Abstract
In the 20 years since the definition by Fleckenstein [1] of drugs selectively blocking the slow calcium channel in myocardial cells and realization of their clinical usefulness, there has been an outburst of pharmacological research producing new agents in this group. This has led to extensive argument as to which drugs are true calcium channel blockers and which prevent calcium ion entry to the cells by other mechanisms.
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References
Fleckenstein, A. (1977) Specific pharmacology of calcium in myocardium, cardiac pacemakers and vascular smooth muscle. Ann. Rev. Pharmaco. Toxicol., 17 149–66.
Opie, L.H. (1984) Calcium antagonists. Mechanisms, therapeutic indications and reservations: a review. Quart. J. Med., 53, 1–16.
Tomlinson, S., MacNeil, S., Walker, S.W., Ollis, C.A., Merritt, J.E. and Brown, B.L. (1984) Calmodulin and cell function. Clin. Sci., 66, 497–507.
Braunwald, E. (1982) Mechanism of action of calcium-channel-blocking agents. N. Engl. J. Med., 307, 1618–27.
Kawai, C., Konishi, T., Matsuyama, E. and Okazaki, H. (1981) Comparative effects of three calcium antagonists, diltiazem, verapamil and nifedipine on the sinoatrial and atrioventricular nodes. Experimental and clinical studies. Circulation, 63, 1035–42.
Drake-Holland, A.J., and Noble, M.I.M. (1983) Editorial: Myocardial protection by calcium antagonist drugs. Eur. Heart J., 4, 823–5.
Meyer, H., Bossert, F., Wehinger, E., Towart, R. and Belleman, N.P. (1983) Chemistry of calcium antagonists. Hypertension, 5, 112–7.
Henry, P.D. (1980) Comparative pharmacology of calcium antagonists: nifedipine, verapamil and diltiazem. Am. J. Cardiol., 46, 1047–56.
Belz, G.G., Aust, P.E. and Munkes, R. (1981) Digoxinplasma concentrations and nifedipine. Lancet, i, 844–5.
Nayler, W.G., Poole-Wilson, P.A. and Williams, A. (1979) Hypoxia and calcium. J. Mol. Cell Cardiol., 11, 683–706.
Baker, J.E. and Hearse, D.J. (1983) The temperature-sensitivity of slow channel calcium blockers in relation to their effect on the calcium paradox. Eur. Heart J., 4, Suppl. H, 97–103.
Clusin, W.T., Buchbinder, M. and Harrison, D.C. (1983) Calcium overload ‘injury’ current, and early iscahemic cardiac arrhythmias - a direct connection, Lancet, i, 272–4.
Bagger, J.P., Toftegaard-Nielsen, T. and Hennigsen, P. (1983) The effect of verapamil on myocardial exchange of free fatty acids, citrate lactate and glucose in coronary artery disease. Eur. Heart J., 4, 406–14.
Smith, H.J., Goldstein, R.A., Griffith, J.M., Kent, K.M. and Epstein, S.E. (1976) Regional contractility: selective depression of ischemic myocardium by verapamil. Circulation, 54; 629–35.
The Danish study group on verapamil in myocardial infarction (1984) Verapamil in acute myocardial infarction. Eur. Heart J., 5, 516–28.
Brooks, W.W., Verrier, R. and Lown, B. (1980) Protective effects of verapamil on vulnerability to ventricular fibrillation during myocardial ischaemia and reperfusion. Cardiovasc. Res., 14, 295–302.
Winslow, E., Marshall, R.J. and Hope, F.G. (1983) Comparative effects of fast and slow ion channel blocking agents on reperfusion-induced arrhythmias in the isolated perfused rat heart. J. Cardiovasc. Pharmacol., 5, 928–36.
Mason, J.W., Swerdlow, C.D. and Mitchell, L.B. (1983) Efficacy of verapamil in chronic, recurrent ventricular tachycardia. Am. J. Cardiol., 51, 1614–17.
