Selective and specific I_f inhibition with ivabradine: new perspectives for the treatment of cardiovascular disease

References

• Jouven X, Empana JP, Buyck JF et al. Resting heart rate and its changes over years as a risk factor for mortality in the general population: the Paris Prospective Study I. Eur. Heart J.27, 333 (2007).
   Web of Science ®Google Scholar
• Mensink GB, Hoffmeister H. The relationship between resting heart rate and all-cause, cardiovascular and cancer mortality. Eur. Heart J.18, 1404–1410 (1997).
   PubMed Web of Science ®Google Scholar
• Gillman MW, Kannel WB, Belanger A, D’Agostino RB. Influence of heart rate on mortality among persons with hypertension: the Framingham Study. Am. Heart J.125, 1148–1154 (1993).
   PubMed Web of Science ®Google Scholar
• Hjalmarson A, Gilpin EA, Kjekshus J et al. Influence of heart rate on mortality after acute myocardial infarction. Am. J. Cardiol.65, 547–553 (1990).
   PubMed Web of Science ®Google Scholar
• Fox K, Ford I, Steg PG, Tendera M, Robertson M, Ferrari R. Heart rate as a prognostic risk factor in patients with coronary artery disease and left-ventricular systolic dysfunction (BEAUTIFUL): a subgroup analysis of a randomised controlled trial. Lancet372, 817–821 (2008).
   PubMed Web of Science ®Google Scholar
• Kolloch R, Legler UF, Champion A et al. Impact of resting heart rate on outcomes in hypertensive patients with coronary artery disease: findings from the International Verapamil-SR/Trandolapril Study (INVEST). Eur. Heart J.29, 1327–1334 (2008).
   PubMed Web of Science ®Google Scholar
• Bohm M, Swedberg K, Komajda M et al. Heart rate as a risk factor in chronic heart failure (SHIFT): the association between heart rate and outcomes in a randomised placebo-controlled trial. Lancet376, 886–894 (2010).
   PubMed Web of Science ®Google Scholar
• Lechat P, Hulot JS, Escolano S et al. Heart rate and cardiac rhythm relationships with bisoprolol benefit in chronic heart failure in CIBIS II Trial. Circulation103, 1428–1433 (2001).
   PubMed Web of Science ®Google Scholar
• Cucherat M. Quantitative relationship between resting heart rate reduction and magnitude of clinical benefits in post-myocardial infarction: a meta-regression of randomized clinical trials. Eur. Heart J.28, 3012–3019 (2007).
   PubMed Web of Science ®Google Scholar
• Flannery G, Gehrig-Mills R, Billah B, Krum H. Analysis of randomized controlled trials on the effect of magnitude of heart rate reduction on clinical outcomes in patients with systolic chronic heart failure receiving β-blockers. Am. J. Cardiol.101, 865–869 (2008).
   PubMed Web of Science ®Google Scholar
• McAlister FA, Wiebe N, Ezekowitz JA, Leung AA, Armstrong PW. Meta-analysis: β-blocker dose, heart rate reduction, and death in patients with heart failure. Ann. Intern. Med.150, 784–794 (2009).
   PubMed Web of Science ®Google Scholar
• Guth BD, Heusch G, Seitelberger R, Ross J Jr. Elimination of exercise-induced regional myocardial dysfunction by a bradycardiac agent in dogs with chronic coronary stenosis. Circulation75, 661–669 (1987).
   Web of Science ®Google Scholar
• Heusch G. Heart rate in the pathophysiology of coronary blood flow and myocardial ischaemia: benefit from selective bradycardic agents. Br. J. Pharmacol.153, 1589–1601 (2008).
   PubMed Web of Science ®Google Scholar
• Schulz R, Rose J, Skyschally A, Heusch G. Bradycardic agent UL-FS 49 attenuates ischemic regional myocardial dysfunction and reduces infarct size in swine: comparison with the ß-blocker atenolol. J. Cardiovasc. Pharmacol.25, 216–228 (1995).
