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Therapeutic range of cardiac glycosides

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Cardiac Glycoside Receptors and Positive Inotropy

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Summary

The narrow therapeutic range of cardiac glycosides continually challenges chemists to synthetize new derivatives with improved therapeutic properties. One of the best investigated semi-synthetic glycosides is 16α-gitoxin. Compared to ouabain and gitoxin, it produces positive inotropic effects on the isolated guinea-pig heart in a wider range of concentrations and causes less pronounced rhythmic disturbances. These results were confirmed by electrophysiological investigations in isolated fibres of the canine myocardium and of the Purkinje system, by investigations in the anaesthetized cat and dog and in healthy volunteers. The effects of various semi-synthetic compounds (e.g. actodigin, ASI-222) are described and possibilities to trigger these effects are discussed. Of some significance seem to be differences in the structure of the (Na++K+)-ATPase system of different tissues, e.g. the working muscle and the Purkinje system of the heart, as well as differences due to the formation and dissociation of the glycoside-enzyme complex. The significance of K+,Ca2+ and of several pharmacokinetic parameters (e.g. the volume of distribution) for these reactions are briefly discussed.

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Author information

Authors and Affiliations

  1. Section of Clinical Pharmacology of the Institute of Pharmacology and Toxicology of the Medical Academy Erfurt, Nordhäuser Str. 74, GDR-5010, Erfurt, Germany

    Prof. Dr. K.-O. Haustein

Authors
  1. Prof. Dr. K.-O. Haustein
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Editors and Affiliations

  1. Munich, Germany

    E. Erdmann

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© 1984 Springer-Verlag Berlin Heidelberg

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Haustein, KO. (1984). Therapeutic range of cardiac glycosides. In: Erdmann, E. (eds) Cardiac Glycoside Receptors and Positive Inotropy. Steinkopff, Heidelberg. https://doi.org/10.1007/978-3-642-72376-6_20

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  • DOI: https://doi.org/10.1007/978-3-642-72376-6_20

  • Publisher Name: Steinkopff, Heidelberg

  • Print ISBN: 978-3-642-72378-0

  • Online ISBN: 978-3-642-72376-6

  • eBook Packages: Springer Book Archive

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