Angiotensin II Receptor Blockers

The Angiotensin II Receptor Blockers (ARBs) are a newer class of drugs that are used to treat hypertension (high blood pressure). They help to lower blood pressure by blocking angiotensin II, a hormone in the body that is an important component of hypertension. Angiotensin II causes blood vessels to constrict (tighten up/close partially) and by blocking the hormone, the blood vessels relax or dilate (open up), and thus ARBs help to reduce blood pressure. ARBs are generally best used for treating hypertension in patients who also have diabetes or heart failure and are intolerant to a related class of blood pressure lowering drugs, the ACE inhibitors.

Drugs in this Class
Telmisartan (Micardis)
Olmesartan Tablets (Benicar Tablets, Olmesartan Medoxomil Tablets)
Irbesartan (Avapro)
Valsartan (Diovan)
Candesartan (Atacand)
Losartan (Cozaar)
Eprosartan Tablets (Eprosartan Mesylate Tablets, Teveten Tablets)

Summarizing the Evidence

  • The Food and Drug Administration (FDA) has approved all of the drugs in this class for the treatment of hypertension. Each ARB has been well-studied and can be used alone or in combination with other blood pressure lowering drugs.

  • Comparative clinical studies between the drugs in this class have shown that the ARBs are similar in their abilities to effectively lower blood pressure. Since the ARBs are similarly effective, the choice of which ARB to use will depend on your doctor's preference and/or your prescription benefits formulary.

  • Studies have shown that when olmesartan, losartan, and valsartan were compared to each other using dose increases of each drug, all three drugs reduced blood pressure similarly. The study compared the doses of olmesartan 40 mg once daily, losartan 50 mg two times a day, and valsartan 320mg once daily which were increased from olmesartan 20 mg once daily, losartan 50 mg once daily, and valsartan 80 mg once daily.

  • One recent study compared olmesartan 20 mg daily to telmisartan 40 mg daily in patients with diabetes. Olmesartan was found to lower blood pressure more than telmisartan. However, more studies need to be done to determine if olmesartan is preferred over telmisartan.

  • The seventh report of the Joint National Committee on the Prevention, Detection, Evaluation and Treatment of High Blood Pressure (JNC 7) recommends thiazide-type diuretics as the initial drug choice in most patients with high blood pressure. JNC 7 also recommends that ARBs be considered as initial therapy in patients with heart failure, diabetes, or chronic kidney disease.

  • Some studies have shown that losartan's "dose-response relationship" is minimal compared to the other ARBs. This means that if a patient starts on losartan at the recommended initial dose (50mg daily) and blood pressure is not controlled to goal levels, increasing the dose of losartan to it's next dose level (100mg daily) will most likely not result in significantly further blood pressure lowering. This is in comparison to the other ARBs where increasing the dose generally provides further blood pressure lowering.

  • Studies have shown that when telmisartan and valsartan were used in combination with hydrochlorothiazide (HCTZ), the telmisartan plus HCTZ combination had a greater effect on reducing blood pressure compared to the combination of valsartan plus HCTZ. These studies also showed that the side effects were similar among the two groups.

  • ARBs are generally well tolerated with mild side effects such as fatigue, dizziness, diarrhea, upper respiratory tract infection, lightheadedness, and headache. No major differences in the frequency of side effects among the ARBs are apparent. None of the ARBs should be taken during pregnancy.

Dosing and Administration

  • Candesartan, eprosartan, and losartan are typically dosed once or twice daily. Irbesartan, olmesartan, telmisartan, and valsartan are typically dosed once daily.

Generic Availability

  • No drugs in this class are currently available in generic formulations. Losartan (Cozaar) is the oldest drug in this class and will most likely be the first of the ARBs to become available generically.

Drug Interactions

Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

Side Effects

To view specific side effect information, please use our Side Effect Checker.

