96
Views
23
CrossRef citations to date
0
Altmetric
Drug Evaluation

Losartan: a selective angiotensin II type 1 (AT1) receptor antagonist for the treatment of heart failure

, &
Pages 1897-1914 | Published online: 23 Feb 2005

Bibliography

  • THE CONSENSUS TRIAL STUDY GROUP: Effects of enala- pril on mortality in severe congestive heart failure. New Engl. J. Med. (1987) 316:1429–1435.
  • •Initial study demonstrating benefit of ACE inhibitors in im-proving survival in patients with symptomatic heart failure.
  • THE SOLVD INVESTIGATORS: Effect of enalapril on sur- vival in patients with reduced left ventricular ejection fraction and congestive heart failure. New Engl. J. Med. (1991) 325:293–302.
  • •Seminal study demonstrating benefit of ACE inhibitors in im-proving survival in patients with heart failure.
  • COHN JN: The management of chronic heart failure. New Engl. J. Med (1996) 335:490–498.
  • •An overview of current standard of care for heart failure.
  • GUIDELINES: The treatment of heart failure. Task Force of the Working Group on Heart Failure of the Euro-pean Society of Cardiology. Eur. Heart 1 (1997) 18:736–753.
  • •Current European guidelines for treatment of heart failure.
  • WILLIAMS JF, BRISTOW MR, FOWLER MB et al.: Guide- lines for the evaluation and management of heart fail-ure. Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Evaluation and Management of Heart Failure). Circulation (1995) 92:2764–2784.
  • •Current American (ACC/AHA) guidelines for treatment of heart failure.
  • BART BA, GATTIS WA, DIEM SJ, O'CONNOR CM: Reasonsfor underuse of angiotensin-converting enzyme in-hibitors in patients with heart failure and left ventricu-lar dysfunction. Am. J. Cardiol. (1997) 79 (8) :118–1120.
  • WEBER KT: Extracellular matrix remodeling in heartfailure: a role for de novo angiotensin II generation Circulation (1997) 96:4065–4082.
  • GARG R, YUSUF S, FOR THE COLLABORATIVE GROUP:Overview of randomized trials of angiotensin convert-ing enzyme inhibitors on mortality and morbidity in patients with heart failure. JAMA (1995) 273:1450–1456.
  • •Excellent overview of ACE-inhibitor heart failure morbid-ity/mortality trials.
  • CREAGER MA, FAXON DP, WEINER DA, RYAN TJ: Haemo-dynamic and neurohumoral response to exercise in patients with congestive heart failure treated with cap-topril. Br. Heart J. (1985) 53:431–435.
  • CLELAND JG, DARGIE HJ, BALL SG et al.: Effects of enala-pril in heart failure: a double-blind study of effects on exercise performance, renal function, hormones, and metabolic state. Br. Heart J. (1985) 54:305–312.
  • DREXLER H, BANHARDT U, MEINERTZ T et al.: Contrast-ing peripheral short-term and long-term effects of converting enzyme inhibition in patients with conges-tive heart failure. A double-blind, placebo-controlled trial. Circulation (1989) 79:491–502.
  • COHN JN, JOHNSON G, ZIESCHE S et al: A comparison ofenalapril with hydralazine-isosorbide dinitrate in the treatment of congestive heart failure. New Engl. J. Med. (1991) 325:303–310.
  • PFEFFER MA, BRAUNWALD E, MOYE LA et al.: Effect ofcaptopril on mortality and morbidity in patients with left ventricular dysfunction after myocardial infarc-tion. Results of the survival and ventricular enlarge-ment trial. The SAVE investigators. New Engl. J. Med. (1992) 327:669–677.
  • •Seminal study of ACE inhibitor therapy improving survival post myocardial infarction.
  • BIOLLAZ J, BRUNNER HR, GAVRAS I etal.: Antihyperten-sive therapy with MK-421: angiotensin II-renin rela-tionships to evaluate efficiency of converting enzyme blockade. J. Cardiovasc. Pharmacol (1982) 4(6):966–972.
  • URATA H HEALY B, STEWART RW et al.: Angiotensin II-forming pathways in normal and failing human hearts. Circ. Res. (1990) 66(4):883–890.
  • •Authors provide evidence of ACE-independent formation of angiotensin II as the predominant pathway in the failing myocardium.
  • SKIDGEL, ERDOS EG: The broad substrate specificity ofhuman angiotensin I converting enzyme. Clin. Exp. Hy-pertens. (1987) A9:243–259.
  • FOGARI R, ZOPPI A, TETTAMANTI F et al.: Effects of nife-dipine and indomethacin on cough induced by angiotensin-converting inhibitors: a double-blind, randomized, cross-over study. J. Cardiovasc. Pharmacol (1992) 19:670–673.
  • DZAU VJ, MUKOYAMA M, PRATT RE: Molecular biology and heterogeneity of angiotensin II receptors. J. Hyper-tens. (1994) 12:S1–S5.
  • ••Excellent overview of biology of angiotensin II receptors.
  • HAYWOOD GA, GULLESTAD L, KATSUYA T et al.: AT1and AT2 angiotensin receptor gene expression in hu-man heart failure. Circulation (1997) 95 (5):1201–1206.
