Pure heart rate reduction: The If channels from discovery to therapeutic target

British Journal of Cardiology

Volumn 13, Issue 1, 2006, Pages 27-35

  Shattock, Michael ^a   Camm, A John ^b  

^a KING'S COLLEGE LONDON   (United Kingdom)

^b ST GEORGE'S UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

Heart rate reduction; If channel; If current; Inhibition; Ivabradine

Indexed keywords

ALINIDINE; AMLODIPINE; ATENOLOL; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; CALCIUM CHANNEL BLOCKING AGENT; DOBUTAMINE; DOPAMINE; FALIPAMIL; ION CHANNEL; IVABRADINE; NIFEDIPINE; NITRATE; PROPRANOLOL; ZATEBRADINE;

ABSENCE OF SIDE EFFECTS; ARTICLE; CLINICAL TRIAL; DISEASE EXACERBATION; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; HEART DEPOLARIZATION; HEART MUSCLE ISCHEMIA; HIGH RISK PATIENT; HUMAN; HYPOTENSION; INOTROPISM; LUNG CONGESTION; NONHUMAN; QT PROLONGATION; STABLE ANGINA PECTORIS; TACHYCARDIA; VISUAL DISORDER;

EID: 33644617978     PISSN: 09696113     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (54)

1. Dyer A, Perski V, Stamler J et al. Heart-rate as a prognostic factor for coronary heart disease and mortality: findings in three Chicago epidemiologic studies. Am J Epidemiol 1980;112:736-49.
2. Kannel W, Wilson P, Blaire S. Epidemiologic assessment of the role of physical activity and fitness in development of cardiovascular disease. Am Heart J 1985;112:736-49.
3. Goldberg R, Larsen M, Levy D. Factors associated with survival to 75 years of age in middle-aged men and women: the Framingham study. Arch Intern Med 1996;156:505-09.
4. Benetos A, Rudnichi A, Thomas F et al. Influence of heart rate on mortality in a French population. Role of age, gender, and blood pressure. Hypertens 1999;33:44-52.
5. Chang M, Havlik RJ, Corti M-C et al. Relation of heart rate at rest and mortality in the women's health and aging study. Am J Cardiol 2003;2003:1294-9.
6. Jouven X, Empana J-P, Schwartz PJ et al. Heart-rate profile during exercise as a predictor of sudden death. N Eng J Med 2005:352:1951-8.
7. Ferrari R. Selective heart rate reduction: a new approach to the management of angina pectoris. Medicographia 2002;24,207-10.
8. Diaz A, Tardif J-C. Clinical applications of exclusive heart rate reduction in emergency cardiology Medicographia 2005;27:82-5.
9. f channel inhibition in cardiology. London: Science Press, 2004;15-24.
10. f current inhibitor Procoralan®. Medicographia 2005;27:67-74.
11. Fox K, Daly C. Angina: identifying and managing the patient at risk. Dialogues Cardiovas Med 2002;7:71-91.
12. Kjekshus JK. Importance of heart rate in determining beta-blocker efficacy in acute and long-term acute myocardial infarction intervention trials. Am J Cardiol 1986;57:43F-49F
13. The MERIT-HF Study Group. Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF) Lancet 1999;353:2001-07.
14. Packer M, Coats AJ, Fowler MB et al. Carvedilol Prospective Randomized Cumulative Survival Study Group. Effect of carvedilol on survival in severe chronic heart failure. N Engl J Med 2001;344:1651-8.
15. Theroux P, Gregoire J, Chin C, Pelletier G, de Guise P, Juneau M. Intravenous diltiazem in acute myocardial infarction. Diltiazem as adjunctive therapy to activase (DATA) trial. J Am Coll Cardiol 1998;32:620-8.
16. The Danish Study Group on Verapamil in Myocardial Infarction. Secondary prevention of death and reinfarction with verapamil after an acute myocardial infarction. J Hum Hypertens 1990;4(suppl 5):19-25.
17. Ragueneau I, Laveille C, Jochemsen R, Resplandy G, Funck-Bretano C, Jaillon P. Pharmacokinetic-pharmacodynamic modeling of the effects of ivabradine, a direct sinus node inhibitor, on heart rate in healthy volunteers. Clin Pharmacol Ther 1998;64:192-203.
18. f channel inhibition in cardiology London: Science Press, 2004;25-36.
19. f inhibition: new perspectives. Medicographia 2005;27:51-4.
20. 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 1996;118:1051-7.
21. f channels by ivabradine. J Gen Physiol 2002;120:1-13.
22. Thollon C, Bidouard JP, Cambarrat C et al. Stereospecific in vitro and in vivo effects of the new sinus node inhibitor (+)-S 16257. Eur J Pharmacol 1997;339:43-51.
23. Brown HF, DiFrancesco D, Noble SJ. How does adrenaline accelerate the heart? Nature 1979;280:235-6.
24. Noble D, Tsien RW. The kinetics and rectifier properties of the slow potassium current in calf Purkinje fibres. J Physiol 1968;195:185-214.
25. DiFrancesco D. A new interpretation of the pacemaker current in calf Purkinje fibres. J Physiol 1981;314:359-76.
26. f current: a target for specific heart rate reduction Medicographia 2002;24:218-24.
27. f current inhibitors: properties of drug-channel interaction In: Fox K (ed). Selective and specific lf channel inhibition in cardiology. London: Science Press, 2004;1-13.
