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6 results
Investigation into the species-specific deacylation of penta-acetyl-gitoxin.
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Penta-acetyl-gitoxin (PAG) shows species-specific deacylation to 16-acetyl-gitoxin (16 AG; I and III) or gitoxin (II and IV) by homogenates of liver and intestinal mucosa of man (I), rabbit (II), guinea-pig (III) and rat (IV), whereas it is degraded into tri- and tetra-acetates by homogenates of
Cardiac effects of 16-acetyl-gitoxin, the active glycoside after penta-acetyl-gitoxin administration.
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The inotropic and arrhythmogenic effects of 16-acetyl-gitoxin and digoxin were studied in isolated cardiac preparations and in anaesthetized dogs. ECG alteration-producing and lethal doses of both glycosides were determined in anaesthetized cats. In the isolated guinea-pig atrium, the properties of
Penta-acetyl-gitoxin: the prototype of a prodrug in the cardiac glycoside series.
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Penta-acetyl-gitoxin is a suitable prodrug of gitoxin since it shows--side-effect latentiation, due to its inactive application form;--bioavailability, due to its improved solubility and thus good enteral absorption and--bioactivation, due to rapid de-acetylation in the body after absorption.
Pharmacokinetic investigations with 3H-penta-acetyl-gitoxin in volunteers and patients with respect to the occurrence of drug latentiation.
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After oral administration of 3H-penta-acetyl-gitoxin (Pengitoxin W.H.O., Pentagit) 1.5 mg to four volunteers, serum radioactivity diclines with a half-life of 62 +/- 10 hours. After an oral maintenance dose of 0.4 mg pengitoxin in five digitalized patients, four of them with a cannulated bile duct,
[Cardiac effect of a new penta-acetylated gitoxin (pengitoxin)].
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[CARDIAC THERAPY WITH PENTA-ACETYL-GITOXIN, A NEW HALF-SYNTHETIC PURPUREAGLYCOSIDE].
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