Additional Information

References

  1. Cozaar [package insert]. Whitehouse Station, NJ: Merck & Co, Inc.; December 2005.
  2. Diovan [package insert]. East Hanover, NJ: Novartis Pharmaceutical Co; June 2007.
  3. Avapro [package insert]. New York, NY: Sanofi-Synthelabo; October 2005.
  4. Atacand [package insert]. Wilmington, DE: AstraZeneca; February 2007.
  5. Micardis [package insert]. Ridgefield, CT: Boehringer Ingelheim; November 2003.
  6. Teveten [package insert]. Morrisville, NC: Biovail Pharmaceuticals; September 2005.
  7. Benicar [package insert]. New York, NY: Sankyo Pharmaceuticals. Ocotober 2006.
  8. Hyzaar [package insert]. Whitehouse Station, NJ: Merck & Co, Inc; December 2005.
  9. Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. The seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. JAMA. 2003; 285:2560-2572.
  10. Hedner T, Oparil S, Rasmussen K, et al. A comparison of the angiotensin II antagonists valsartan and losartan in the treatment of essential hypertension. Am J Hypertens. 1999;12(4 Pt 1):414-417.
  11. Kassler-Taub K, Littlejohn T, Elliott W, et al. Comparative efficacy of two angiotensin II receptor antagonists, irbesartan and losartan in mild-moderate hypertension. Irbesartan/Losartan study investigators. Am J Hypertens. 1998;11(4 Pt 1):445-453.
  12. Oparil S, Guthrie R, Lewin AJ, et al. An elective-titration study of the comparative effectiveness of two angiotensin II-receptor blockers, irbesartan and losartan. Irbesartan/Losartan study investigators. Clin Ther. 1998;20(3):398-409.
  13. Andersson OK, Neldam S. The antihypertensive effect and tolerability of candesartan cilexetil, a new generation angiotensin II antagonists, in comparison with losartan. Blood Pressure. 1998;7(1):53-59.
  14. Gradman AH, Lewin A, Bowling BT, et al. Comparative effects of candesartan cilexetil and losartan in patients with systemic hypertension. Heart Dis. 1999;1:52-57.
  15. Lacourciere Y, Asmar R, for the Candesartan/Losartan study investigators. A comparison of the efficacy and duration of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients. A placebo-controlled, forced titration study. Am J Hypertens. 1999;12:1181-1187.
  16. Ohma KP, Milon H, Valnes K. Efficacy and tolerability of a combination tablet of candesartan cilexetil and hydrochlorothiazide in insufficiently controlled primary hypertension-comparison with a combination of losartan and hydrochlorothiazide. Blood Press. 2000;9:214-220.
  17. Manolis AJ, Grossman E, Jelakovic B, et al. Effects of losartan and candesartan monotherapy and losartan/hydrochlorothiazide combination therapy in patients with mild to moderate hypertension. Losartan Trial Investigators. Clin Ther. 2000;22:1186-1203.
  18. Mallion J, Siche J, Lacourciere Y. ABPM comparison of the antihypertensive profiles of the selective angiotensin II receptor antagonists telmisartan and losartan in patients with mild-to-moderate hypertension. J Hum Hypertens. 1999;13:657-664.
  19. Puig JG, Mateos F, Buno A, et al. Effect of eprosartan and losartan on uric acid metabolism in patients with essential hypertension. J Hypertens. 1999;17:1033-1039.
  20. Oparil S, Williams D, Chrysant SG, et al. Comparative efficacy of olmesartan, losartan, valsartan, and irbesartan in the control of essential hypertension. J Clin Hypertens 2001; 3(5):283-91.
  21. White WB, Punzi HA, Murwin D, et al. Effects of the angiotensin II receptor blockers telmisartan vs. valsartan in combination with hydrocholorothaizide 25 mg once daily for the treatment of hypertension. Journal of Clinical Hypertension. 2006 September;8(9): 626-633.
  22. Giles TD, Oparil S, Silfani TN, Wang A, and Walker JF. Comparison of increasing doses of olmesartan medoxomil, losartan potassium, and valsartan in patients with essential hypertension. Journal of Clinical Hypertension. 2007 March;9(3): 187-195.
  23. Nakayama S, Watada H, Mita T, et al. Comparison of effects of olmesartan and telmisartan on blood pressure and metabolic parametes in Japanese early-stage type-2 diabetics with hypertension. Hypertens Res 2008;31:7-13.

Last Updated: April 2008

Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.

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