28. DiFrancesco D. Pacemaker mechanisms in cardiac tissue. Ann Rev Physiol 1993;55:451-67.
29. DiFrancesco D, Mangoni M. Modulation of single hyperpolarization-activated channels (i(f)) by cAMP in the rabbit sino-atrial node. J Physiol 1994;474:473-82.
30. f current and its inhibition by heart rate reducing agents. Curr Med Res Opin 2005;21:1115-22.
31. Borer JS. If inhibition as a therapeutic approach in stable angina: experimental and clinical studies. Medicographia 2005;27:44-50.
32. f pacemaker current in sheep cardiac Purkinje fibres. Eur J Pharmacol 1990; 187:241-56.
33. f) in rabbit sinoatrial node cells by zatebradine (UL-FS 49). On the mode of action of sinus node inhibitors. Circulation 1993;88: 2389-401.
34. Frishman WH, Pepine CJ, Weiss RJ, Baiker WM. Addition of zatebradine, a direct sinus node inhibitor, provides no greater exercise tolerance benefit in patients with angina taking extencled-release nifedipine: results of a multicenter, randomized, double-blind, placebo-controlled, parallel-group study. The Zatebradine Study Group. J Am Coll Cardiol 1995;26:305-12.
35. 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 2003;42: 688-96.
36. Monnet X, Ghaleh B, Colin P, de Curzon OP, Giudicelli JF, Berdeaux A. Effects of heart rate reduction with ivabradine on exercise-induced myocardial ischemia and stunning. J Pharmacol Exp Ther 2001;299: 1133-9.
37. Colin P, Ghaleh B, Hittinger L et al. Differential effects of heart rate reduction and beta-blockade on left ventricular relaxation during exercise. Am J Physiol Heart Circ Physiol 2002;282:H672-9.
38. Camm AJ, Lau C-P. Electrophysiological effects of a single intravenous administration of ivabradine (S 16257) in adult patients with normal baseline electrophysiology. Drugs R D 2003;4:83-9.
39. Task Force of the European Society of Cardiology Management of stable angina pectoris. Recommendations of the Task Force of the European Society of Cardiology. Eur Heart J 1997;18:394-413.
40. f inhibition. Medicographia 2005;27:3-5.
41. Pepine CJ, Abrams J, Marks RG, Morris JJ, Scheidt SS, Handberg E. Characteristics of a contemporary population with angina pectoris. TIDES Investigators. Am J Cardiol 1994;74:226-31.
42. Borer JS, Fox K, Jaillon P, Lerebours G for the Ivabradine Investigators Group. Antianginal and antiischemic effects of ivabradine, an If inhibitor, in stable angina: a randomized, double-blind, multicentered, placebo-controlled trial. Circulation 2003;107:817-23.
43. Tardif JC, Ford I, Tendera M, Bourassa MG. Efficacy of ivabradine, a new selective If inhibitor, compared with atenolol in patients with chronic stable angina. Eur Heart J 2005;26:2529-36.
44. f current inhibitor ivabradine compared to amlodipine as monotherapy in patients with chronic stable angina: a 3-month randomized, controlled, double-blind, multicenter trial. Eur Heart J 2004; 25:878.
45. f current inhibitor ivabradine in patients with chronic stable angina. A one-year randomized, double-blind, multicentre trial. Eur Heart J 2004;25:876.
46. Fox KM, Tardif JC, Ford M, Tendera M on behalf of the INITIATIVE study investigators. Anti-anginal and anti-ischemic efficacy of ivabradine - a selective and specific sinus node If current inhibitor - compared to atenolol in elderly patients with chronic stable angina. Heart 2005;91 (suppl 1):A69.
47. Lewis RV, Lofthouse C. Adverse reactions with beta-adrenergic blocking drugs: an update. Drug Safety 1993;9:272-9.
48. Tardif JC, Fox K, Tendera M, Ford I. Absence of rebound phenomenon after abrupt discontinuation of ivabradine, a new selective and specific If inhibitor, in patients with coronary artery disease, Eur Heart J 2005;26:580.
49. Tardif J. Clinical efficacy of ivabradine. Heart Drug 2005;5:25-8.
50. Perski A, Hamsten A, Lindvall K et al. Heart rate correlates with the severity of coronary atherosclerosis in young post-infarction patients. Am Heart J 1998;116:1369-73.
51. Beere PA, Glagov S, Zarins CK. Retarding effect of lowered heart rate on coronary atherosclerosis. Science 1984;226:180-2.
52. Heidland UE, Strauer BE. Left ventricular muscle mass and elevated heart rate are associated with coronary plaque disruption. Circulation 2001;104:1477-82.
53. Aronow WS, Ahn C, Mercando AD, Epstein S. Association of average heart rate on 24-hour ambulatory electrocardiograms with incidence of new coronary events at 48-month follow-up in 1,311 patients (mean age 81 years) with heart disease and sinus rhythm. Am J Cardiol 1996;78: 1175-6.
54. f) current inhibitor ivabradine improves left ventricular function and intrinsic myocardial structure in congestive heart failure. Circulation 2004;109:1674-9.