Cardiac Glycosides 1785–1985: Biochemistry — Pharmacology — Clinical Relevance PDF
Preview Cardiac Glycosides 1785–1985: Biochemistry — Pharmacology — Clinical Relevance
Cardiac Glycosides 1785-1985 Boehringer Mannheim International Symposia E. Erdmann, K. Greef, J. C. Skou ( eds.) Cardiac Glycosides 1785-1985 Biochemistry - Pharmacology - Clinical Relevance With Contributions by C. Achenbach, K. vanA ckern, T. Akera, M. F. Andersen, K. Andersson, J. K. Aronson, P. Bach, H. Bardenheuer, I. Blömer, H. H. Bodemann, D. Branco, E. Braunwald, D. Brent, L. Brown, D. L. Brutsaert, E. Bucha, C. Bufalino, V. P. Butler, M. B. Cannell, M. C. Chan, D. Charlemagne, K. Chatterjee, R. Dahlqvist, T. Daldrup, H. Daying, R. Dietz, W.D oelle, W. Doering, R. Doliwa, W. Drohn, D. A. Eisner, E. Erdmann, 0 . Faergeman, M. Fagoo, H. Fasold, B. Ficht!, K. Fischer, M. Fischer, J. L. Fleg, A. A. L. Fox, C. Freiin, L. Frey, L.,Fridrich, A. Gaßner, M. H. Gault, R. A. Gillis, T. Godfraind, H. K. Gold, M. L. Gon~alves, B. Grabensee, K. Greeff, W. Grille, G. Grupp, I. L. Grupp, N. Gustafson, E. Haber, T. Hair, S. Halbach, 0. Hansen, K.-0. Haustein, S. Herzig, T. Hickerson, P. M. Hooymans, E. Hug, P. G. Hugenholtz, G. Hüller, I. Hutton, A. S. Jaffe, W. Jenkel, T. Jogestrand, W. Johnsen, E. Johnson, T. Joreteg, P. H. Joubert, L. M. Jung, A. M. Katz, B. Kaufmann, T. L. Kirley, K. Kjeldsen, W. Knippenberg, K. Kochsiek, K.-D. Kolenda, M. L. P. Koten, M. Krekler, W. Kübler, R. Kuske, C. Lafleur, M. Lazdunski, W. J. Lederer, G. Lee, S. W. Lee, L. G. Lelievre, J. Lindenbaum, J. J. H. ML. ohman, L. Longerich, B. Lorenz, H. Lüllmann, D. Magometschnigg, C. Maier, J. M. Maixent, D. T.M ason, W. Mäurer, E. Mayoux, W. Meister, F. WH. . M. Merkus, L. von Meyerinck, K. Mohr, K. Moreth, C. Mouas, R. G. Murray, J. E. Muller, M. S. Nieminen, G. Oltmanns, W. Osswald, H. J. Partanen, E. Passamani, T.J . Pellinen, E. Petzinger, M. Pichler, F. Piscione, J. Plum, W. K. Poole, R. Preisler, M. Preteseille, J. A. Quest, D. S. Raabe, D. S. Regal, C. Reithmann, D. Renner, K. R. H. Repke, T. Risler, R. E. Rude, U. Rüegg, J. Sander, H. Schadewaldt, S. G. Schäfer, W. Schaumann, M.S cheininger, K. Schenk Gustafsson, P.S chlieper, W.-D. Schlott, A. Schmoldt, G. Scholtysik, H. Scholz, A. Schömig, W. Schoner, W. Schönfeld, G.S chönsteiner, H. Schühlen, K. P. Schüren, A. Schwartz, H. Schweitzer, 0. M. Sejersted, P. W.S erruys, J. C. Skou, T. W. Smith, G. Sommer, G. Steinbeck, B. Sterndorff, P. H. Stone, H. Strobach, B. Swynghedauw, S. U. Sys, L. B. Tan, K. A. Taubert, H. Tawfik, K. Theisen, G. Tittel, Z. G.T uri, A. C. Tweddel, M. Valdeolmillos, S. Vasdev, E.V igholt-Sv;rensen, P. Vigne, H. Waginger, H. Wagner, E. T. Wallick, E. Weber, K. TW. eber, J. Wieland, T. Wenger, K. Werdan, K. E. Wirth. Springer-Verlag Berlin Heidelberg GmbH Prof. Dr. E. Erdmann Prof. Dr. K. Greeff Prof. Dr. J. C. Skou Klinikum Großhadern Institut für Pharmakologie Biophysik Institut der Universität München der Universität Düsseldorf Aarhus Universitet Medizinische Klinik I Moorenstraße 5 U niversitetparken Marchioninistraße 15 4000 Düsseldorf 8000 Aarhus/Denmark 8000 München 70 West Germany West Germany CIP-Kurztitelaufnahme der Deutschen Bibliothek [Cardiac glycosides seventeen hundred and eighty-five to nineteen hundred and eighty-five] Cardiac glycosides 1785 - 1985 : biochemistry - pharmacology - clin. relevance / E. Erdmann .. . (eds.). With contributions by C. Achenbach .. . (Boehringer Mannheim international symposia) ISBN 978-3-662-11294-6 ISBN 978-3-662-11292-2 (eBook) DOI 10.1007/978-3-662-11292-2 NE: Erdmann, Erland [Hrsg.]; Achenbach, Christopher [Mitverf.] This work is subject to copyright. All rights are reserved, whether the whole or part of the material is concerned, specifically those