Angiotensin II receptor antagonists: The prototype losartan

Annals of Pharmacotherapy

Volumn 30, Issue 6, 1996, Pages 625-635

  Schaefer, Karen L ^a   Porter, Julie A ^a  

^a KAISER PERMANENTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4 AMINO 3 METHYLBENZYL) 5 DIPHENYLACETYL 4,5,6,7 TETRAHYDROIMIDAZO[4,5 C]PYRIDINE 6 CARBOXYLIC ACID; 2 BUTYL 1 (4 CARBOXYBENZYL) 4 CHLORO 5 IMIDAZOLEACETIC ACID; 2 BUTYL 1 [4 (2 CARBOXYBENZAMIDO)BENZYL] 4 CHLORO 5 IMIDAZOLEACETIC ACID METHYL ESTER; 2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; 4' (2 BUTYL 4 CHLORO 5 HYDROXYMETHYL 1H IMIDAZOL 1 YLMETHYL) 2 BIPHENYLCARBOXYLIC ACID; ALDOSTERONE; AMINO ACID; ANGIOTENSIN; ANGIOTENSIN RECEPTOR; ANGIOTENSIN RECEPTOR ANTAGONIST; ANGIOTENSINOGEN; ATENOLOL; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; BRADYKININ; CAPTOPRIL; CYTOCHROME P450; DIPEPTIDYL CARBOXYPEPTIDASE; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; DIPHENHYDRAMINE; ENALAPRIL; HYDROCHLOROTHIAZIDE; HYDROCHLOROTHIAZIDE PLUS LOSARTAN; LOSARTAN; LOSARTAN POTASSIUM; NORADRENALIN; RENIN; RENIN INHIBITOR; SARALASIN; THIAZIDE DIURETIC AGENT; UNINDEXED DRUG; VASOPRESSIN;

ANGIONEUROTIC EDEMA; ARTICLE; ASTHENIA; CLINICAL TRIAL; CONGESTIVE HEART FAILURE; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; COUGHING; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG EFFICACY; GLOMERULUS FILTRATION RATE; HEADACHE; HEART LEFT VENTRICLE HYPERTROPHY; HUMAN; HYPERTENSION; INTRAVENOUS DRUG ADMINISTRATION; MULTICENTER STUDY; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RENIN ANGIOTENSIN ALDOSTERONE SYSTEM; VERTIGO;

ANGIOTENSIN II; ANIMALS; ANTIHYPERTENSIVE AGENTS; BIPHENYL COMPOUNDS; CLINICAL TRIALS; HUMANS; IMIDAZOLES; LOSARTAN; RECEPTORS, ANGIOTENSIN; RENIN-ANGIOTENSIN SYSTEM; TETRAZOLES;

EID: 0029954329     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1177/106002809603000611     Document Type: Article

References (81)