  • ASANO K, DUTCHET R, PORTER JD et al.: Selective downregulation of the angiotensin II AT-receptor subtype in failing human ventricular myocardium. Circulation (1997) 95 (5): 1193–1200.
  • WONG PC, CHIU AT, PRICE WA et al: Nonpeptide angio-tensin II receptor antagonists. I. Pharmacological characterization of 2-n-butyl-4-chloro-1-(2-chlorobenzyfiimidazole-5-acetic acid, sodium salt (5–8307). Pharmacol. Exp. Ther. (1988) 247:1–7.
  • WEXLER RR, GREENLEE WJ, IRVIN JD et al.: Nonpeptide angiotensin II receptor antagonists: the next genera-tion in antihypertensive therapy. J. Med. Chem. (1996) 39:625–656.
  • BOVY PR, OLINS GM: Recent advances in nonpeptidicangiotensin II receptor antagonists. In: Current Drugs: Renin Angiotensin System. Current Patents, Ltd. (1992) B17–34.
  • BUHLMAYER P: Angiotensin II antagonists: patent ac-tivity since the discovery of DuP 753. Curr. Opin. Ther. Pat. (1992) 2(0:1693–1718.
  • CARINI DJ, DUNCIA JV, ALDRICH PE, et al.: Nonpeptideangiotensin II receptor antagonists: the discovery of a series of N-(biphenylmethyl)imidazoles as potent, orally-active antihypertensives. J. Med. Chem. (1991) 34:2525–2547.
  • •Description of the discovery of the non-peptide angiotensin II receptor antagonists.
  • TIMMERMANS PBMWM, WONG PC, CHIU AT et al: Angio- tensin II receptors and angiotensin II receptor antago-nists. Pharmacol Rev. (1993) 45(2):205–251.
  • ••The most extensive overview of the subject matter.
  • WHITEBREAD S, MELE M, KAMBER B, DEGASPARO M: Preliminary biochemical characterization of two angiotensin II receptor subtypes. Biochem. Biophys. Res. Commun. (1989) 163:284–291.
  • CHIU AT, HERBLIN WF, ARDECKY RJ et al: Identification of angiotensin II receptor subtypes. Biochem. Biophys. Res. Commun. (1989) 165(0:196–203.
  • BUMPUS FM, CATT KJ, CHIU AT et al: Nomenclature for angiotensin receptors. A report of the nomenclature Committee of the Council for High Blood Pressure Re-search. Hypertension (1991) 17(5):720–721.
  • WONG PC, TAM SW, HERBLIN WF, TIMMERMANS PBMWM: Further studies on the selectivity of DuP 753, a nonpeptide angiotensin II receptor antagonist. Eur. J. Pharmacol. (1991) 196:201–203.
  • LI P, FERRARIO CM, BROSNIHAN KB: Nonpeptide an-giontensin II antagonist losartan inhibits thrombox-ane A2-induced contractions in canine coronary arteries. J. Pharmacol. Exp. Ther. (1997) 281:1065–1070.
  • CHRÉTIEN L, GUILLEMETTE G, REGOLI D: Non-peptide and angiotensin receptor antagonists bind to tachyki-nin NK3 receptors of rat and guinea-pig brain. Eur. J. Pharmacol. (1994) 256(0:73–78.
  • WONG PC, HART SD, ZASPEL A et al.: Functional studies of nonpeptide angiotensin II receptor subtype-specific ligands: DUP 753 (All-1) and PD123177 J. Pharmacol. Exp. Ther. (1990) 255(2):584–592.
  • WIENEN W, MAUZ ABM, VAN MEEL JCA, ENTZEROTH M: Different types of receptor interaction of peptide and nonpeptide angiotensin II antagonists revealed by re-ceptor binding and functional studies. Mol Pharmacol (1992) 41(6):1081–1088.
  • CRISCIONE L, THOMANN H, WHITEBREAD S etal.: Bind-ing characteristics and vascular effects of various angiotensin II antagonists. J. Cardiovasc. Pharmacol (1990) 16\(Suppl. 4):S56–59.
  • RHALEB NE, ROUISSI N, NANTEL F, D'ORLEANS-JUSTE P, REGOLI D: DuP 753 is a specific antagonist for the angiotensin receptor. Hypertension (1991) 17:480–484.
  • SMITH RD, CHIU AT, WONG PC, HERBLIN WF, TIMMER-MANS PBMWM: Pharmacology of nonpeptide angio-tensin II receptor antagonists. Ann. Rev. Pharmacol Toxicol. (1992) 32:135–165.
  • •Review of the pharmacology of the nonpeptide angiotensin II receptor antagonists.
  • MACFAYDEN RJ, TREE M, LEVER AF, REID JL: Effects of the angiotensin II receptor antagonist losartan (DuP 753/MK 954) on arterial blood pressure, heart rate, plasma concentration of angiotensin II and renin and the pressor response to infused angiotensin II in the salt deplete dog. Clin. Sci. (1992) 83:549–556.