Fazzini, P.F., Marchi, F., Pucci, P., Ledda, F. and Mugelli, A. (1979) Effects of verapamil on ventricular premature beats of acute myocardial infarction. Am. Heart J., 98, 816–18.
van Zweiten, P.A., van Meel, J.C.A. and Timmermans, P.B.M.W.M. (1983) Pharmacology of calcium entry blockers: interaction with vascular alphaadrenoceptors. Hypertension, 5, 118–17.
Johnston, A., Burgess, C.D. and Hamer, J. (1981) Systematic availability of oral verapamil and effect on PR interval in man. Brit. J. Clin. Pharmacol., 12, 397–400.
Shand, D.G., Hammill, S.C., Aanonsen, L. and Pritchett, E.L.C. (1981) Reduced verapamil clearance during long-term oral dministration. Clin. Pharm. Ther., 30, 701–3.
Somogyi, A., Albrecht, M., Kleims, G., Schafter, K. and Eichelbaum, M. (1981) Pharmacokinetics, bioavailabilities, and ECG response to verapamil in patients with liver cirrhosis. Br. J. Clin. Pharmacol., 12, 51–60.
Eichelbaum, M., Mikas, G. and Vogelgesang, B. (1984) Pharmacokinetics at (+)- (-)- and (±)-verapamil after intravenous administration. Br. J. Clin. Pharmacol., 17, 453–8.
Vlietstra, R.E., Farias, M.A.C., Frye, R.L., Smith, H.C. and Ritman, E.L. (1983) Effect of verapamil on left ventricular function: a randomized placebo-controlled study. Am. J. Cardiol., 51, 1213–17.
Packer, M., Meiler, J., Medina, N., Yushak, M., Smith, H., Holt, J., Guererro J., Todd, G.D., McAllister, R.G. and Gorlin, R. (1982) Hemodynamic consequences of combined beta-adrenergic and slow calcium channel blockade in man. Circulation, 65, 660–8.
Woie, L. and Storstein, L. (1981) Successful treatment of suicidal verapamil poisoning with calcium gluconate. Eur. Heart J., 2, 239–42.
Gmeiner, R. and Ng, C.K. (1981) Effect of tiapamil in the Wolff-ParkinsonWhite syndrome. J. Cardiovasc. Pharmacol, 3, 237–50.
Flammang, D., Waynberger, M., Jansen, F.H., Paillet, R. and Courmel, Ph. (1983) Electrophysiological profile of bepridil, a new anti-anginal drug with calcium blocking properties. Eur. Heart J., 4, 647–54.
Maclean, D. and Feely, J. (1983) Calcium antagonists, nitrates, and new antianginal drugs. Br. Med. J., 286, 1127–30.
Robinson, B.F., Dobbs, R.J. and Kelsey, C.R. (1980) Effects of nifedipine on resistance vessels, arteries and veins in man. Br. J. Clin. Pharmacol, 10, 433–8.
Raemsch, K.D. and Sommer, J. (1983) Pharmacokinetics and metabolism of nifedipine. Hypertension, 5, II18–II24.
Charles, S., Ketelslegers, J.-M. Buysschaert, M. and Lambert, A.E. (1981) Hyperglycaemic effect of nifedipine. Br. Med. J., 283, 19–20.
Joshi, P.I., Dalai, J.J., Ruttley, M.S.J., Sheridan, D.J. and Henderson, A.H. (1981) Nifedipine and left ventricular function in beta-blocked patients. Br. Heart J., 45, 457–9.
Opie, L.H. and White, D.A. (1980) Adverse interaction between nifedipine and beta-blockade. Br. Med. J., 281, 1462.
Harris, L., Dargie, H.J., Lynch, P.G., Bulpitt, C.J. and Krikler, D.M. (1982) Blood pressure and heart rate in patients with ischaemic heart disease receiving nifedipine and propranolol. Br. Med. J., 284, 1148–51.
Iliopoulou, A., Turner, P. and Warrington, S.J. (1983) Acute haemodynamic effects of a new calcium antagonist, nicardipine, in man. A comparison with nifedipine. Br. J. Clin. Pharmacol., 15, 59–66.
