digitoxin and pentaacetylgitoxin

Topics: Acetyldigoxins; Digitalis Glycosides; Digitoxin; Digoxin; Drug Utilization; Germany, East; Humans; Lanatosides

Color discrimination ability of 100 in-patients suffering from congestive heart failure and treated with digitoxin (D), pengitoxin (P), or digoxin (Dg) was determined with the Farnsworth-Munsell 100 Hue test (FM 100) and compared with the color discrimination of 72 in-patients who were not treated with digitalis glycosides (control group C). Parallel to the performance of the FM 100, the glycoside plasma level was measured by radioimmunoassay. The total error score (TES) of the FM 100 was correlated with the glycoside plasma level and the patient's age. In the C as well as in the D or P groups up to 172 errors and in the Dg group up to 586 errors were observed. With the exception of Dg, no differences were observed between the regression lines indicating an age-dependent increase in TES even under D or P treatment. In contrast to the two glycosides, Dg enhances the TES in therapeutically relevant plasma concentrations. The differences between the glycosides are due to differences in their volume of distribution and their plasma protein binding.

Topics: Acetyldigoxins; Adolescent; Adult; Aged; Aged, 80 and over; Color Perception; Digitoxin; Digoxin; Discrimination, Psychological; Female; Heart Failure; Humans; Male; Middle Aged

In six volunteers the pharmacokinetics of 16-acetyl-gitoxin (16AG, 0.5 mg) administered intravenously (A1) and as an oral solution (A2) and of pengitoxin (PAG, 0.6 mg) administered intravenously (A3) was evaluated. In six volunteers the bioavailability of 16AG from two PAG tablet formulations (1.2 mg) (B2, B3) was measured by comparison with the absorption after administration of a pengitoxin solution (1.2 mg) (B1). In both studies the test was performed using a crossover design. After a single i.v. injection of equimolar doses, 16AG and PAG showed similar mean kinetic parameters: t1/2 = 51.6 hr (16AG) and 60.8 hr (PAG), CL = 11.7 ml min-1 (16AG) and 12.7 ml min-1 (PAG), CLR = 4.1 ml min-1 (16AG) and 4.2 ml min-1 (PAG). The 16AG was absorbed from solution with a mean half-life of 0.2 hr to an extent of 98.6%. The mean urinary excretion/Ae (0,4)/of 16AG amounted to 24.6% (A1), 20.8% (A2) and 28.1% (A3). On the basis of AUC values, the mean bioavailability of PAG from either tablet formulation amounted to 79.6% (B2) and 89.6% (B3). The pharmacokinetic parameters of 16AG (PAG) are closer to those of digitoxin than those of digoxin. In general, 16AG is characterized as a digitoxin with a digoxin-like elimination half-life.

Topics: Acetyldigoxins; Administration, Oral; Adult; Biological Availability; Digitoxin; Digoxin; Female; Humans; Injections, Intravenous; Kinetics; Male; Tablets

Topics: Acetyldigoxins; Digitalis Glycosides; Digitoxin; Mice; Pharmacology; Rats; Research; Toxicology