1. National Institutes of Health. The Fifth Report of the Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure. NIH publication No. 93-1088. Bethesda, MD: National Institutes of Health, January 1993.
2. National High Blood Pressure Education Program Working Group. National High Blood Pressure Education Program Working Group report on primary prevention of hypertension. Arch Intern Med 1993;153:186-208.
3. Kaplan NM. Clinical hypertension. 6th ed. Baltimore: Williams and Wilkins, 1994:1-9.
4. Gross TP, Wise RP, Knapp DE. Antihypertensive drug use: trends in the United States from 1973 to 1985. Hypertension 1989;13(suppl I):1113-8.
5. Manolio TA, Cutler JA, Furberg CD, Psaty BM, Whelton PK, Applegate WB. Trends in pharmacologic management of hypertension in the United States. Arch Intern Med 1995;155:829-37.
6. Ferrario CM. Importance of the renin-angiotensin-aldosterone system (RAS) in the physiology and pathology of hypertension. Drugs 1990;39 (suppl 2):1-8.
7. Vallotton MB. The renin-angiotensin system. Trends Pharmacol Sci 1987;8:69-74.
8. Eberhardt RT, Kevak RM, Rang PM, Frishman WH. Angiotensin II receptor blockade: an innovative approach to cardiovascular pharmacotherapy. J Clin Pharmacol 1993;33:1023-38.
9. Kurtz A, Scholz H, Della-Bruna R. Molecular mechanism of renin release. J Cardiovasc Pharmacol 1990; 16(suppl 4):51-7.
10. Cody RJ. The clinical potential of renin inhibitors and angiolensin antagonists. Drugs 1994;47:586-98.
11. Timmermans PBMWM, Benfield P, Chiu AT, Herblin WF, Wong PC, Smith RD. Angiotensin II receptors and functional correlates. Am J Hypertens 1992;5(suppl):221-35S.
12. Kang PM, Landau AJ, Eberhardt RT, Frishman WH. Angiotensin II receptor antagonists: a new approach to blockade of the renin-angiotensin system. Am Heart J 1994;127:1388-401.
13. Dzau VJ. Circulating versus local renin-angiotensin system in cardiovascular homeostasis. Circulation 1988;77(suppl I):14-13.
14. Dzau VJ. Local expression and pathophysiological role of renin-angiotensin in the blood vessels and heart. Basic Res Cardiol 1993;88(suppl 1):1-14.
15. Dzau VJ. Tissue renin-angiotensin system in myocardial hypertrophy and failure. Arch Intern Med 1993;153:937-42.
16. Dzau VJ, Pratt R, Gibbons GH. Angiotensin as local modulating factor in ventricular dysfunction and failure due to coronary artery disease. Drugs 1994;47(suppl 4):1-13.
17. Frishman WH, Fozailoff A, Lin C, Dike C. Renin inhibition: a new approach to cardiovascular therapy. J Clin Pharmacol 1994;34:873-80.
18. Clozel JP, Fischli W. Discovery of remikiren as the first orally active renin inhibitor. Drug Res 1993;43:260-2.
19. Burris JF. The expanding role of angiotensin converting enzyme inhibitors in the management of hypertension. J Clin Pharmacol 1995;35: 337-42.
20. Schror K. Prostaglandin-mediated actions of the renin-angiotensin system. Drug Res 1993;43:236-40.
21. Skidgel RA. Bradykinin-degrading enzymes: structure, function, distribution, and potential roles in cardiovascular pharmacology. J Cardiovasc Pharmacol 1992;20(suppl 10):S4-9.
22. Ravid D, Lishner M, Lang R, Ravid M. Angiotensin-converting enzyme inhibitors and cough: a prospective evaluation in hypertension and in congestive heart failure. J Clin Pharmacol 1994;34:1116-20.
23. Israili AH, Hall WD. Cough and angioneurotic edema associated with angiotensin-converting enzyme inhibitor therapy: a review of the literature and pathophysiology. Ann Intern Med 1992;117:234-42.
24. Just PM. The positive association of cough with angiotensin-converting enzyme inhibitors. Pharmacolherapy 1989;9:82-7.
25. Bonner G. Effect of bradykinin on arteries and veins in systemic and pulmonary circulation. J Cardiovasc Pharmacol 1992;20(suppl 10):S21-7.
26. Hedner T. Angio-oedema in relation to treatment with angiotensin-converting enzyme inhibitors. BMJ 1992;304:941-6.
27. Slater EE, Merrill DD, Guess HA, Roylance PJ, Cooper WD, Inman WH, et al. Clinical profile of angioedema associated with angiotensin-converting enzyme inhibition. JAMA 1988;260:967-70.
28. Aldigier JC, Huang H, Dalmay F, Lartigue M, Baussant T, Chassain AP, et al. Angiolensin-converting enzyme inhibition does not suppress plasma angiotensin II increases during exercise in humans. J Cardiovasc Pharmacol 1993;21:289-95.
29. Pals DT, Masucci FE, Sipos F, Denning GS Jr. A specific competitive antagonist of vascular actions of angiotensin II. Circ Res 1971;29:664-72.
30. Timmermans PBMWM, Wong PC, Chiu AT, Herblin WF. Nonpeptide angiotensin II receptor antagonists. Trends Pharmacol Sci 1991;12:55-62.