  • CHAN DP, SANDOK EK, AARHUS LL, HEUBLEIN DM, BUR-NETT JC, Jr. Renal specific actions of angiotensin II re-ceptor antagonism in the anesthetized dog. Am. J. Hypertens. (1992) 5:354–360.
  • EL AMRANI AIK, MENARD J, GONZALES MF, MICHEL JB: Effects of blocking the angiotensin II receptor, converting enzyme, and renin activity on the renal he-modynamics of normotensive guinea pigs. J. Cardio-vasc. Pharmacol (1993) 22(2):231–239.
  • DEGRAAF GL, PALS DT, COUCH SJ, LAWSON JA: Hormo-nal and cardiovascular effects of losartan (DuP 753), an angiotensin receptor antagonist, in nonhuman pri-mates. J. Pharmacol. Exp. Ther. (1993) 264(0:6–10.
  • SMID SD, HIME NJ, FREWIN DB, HEAD RJ: Losartan re-verses the angiotensin II mediated facilitation of sym-pathetic nerve transmission in the perfused rat mesenteric preparation. Clin. Exp. Pharmacol. Physic)]. (1992) 21 (Suppl.):65. Abstract
  • BALLA T, BAUKA AJ, ENG S, CATT KJ: Angiotensin II re-ceptor subtypes and biological responses in the adre-nal cortex and medulla. Mol. Pharmacol. (1991) 40:401–406.
  • TOFOVIC SP, PONG AS, JACKSON EK: Effects of angio-tensin subtype 1 and subtype 2 receptor antagonists in normotensive versus hypertensive rats. Hypertension (1991) 18(6):774–782.
  • MIZUNO K, NIIMURA S, TANI M, HAGA H, GOMIBUCHI Tet al.: Antihypertensive and hormonal activity of MK 954 in spontaneously hypertensive rats. Eur. J. Phar-macol (1992) 215:305–308.
  • SONG K, ZHUO J, MENDELSOHN FA: Access of peripher-ally administered DuP 753 to rat brain angiotensin II receptors. Br. J. Pharmacol (1991) 104:771–772.
  • BLAIR-WEST JR, BURNS P, DENTON DA et al Thirst in- duced by increasing brain sodium concentration is mediated by brain angiotensin. Brain Res (1994) 637(1–2)335–338.
  • VELTMAR A, CULMAN J, QADRI F, RASCHER W, UNGER T:Involvement of adrenergic and angiotensinergic re-ceptors in the paraventricular nucleus in the angio-tensin II induced vasopressin release. J. Pharmacol Exp. Ther. (1992) 263(3):1253–1260.
  • TONEY GM, PORTER JP: Functional roles of brain AT1and AT2 receptors in the central angiotensin II pressor response in conscious young spontaneously hyper-tensive rats. Dev. Brain Res. (1993) 71:193–199.
  • HOGARTY DC, SPEAKMAN EA, PUIG V, PHILLIPS MI: Therole of angiotensin, ATi and AT2 receptors in the pres-sor, drinking and vasopressin responses to central angiotensin. Brain Res. (1992) 586(2)289–294.
  • WONG PC, PRICE WA, CHIU AT et al.: Nonpeptide angio-tensin II receptor antagonists: studies with EXP9270 and DuP 753. Hypertension (1990) 15:823–834.
  • GOLDBERG Al, DUNLAY MC, SWEET CS: Safety and toler-ability of losartan potassium, an angiotensin II recep-tor antagonist, compared with hydrochlorothiazide, atenolol, felodipine ER, and angiotensin-converting enzyme inhibitors for the treatment of systemic hy-pertension. Am. J. Cardiol. (1995) 75(12):793–795.
  • INAGAMI T, GUO DF, KITAMI Y: Molecular biology ofangiotensin II receptors: an overview. J. Hypertens. (1994) 12(S10):583–94.
  • •Excellent overview of the molecular biology of the angio-tensin II receptors.
  • RUMP LC, SCHWERTFEGER E, SCHAIBLE U, FRAEDRICH G, SCHOLLMEYER P: 132 Adrenergic receptor and angio-tensin II receptor modulation of sympathetic neuro-transmission in human atria. Circ. Res. (1994) 74 (3) :434–440.
  • RUMP LC: Angiotensin (A) II receptor blockade and neurotransmission in human kidney cortex. J. Hyper-tens. (1994) 12\(Suppl. 3):868. Abstract
  • NIEDERBERGER M, NUSSBERGER J, BRUNNER HR, WAE-BER B: Effects of ACE inhibition angiotensin II receptor blockade and Na-nitroprusside on sympathetic nerve activity of renal hypertensive rats. Circulation (1990) 82 (4):III-684. Abstract
  • WONG PC, BERNARD R, TIMMERMANS PBMWM: Effect ofblocking angiotensin II receptor subtype on rat sym-pathetic nerve function. Hypertension (1992) 19(6, Pt. 2):663–667.
  • HILGERS KF, VEELKEN R, GANTEN D et al Vascular angiotensin formation and the sympathetic nervous system in Ren-2 transgenic hypertensive and control rats. Hypertension (1993) 22(3):424.Abstract
  • SCHWIELER JH, KAHAN T, NUSSBERGER J, HJEMDAHL P: Converting enzyme inhibition modulates sympathetic neurotransmission in vivo via multiple mechanisms. Am. J. Physic)]. (1993) 264(27):E631–637.
