References
- Yang EH, Barsness GW, Gersh BJ et al. Current and future treatment strategies for refractory angina. Mayo Clin. Proc. 79, 1284–1292 (2004).
- Pepine CJ, Cohn PF, Deedwania PC et al. Effects of treatment on outcome in mildly symptomatic patients with ischaemia during daily life. The Atenolol Silent Ischaemia Study (ASIST). Circulation 90, 762–768 (1994).
- McCormack JG, Stanley WC, Wolff AA. Ranolazine: a novel metabolic modulator for the treatment of angina. Gen. Pharmacol. 30, 639–645 (1998).
- Packer M. Drug therapy. Combined β-adrenergic and calcium-entry blockade in angina pectoris. N. Engl. J. Med. 320, 709–718 (1989).
- Akhras F, Jackson G. Efficacy of nifedipine and isosorbide mononitrate in combination with atenolol in stable angina. Lancet 338, 1036–1039 (1991).
- Fox KM, Mulcahy D, Findlay I et al. 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).
- Savonitto S, Ardissiono D, Egstrup K et al. Combination therapy with metoprolol and nifedipine versus monotherapy in patients with stable angina pectoris. Results of the International Multicenter Angina Exercise (IMAGE) Study. J. Am. Coll .Cardiol. 27, 311–316 (1996).
- Stanley WC, Lopaschuk GD, Hall JL et al. Regulation of myocardial carbohydrate metabolism under normal and ischaemic conditions. Potential for pharmacological interventions. Cardiovasc. Res. 33, 243–257 (1997).
- Stanley WC. Myocardial energy metabolism during ischaemia and the mechanisms of metabolic therapies. J. Cardiovasc. Pharmacol. Ther. 9(Suppl. 1), S31–S45 (2004).
- Fleming T, Nissen SE, Borer JS et al. Report from the 100th Cardiovascular and Renal Drugs Advisory Committee meeting: US Food and Drug Administration: December 8–9, 2003 Gaithersburg, MD, USA. Circulation 109, e9004–e9005 (2004).
- Stanley WC, Marzilli M. Metabolic therapy in the treatment of ischaemic heart disease: the pharmacology of trimetazidine. Fundam. Clin. Pharmacol. 17, 133–145 (2003).
- Szwed H, Sadowski Z, Elikowski W et al. Combination treatment in stable effort angina using trimetazidine and metoprolol: results of a randomized, double-blind, multicentre study (TRIMPOL II). TRIMetazidine in POLand. Eur. Heart J. 22, 2267–2274 (2001).
- Kantor PF, Lucien A, Kozak R et al. The anti-anginal drug trimetazidine shifts cardiac energy metabolism from fatty acid oxidation to glucose oxidation by inhibiting mitochondrial long-chain 3-ketoacyl coenzyme A thiolase. Circ. Res. 86, 580–588 (2000).
- Wolff AA, Rotmensch HH, Stanley WC et al. Metabolic approaches to the treatment of ischemic heart disease: the clinicians’ perspective. Heart Fail Rev. 7, 187–203 (2002).
- Killalea SM, Krum H. Systematic review of the efficacy and safety of perhexiline in the treatment of ischemic heart disease. Am. J. Cardiovasc. Drugs. 1, 193–204 (2001).
- Kennedy JA, Unger SA, Horowitz JD. Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone. Biochem. Pharmacol. 52, 273–280 (1996).
- Jain D, Dasgupta P, Hughes LO et al. Ranolazine (RS-43285): a preliminary study of a new anti-anginal agent with selective effect on ischaemic myocardium. Eur. J. Clin. Pharmacol. 38, 111–114 (1990).
- Cocco G, Rousseau MF, Bouvy T et al. Effects of a new metabolic modulator, ranolazine, on exercise tolerance in angina pectoris patients treated with β-blocker or diltiazem. J. Cardiovasc. Pharmacol. 20, 131–138 (1992).
- Thadani U, Ezekowitz M, Fenney L et al. Double-blind efficacy and safety study of a novel anti-ischemic agent, ranolazine, versus placebo in patients with chronic stable angina pectoris. Ranolazine Study Group. Circulation 90, 726–734 (1994).
