Angiotensin II-Receptor Antagonists: An Overview

Indications

All currently available AT-II-receptor antagonists have received FDA-approved labeling for use in the treatment of hypertension either alone or in combination with other antihypertensive agents.

Several large trials are under way to evaluate the effects of AT-II-receptor antagonists on cardiovascular-associated morbidity and mortality in patients with hypertension and congestive heart failure. The LIFE (Losartan Intervention for Endpoint Reduction in Hypertension) study will, in hypertensive patients with documented left ventricular hypertrophy, evaluate long-term effects of losartan versus atenolol on cardiovascular morbidity and mortality. The Valsartan Heart Failure Trial (Val-HeFT), a multinational trial involving more than 4000 patients with congestive heart failure, will evaluate the addition of valsartan to current standard treatments for heart failure, including ACE inhibitors.

The ELITE (Evaluation of Losartan in the Elderly) study compared the efficacy and safety of losartan and captopril in 722 elderly patients (≥65 years old) with class II-IV heart failure and ejection fraction below 0.40. ^[89] Patients were treated with captopril 50 mg three times daily or losartan potassium 50 mg once daily for 48 weeks. There was no difference in the frequency of renal dysfunction (persistent increases in serum creatinine concentration) between the captopril and losartan groups (10.5% in each group). The rate of mortality from all causes was lower in the losartan group (4.8%) than in the captopril group (8.7%). Fewer losartan recipients than captopril recipients discontinued therapy because of adverse reactions (12.2% versus 20.8%). The results of this study have led to an additional study, ELITE II, to confirm the findings.

Cite this: Angiotensin II-Receptor Antagonists: An Overview - Medscape - Jul 01, 2000.

Table 1. Comparison of Angiotensin II-Receptor Antagonists
Drug	Active Metabolite	Bioavailability (%)	Daily Dose (mg)	Half-life (hr)	Cost ($)a
Losartan	Yes	33	25-100	2 (losartan) 6-9 (EXP-3174)	38
Valsartan	No	25	80-320	6	36
Irbesartan	No	60-80	150-300	11-15	36
Candesartan	No	42	8-32	3-4 3-11	36
Eprosartan	No	13	600-800	5-9	37
Telmisartan	No	42-58	20-80	24	39

a Estimated cost, based on average wholesale price (Drug Topics Red Book, 1999), to the pharmacist for a one-month supply at the usual starting dosage.

Table 2. Clinical Trials Comparing Angiotensin-II-Receptor Antagonists with Angiotensin-Converting-Enzyme Inhibitors a
a	Losartan dosages are expressed in terms of losartan potassium, and candesartan dosages are expressed in terms of candesartan cilexetil. BP = blood pressure, SBP = systolic blood pressure, DBP = diastolic blood pressure, NR = not reported, HCTZ = hydrochlorothiazide.
b	Primary efficacy variable was assessed after eight weeks of therapy.

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Angiotensin II-Receptor Antagonists: An Overview

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