31. Wexler RR, Carini DJ, Duncia JV, Johnson AL, Wells GJ, Chiu AT, et al. Rationale for the chemical development of angiotensin II receptor antagonists. Am J Hypertens 1992;5(suppl):209-20S.
32. Chang RS, Siegl PK, Clineschmidt BV, Mantlo NB, Chakravarty PK, Greenlee WJ, et al. In vitro pharmacology of L-158,809, a new highly potent and selective angiotensin II receptor antagonist. J Pharmacol Exp Ther 1992;262:133-8.
33. De B, Winn M, Zydowsky TM, Kerkman DJ, DeBernardis JF, Lee J, et al. Discovery of a novel class of orally active, non-peptide angiotensin II antagonists. J Med Chem 1992;35:3714-7.
34. 1 receptor antagonist irbesartan in hypertension. Hypertension 1995;25:22-9.
35. Edwards RM, Aiyar N, Ohlstein EH, Weidley EF, Griffin E, Ezekiel M, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther 1992;260: 175-81.
36. Mizuno K, Niimura S, Tani M, Saito I, Sanada H, Takahashi M, et al. Hypotensive activity of TCV-116, a newly developed angiotensin II receptor antagonist, in spontaneously hypertensive rats. Life Sci 1992;51: 183-7.
37. 1 receptor antagonist. Br J Pharmacol 1992;107:1173-80.
38. Zhang J, Entzeroth M, Wienen W, van Meel JC. Characterization of BIBS 39 and BIBS 222: two new nonpeptide angiotensin II receptor antagonists. Eur J Pharmacol 1992;218:35-41.
39. Olins GM, Corpus VM, McMahon EG, Palomo MA, Schuh JF, Blehm DJ, et al. In vitro pharmacology of a nonpeptide angiotensin II receptor antagonist, SC-51316. J Pharmacol Exp Ther 1992;42:1077-82.
40. Siegl PKS. Discovery of Iosartan, the first specific non-peptide angiotensin II receptor antagonist. J Hypertens 1993;11(suppl 3):S19-22.
41. Chiu AT, McCall DE, Price WA Jr, Wong PC, Carini DJ, Duncia JV, et al. Nonpeptide angiotensin II receptor antagonists. VII. Cellular and biochemical pharmacology of DuP 753, an orally active antihypertensive agent. J Pharmacol Exp Ther 1990;252:711-8.
42. Rhaleb NE, Rouissi N, Nantel F, D'Orleans-Juste P, Regoli D. DuP 753 is a specific antagonist for the angiotensin receptor. Hypertension 1991; 17:4804.
43. Package insert. Cozaar (losartan potassium). West Point, PA: Merck and Co., Inc., April 1995.
44. Munafo A, Christen Y, Nussberger J, Shum LY, Borland RM, Lee RJ, et al. Drug concentration response relationships in normal volunteers after oral administration of losartan, an angiotensin n receptor antagonist. Clin Pharmacol Ther 1992;51:513-21.
45. Christen Y, Waeber B, Nussberger J, Porchet M, Borland RM, Lee RJ, et al. Oral administration of DuP 753, a specific angiotensin II receptor antagonist, to normal male volunteers: inhibition of pressor response to exogenous angiotensin I and II. Circulation 1991;83:1333-42.
46. Goldberg MR, Tanaka W, Barchowsky A, Bradstreet TE, McCrea J, Lo MW, et al. Effects of losartan on blood pressure, plasma activity, and angiotensin II in volunteers. Hypertension 1993;21:704-13.
47. Burnier M, Brunner HR. Angiotensin II receptor antagonists and the kidney. Curr Opin Nephrol Hypertens 1994;3:537-45.
48. Goldberg MR, Bradstreet TE, McWilliams EJ, Tanaka WK, Lipert S, Bjornsson TD, et al. Biochemical effects of losartan, a nonpeplide angiotensin II receptor antagonist, on the renin-angiotensin-aldosterone system in hypertensive patients. Hypertension 1995;25:37-46.
49. FDC reports. The pink sheet. April 17, 1995:22.
50. FDC reports. The pink sheet. May 8, 1995:4-5.
51. Ohtawa M, Takayama F, Saitoh K, Yoshinaga T, Nakashima M. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br J Clin Pharmacol 1993;35:290-7.
52. Bui JD, Kimura B, Phillips MI. Losartan potassium, a nonpeptide antagonist of angiotensin II, chronically administered p.o. does not readily cross the blood-brain barrier. Eur J Pharmacol 1992;219:147-51.
53. Weber MA. Clinical experience with the angiotensin II receptor antagonist losartan. A preliminary report. Am J Hypertens 1992;5(suppl):247-51S.
54. Weber MA, Byny RL, Prall JH, Faison EP, Snavely DB, Goldberg AI, et al. Blood pressure effects of the angiotensin II receptor blocker, losartan. Arch Intern Med 1995;155:405-11.
55. Tsunoda K, Abe K, Hagino T, Omata K, Misawa S, Imai Y, et al. Hypotensive effect of losartan, a nonpeptide angiotensin II receptor antagonist, in essential hypertension. Am J Hypertens 1993;6:28-32.
56. Nelson E, Arcuri K, Ikeda L, Snavely D, Sweet C. Efficacy and safety of losartan in patients with essential hypertension (abstract). Am J Hypertens 1992;5:19A.
57. Keller SE, Makris L, Nelson EB, Sweet CS. Antihypertensive efficacy and tolerability of losartan compared to atenolol in patients with mild to moderate essential hypertension (abstract). Am J Hypertens 1994;7:D2.