- Rousseau MF, Pouleur H, Cocco G et al. Comparative efficacy of ranolazine versus atenolol for chronic angina pectoris. Am. J. Cardiol. 95, 311–316 (2005).
- Pepine CJ, Wolff AA. A controlled trial with a novel anti-ischemic agent, ranolazine, in chronic stable angina pectoris that is responsive to conventional anti-anginal agents. Ranolazine Study Group. Am. J. Cardiol. 84, 46–50 (1999).
- Chaitman BR, Pepine CJ, Parker JO et al. Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial. JAMA 291, 309–316 (2004).
- Chaitman BR, Skettino SL, Parker JO et al. Anti-ischemic effects and long-term survival during ranolazine monotherapy in patients with chronic severe angina. J Am Coll Cardiol. 43, 1375–1382 (2004).
- Allely MC, Alps BJ. The effects of the novel anti-anginal compound RS 43285 on myocardial conduction in the anaesthetized dog. Br. J. Pharmacol. 93, 375–382 (1988).
- Allely MC, Alps BJ. A comparison of the effects of a series of anti-anginal agents in a novel canine model of transient myocardial ischaemia. Br. J. Pharmacol. 96, 977–985 (1989).
- Wang JX, Maruyama K, Murakami M et al. Anti-anginal effects of ranolazine in various experimental models of angina. Arzneimittelforschung 49, 193–199 (1999).
- Clarke B, Spedding M, Patmore L et al. Protective effects of ranolazine in guinea-pig hearts during low-flow ischaemia and their association with increases in active pyruvate dehydrogenase. Br. J. Pharmacol. 109, 748–750 (1993).
- Gralinski MR, Black SC, Kilgore KS et al. Cardioprotective effects of ranolazine (RS-43285) in the isolated perfused rabbit heart. Cardiovasc. Res. 28, 1231–1237 (1994).
- McCormack JG, Barr RL, Wolff AA et al. Ranolazine stimulates glucose oxidation in normoxic, ischemic, and reperfused ischemic rat hearts. Circulation93,135–142 (1996).
- MacInnes A, Fairman DA, Binding P et al. The anti-anginal agent trimetazidine does not exert its functional benefit via inhibition of mitochondrial long-chain 3-ketoacyl coenzyme A thiolase. Circ. Res. 93, e26–e32 (2003).
- Allely MC, Alps BJ. Prevention of myocardial enzyme release by ranolazine in a primate model of ischaemia with reperfusion. Br. J. Pharmacol. 99, 5–6 (1990).
- Zacharowski K, Blackburn B, Thiemermann C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur. J. Pharmacol. 418, 105–110 (2001).
- Black SC, Gralinski MR, McCormack JG et al. Effect of ranolazine on infarct size in a canine model of regional myocardial ischaemia/reperfusion. J. Cardiovasc. Pharmacol. 24, 921–928 (1994).
- Bagger JP, Botker HE, Thomassen A et al. Effects of ranolazine on ischemic threshold, coronary sinus blood flow, and myocardial metabolism in coronary artery disease. Cardiovasc. Drugs Ther. 11, 479–484 (1997).
- Allely MC, Brown CM, Kenny BA et al. Modulation of α-1-adrenoceptors in rat left ventricle by ischaemia and acyl carnitines: protection by ranolazine. J. Cardiovasc. Pharmacol. 21, 869–873 (1993).
- Allen TJ, Chapman RA. Effects of ranolazine on L-type calcium channel currents in guinea-pig single ventricular myocytes. Br. J. Pharmacol. 118, 249–254 (1996).
- McCormack JG, Baracos VE, Barr R et al. Effects of ranolazine on oxidative substrate preference in epitrochlearis muscle. J. Appl. Physiol. 81, 905–910 (1996).
- Clarke B, Wyatt KM, McCormack JG. Ranolazine increases active pyruvate dehydrogenase in perfused normoxic rat hearts: evidence for an indirect mechanism. J. Mol. Cell Cardiol. 28, 341–350 (1996).
