopril ACE inhibitor • reduces Hypertension. other dihydropyridines: oral and parenteral. central nervous system. ANS. diabetic Oral Hyperkalemia • teratogen angiotensin II synthesis renal disease. very short Excessive hypotension dilation emergencies duration Renin antagonist Aliskiren Renin inhibitor • reduces Hypertension Oral Angioedema. parenteral Nitroprusside Releases NO from drug Hypertensive Parenteral only Excessive hypotension • molecule emergencies • cardiac Duration: minutes • requires prolonged infusion may decompensation constant infusion cause thiocyanate and cyanide toxicity + Diazoxide K channel opener in smooth Hypertensive Parenteral for hypertension. salt + opens K channels. salt and nitric acid (NO) by endothelial used in heart failure in Duration: 6–8 h water retention. . Subclass of Action Applications Pharmacokinetics Interactions Vasodilators. cells • causes arteriolar dilation combination with lupus-like syndrome isosorbide dinitrate) Minoxidil Prodrug. angina. SANS. others: like captopril but longer half-lives Angiotensin II receptor blockers (ARBs) Losartan Blocks AT1 receptors Hypertension Oral Hyperkalemia • teratogen Duration: 6–8 h Candesartan. diltiazem Prototype L-type calcium Hypertension. angiotensin-converting enzyme. others: like losartan ACE. autonomic nervous system.