Advertisement

β-methyl-digoxin

VIII. Relation of cerebral side-effects in cats to concentrations in the plasma and in the brain
  • K. Dietmann
  • E. Hrstka
  • K. Koch
  • W. Schaumann
Article

Summary

The tissue/plasma ratio of β-methyl-digoxin for cardiac muscle in cats was about the same 24 h after a single dose of 30 μg/kg as after a loading dose of 30 μg/kg followed by 3 maintenance doses of 7.5 μg/kg at 24 h intervals. The ratio for the brain increased 2-fold during that time.

After the i.v. injection of a toxic loading dose of 70 μg/kg β-methyl-digoxin or digoxin, maintenance doses of as little as 15 μg/kg at 48 h intervals sufficed to maintain the minimum plasma glycoside concentrations determined by RIA at about 3 ng/ml. There was no difference in the plasma concentrations or in the severity of intoxication produced by both glycosides.

Cats vomited within 3 h after i.v. injection of 100 μg/kg β-methyl-digoxin, whereas a loading dose of 30 μg/kg followed by 3 injections of 7.5 μg/kg at 24 h intervals were well tolerated. The concentration of radioactivity in the brain 3 h after 100 μg/kg was less than 24 h after the last injection of 7.5 μg/kg in the experiments with repeated dosage.

Cerebral side-effects such as vomiting, loss of appetite and weight were better correlated with the glycoside concentrations in the plasma than with those in the brain.

Key words

Cats Cardiac glycosides Brain Distribution Side-effects 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Benthe, H. F.: Organverteilung verschiedener Herzglykoside. Digitalistherapie. In: Beiträge zur Pharmakologie und Klinik, pp. 19–34. Berlin-Heidelberg-New York: Springer 1975Google Scholar
  2. Flasch, H., Heinz, N.: Konzentration von Herzglykosiden im Myokard und im Gehirn. Arzneimittel-Forsch.26, 1213–1216 (1976)Google Scholar
  3. Haasis, R., Larbig, D.: Radioimmunologische Bestimmung der Glykosidkonzentrationen im menschlichen Gehirngewebe. Verh. Dtsch. Ges. Kreislaufforsch.42, 275–277 (1976a)Google Scholar
  4. Haasis, R., Larbig, D.: Vergleichende Untersuchungen der Serum-Glykosidkonzentrationen bei Glykosidintoxikationen mit extrakardialen Nebenwirkungen nach Einnahme von Beta-Methyl-digoxin, Beta-Acetyldigoxin und Digoxin. Verh. Dtsch. Ges. Inn. Med.82, 1702–1704 (1976b)Google Scholar
  5. Kaiser, F., Popelak, A., Schaumann, W.: Arzneistoffe aus Pflanzen. Therapiewoche17, 1–10 (1967)Google Scholar
  6. Kuhlmann, J., Reiche, J., Bruns, J.: Distribution of digoxin, β-methyldigoxin and ouabain after single and multiple doses in dogs. Naunyn-Schmiedeberg's Arch. Pharmacol.293, R29 (1976)Google Scholar
  7. Schaumann, W., Koch, K.: β-Methyl-Digoxin. VII. Tissue distribution, positive inotropic and central action in cats in comparison with other digitalis glycosides. Naunyn-Schmiedeberg's Arch. Pharmacol.286, 195–210 (1974)Google Scholar
  8. Schaumann, W., Wegerle, R.: β-Methyl-Digoxin: I. Cardiotoxizität bei enteraler und parenteraler Gabe. Arzneimittel-Forsch.21, 225–231 (1971)Google Scholar
  9. Wartburg, A. v., Kalberer, F., Rutschmann, J.: Tritium-labelled cardiac glycosides: digoxin-[12α-3H]. Biochem. Pharmacol.14, 1883–1889 (1965)Google Scholar

Copyright information

© Springer-Verlag 1978

Authors and Affiliations

  • K. Dietmann
    • 1
  • E. Hrstka
    • 1
  • K. Koch
    • 1
  • W. Schaumann
    • 1
  1. 1.Abteilung für Medizinische und Chemische ForschungBoehringer Mannheim GmbHMannheim 31Germany

Personalised recommendations