Hansson, L., Andren, L., Oro, L. and Ryman, T. (1983) Pharmacokinetic and pharmacodynamic parameters in patients treated with nitrendipine. Hypertension, 5, I125–1128.
Allen, G.S., Ahn, H.S., Preziosi, T.J., Battye, R., Boone, S.C., Chou, S.N., Kelly, D.L., Weir, B.K., Crabbe, R.A., Lavik, P.J., Rosenbloom, S.B., Dorsey, F.C., Ingram, C.R., Mellits, D.E., Bertsch, L.A., Boisvert, D.P.J., Hundley, M.B., Johnson, R.K., Strom, J. A. and Transou, C.R. (1983) Cerebral arterial spasm–a controlled trial of nimodipine in patients with subarachnoid hemorrhage. N. Engl. J. Med., 308, 619–24.
Tweddel, A.C., Johnsson, G., Pringle, T.H., Murray, R.G., and Hutton, I. (1983) The systemic coronary haemodynamic effects of felodipine in patients with coronary heart disease. Eur. Heart J., 4, 699–705.
Smith, M.S., Verghese, C.P., Shand, D.G. and Pritchett, E.L.C. (1982) Pharmacokinetic and pharmacodynamic effects of diltiazem. Am. J. Cardiol., 51, 1369–74.
Valette, H. and Apoil, E. (1980) Haemodynamic effects of dilitiazem in healthy volunteers. Br. J. Clin. Pharamcol., 10, 623–4.
Hossack, K.F. (1982) Conduction abnormalities due to diltiazem. N. Engl. J. Med., 307, 953–4.
Grenadier, E., Keidar, S., Alpan, G., Marmor, A. and Palant A. (1980) Prenylamine-induced ventricular tachycardia and syncope controlled by ventricular pacing. Br. Heart J., 44, 330–4.
Shah, R.R., Oates, N.S., Idle, J.R., Smith, R.L. and Lockhart, J.D.F. (1982) Impaired oxidation of debrisoquine in patients with perhexiline neuropathy. Br. Med. J., 284, 295–9.
Dawes, F. and Moulder, C. (1982) Perhexiline hepatitis and HLA B8. Lancet, ii, 109.
Sebille, A. (1978) Prevalence of latent perhexiline neuropathy. Br. Med. J., i, 1321–2.
Horgan, J.H., O’Callaghan, W.G. and Tee, K.K. (1981) Therapy of angina pectoris with low-dose perhexiline. J. Cardiovasc. Pharmacol., 3, 566–72.
Holmes, B., Brodgen, R.N., Heel, R.C., Speight, T.M. and Avery, G.S. (1984) Flunarizine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use. Drugs, 27, 6 44.
Towse, G. (ed.) (1980) Myocardial protection and exercise tolerance: the role of lidoflazine a new anti-anginal agent. Roy. Soc. Med. Int. Congr. Symp. Series, 29.
Hanley, S.P. and Hampton, J.R. (1983) Ventricular arrhythmias associated lidoflazine: side-effects observed in a randomized trial. Eur. Heart J., 4, 889–93.
Valette, H., Barnay, C., Lopez, M., Hebert, J.L., Gallet, M., Apoil, E., Moyse, D. and Medvedowsky, J.L. (1983) Effect of intravenous diltiazem on sinus node function and atrioventricular conduction in patients. J. Cardiovasc. Pharmacol., 5, 62–6.
Rowland, E., Evans, T. and Krikler, D.M. (1979) Effect of nifedipine on atrioventricular conduction as compared with verapamil. Intracardiac-electrophysiological study. Br. Heart J., 42, 126–7.
Mitchell, L.B., Jutzy, K.R., Lewis, S.J., Schroeder, J.S. and Mason, J.W. (1982) Intracardiac electrophysiological study of intravenous diltiazem and combined diltiazem-digoxin in patients. Am. Heart J., 103, 57–66.
Harper, R.W., Whitford, E., Middlebrook, K., Federman, J., Anderson, S. and Pitt, A. (1982) Effects of verapamil on the electrophysiologic properties of the accessory pathway in patients with the Wolff-Parkinson-White syndrome. Am. J. Cardiol., 50, 1323–30.