  • WONG PC: Angiotensin antagonist in models of hyper-tension. In: Angiotensin Receptors. Saavedra JM, Timmer-mans PBMWM (Eds.), Plenum Press, New York (1994):319–336.
  • WONG PC, PRICE WA, CHIU AT et al: Nonpeptide angio-tensin II receptor antagonists. IX. Antihypertensive activity in rats of DuP 753, an orally active antihyper-tensive agent. J. Pharmacol. Exp. Ther. (1990) 252(2)726–732.
  • TABRIZCHI R, LUPICHUK SM: The effects of losartan andcaptopril on vasopressor actions of cirazoline in the absence and presence of SZL-49 and nifedipine. J. Car-diovasc. Pharmacol. (1995) 26(0:137–144.
  • BUNKENBURG B, SCHNELL C, BAUM HP, CUMIN F, WOOD JM: Prolonged angiotensin II antagonism in spontaneously hypertensive rats - hemodynamic and biochemical consequences. Hypertension (1991) 18(3)278–288.
  • SOLTIS EE, JEWELL AL, DWOSKIN LP, CASSIS LA: Acuteand chronic effects of losartan (DuP 753) on blood pressure and vascular reactivity in normotensive rats. Clin. Exp. Hypertension (1993) 15 (1) :171–184.
  • WONG PC, HART SD, DUNCIA JV, TIMMERMANS PBMWM:Nonpeptide angiotensin II receptor antagonists. XIII. Studies with DuP 753 and 003174 in dogs. Eur. J. Phar-macol (1991) 202:323–330.
  • DOIG JK, MACFADYEN RJ, SWEET CS, REID JL: Hemody-namic and renal responses to oral losartan potassium during salt depletion in normal human volunteers. J. Cardiovasc. Pharmacol (1995) 25(4):511–517.
  • DOSTAL DE, BAKER KM: Angiotensin II stimulation of left ventricular hypertrophy in adult rat heart. Media-tion by the AT1 receptor. Am. J. Hypertens. (1992) 5:276–280.
  • LING Q, GUO ZG, SU Z, GUO X: Regression of cardiac hypertrophy and myosin isoenzyme patterns by losar-tan and captopril in renovascular hypertensive rats. Acta Pharmacol. Sin. (1994) 15(3):206–210.
  • WILM C, LUES I, SCHELLING P: Regression of vascular hypertrophy in renal hypertensive rats treated with the angiotensin II antagonist losartan. J. Hypertens. (1994) 12 (Suppl. 3):590.
  • SCHUDECK R, JALIL JE, VIO C et al.: Regression of renal fibrosis and damage in experimental renovacular hy-pertension using an angiotensin type 1 receptor an-tagonist. J. Am. Coll. Cardiol. (1994) Special Issue :332A. Abstract
  • EVERETT AD, TUFRO-MCREDDIE A, FISHER A, GOMEZRA: Angiotensin receptor regulates cardiac hypertro-phy and transforming growth factor th expression. Hypertension (1994) 23(5):587–592.
  • BRUCKSCHLEGEL G, HOLMER SR, JANDELEIT K et al: Therole of cardiac angiotensin conversion enzyme in ex-perimentally induced myocardial hypertrophy in the rat. Nier. Hochdruckkrank (1994) 23 (4) 144–146.
  • BRUCKSCHLEGEL G, HOLMER SR, JANDELEIT K et al.: Blockade of the renin-angiotensin system in cardiac pressure-overload hypertrophy in rats. Hypertension (1995) 25(2):250–259.
  • WONG PC, PRICE WA, CHIU AT et al: In vivo pharmacol-ogy of DuP 753. Am. J. Hypertens. (1991) 4(4):288–298S.
  • TIMMERMANS PBMWM, WONG PC, CHIU AT, SMITH RD: The preclinical basis of the therapeutic evaluation of losartan. j Hypertens. (1995) 13 (Suppl. 1):S1–13.
  • MORTON JJ: Inhibiting the effects of angiotensin II on cardiovascular hypertrophy in experimental hyper-tension. In: Angiotensin Receptors. Saavedra JM, Timmer-mans PBMWM (Eds.), Plenum Press, New York (1994):221–234.
  • SOLTIS EE: Alterations in vascular structure and func-tion after short term losartan treatment in spontane-ously hypertensive rats. J. Pharmacol. Exp. Ther. (1993) 266(2)642–646.
  • CAMARGO MJ, VONLUTTEROTTI N, PECKER MS et al.:DuP 753 increases survival in spontaneously hyper-tensive stroke-prone rats fed a high sodium diet. Am. J. Hypertens. (1991) 4(2):341–345S.
  • VONLUTTEROTTI N, CAMARGO MJ, MUELLER FB, TIM-MERMANS PBMWM, LARAGH JH: Angiotensin II recep-tor antagonist markedly reduces morbidity in salt-loaded Dahl S rats. Am. J. Hypertens. (1991) 4(4 Pt. 2):346-349S.