   Web of Science ®Google Scholar
• Brown HF, DiFrancesco D, Noble SJ. How does adrenaline accelerate the heart? Nature280, 235–236 (1979).
   PubMed Web of Science ®Google Scholar
• DiFrancesco D. Pacemaker mechanisms in cardiac tissue. Annu. Rev. Physiol.55, 455–472 (1993).
   PubMed Web of Science ®Google Scholar
• Vilaine JP. The discovery of the selective I(f) current inhibitor ivabradine. A new therapeutic approach to ischemic heart disease. Pharmacol. Res.53, 424–434 (2006).
   PubMed Web of Science ®Google Scholar
• Bois P, Bescond J, Renaudon B, Lenfant J. Mode of action of bradycardic agent, S 16257, on ionic currents of rabbit sinoatrial node cells. Br. J. Pharmacol.118, 1051–1057 (1996).
   PubMed Web of Science ®Google Scholar
• DiFrancesco D. Funny channels in the control of cardiac rhythm and mode of action of selective blockers. Pharmacol. Res.53, 399–406 (2006).
   PubMed Web of Science ®Google Scholar
• Borer JS, Heuzey JY. Characterization of the heart rate-lowering action of ivabradine, a selective I(f) current inhibitor. Am. J. Ther.15, 461–473 (2008).
   PubMed Web of Science ®Google Scholar
• Camm AJ, Lau CP. Electrophysiological effects of a single intravenous administration of ivabradine (S 16257) in adult patients with normal baseline electrophysiology. Drugs R D4, 83–89 (2003).
   PubMedGoogle Scholar
• Simon L, Ghaleh B, Puybasset L, Giudicelli JF, Berdeaux A. Coronary and hemodynamic effects of S 16257, a new bradycardic agent, in resting and exercising conscious dogs. J. Pharmacol. Exp. Ther.275, 659–666 (1995).
   PubMed Web of Science ®Google Scholar
• Thollon C, Cambarrat C, Vian J, Prost JF, Peglion JL, Vilaine JP. Electrophysiological effects of S 16257, a novel sino-atrial node modulator, on rabbit and guinea-pig cardiac preparations: comparison with UL-FS 49. Br. J. Pharmacol.112, 37–42 (1994).
   PubMed Web of Science ®Google Scholar
• Vilaine JP, Bidouard JP, Lesage L, Reure H, Peglion JL. Anti-ischemic effects of ivabradine, a selective heart rate-reducing agent, in exercise-induced myocardial ischemia in pigs. J. Cardiovasc. Pharmacol.42, 688–696 (2003).
   PubMed Web of Science ®Google Scholar
• Colin P, Ghaleh B, Monnet X et al. Contributions of heart rate and contractility to myocardial oxygen balance during exercise. Am. J. Physiol. Heart Circ. Physiol.284, H676–H682 (2003).
   PubMed Web of Science ®Google Scholar
• Colin P, Ghaleh B, Monnet X, Hittinger L, Berdeaux A. Effect of graded heart rate reduction with ivabradine on myocardial oxygen consumption and diastolic time in exercising dogs. J. Pharmacol. Exp. Ther.308, 236–240 (2004).
   PubMedGoogle Scholar
• Heusch G. α-adrenergic mechanisms in myocardial ischemia. Circulation81, 1–13 (1990).
   PubMed Web of Science ®Google Scholar
• Heusch G, Baumgart D, Camici P et al. α-adrenergic coronary vasoconstriction and myocardial ischemia in humans. Circulation101, 689–694 (2000).
   PubMedGoogle Scholar
• Ceconi C, Cargnoni A, Francolini G, Parinello G, Ferrari R. Heart rate reduction with ivabradine improves energy metabolism and mechanical function of isolated ischaemic rabbit heart. Cardiovasc. Res.84, 72–82 (2009).