Lang, R., Klein, H.O., DiSegni, E., Gefen, J., Sareli, P., Libhaber, C., David, D., Weiss, E., Guerrero, J. and Kaplinsky, E. (1983) Verapamil improves exercise capacity in chronic atrial fibrillation: double-blind crossover study. Am. Heart J., 105, 820–5.
Johnson, S.M., Mauristen, D.F., Willerson, J.T. and Hillis, L.D. (1981) A controlled trial of verapamil for Prinzmetal’s variant angina. N. Engl. J. Med., 304, 862–6.
Yasue, H., Omote, S., Takizawa, A., Nagao, M., Miwa, K. and Tanaka, S. (1979) Exertional angina pectoris caused by coronary arterial spasm: effects of various drugs. Am. J. Cardiol., 43, 647–52.
Editorial (1984) Nitrates and angina. Lancet, i, 998–9.
McIlwraith, G.R., Kidner, P.H. and Oram, S. (1980) Effect of nifedipine on exercise tolerance in angina pectoris. Br. Heart J., 44, 335–341.
Lown, B. (ed.) (1979) Symposium on nifedipine and calcium flux inhibition in the treatment of coronary arterial spasm and myocardial ischemia. Am. J. Cardiol., 44, 779–844.
Winniford, M.D., Johnson, S.M., Mauritson, D.R. and Hillis, L.D. (1983) Ergonovine provocation to assess efficacy of long-term therapy with calcium antagonists in Prinzmetal’s variant angina. Am. J. Cardiol., 51, 684–8.
Gerstenblith, G., Ouyang, P., Achuff, S.C., Bulkley, B.H., Becker, L.C., Mellits, E.D., Baughman, K.L., Weiss, J.L., Flaherty, J.T., Kallman, C.H., Llewellyn, M. and Weisfedlt, M.L. (1982) Nifedipine in unstable angina. A double-blind randomized trial. N. Engl. J. Med., 306, 885–9.
Thuesen, L., Jorgensen, J.R., Kvistgaard, H.J., Sorensen, J.A., Vaeth, M., Jensen, E.B., Jensen, J.J. and Hagerup, L. (1983) Effect of verapamil on enzyme release after early intravenous administration in acute myocardial infarction: double blind randomised trial. Br. Med. J., 286, 1107–8.
Lehmann, H.-U., Hochrein, H., Witt, E. and Mies, H.W. (1983) Hemodynamic effects of calcium antagonists. Rev. Hypertension, 5, I166–1173.
Zacca, N.M., Verani, M.S., Chahine, R.A. and Miller, R.R. (1982) Effect of nifedipine on exercise-induced left ventricular dysfuntion and myocardial hypoperfusion in stable angina. Am. J. Cardiol., 50, 689–95.
Serruys, P.W., Hooghoudt, T.E.M., Reiber, J.H.C., Slager, C., Brower, R.W. and Hugenholtz, P.G. (1983) Influence of intravenous nifedipine on left ventricular function, coronary vasomotility and myocardial oxygen consumption. Br. Heart J., 49, 427–41.
Dagenais, G.R., Moisan, A., Marquis, Y., Davies, R.O. and Blouin, S. (1976) Effects of practolol on exercise tolerance, and cardiac haemodynamics and metabolism in patients with coronary artery disease. Cardiovasc. Res., 10, 25–36.
Schazenbacher, P., Liebau, G., Deeg, P. and Kochsiek, K. (1983) Effect of intravenous and intracoronary nifedipine on coronary blood flow and myocardial oxygen consumption. Am. J. Cardiol., 49, 442–6.
Stone, D.L., Stephens, J.D. and Banim, S.O. (1983) Coronary haemodynamic effects of nifedipine. Comparison with glyceryl trinitrate. Br. Heart J., 49, 422–6.
Rouleau, J-L., Chatterjee, K., Ports, T.A., Doyle, M.B., Hiramatsu, B. and Parmley, W.W. (1983) Mechanism of relief of pacing-induced angina with oral verapamil: reduced oxygen demand. Circulation, 67, 94–100.