  • BEINLICH CJ, MORGAN HE: Control of growth in neona-tal pig hearts. Mol Cell. Biochem. (1993) 119(1-2):3–9.
  • TIMMERMANS PBMWM, SMITH RD: Angiotensin II recep-tor subtypes: selective antagonists and functional cor-relates. Eur. Heart1 (1994) 15(Suppl. D):79–87.
  • LAFAYETTE RA, MAYER G, PARK SK, MEYER TW: Angio-tensin II receptor blockade limits glomerular injury in rats with reduced renal mass. J. Clin. Invest. (1992) 90 (3) :766–771.
  • CAMARGO MJF, VONLUTTEROTTI N, CAMPBELL WG etal.: 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 (0 :31–40.
  • REMUZZI A, PERICO N, AMUCHASTEGUI CS Et al.: Shortand long term effect of angiotensin II receptor block-ade in rats with experimental diabetes. J. Am. Soc. Neph-rol. (1993) 4:40–49.
  • SALADINI D, JOVER B, RIBSTEIN J: Renal compensation to uninephrectomy (UNX) and the renin angiotensin system. J. Am. Soc. Nephrol. (1992) 3(3):478. Abstract
  • JACKSON EK, INAGAMI T: Blockade of the pre- and post-junctional effects of angiotensin in vivo with a non-peptide angiotensin receptor antagonist. Life Sci. (1990) 46:945–953.
  • YAYAMA K, KAWAO M, TUJII H, ITOH N, OKAMOTO H:DuP 753 prevents the development of puromycin ami-nonucleoside induced nephrosis. Eur. J. Pharmacol (1993) 236:337–338.
  • PIMENTEL JL, WANG S, MARTNEZ-MALDONADO M: Regulation of the renal angiotensin II receptor gene in acute unilateral ureteral obstruction. Kidney Int. (1994) 45 (0:1614–1621.
  • GEKLE M, SILBERNAGL S: Mechanism of ochratoxin A-induced reduction of glomerular filtration rate in rats. J. Pharmacol. Exp. Ther. (1993) 267(0:316–321.
  • SAKEMI T, BABA N: Effects of an angiotensin II receptorantagonist on the progression of renal failure in hyperlipidemic Imai rats. Nephron (1993) 65(3):426–432.
  • HUTCHISON FN: Hormonal modulation of proteinuriain the nephrotic syndrome. Am. J. Nephrol. (1993) 13 (5):337–346.
  • MILAVETZ JJ, RAYA TE, MORKIN E, GOLDMAN S: Survivalafter large myocardial infarction in rats: comparison of ACE inhibition with captopril versus direct angio-tensin II blockade with losartan. J. Am. Coil. Cardiol. (1995) 221A. Abstract
  • •Long-term animal study of benefits of losartan vs. captopril in post myocardial infarction model.
  • MILAVETZ JJ, RAYA TE, JOHNSON CS, MORKIN E, GOLD- MAN S: Survival after myocardial infarction in rats: captopril versus losartan. J. Am. Coll. Cardiol. (1996) 27:714–719.
  • •Long-term animal study of benefits of losartan vs. captopril in post myocardial infarction model.
  • SMITH RD, TIMMERMANS PBMWM: Inhibition of the renin angiotensin system in congestive heart failure. Curr. Drugs (1992):A127–A150.
  • •Excellent review of the role of the RAAS in heart failure.
  • RUZICKA M, YUAN B, LEENEN FH: Effects of enalapril versus losartan on regression of volume overload in-duced cardiac hypertrophy in rats. Circulation (1994) 90:484–491.
  • QING G, GARC1A R: Chronic captopril and losartan (DuP 753) administration in rats with high output heart failure. Am. J. Physiol. (1992) 263(3):883–840H.
  • FITZPATRICK MA, RADEMAKER MT, CHARLES CJ et al.: Angiotensin II receptor antagonism in ovine heart fail-ure: acute hemodynamic, hormonal, and renal effects. Am. J. Physic)]. (1992) 263:H250–256.
  • BARBE F, JINBO S, GUYENNE TT, LAPLACE M et al.: The hypotensive effect of the angiotensin II antagonist 003174 depends upon the renin-angiotensin system activation in conscious dogs with heart failure. J. Am. Coll. Cardiol (1995) 371A. Abstract
  • SPINALE FG, HIRD RB, MUKHERJEE R et al.: Chronicangiotensin II receptor blockade (AT1AT-I) affects myocyte sarcolemmal function and electrophysiology in dialated cardiomyopathy. J. Am. Coll. Cardiol. (1995):235A. Abstract
  • RAYA TE, FONKEN SJ, LEE RW et al.: Hemodynamic ef-fects of direct angiotensin II blockade compared to converting enzyme inhibition in a rat model of heart failure. Am. J. Hypertens. (1991) 4(2):334–3405.
  • SMITS JF, VANKRIMPEN C, SCHOEMAKER RG, CLEUTJENS JP, DAEMEN MJ: Angiotensin II receptor blockade after myocardial infarction in rats: effects on hemodynam-ics, myocardial DNA synthesis, and interstitial colla-gen content./ Cardiovasc. Pharmacol. (1992) 20:772–778.
