Table 1.
Comparison of the eight currently available angiotensin-receptor blockers
Generic name | Brand name | Dose (mg) | Cost (28-tab pack) | Metabolism | Half-life (h) | Primary function | Dosing | AT1/AT2 receptor selectivity | Pressor inhibition at 24 hours |
---|---|---|---|---|---|---|---|---|---|
Azilsartan | Edarbi (Takeda) | 40 80 |
£54.19 £54.19 |
Hepatic: mainly CYP2C9 (also CYP2B6 and CYP2C8); no CYP inhibition; inhibits p-glycoprotein |
11 | Hypertension | 80 mg once daily for hypertension | >10,000-fold | 32 mg 60% |
Candesartan | Atacand | 4 32 |
£9.78 £16.13 |
Ester hydrolysis within gastrointestinal wall | 9 | Hypertension, heart failure | 8–32 mg once daily over 4-(for hypertension) or 2-(for heart failure) week intervals | >10,000-fold | 8 mg 50% |
Eprosartan | Teveten | 300 600 |
£7.31 £14.31 |
Not metabolized and eliminated unchanged | 20 | Hypertension | 400–800 mg once daily, increase after 2–3 weeks | 1000-fold | 350 mg 30% |
Irbesartan | Aprovel (Bristol-Myers Squibb) (Sanofi-Aventis) | 75 300 |
£9.69 £15.93 |
Hepatic: glucuronidation and oxidation by CYP2C9 | 11–15 | Hypertension, diabetic nephropathy | 150–300 mg once daily for hypertension and renal disease in hypertensive type 2 diabetes mellitus | >8500-fold | 150 mg 40% 300 mg 60% |
Losartan | Losartan Potassium, Cozaar | 25 100 |
£1.45 £16.18 £1.47 £16.18 |
Hepatic: CYP2C9 and CYP3A4 | 2 | Hypertension, diabetic nephropathy | 25–100 mg once daily over several weeks for hypertension and diabetic nephropathy; 12.5–150 mg once daily over weekly intervals for chronic heart failure | 1000-fold | 100 mg 25%–40% |
Olmesartan | Olmetec | 20 40 |
£12.95 £17.50 |
Ester hydrolysis within gastrointestinal wall | 13 | Hypertension | 10–40 mg once daily for hypertension | >12,500-fold | 20 mg 61% 40 mg 74% |
Telmisartan | Micardis (Boehringer Ingelheim) | 40 80 |
£8.00 £17.00 |
Minimally conjugated, no CYP450 activation | 24 | Hypertension | 40–80 mg once daily after 4 weeks for hypertension; 80 mg once daily to prevent cardiovascular events | >3000-fold | 80 mg 40% |
Valsartan | Diovan (Novartis) | 40 160 |
£13.97 £18.41 |
Minimal metabolism (CYP2C9) and eliminated largely unchanged | 6 | Hypertension, heart failure, myocardial infarction | 80–320 mg once daily over 4 weeks for hypertension; 40 mg twice daily, up to 160 mg twice daily, over 2-week intervals for heart failure; 20 mg twice daily, up to 160 mg twice daily, over 2-week intervals for myocardial infarction | 20,000-fold | 80 mg 30% |
Notes: Data drawn from Zaiken K, Cheng JW. Azilsartan medoxomil: a new angiotensin receptor blocker. Clin Ther. 2011;33(11):1577–1589.23