The pharmacokinetics of 14C-propiverine was studied in 13 volunteers and in 2 patients after a single i.v. injection of 5 mg or after oral administration of 15 mg. To each dose 1.11 MBq 14C-propiverine was added. The radioactivity measured in plasma, urine (and bile fluid), and the metabolites were estimated by an extraction procedure together with TLC and radiochromatography. Propiverine was eliminated from the plasma with a half-life time (t0.5) of 4.1 h (i.v. and per os), while the plasma radioactivity decreased with a t0.5 of 21.2 (i.v.) or 10.4 h (per os). Within 4 days, 84.5 (i.v.) or 53.5% (per os) of the administered radioactivity was excreted in urine. The absorption of radioactivity of propiverine amounted to 84.5%, while the amount of available propiverine was only 48.9%. In two patients with cannulated ductus choledochus, 21.5 or 14.7% of the administered radioactivity was excreted within 2 days. The metabolic pattern of plasma, urine and bile fluid mainly consisted of amine oxides, substances oxidized in the propyl side chain, desalkylated metabolites, substances with a N-demethylated piperidino group or with ester cleavage, and glucuronide conjugates. Unchanged propiverine appeared in plasma, urine and bile at about 6 to 8% of the administered dose.

Adult↗

PubMedDate not supplied

Differences in color vision impairment caused by digoxin, digitoxin, or pengitoxin.

Color discrimination ability of 53 patients with congestive heart failure and 32 healthy volunteers treated with digoxin, digitoxin, or pengitoxin was determined with the Farnworth's Munsell 100 hue test. The patients had been treated with digitalis glycosides for several months prior to color vision testing. The volunteers received glycosides until a steady-state plasma concentration was reached. Glycoside plasma levels were measured by radioimmunoassay on the 3 days prior to color vision testing. The total error scores, indices of color discrimination, increased with the glycoside plasma levels. Subjects treated with digitoxin or pengitoxin exhibited no marked elevation in total error score at therapeutic concentrations, whereas 17 of 28 subjects with therapeutic digoxin plasma concentrations (less than 2.0 ng/ml) showed disturbed color discrimination. At toxic plasma levels all 5 digoxin-treated subjects, 7 of 13 digitoxin-treated subjects, and 3 of 8 pengitoxin-treated subjects showed impairment of color discrimination. The greater tendency of digoxin to impair color vision in comparison with digitoxin and pengitoxin may be related to a higher uptake or different distribution in the retina.

Acetyldigoxins↗

PubMedDate not supplied

[Clinico-pharmacological and clinical evaluation of pengitoxin].

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Acetyldigoxins↗