  • SMITS JFM, SCHOEMAKER RG, DAEMEN MJAP, DEBETS JJM: Haemodynamic consequences of interference with the renin-angiotensin system following myocar-dial infarction in rats. Br. J. Pharmacol. (1991) 102 (Suppl.):99P. Abstract
  • DECK CC, GABALLA MA, RAYA TE: Renal function in rats with experimental heart failure: angiotensin II block-ade versus converting enzyme inhibition. Circulation (1993) 88(4, Pt. 2, Suppl.):I-514. Abstract
  • STAUSS HM, ZHU YC, REDLICH T et al: Angiotensin con-verting enzyme inhibition in infarct induced heart failure in rats: bradykinin versus angiotensin II. J. Car-diovasc. Risk (1994) 1:255–262.
  • SCHIEFFER B, WIRGER A, MEYBRUNN M et al.: Compara-tive effects of chronic angiotensin converting enzyme inhibition and angiotensin II type 1 receptor blockade on cardiac remodeling after myocardial infarction in the rat. Circulation (1994) 89(5):2273–2282.
  • WONG PC, PRICE WA, CHIU AT et al.: Nonpeptide angio-tensin II receptor antagonists. XI. Pharmacology of EXP3174, an active metabolite of DuP 753 - an orally active antihypertensive agent. J. Pharmacol. Exp. Ther. (1990) 255:211–217.
  • MCMAHON TJ, KAYE AD, HOOD S et al.: Inhibitory ef-fects of DuP 753 and 003174 on responses to angio-tensin II in the pulmonary vascular bed of the cat. J. Appl. Physiol. (1992) 73 (5) :2054–2061.
  • CHRIST DD, WONG PC, WONG YN et al.: The pharma-cokinetics and pharmacodynamics of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) in the dog. J. Pharmacol. Exp. Ther. (1994) 268(3):1199–1205.
  • STEARNS RA, MILLER RR, DOSS GA et al: The metabolism of DuP 753, a nonpeptide angiotensin II receptor an-tagonist, by rat, monkey and human liver slices. Drug Metab. Dispos. (992) 20(2):281–287.
  • KRIETER PA, COLLETTI AE, MILLER RR, STEARNS RA: Ab-sorption and glucuronidation of the angiotensin II re-ceptor antagonist losartan by the rat intestine. J. Pharmacol. Exp. Ther. (1995) 273(2):816–822.
  • CHRIST DD, KILKSON T, WONG N, LAM GN: Formation and disposition of EXP3174, a pharmacologically ac-tive metabolite of the novel angiotensin II receptor an-tagonist DuP 753. Third North American ISSX Meeting (1990) 137. Abstract
  • STEARNS RA, DOSS GA, MILLER RR, CHIU SHL: Synthesis and identification of a novel tetrazole metabolite of the angiotensin II receptor antagonist DuP 753. Drug Me-tab. Dispos. (1991) 19(6):1160–1162.
  • LO M-W, GOLDBERG MR, MCCREA JB et al.: Pharmacoki-netics of losartan, an angiotensin II receptor antago-nist, and its active metabolite 003174 in humans. Pharmacol. Ther. (1995) 58:641–649.
  • •Description of the pharmacokinetics of losartan in humans.
  • LO M-W, TOH J, EMMERT SE et al.: Pharmacokinetics of intravenous and oral losartan in patients with heart failure. J. Clin. Pharmacol (1998) 38:525–532.
  • SICA DA, LO M-W, SHAW WC et al.: The pharmacokinet-ics of losartan in renal insufficiency. J. Hypertension (1995) 13 (Suppl. 1):549–S52.
  • •Effect of renal insufficiency on pharmacokinetics of losartan.
  • SPIELBERG S, MCCREA J, CRIBB A et al.: A mutation in CyP2C9 is responsible for decreased metabolism of lo-sartan. Clin. Pharmacol. Ther. (1996) 59(2):215.
  • MCCREA J, LO M-L, KONG T et al.: A rare deficiency of the conversion of losartan to its active metabolite, E3174. Clin. Pharmacol. Ther. (1995) 57(2):154.
  • CHRIST DD: Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite 003174. J. Clin. Pharmacol (1995) 35:515–520.
  • GOLDBERG M, LO M-L, DEUTSCH PJ et al.: Phenobarbital minimally alters plasma concentrations of losartan and its active metabolite E-3174. Gun. Pharmacol Ther. (1996) 59:268–74.
  • GOLDBERG MR, LO M-W, BRADSTREET TE, RITTER MA, HOGLUND P: Effects of cimetidine on pharmacokinet-ics and pharmacodynamics of losartan, a n ATi-selective non-peptide angiotensin II receptor antagonist. Eur. J. Clin. Pharmacol. (1995) 49:115–119.
  • DE SMET M, SCHOORS DF, DE MEYER G et al.: Effect of multiple doses of losartan on the pharmacokinetics of single doses of digoxin in healthy volunteers. Br. J. Pharmacol. (1995) 40:571–575.
