J Clin Pharmacol
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The Journal of Clinical Pharmacology and the Journal of New Drugs, 1969; 9:148-154
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The Role of the Sugar Component in Cardiac Glycosides on Their Action in Patients With Auricular Fibrillation and Congestive Failure

Harry Gold M.D.1, Nathanial T. Kwit M.D.1, Samuel J. Shane M.D.1, and Conrado Dayrit M.D.1

1 Cornell University Medical College, Beth Israel Medical Center, and Hospital for Joint Diseases and Medical Center, New York, N.Y.

The cardiac glycosides digitoxin, digoxin, and lanatoside C were compared with their respective aglycones digitoxigenin and digoxigenin by intravenous injection in six patients with auricular fibrillation and congestive failure. The glycoside and its genin were compared in the same patient and in the same milligram dose. The effect which was measured was the slowing of the ventricular rate, and the comparison was made in terms of the speed of onset, the degree of maximum effect, the time it takes to reach the maximum slowing, the time it takes for the rate to return to the initial level, and the toxic effects. The results show that the glycoside and its genin have the same kind of action but that the onset of the effect of the genin is almost immediate, that it reaches its maximum effect more quickly, that the degree of effect is less, and that the duration of the effect is shorter than that of the corresponding glycoside. Two of the patients showed toxic effects after digitoxigenin: vomiting, weakness, sweating, and anxiety, suggesting an action on the central nervous system. More experiments are needed to ascertain whether in this respect digitoxigenin differs from digoxigenin. A large oral dose (9 mg) of digoxigenin in one patient produced a negligible effect, indicating that the genin is very poorly absorbed from the gastrointestinal tract. These results in man are in line with the behavior of the genins in laboratory animals.


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