of translation, reprinting, re-use of illustrations, broadcasting, reproduction by photocopying machine or similar means, and storage in data banks. Copyright © 1986 by Springer-Verlag Berlin Heidelberg Originally published by Dr. Dietrich Steinkopff Verlag, GmbH & Co. KG, Darmstadt in 1986 Softcover reprint of the hardcover I st edition 1986 Medical Editorial: Juliane K. Weller - Copy Editing: Cynthia Feast - Production: Hcinz J. Schäfer The use of registered namcs, trademarks, etc. in this publication does not imply, evcn in thc absence of a specific statement, that such names are excmpt from thc relevant protcctive laws and regulations and therefore free for general usc. Preface The bicentenary of William Withering's now famous medical report entitled "An Account of the Foxglove and Some of its Medical Uses" has given us the occasion to analyze the state of the art. Cardiac glycosides in 1985 are considered tobe the basis for medical treatment of myocardial failure, together with diuretics and vasodilators in the more severe cases. Nevertheless, the controversy as to their exact place in the treatment of heart failure with sinus rhythm has never ceased. Although cardiac glycosides are of unquestionable value in tachycardia caused by atrial fibrillation or atrial flutter, the chronic use of these drugs in sinus rhythm is not generally accepted. The development of tolerance has been reported. It is of interest that Withering hirnself wrote: "- let it (foxglove) be continued until it either acts on the kidneys, the stomach, the pulse, or the bowels; Iet it be stopped upon the first appearance of any of these effects, and I will maintain that the patient will not suffer from its exhibition, nor the practitioner be disappointed in any reasonable expectation." In West Germany alone, more than three million patients (about 5% of the total population) are constantly taking cardiac glycosides. These drugs are the most prescribed medicaments in many countries. Thus, we considered it worthwhile and necessary to review in a critical way today's knowledge about the foxglove; to report new findings and to evaluate old Statements. Cardiac glycosides are used as tools in biochemistry and as model substances in pharmacokinetics. We know that they bind specifically and reversibly to the (Na+ + K+) ATPase, the enzyme that actively transports Na+ and K+ through the cell membraneofall mammalian cells. Therefore, biochemists, physiologists and pharmacologists as weil as clinicians have always been interested in the actions of cardiac glycosides at the molecular Ievel. Their work has added greatly to the understanding of glycoside effects and side effects in our patients and recently has resulted in producing specific antibodies to cardiac glycosides (Fab-fragments). These antibodies have a higher affinity for these drugs than the myocardial receptor enzyme itself, the (Na+ + K+)-ATPase. Thus, the treatment of severe glycoside intoxication with these antibodies has now become possible. Cardiac glycoside research is a good example of the value of mutual interaction and the interrelation of basic and clinical sciences. Problems of treating heart failure with glycosides can often be traced to changes in the quantity or affinity of cardiac glycoside receptors in the myocardial cell membrane. Therefore, Kurt Greeff, Jens C. Skou and I decided to assemble biochemists, physiologists, pharmacologists and clinicians for discussion and evaluation of the present knowledge 200 years after Withering, and to encourage theoreticians and clinicians to speak if not the same, at least a similar language. There are perhaps no other drugs about which we know so much - however, when going into detail, it seems to be the same as always in science - we