   Google Scholar
• Heusch G, Skyschally A, Gres P, Van Caster P, Schilawa D, Schulz R. Improvement of regional myocardial blood flow and function and reduction of infarct size with ivabradine: protection beyond heart rate reduction. Eur. Heart J.29, 2265–2275 (2008).
   PubMed Web of Science ®Google Scholar
• Heusch G. Pleiotropic action(s) of the bradycardic agent ivabradine: cardiovascular protection beyond heart rate reduction. Br. J. Pharmacol.155, 970–971 (2008).
   PubMed Web of Science ®Google Scholar
• Custodis F, Schirmer SH, Baumhakel M, Heusch G, Bohm M, Laufs U. Vascular pathophysiology in response to increased heart rate. J. Am. Coll. Cardiol.56, 1973–1983 (2010).
   PubMed Web of Science ®Google Scholar
• Drouin A, Gendron ME, Thorin E, Gillis MA, Mahlberg-Gaudin F, Tardif JC. Chronic heart rate reduction by ivabradine prevents endothelial dysfunction in dyslipidaemic mice. Br. J. Pharmacol.154, 749–757 (2008).
   PubMed Web of Science ®Google Scholar
• Custodis F, Baumhakel M, Schlimmer N et al. Heart rate reduction by ivabradine reduces oxidative stress, improves endothelial function, and prevents atherosclerosis in apolipoprotein E-deficient mice. Circulation117, 2377–2387 (2008).
   PubMed Web of Science ®Google Scholar
• Walcher T, Bernhardt P, Vasic D et al. Ivabradine reduces chemokine-induced CD4-positive lymphocyte migration. Mediators Inflamm.2010, 751313 (2010).
   Google Scholar
• Heusch G. Heart rate and heart failure. Not a simple relationship. Circ. J.75, 229–236 (2011).
   PubMed Web of Science ®Google Scholar
• Ceconi C, Comini L, Suffredini S et al. Heart rate reduction with ivabradine prevents the global phenotype of left ventricular remodeling. Am. J. Physiol. Heart Circ. Physiol.300, H366-H373 (2010).
   Google Scholar
• Mulder P, Barbier S, Chagraoui A et al. Long-term heart rate reduction induced by the selective I(f) current inhibitor ivabradine improves left ventricular function and intrinsic myocardial structure in congestive heart failure. Circulation109, 1674–1679 (2004).
   PubMed Web of Science ®Google Scholar
• Fox K, Ford I, Steg PG, Tendera M, Ferrari R. Ivabradine for patients with stable coronary artery disease and left-ventricular systolic dysfunction (BEAUTIFUL): a randomised, double-blind, placebo-controlled trial. Lancet372, 807–816 (2008).
   PubMed Web of Science ®Google Scholar
• Swedberg K, Komajda M, Bohm M et al. Ivabradine and outcomes in chronic heart failure (SHIFT): a randomised placebo-controlled trial. Lancet376, 875–885 (2010).
   PubMed Web of Science ®Google Scholar
• Borer JS, Fox K, Jaillon P, Lerebours G. Antianginal and antiischemic effects of ivabradine, an I(f) inhibitor, in stable angina: a randomized, double-blind, multicentered, placebo-controlled trial. Circulation107, 817–823 (2003).
   PubMed Web of Science ®Google Scholar
• Ruzyllo W, Tendera M, Ford I, Fox KM. Antianginal efficacy and safety of ivabradine compared with amlodipine in patients with stable effort angina pectoris: a 3-month randomised, double-blind, multicentre, noninferiority trial. Drugs67, 393–405 (2007).
   PubMed Web of Science ®Google Scholar
• Tardif JC, Ford I, Tendera M, Bourassa MG, Fox K. Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina. Eur. Heart J.26, 2529–2536 (2005).
   PubMed Web of Science ®Google Scholar
• Tardif JC, Ponikowski P, Kahan T. Efficacy of the If current inhibitor ivabradine in patients with chronic stable angina receiving β-blocker therapy: a 4 month, randomized, placebo-controlled trial. Eur. Heart J.30, 540–548 (2009).