  • LACOURCIERE Y, BRUNNER H, IRWIN R, KARLBERG BE et al. AND THE LOSARTAN COUGH STUDY GROUP: Effects of modulators of the renin-angiotensin-aldosterone system on cough. J. Hypertension (1994) 12:1387–1393.
  • GOTTLEIB S, DICKSTEIN K, FLECK E et al: Hemodynamic and neurohumoral effects of the angiotensin II antago-nist losartan in patients with congestive heart failure. Circulation (1993) 88:1602–1609.
  • ••Initial single dose haemodynamic study with losartan in pa-tients with heart failure.
  • CROZIER I, IKRAM H, AWAN N et al.: Losartan in heart failure: hemodynamic effects and tolerability. Losar-tan Hemodynamic Study Group. Circulation (1995) 91:691–97.
  • ••Multiple dose haemodynamic study with losartan in patientswith heart failure.
  • LANG RM, ELKAYAM U, YELLEN LG et al: ON BEHALF OF THE LOSARTAN PILOT EXERCISE STUDY INVESTIGA-TORS: Comparative effects of losartan and enalapril on exercise capacity and clinical status in patients with heart failure. J. Am. Coll. Cardiol. (1997) 30:983–991.
  • ••First of two pilot exercise studies of losartan in heart failure.
  • DICKSTEIN K, CHANG P, WILLENHEIMER R et al.: Com-parison of the effects of losartan and enalapril on clinical status and exercise performance in patients with moderate or severe heart failure. J. Am. Coll. Car-diol (1995) 26:438–445.
  • ••Second of two pilot exercise studies of losartan in heartfailure.
  • KON V, FOGO A, ICHIKAWA I: Bradykinin causes selec-tive efferent arteriolar dilation during angiotensin I converting enzyme inhibition. Kidney InL (1993) 44:545–50.
  • KLINGER G, JARAMILLO N, IKRAM H et al.: Effects of lo-sartan on exercise capacity, morbidity and mortality in patients with symptomatic heart failure. J. Am. Coll. Cardiol. (1997) :29:205A.
  • ••Description of Phase III losartan exercise studies.
  • NARANG R, SWEDBERG K, CLELAND JG: What is the ideal design for evaluation of treatment for heart failure? In-sights from trials assessing the effect of ACE inhibitors on exercise capacity. Eur. Heart J. (1996) :120–134.
  • •Review of ACE inhibitor exercise studies demonstrating that exercise times improved generally in only half of the studies after 1987.
  • PITT B, CHANG P, TIMMERMANS P: Angiotensin II recep-tor antagonists in heart failure: rationale and design of the Evaluation of Losartan In The Elderly (ELITE) trial. Cardiovasc. Drugs Ther. (1995) 9:693–700.
  • ••The rationale and design manuscript describing the ELITElosartan heart failure study.
  • PITT B, SEGAL R, MARTINEZ FA et al.: Randomised trial of losartan versus captopril in patients over 65 with heart failure. Lancet (1997) 349:747–52.
  • ••The results of the ELITE losartan heart failure study describ-ing the unexpected improvement in survival with losartan vs. captopril in elderly symptomatic heart failure patients.
  • WALDO AL, CANN AJ, DE RUYTER H et al. FOR THE SWORD INVESTIGATORS: Effect of d-sotalal on mortal-ity in patients with left ventricular dysfunction after recent and remote myocardial infarction. Lancet (1996) 348:7–12.
  • YUSUF S, MAGGIONI AP, HELD P, ROULEAU J-L: Effects of candesartan, enalapril or their combination on exer-cise capacity, ventricular function, clinical deteriora-tion and quality of life in heart faulure: Randomized Evaluation of Strategies of Left Ventricular Dysfunc-tion (RESOLVD). Circulation (1997) 96 (Suppl.) :1–452.
  • •Pilot study of candesartan in heart failure.
  • COHN JN, TOGNONI G, SPORMANN D, GLAZER R FOR THE VAL-HEFT GROUP: Valsartan in heart failure trial (Val-HeFT). J. Cardiac Failure (1998) 4:156. Abstract
  • •Outline of the valsartan endpoint study in heart failure.
  • COHN JN: Effects of ARB-ACEI combination therapy on morbidity and mortality in heart failure. Am. J. Hyper-tens. (1998) II:257A. Abstract
  • SPINALE FG, DE GASPARO M, WHITEBREAD S et al.: Modulation of the renin-angiotensin pathway through enzyme inhibition and specific receptor blockade in pacing induced heart failure. I. Effects on left ventricu-lar performance and neurohumoral systems. Circula-tion (1997) 96:2385–96.
  • SPINALE FG, MUKHERJEE R, IANNINI JP et al. Modulation of the renin-angiotensin pathway through enzyme in-hibition and specific receptor blockade in pacing in-duced heart failure. II. Effects on myocyte contractile process. Circulation (1997) 96:2397–406.
  • TONKON M, AWAN N, NIAZI I et al FOR THE IRBESARTAN HEART FAILURE GROUP: Irbesartan combined with conventional therapy, including angiotensin convert-ing enzyme inhibitors, in heart failure. J. Am. Coll. Car-diol (1998) 31:188A.
