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Extraordinary efficacy of 16 alpha-gitoxin, an ultra-short acting semi-synthetic digitalis glycoside.

Abstract
The positive inotropic effect of 16 alpha-gitoxin was studied in 52 female and male healthy volunteers between the ages of 21 and 27 years and a body weight between 55 and 76 kg after the single i.v. injection or oral administration in doses between 2.5 and 15 mg. The inotropic effect was evaluated by the use of the systolic time intervals (left ventricular ejection time, LVET, and electromechanic systole, QS2) and by the QT-Interval of the ECG. The glycoside plasma level was measured simultaneously to the pharmacodynamic parameters by a radioimmunoassay, 16 alpha-gitoxin abbreviated dose-dependently the STI (LVET and QS2) for 30 (i.v.) or 15 ms (per os) and the QT interval for 35 ms. A mean plasma concentration of 401 ng/ml was measured 15 minutes after the i.v. injection of 5 mg and a mean plasma level of 402 ng/ml was measured 1 hour after the oral intake of 10 mg 16 alpha-gitoxin as an aqueous-ethanolic solution. The shortening of the STI-values and of the QT-interval correlated with the administered glycoside dose and with the AUC0-6-value. The AUC-values increased linearly with the administered dose. The ratio of the AUC0-6-values after i.v. or oral administration of 7.5 mg 16 alpha-gitoxin amounted to 0.673. Doses of 16 alpha-gitoxin which induce a maximum abbreviation of STI or QT did neither provoke a distinct decrease in heart rate nor cardiac disturbances. Sixteen-alpha-gitoxin develops a positive inotropic effect within a few minutes after i.v. injection and also after oral intake.(ABSTRACT TRUNCATED AT 250 WORDS)
AuthorsK O Haustein, R Bauer
JournalInternational journal of clinical pharmacology and therapeutics (Int J Clin Pharmacol Ther) Vol. 32 Issue 6 Pg. 299-304 (Jun 1994) ISSN: 0946-1965 [Print] Germany
PMID7921531 (Publication Type: Clinical Trial, Controlled Clinical Trial, Journal Article)
Chemical References
  • Cardiac Glycosides
  • Cardiotonic Agents
  • Digoxin
  • gitoxin
Topics
  • Administration, Oral
  • Adult
  • Cardiac Glycosides (pharmacology)
  • Cardiotonic Agents (blood, pharmacology)
  • Digoxin (analogs & derivatives, blood, pharmacology)
  • Electrocardiography (drug effects)
  • Female
  • Heart Rate (drug effects)
  • Humans
  • Injections, Intravenous
  • Male
  • Radioimmunoassay

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