   PubMed Web of Science ®Google Scholar
• Lopez L, Filipova S, Martos R. Long-term safety and efficacy of ivabradine in patients with chronic stable angina. Cardiology108, 387–396 (2007).
   Google Scholar
• Tendera M, Borer J, Tardif J. Efficacy of I(f) inhibition with ivabradine in different subpopulations with stable angina pectoris. Cardiology114, 116–125 (2009).
   PubMed Web of Science ®Google Scholar
• Fox KM, Mulcahy D, Findlay I, Ford I, Dargie HJ. The Total Ischaemic Burden European Trial (TIBET). Effects of atenolol, nifedipine SR and their combination on the exercise test and the total ischaemic burden in 608 patients with stable angina. The TIBET Study Group. Eur. Heart J.17, 96–103 (1996).
   PubMed Web of Science ®Google Scholar
• Klein WW, Jackson G, Tavazzi L. Efficacy of monotherapy compared with combined antianginal drugs in the treatment of chronic stable angina pectoris: a meta-analysis. Coron. Artery Dis.13, 427–436 (2002).
   Google Scholar
• Fox K, Ford I, Steg PG, Tendera M, Robertson M, Ferrari R. Relationship between ivabradine treatment and cardiovascular outcomes in patients with stable coronary artery disease and left ventricular systolic dysfunction with limiting angina: a subgroup analysis of the randomized, controlled BEAUTIFUL trial. Eur. Heart J.30, 2337–2345 (2009).
   PubMed Web of Science ®Google Scholar
• Heusch G. A BEAUTIFUL lesson – ivabradine protects from ischaemia, but not from heart failure: through heart rate reduction or more? Eur. Heart J.30, 2300–2301 (2009).
   PubMed Web of Science ®Google Scholar
• Koster R, Kaehler J, Meinertz T. Treatment of stable angina pectoris by ivabradine in every day practice: the REDUCTION study. Am. Heart J.158, e51–e57 (2009).
   PubMed Web of Science ®Google Scholar
• Koester R, Kaehler J, Meinertz T. Ivabradine for the treatment of stable angina pectoris in octogenarians. Clin. Res. Cardiol.100(2), 121–128 (2010).
   Google Scholar
• Koester R, Kaehler J, Ebelt H, Soeffker G, Werdan K, Meinertz T. Ivabradine in combination with β-blocker therapy for the treatment of stable angina pectoris in every day clinical practice. Clin. Res. Cardiol.99, 665–672 (2010).
   Web of Science ®Google Scholar
• Savelieva I, Camm AJ. I(f) inhibition with ivabradine: Electrophysiological effects and safety. Drug Saf.31, 95–107 (2008).
   PubMed Web of Science ®Google Scholar
• Tendera M, Talajic M, Robertson M et al. Safety of ivabradine in patients with coronary artery disease and left ventricular systolic dysfunction (from the BEAUTIFUL Holter Substudy). Am. J. Cardiol.107, 805–811 (2011).
   PubMed Web of Science ®Google Scholar
• Daly C, Clemens F, Lopez-Sendon J et al. Indequate control of heart rate in patients with stable angina: results from the European Heart Survey. Postgrad. Med. J.86(1014), 212–217 (2010).
   PubMed Web of Science ®Google Scholar
• Bax J, Achenbach S, Cademartiri F, Garot J, Tendera M, Zamorano J. A randomized double blind trial on the efficacy and safety of a single intravenous bolus of ivabradine versus placebo for heart rate control during coronary CT angiography. Eur. Heart J.31(Suppl.), 151 (2010) (Abstract 950).
   Google Scholar
• Steg PG, Lopez-Sendon JL. A pilot randomized trial of intravenous ivabradine vs placebo on top of usual care following percutaneous coronary intervention for ST-segment-elevation myocardial infarction. Circulation122, A14196 (2010).
   Google Scholar