Comparative Efficacy and Safety of the Angiotensin Receptor Blockers (ARBs)

The appearance of angiotensin receptor blockers (ARBs) amongst the therapeutic options in the treatment of cardiovascular diseases (CVDs) was a new milestone in the history of hypertension treatment. It further widened the range of possibilities for personalized therapy, especially for patients who cannot tolerate the use of angiotensin converting enzyme inhibitors (ACEIs).
Pharmacologic Characteristics of the Angiotensin Receptor Blockers
 

ARBs

Half-life (h) 

Tmax (h)

Bio-availability

Route of elimination:
renal (R) biliary/fecal (B)

Food Interaction

Losartan*

2

1–1.5

33%

35% R; 60% B

 Yes

Candesartan cilexetil

9

2-5

42%

33% R; 67% B

 No

Eprosartan

5–9

1–3

63%

7% R; 90% B

 Yes

Irbesartan

11–15

1.3–3

60–80%

20% R; 80% B

 No

Telmisartan

24

0.5–1

43%

<1% R; >97% B

 No

Valsartan

6

2–4

23%

13% R; 83% B

 Yes

Olmesartan medoxomil

12–14

1.7–2.5

26%

35–50%R; 50–65% B

 No

Azilsartan medoxomil

12

1.5–3

60%

42% urine; 55% B

 No

*Losartan is converted to EXP-3174 with terminal half-life of 6–9 hours and Tmax of 4–6 hours.

 

Doses for Hypertension and Other Indications of the Angiotensin Receptor Blockers
  

ARBs

Starting dose (mg/day)

Maximum dose (mg/day)

Dosing interval

Other Indications Approved Outside of Hypertension

Losartan

50

 100

Once a day or twice a day

Diabetic nephropathy when serum creatinine is increased and proteinuria present in patients with hypertension and type 2 diabetes; Stroke reduction in patients with hypertension and left ventricular hypertrophy (non-black only)

Candesartan cilexetil

16

 32 

Once a day or twice a day 

Treatment of heart failure (NYHA Classes II–IV)

Eprosartan

600

 800

Once a day or twice a day

None

Irbesartan

150

 300

Once a day

Diabetic nephropathy when serum creatinine is increased and proteinuria present in patients with hypertension and type 2 diabetes

Telmisartan

40

 80

Once a day 

Cardiovascular risk reduction in patients unable to take ACE inhibitors

Valsartan

80 or 160

 320

Once a day

Treatment of heart failure (NYHA Classes II–IV); Reduction of CV mortality in clinically stable patients with left ventricular failure or dysfunction following myocardial infarction.

Olmesartan medoxomil

20

 40

Once a day

None

Azilsartan medoxomil

40 or 80

 80

Once a day

None

 

References:
  1. Abraham HM, White CM, White WB. The comparative efficacy and safety of the angiotensin receptor blockers in the management of hypertension and other cardiovascular diseases. Drug Saf. 2015 Jan;38(1):33-54. [Medline]
  2. Makani H, Bangalore S, Supariwala A, Romero J, Argulian E, Messerli FH. Antihypertensive efficacy of angiotensin receptor blockers as monotherapy as evaluated by ambulatory blood pressure monitoring: a meta-analysis. Eur Heart J. 2014 Jul;35(26):1732-42. [Medline]
  3. Dézsi CA. The Different Therapeutic Choices with ARBs. Which One to Give? When? Why? Am J Cardiovasc Drugs. 2016 Aug;16(4):255-66. [Medline]
Created Sep 28, 2017.