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PubMed1994

[The use of digitalis glycosides in atrial fibrillation].

The role of cardiac glycosides for conversion of atrial fibrillation to simus rhythm is controversially discussed. In a prospective study, 45 patients with paroxysmal atrial fibrillation were randomly assigned to one of three treatment groups (of 15 patients each). Group I received oral digoxin, three times 0.125 mg up to twice 0.25 mg daily; group II oral digoxin twice 0.125 mg and quinidine hydrogen sulphate 750-1000 mg daily; group III oral digoxin three times 0.125 mg and flecaimide 200-300 mg daily. During a mean observation period of 11 months, digoxin alone was significantly less effective (p < 0.05) in reducing or suppressing paroxyms of atrial fibrillation than digoxin plus quinidine or flecainide. The use of digoxin remains a mainstay of treatment for rate control in atrial fibrillation. To convert atrial fibrillation to sinus rhythm, however, the addition of a type I or III antiarrhythmic agent is necessary.

Administration, Oral↗
PubMed1994

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

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)

Administration, Oral↗