know astonishingly little about the cardiac glycosides. Therefore, this symposiumwas planned to demonstrate what we do know and what is still obscure about the most ingested drugs in medicine. Hopefully, the next anniversary symposium will succeed in clarifying these problems. Last but not least, I should like to express my thanks to all who participated in this symposium. Especially, I thank all authors for submitting their manuscripts on time, although they are constantly pressed by important work. The Steinkopff Verlag has made it possible for this book to appear so quickly by rapid, efficient, and expert work. Most of all, I should like to express my sincere gratitude to Dr. Wenzel, Dr. Bergmeyer and Mr. Rühl from Boehringer Mannheim. They have generously supported this symposium and this book but moreover, they have themselves carried most of the heavy burden of organisational work. Without their skills, we would not have succeeded. Even if William Withering may not have noticed that cardiac glycosides act by slowing the ventricular rate and by increasing the force and the speed of myocardial contraction, hislast sentence of the "inferences" is certainly still valid: "That it (foxglove) has apower over the motion of the heart, to a degree yet unobserved in any other medicine, and that this power may be converted to salutary ends." Munich 1986 Erland Erdmann Contents Preface . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . V 1. Historial aspects William Withering - The man and bis work Skou, J. C. ................ . Fruitful routes and blind alleys taken by digitalis therapy since its introduction by Withering Schadewaldt, H.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . II Therapeutic use of digitalis until the time of William Withering Jung, L. M ............................ . 17 2. Cardiac glycosides, (Na+ + K+)-ATPase and cation transport The function of Na+, K+-ATPase and its importance for drug action Akera, T ................................ . 19 Structural studies on the cardiac glycoside receptor Wallick, E. T., T. L. Kirley, A. Schwartz ..... . 27 Isoenzymes of Na/K-ATPase identitied by pyrithiamin Hansen, 0 ....................... . 35 Interaction of cardiac glycosides with Na/K-ATPase in intact myocardium Herzig, S., H. Lüllmann, K. Mohr .................... . 41 The human red blood cell: A model for ouabain receptor regulation in the heart? Brown, L., K. Werdan, E. Erdmann . . . . . . . . . . . . . . . . . . . . . . . . . 49 Binding and release of ouabain at low Mg2+ in reconstituted human red blood cell ghosts Bodemann, H. H.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 55 The ouabain receptor in the myocardium and conduction system of the sheep heart Hug, E., L. Brown, E. Erdmann . . . . . . . . . . . . . . . . . . . . . . . . . . . 61 Electrophysiological effects of cardiac glycosides Eisner, D. A., M. Valdeolmillos, W. J. Lederer, M. B. Cannell 69 Electrophysiological assay of glycoside-induced sodium pump inhibition in isolated sheep heart Purkinje fibres at the onset of toxicity Achenbach, C., H. Daying, R. Preisler . . . . . . . . . . . . . . . . . . . . . . . . . 79 Rat cardiac hypertrophy: Contribution of heteregeneous digitalis receptor forms Lelievre, L. G., J. M. Maixent, D. Charlemagne, B. Swynghedauw. . . . . . . . . '!<,7 Digitalis receptors in normal and hypertrophied rat hearts. Differential effects of a Ca2+ free perfusion Charlemagne, D., E. Mayoux, M. Preteseille, J. M. Maixent, Ch. Mouas, B. Swynghe- dauw, L. G. Lelievre . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1)3 Biphasic contractile response to ouabain: Species specific? Calcium dependent? Altered sensitivity? Grupp, G., I. L. Grupp, T. Hickerson, S. W. Lee, A. Schwartz. . . . . . . . . . 