Klein, H.O., Ninio, R. Oren, V., Lang, R., Sareli, P., DiSegni, E. David, D., Guerrero, J. and Kaplinksy, E. (1983) The acute hemodynamic effects of intravenous verapamil in coronary artery disease: assessment of equilibrium-gated radionuclide ventriculography. Circulation, 67, 101–10.
Deanfield, J. Wright, C. and Fox, K. (1983) Treatment of angina pectoris with nifedipine: importance of dose titration. Br. Med. J., 286, 1467–70.
Subramanian, V.B., Bowles, M.J., Khurmi, N.S., Davies, A.B., O’Hara, M.J. and Raftery, E.B. (1983) Calcium antagonist withdrawal syndrome: objective demonstration with frequency-modulated ambulatory ST-segment monitoring. Br. Med. J., 286, 520–1.
Editorial (1983) Calcium-channel blockers and asthma. Thorax, 38, 481–5.
Packer, M. and Frishman, H. (eds) (1982) Symposium on verapamil therapy for angina pectoris. Am. J. Cardiol., 50, 881–912, 913–28, 1153–95.
Bowles, M.J., Subramanian, V.B., Davies, A.B. and Raftery, E.B. (1981) Comparison of antianginal actions of verapamil and propranolol. Br. Med. J., 282, 1754.
Subramanian, V.B., Bowles, M.J., Shurmi, N.S., Davies, A.B. and Raftery, E.B. (1982) Randomized double-blind comparison of verapamil and nifedipine in chronic stable angina. Am. J. Cardiol., 50, 696–703.
Wagniart, P., Ferguson, R.J., Cheitman, B.R., Achard, F., Benacerraf, A., Delanguenhagen, B., Morin, B., Pasternac, A. and Bourassa, M.G. (1982) Increased exercise tolerance and reduced electrocardiographic ischemia with diltiazem in patients with stable angina pectoris. Circulation, 66, 23–8.
Winniford, M.D., Markham, R.V., Firth, B.G., Nicod, P. and Hillis, L.D. (1982) Hemodynamic and electrophysiologic effects of verapamil and nifedipine in patients on propranolol. Am. J. Cardiol., 50, 704–10.
Robinson, B.F., Dobbs, R.J. and Bayley, S. (1982) Response of forearm resistance vessels to verapamil and sodium nitroprusside in normotensive and hypertensive men: evidence for a functional abnormality of vascular smooth muscle in primary hypertension. Clin. Sci., 63, 33–42.
de Wardener, H.E. and MacGregor, G. (1983) Sodium efflux and essential hypertension. Lancet, i, 185–6.
Heagerty, A.M., Bing, R.F., Thurston, H. and Swales, J.D. (1983) Calcium antagonists in hypertension: relation to abnormal sodium transport. Br. Med. J., 287, 1405–7.
Bianchetti, M.G. Beretta-Piccoli, C., Weidmann, P., Link, L., Boehringer, K., Ferrier, C. and Morton, J.J. (1983) Calcium and blood pressure regulation in normal and hypertensive subjects. Hypertension, 5, I157 - I165.
Erne, P., Bolli, P., Burgisser, E. and Buhler, F.R. (1984) Correlation of platelet calcium with blood pressure. Effect of antihypertensive therapy. N. Engl. J. Med., 310, 1084–8.
McLeay, R.A.B., Stallard, T.J., Watson, R.D.S. and Littler, W.A. (1983) The effect of nifedipine on arterial pressure and reflex cardiac control. Circulation, 67, 1084–90.
Erne, P., Bolli, P., Bertel, O., Hulthen, L., Kiowski, W., Muller, F.B. and Buhgler, F. (1983) Factors influencing the hypotensive effects of calcium antagonists. Hypertension, 5, II97–II102.
Andersson, O., Bengtsson, C., Elmfedt, D., Haglund, K., Hedner, T., Seideman, P., Sjoberg, K.H., Stromgren, E., Aberg, H. and Ostman, J. (1984) Short-term effects of felodpine, a new dihydropyridine, in hypertension. Br. J. Clin. Pharmacol., 17, 257–63.
