Absorption and metabolism in man of 16-epi-gitoxin, a new semi-synthetic cardioactive glycoside

  • K. O. Haustein
  • Published 1977 in European Journal of Clinical Pharmacology

Abstract

The pharmacokinetics of3H-16-epi-gitoxin have been investigated after oral administration: The peak serum level occurred after 30–60 min, and its subsequent decline was in two phases with halflives of 3.5 and 19.5 h, respectively. Within 3 days 66–70% of the administered radioactivity were eliminated by renal excretion. In the first 16 h 15% of excreted activity was in metabolites, but thereafter the glycoside was excreted in unchanged form. The metabolites were characterized by thin-layer chromatography and radio-scanning; it is assumed that they correspond to the bis- and monodigitoxosides as well as to the genin of 16-epi-gitoxin. The unusual pharmacokinetics of the glycoside are discussed in relation to its special kinetics at the molecular level, i.e. the rapid dissociation rate of the glycoside-(Na++K+)-ATPase-complex.

DOI: 10.1007/BF00562938

3 Figures and Tables

Statistics

05001000'04'05'06'07'08'09'10'11'12'13'14'15'16'17
Citations per Year

141 Citations

Semantic Scholar estimates that this publication has 141 citations based on the available data.

See our FAQ for additional information.

Cite this paper

@article{Haustein1977AbsorptionAM, title={Absorption and metabolism in man of 16-epi-gitoxin, a new semi-synthetic cardioactive glycoside}, author={K. O. Haustein}, journal={European Journal of Clinical Pharmacology}, year={1977}, volume={11}, pages={455-458} }