1)9 The influence of a-tocopherol-nicotinate (Renascin®) on cardiac glycoside effects Tawfik, H., P. Schlieper. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109 On the connection between cardiac glycosides and calcium action Waginger, H., D. S. Regal .................... . 119 Biochemical basis for the targeted s.ynthesis of cardiac glycosides with selective action Schönfeld, W., J. Weiland, K. R. H. Repke ....................... 127 3. Digitalis-like substances The "endogenous cardiac glycoside" Schoner, W., K. Moreth, R. Kuske, D. Renner. ..... 135 Endogenous digitalis, cardiodigin and other regulators of the sodium pump Godfraind,T., M. Fagoo ................................ 143 Digitalis-like factors in plasma of healthy human adults Vasdev, S., L. Longerich, E. Johnson, D. Brent, M. H. Gault ............. 157 A Na+,K+-ATPase inhibitor isolated from pig kidney Krekler, M., A. A. L. Fox, H. Strobach, K. Greeff ... . . . . . 165 Cardiac glycoside-Iike effects of a bufadienolide extracted from Kalanchoe Daigremontiana Scholtysik, G., H. Wagner, M. Fischer, U. Rüegg ................... 171 4. Mechanism of inotropic effects - cardiac glycosides and other positive inotropic agents Positive inotropic agents: Different mechanisms of action Scholz, H .......................... . . . . . . . . 1' !<,1 Significance of calcium ions in the regulation of myocardial contractility Katz, A. M. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 189 Additive and non-additive positive inotropic effects in human and guinea-pig myocardium Brown, L., B. Lorenz, E. Erdmann ................. . 195 The cardiac Na+ /H+ exchange system. lts role in inotropy Freiin, C., P. Vigne, M. Lazdunski ............ . 207 Evidence for pharmacodynamic differences between cardiac glycosides of different polarities Joubert, P. H. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 215 The positive inotropic action of mercury compounds on isolated heart muscle Halbach, S., G. Schönsteiner . . . . . . . . . . . . . . . . . . . . . . . . . . 221 Chronic pretreatment with amrinone or milrinone induces no tachyphylaxis in mammalian cardiac muscle Sys, S. U., D. L. Brutsaert ............................... 229 Left ventricular function after oral milrinone in patients with congestive heart failure. A hemodynamic and angiographic study Piscione, F., P. W. Serruys, P. G. Hugenholtz ..................... 237 5. Cardiac glycosides - metabolism, interactions and volume of distribution The importance of skeletal musdes as a distribution volume for digitalis glycosides in guinea-pigs and human subjects Kjeldsen\K. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 245 Relevant metabolism of cardiac glycosides Wirth, K. E.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257 The dihydrogenation of digoxin Lindenbaum, J. ........ . 263 Renal excretion and plasma Ievels of dihydrodigitoxin in volunteers and renally healthy and renally insufficient patients being treated with digitoxin Strobach, H. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269 Enzymatic basis for digitoxin metabolism and possible drug interactions in man Schmoldt, A., L. v. Meyerinck, W. Drohn, I. Blömer. . . . . . . . . . . . . . . 273 Effect of quinidine on the inotropic effect of digoxin in isolated cat or guinea-pig papillary muscle Taubert, K.A., C. Bufalino, T. Hair, C. Lafleur .................... 281 Quinidine decreases the intestinal secretion of digoxin and digitoxin in the guinea-pig Schäfer, S. G., B. Ficht!, W. Doering .......................... 287 Quinidine-induced reduction of the biiiary excretion of digoxin in patients Schenck-Gustafsson, K. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 293
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