- Todor A, Sharov V, Sabbah HN. Ranolzaine increases ATP synthesis in failing cardiomyocytes through timulation of mitochondrial respiratory activity. Eur. Heart J. 25, 197 (2004).
- Wyatt KM, Skene C, Veitch K et al. The anti-anginal agent ranolazine is a weak inhibitor of the respiratory complex I, but with greater potency in broken or uncoupled than in coupled mitochondria. Biochem. Pharmacol. 50, 1599–1606 (1995).
- Chaitman BR. Efficacy and safety of a metabolic modulator drug in chronic stable angina: review of evidence from clinical trials. J. Cardiovasc. Pharmacol. Ther. 9(Suppl. 1), S47–S64 (2004).
- Antzelevitch C, Belardinelli L, Zygmunt AC et al. Electrophysiological effects of ranolazine, a novel anti-anginal agent with anti-arrhythmic properties. Circulation 110, 904–910 (2004).
- Antzelevitch C, Belardinelli L, Wu L et al. Electrophysiologic properties and anti-arrhythmic actions of a novel anti-anginal agent. J. Cardiovasc. Pharmacol. Ther. 9(Suppl. 1), S65–S83 (2004).
- Schram G, Zhang L, Derakhchan K et al. Ranolazine: ion-channel-blocking actions and in vivo electrophysiological effects. Br. J. Pharmacol. 142, 1300–1308 (2004).
- Stanley WC. Partial fatty acid oxidation inhibitors for stable angina. Expert Opin. Investig. Drugs 11, 615–629 (2002).
- Murphy E, Perlman M, London RE et al. Amiloride delays the ischaemia-induced rise in cytosolic free calcium. Circ. Res. 68, 1250–1258 (1991).
- Liu Q, Docherty JC, Rendell JC et al. High levels of fatty acids delay the recovery of intracellular pH and cardiac efficiency in post-ischemic hearts by inhibiting glucose oxidation. J. Am. Coll. Cardiol. 39, 718–725 (2002).
- Liu B, Clanachan AS, Schulz R et al. Cardiac efficiency is improved after ischaemia by altering both the source and fate of protons. Circ. Res. 79, 940–948 (1996).
- Rousseau MF, Visser FG, Bax JJ et al. Ranolazine: anti-anginal therapy with a novel mechanism: controlled comparison versus atenolol. Eur. Heart J. 15, 95 (1994).
- Chaitman B, Skettino S, Jerling M et al. Ranolazine decreases hemoglobin A1c (HbA1c) in angina patients with diabetes: carbohydrate and lipid parameters in MARISA and CARISA. Eur. Heart J. 24, 21 (2003).
- Thadani U, Glasser S, Bittar N et al. Dose-response evaluation of once-daily therapy with a new formulation of diltiazem for stable angina pectoris. Diltiazem CD Study Group. Am. J. Cardiol. 74, 9–17 (1994).
- Stone PH, Gibson RS, Glasser SP et al. Comparison of propranolol, diltiazem, and nifedipine in the treatment of ambulatory ischaemia in patients with stable angina. Differential effects on ambulatory ischaemia, exercise performance, and anginal symptoms. The ASIS Study Group. Circulation 82, 1962–1972 (1990).
- Wu L, Shryock JC, Song Y et al. Anti-arrhythmic effects of ranolazine in a guinea-pig in vitro model of long-QT syndrome. J. Pharmacol. Exp. Ther. 310, 599–605 (2004).
- Song Y, Shryock JC, Wu L et al. Antagonism by ranolazine of the pro-arrhythmic effects of increasing late INa in guinea-pig ventricular myocytes. J. Cardiovasc. Pharmacol. 44, 192–199 (2004).
- Chandler MP, Stanley WC, Morita H et al. Short-term treatment with ranolazine improves mechanical efficiency in dogs with chronic heart failure. Circ. Res. 91, 278–280 (2002).
- Sabbah HN, Chandler MP, Mishima T et al. Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, improves left ventricular function in dogs with chronic heart failure. J. Card. Fail. 8, 416–422 (2002).
- Sabbah HN, Imai M, Morita H et al. Long-term therapy with ranolazine prevents progressive left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 110 (2004).
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