  • •Pilot study with irbesartan in heart failure.
  • TOCCHI M, ROSANIO S, ANZUINI A, SPOSI A, MATTIOLI D: Angiotensin II receptor blockade combined to ACE-inhibition improves left ventricular dilation and exer-cise ejection fraction in congestive heart failure. J. Am. Coll. Cardiol (1998) 31:188A.
  • HAMROFF G, BLAUFARB I, MANCINI D et al.: Clinical benefits of long-term angiotensin II receptor blockade in patients with severe symptoms of congestive heart failure despite full angiotensin converting enzyme in-hibition. J. Am. Coll. Cardiol (1998) 31:188A.
  • THOMAS G, FERRIER G, HOWLETT S: Losartan exerts anti-arrhythmic activity independent of angiotensin II receptor blockade in simulated ventricular ischemia and reperfusion. J. Pharm. Exp. Ther. (1997) 278.
  • HARADA K, KOMURO I, HAYASHI D et al: Angiotensin II type la receptor is involved in the occurrence of reper-fusion arrhythmias. Circulation (1998)97(4):315–317.
  • RUMP L, OBERHAUSER V, SCHWERTFEGER E, SCHOLL-MEYER P: Experimental evidence to support ELITE. Lancet (1998) 351:644–645.
  • ••Authors describe potential mechanism to explain the ob-served and unexpected reduction in sudden cardiac death with losartan vs. captopril in the losartan ELITE heart failure study.
  • BENEDICT CR, SHELTON B, JOHNSTONE DE et al. FOR THE SOLVD INVESTIGATORS: Prognostic significance of plasma norepinephrine in patients with asympto-matic left ventricular dysfunction. Circulation (1996) 94:690–697.
  • SCHIEFFER B, WIRGER A, MEYBRUNN M et al. Compara-tive effects of chronic angiotensin-converting enzyme inhibition and angiotensin II type 1 receptor blockade on cardiac remodeling after myocardial infarction in the rat. Circulation (1994) 89(5):2273–2282.
  • ROGG H, DE GASPARO M, GRAEDEL E et al: Angiotensin ffreceptor subtypes in human atria and evidence for alterations in patients with cardiac dysfunction. Eur. Heart J. (1996) 17:1112–1120.
  • DAHLOF B: The Losartan Intervention For Endpoint re-duction (LIFE) in hypertension study: rationale, de-sign and methods. Am. J. Hypertens. (1997) 10:705–713.
  • •Description of the losartan in hypertensive left ventricular hypertrophy LIFE endpoint study.
  • DAHLOF B, BEEVERS G, DEVEREUX RB et al. FOR THE LIFE STUDY GROUP: The Losartan Intervention for Endpoint (LIFE) Reduction in Hypertension Study - baseline characteristics of 9,194 patients with left ven-tricular hypertrophy. Hypertension (In Press.)
  • •Additional description of the losartan in hypertensive left ventricular hypertrophy LIFE endpoint study including baseline characteristic.
  • THE ACUTE INFARCTION RAMIPRIL EFFICACY (AIRE) STUDY INVESTIGATORS: Effects of ramipril on mortal-ity and morbidity of survivors of acute myocardial in-farction with clinical evidence of heart failure. Lancet (1993) 342:821–828.
  • KOBEL L, TORP-PEDERSEN C, ON BEHALF OF THE TRACE STUDY GROUP: Clinical characteristics and mortality of patients screened for entry into the trandolapril cardiac evaluation (TRACE) study. Am. J. Cardiol. (1995) 76:1–5.
  • BONARJEE VV, CARSTENSEN S, CAIDAHL K et al.: At-tenuation of left ventricular dilatation after acute myo-cardial infarction by early initiation of enalapril therapy. CONSENSUS II Multi-Echo Study Group. Am. J. Cardiol. (1993) 72 (14): 1004–1009 .
  • LIU Y-H, YANG X-P, SHAROV VG et al: Effects of angiotensin-converting enzyme inhibitors and angio-tensin II type 1 receptor antagonists in rats with heart failure. Role of kinins and angiotensin II type 2 recep-tors. J. Clin. Invest. (1997) 99 (8) :1926–1935.
  • COTTONE S, VADALA A, VELLA MC et al.: Changes of plasma endothelin and growth factor levels, and of left ventricular mass, after chronic ATi-receptor blockade in human hypertension. Am. J. Hypertens. (1998) 11:548–553.
  • •Evidence to suggest that losartan reduces left ventricular hy-pertrophy in humans.
  • CUSPIDI C, LONATI L, SAMPIERI L et al.: Effects of losar-tan on blood pressure and left ventricular mass in es-sential hypertension. High Blood Press. (1998) 7:75–79.
  • •Another study providing evidence to suggest that losartan reduces left ventricular hypertrophy in humans.
  • ROTHMAN KJ, MICHELS KB: The continuing unethical use of placebo controls. New Engl. J. Med (1994) 6:394–398.
  • GAVRAS I: Bradykinin-mediated effects of ACE inhibi-tion. Kidney Int. (1992) 42:1020–1029.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.