58. Soffer BA, Wright JT, Pratt JH, Wiens B, Dai CX, Turpin J, et al. Anti-hypertensive effect of the combination therapy with losartan and hydrochlorothiazide in mild to severely hypertensive patients who are not adequately controlled on HCTZ alone (abstract). Am J Hypertens 1994;7 (4):42A.
59. Simpson RL, Morlin C, Toh C, Snavely DB, Nelson EB, Goldberg AI. Efficacy and safety of losartan combined with hydrochlorothiazide in patients with mild to severe hypertension (abstract). Am J Hypertens 1994; 7(4):37A.
60. Millet D, Desgranges C, Camoan M, Gadeau AP, Costerousse O. Effects of angiotensins on cellular hypertrophy and c-fos expression in cultured arterial smooth muscle cells. Eur J Biochem 1991;206:367-72.
61. Simpson PC. Proto-oncogenes and cardiac hypertrophy. Ann Rev Physiol 1988;51:189-202.
62. Mizuno K, Tani M, Hashimoto S, Niimura S, Sanada H, Watanabe H, et al. Effects of losartan, a nonpeptide angiotensin II receptor antagonist, on cardiac hypertrophy and the tissue angiotensin D content in spontaneously hypertensive rats. Life Sci 1992;51:364-74.
63. Bovee KC, Wong PC, Timmerman PBMWM, Thoolen MJMC. Effects of nonpeptide angiotensin II receptor antagonists DuP 753 on blood pressure and renal functions in spontaneously hypertensive PH dogs. Am J Hypertens 1991;4(suppl):327-33S.
64. Camargo MJF, von Lutterotti N, Campbell WG, Pecker MS, James GD, Timmermans PBMWM, et al. Control of blood pressure and end-organ damage in maturing salt-loaded stroke-prone spontaneously hypertensive rats by oral angiotensin II receptor blockade. J Hypertens 1993;11:31-40.
65. Gansevoort RT, de Zeeuw D, Shahinfar S, Redfield A, de Jong PE. Effects of the angiotensin II antagonist losartan in hypertensive patients with renal disease. J Hypertens 1994;12(suppl 2):S37-42.
66. Cohn JN, Levine TB, Francis GS, Goldsmith S. Neurohormonal control mechanisms in congestive heart failure. Am Heart J 1981;102:509-14.
67. Gomez HJ, Cirillo VJ, Davies RO, Bolognese JA, Walker JF. Enalapril in congestive heart failure: acute and chronic invasive hemodynamic evaluation. Int J Cardiol 1986;11:37-48.
68. The CONSENSUS Trial Study Group. Effects of enalapril on mortality in severe congestive heart failure: results of the Cooperative North Scandinavian Enalapril Survival Study (CONSENSUS). N Engl J Med 1987; 316:1429-35.
69. The SOLVD Investigators. Effect of enalapril on survival in patients with reduced left ventricular ejection fractions and congestive heart failure. N Engl J Med 1991;325:293-302.
70. Qing G, Garcia R. Chronic captopril and losartan (DuP 753) administration in rats with high-output heart failure. Am J Physiol 1992;263:H833-40.
71. Raya TE, Fonken SJ, Lee RW, Daugherty S, Goldman S, Wong PC, et al. Hemodynamic effects of direct angiotensin II blockade compared to converting enzyme inhibition in rat model of heart failure. Am J Hypertens 1991;4(suppl):344-50S.
72. Crazier I, Ikram H, Awan N, Cleland J, Stephen N, Dickstein K, et al. Losartan in heart failure. Hemodynamic effects and tolerability. Circulation 1995;91:691-7.
73. 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;75:793-5.
74. Faison EP, Snavely DB, Thiyagarajan B, Nelson EB. The incidence of cough with the angiotensin II receptor antagonist, losartan, is significantly less than with angiotensin-converting enzyme inhibitors and is similar to that of placebo (abstract). Am J Hypertens 1994;7:A8.
75. Acker CG, Greenberg A. Angioedema induced by the angiotensin II blocker losartan (letter). N Engl J Med 1995;333:1572.
76. Nakashima M, Uematsu T, Kosuge K, Kanamaru M. Pilot study of the uricosuric effect of DuP-753, a new angiotensin II receptor antagonist, in healthy subjects. Eur J Clin Pharmacol 1992;42:333-5.
77. Grossman E, Peleg E, Carroll J, Shamiss A, Rosenthal T. Hemodynamic and humoral effects of the angiotensin II antagonist losartan in essential hypertension. Am J Hypertens 1994;7:1041-4.
78. Kong AT, Tomasko L, Waldman SA, Osborne B, Deutsch PJ, Goldberg MR, et al. Losartan does not affect the pharmacokinetics and pharmaco-dynamics of warfarin. J Clin Pharmacol 1995;35:1008-15.
79. Christ DD. Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite EXP3174. J Clin Pharmacol 1995;35:515-20.
80. Lo MW, Shahinfar S, Furtek CI, Ritter M, Shaw WC, Gehr T, et al. Pharmacokinetics of losartan (MK-954 or DuP 753) in patients with renal insufficiency (abstract). Clin Pharmacol Ther 1993;53:160.
81. Shaw W, Keane W, Sica D, Halstenson C, Gehr T, Marshall C. Safety and antihypertensive effects of losartan (MK-954; DuP 753), a new angiotensin II receptor antagonist, in patients with hypertension and renal disease (abstract). Clin Pharmacol Ther 1993;53:140.