Losartan was the first of a new class of oral antihypertensive agents called angiotensin receptor blockers (ARBs).1-5 It was approved for the treatment of hypertension by the FDA in 1995.
ARBs selectively inhibit the binding of angiotensin II (ANG II) to angiotensin II type 1 (AT1) receptors.4-8 Most pathological cardiovascular actions of ANG II come from its interaction with the AT1 receptor.4-6,9
Seven additional ARBs have been approved since 199510-17:
ARB
|
Approved
|
Losartan (Cozaar)
|
1995
|
Valsartan (Diovan)
|
1996
|
Irbesartan (Avapro)
|
1997
|
Candesartan (Atacand)
|
1998
|
Telmisartan (Micardis)
|
1998
|
Eprosartan (Teveten)
|
2001
|
Olmesartan (Benicar, Olmetec)
|
2002
|
Azilsartan (Edarbi)
|
2011
|
References
- Goa KL, Wagstaff AJ. Losartan potassium: a review of its pharmacology, clinical efficacy and tolerability in the management of hypertension. Drugs 1996; 51 (5): 820-845.
- Carr AA, Prisant LM. Losartan: first of a new class of angiotensin antagonists for the management of hypertension. J Clin Pharmacol 1996; 36 (1): 3-12.
- Goldberg AI, Dunlay MC, Sweet CS. Safety and tolerability of losartan potassium, an angiotensin II receptor antagonist, compared with hydrochlorothiazide, atenolol, felodipine ER, and angiotensin-converting enzyme inhibitors for the treatment of systemic hypertension. Am J Cardiol 1995; 75 (12): 793-795.
- Goldberg MR, Bradstreet TE, McWilliams EJ, et al. Biochemical effects of losartan, a nonpeptide angiotensin II receptor antagonist, on the renin-angiotensin-aldosterone system in hypertensive patients. Hypertension 1995; 25 (1): 37-46.
- Timmermans PB, Duncia JV, Carini DJ, et al. Discovery of losartan, the first angiotensin II receptor antagonist. J Hum Hypertens 1995; 9 Suppl 5: S3-18.
- Guthrie GP, Jr. Angiotensin receptors: physiology and pharmacology. Clin Cardiol 1995; 18 (6 Suppl 3): Iii 29-34.
- Fyhrquist F, Metsarinne K, Tikkanen I. Role of angiotensin II in blood pressure regulation and in the pathophysiology of cardiovascular disorders. J Hum Hypertens 1995; 9 Suppl 5: S19-24.
- Oparil S, Williams D, Chrysant SG, Marbury TC, Neutel J. Comparative efficacy of olmesartan, losartan, valsartan, and irbesartan in the control of essential hypertension. J Clin Hypertens (Greenwich) 2001; 3 (5): 283-291, 318.
- Dell'Italia LJ. Translational success stories: angiotensin receptor 1 antagonists in heart failure. Circ Res 2011; 109 (4): 437-452.
- Benicar [package insert]. Parsippany, NJ: Daiichi Sankyo, Inc; 2009.
- Micardis [package insert]. Ridgefield, CT: Boehringer Ingelheim Pharmaceuticals, Inc.; 2014.
- Teveten [package insert]. North Chicago, IL: AbbVie Inc.; 2014.
- Cozaar [package insert]. Whitehouse Station, NJ: Merck Sharp & Dohme Corp; 2015.
- Avapro [package insert]. Bridgewater, NJ: Sanofi-Aventis U.S. LLC; 2016.
- Atacand [package insert]. Wilmington, DE: AstraZeneca Pharmaceuticals LP; 2016.
- Edarbi [package insert]. Atlanta, GA: Arbor Pharmaceuticals, LLC; 2016.
- Diovan [package insert]. East Hanover, NJ: Novartis Pharmaceuticals Corp; 2017.