Simmonneau, G., Escourrou, P., Duroux, P. and Lockhart, A. (1981) Inhibition of hypoxic pulmonary vasoconstriction by nifedipine. N. Engl. J. Med., 304, 1582–5.
Kennedy, T.P., Michael, J.R., Huang, C.-K., Kallman, C.H., Zahka, K., Schlott, W. and Sommer, W. (1984) Nifedipine inhibits hypoxic pulmonary vasoconstriction during rest and exercise in patients with chronic obstructive pulmonary disease. A controlled double-blind study. Am. Rev. Resp. Dis., 129, 544–51.
Guazzi, M.D., Cipolla, C., Sganzerla, P., Agostoni, P.G., Fabbiocchi, F. and Pepi, M. (1983) Clinical use of calcium channel blockers as ventricular unloading agents. Eur. Heart J., 4, Suppl A, 181–7.
Factor, S.M. and Sonnenblick, E.H. (1982) Editorial. Hypothesis: is congestive cardiomyopathy caused by a hyperactive myocardial micro-circulation (microvascular spasm)? Am. J. Cardiol., 50, 1149–52.
Bellocci, F., Ansalone, G., Santarelli, P., Loperfido, F., Scabbia, E., Zecchi, P. and Manzoli, U. (1983) Oral nifedipine in the long-term management of severe chronic heart failure. J. Cardiovasc. Pharmacol., 4, 847–55.
Brooks, N., Cattell, M., Pidgeon, J. and Balcon, R. (1980) Unpredictable response to nifedipine in severe cardiac failure. Br. Med. J., 281, 1324.
Alves, L.E. and Rose, E.P. (1982) Use of nifedipine in older patients and patients with congestive heart failure. Am. J. Med., 72, 462, 472.
Ferlinz, J. and Citron, P.D. (1983) Hemodynamic and myocardial performance characteristics after verapamil use in congestive heart failure. Am. J. Cardiol., 51, 1339–45.
Kinoshita, M., Kusukawa, R., Shimono, Y., Motomura, M., Tomonaga, G. and Hoshino, T. (1979) The effect of diltiazem hydrochloride upon sodium diuresis and renal function in chronic congestive heart failure. Arzneim. Forsch., 29, 676–81.
Timmis, A.D., Campbell, S., Monaghan, M.J., Walker, L. and Jewitt, D.E. (1984) Acute haemodynamic and metabolic effect of felodipine in congestive heart failure. Br. Heart J., 51, 445–51.
Given B.D., Lee, T.H., Stone, P.H. and Dzau, V.J. (1985) Nifedipine in severely hypertensive patients with congestive heart failure and preserved ventricular systolic function. Arch. Intern. Med., 141, 281–5.
Rosing, D.R., Kent, K.M., Maron, B.J. and Epstein, S.E. (1979) Verapamil therapy: a new approach to the pharmacological treatment of hypertrophic cardiomyopathy. II Effects on exercise capacity and symptomatic status. Circulation, 60, 1208–13.
Kaltenbach, M., Hopf, R., Kober, G., Bussmann, W.-D., Keller, M. and Petersen, Y. (1979) Treatment of hypertrophic obstructive cardiomyopathy with verapamil. Br. Heart J., 42, 35–42.
Epstein, S.E. and Roising, D.R. (1981) Verapamil: Its potential for causing serious complications in patients with hypertrophic cardiomyopathy. Circulation, 64, 437–41.
Landmark, K., Sire, S., Thaulow, E., Amile, J.P. and Nitter-Hauge, S. (1982) Haemodynamic effects of nifedipine and propranolol in patients with hypertrophic obstructive cardiomyopathy. Br. Heart J., 48, 19–26.
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Hamer, J. (1987). Calcium antagonists. In: Hamer, J. (eds) Drugs for Heart Disease. Springer, Boston, MA. https://doi.org/10.1007/978-1-4899-3294-5_3
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