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Results for “Proscillaridin”

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At least 37 records · Page 2Linked to original sources

PubMed1979

Disposition rate of proscillaridin A in man after multiple oral doses.

After multiple oral doses, the disposition rate constant (beta) of proscillaridin was studied in 4 young healthy volunteers and 33 elderly patients with congestive heart failure. Glycoside activity in plasma was assayed by the 86Rb-technique. In the volunteers the beta averaged 0.0299 corresponding to a half-life (t 1/2) of 23 h. beta could be determined in 24 patients and was 0.0139 +/- 0.0077 (mean +/- SD). The SD of beta due to biological factors was estimated to be 0.0072. The total variation of beta was 10fold. The mean beta corresponded to a t 1/2 of 49 h with a range from 19 to 209 h. It is concluded that the great variation of beta means difficulty in obtaining adequate plasma levels of proscillaridin and that a rapid elimination of the glycoside cannot be presumed.

Administration, Oral↗

PubMed1976

[Enteral availability and therapeutic activity of proscillaridin-4'-methyl ether (author's transl)].

20 cardiac patients with the clinical and radiological signs of heart failure were treated alternately intravenously and orally with proscillaridin-4'-methyl ether in a 2-period change-over procedure. With medium rate full saturation a steady state was maintained under observation of electrocardiographic parameters. The maintenance dose was determined to be 1.00 mg intravenously and 1.71 mg orally. Thus, relative enteral availability was 60%. In 70% of patients cardiac recompensation could be reached only by treatment with proscillaridin-4'-methyl ether. In 9 of 20 patients undesirable side effects consisted of laxative effects.

Administration, Oral↗

PubMed1976

Pharmacokinetics and pharmacodynamics of methyl proscillaridin in healthy man.

The aim of this study was to obtain data about the pharmacological properties of a new glycoside derivative in man. Plasma concentrations and ECG parameters were measured after oral and intravenous administration of a single dose of 1.2 mg methyl proscillaridin in 16 healthy volunteers, using a strictly randomized, two-period change-over design. Glycoside concentrations were measured using a modified 86Rb-erythrocyte-assay. QT-duration, corrected for frequency (QTc), was the principal variable measured in the ECG. By either route, there was a maximum plasma level after 1 hour, which had decreased to a minimum at 3 hours, followed by a second peak at 4 to 10 hours (orally greater than iv). From 10 to 72 hours the concentrations decreased with a median t 1/2 of 23.3 hours (iv) and 33.0 hours (orally). Comparison of the ratio of plasma concentrations following oral and iv administration resulted in a bioavailability of 69% using the 48 hour plasma levels, and 59% using the areas under the concentration-time curves. The mean QTc was maximally shortened to 28 msec at 1 hour after iv and to 19 msec at 10 hours after the oral dose. A distinct similarity between time-concentration and time-QTc curves was seen after the initial distribution phase, both after oral and intravenous administration. The new derivative shows a rapid elimination. Its bioavailability is reasonably high.

Administration, Oral↗

PubMed1992

Studies on cardiac ingredients of plants. IX. Chemical transformation of proscillaridin by utilizing its 1,4-cycloadducts as key compounds and biological activities of their derivatives.

Three aromatic compounds (2-4) possessing a carbomethoxyl group or a dimethoxyphthaloyl group, prepared by the Diels-Alder reaction of the cardiac glycoside, proscillaridin (1), with dimethyl acetylenedicarboxylate and methyl propiolate, were transformed into alcohols, carboxylic acids and amides. The biological activities of the resulting derivatives were evaluated by the use of Na+, K(+)-adenosine triphosphatase (Na+,K(+)-ATPase) from dog kidney and isolated guinea-pig papillary muscle. Although the biological activities of the resulting derivatives were less potent than that of 1, a para-substituted benzylalcohol (5), methylbenzamides (9a and 10a), and ethylbenzamides (9b and 10b) inhibited the activity of Na+,K(+)-ATPase almost as potently as naturally occurring cardiac glycosides such as digoxin and digitoxin.

Animals↗

PubMed1976

Plasma concentrations during repeated intravenous and oral methyl-proscillaridin application in man.

The aim of this study was to establish data on the plasma levels of the glycoside derivative methyl-proscillaridin (MP) following repeated intravenous and oral doses. The study was carried out on healthy male volunteers. Each received 0.5 mg of MP daily at 8 a.m. for 7 days. 6 volunteers received the drug i.v., 6 p.o. as tablets and 5 p.o. as elixir. Plasma glycoside concentrations were measured utilizing a 86Rb-erythrocyte assay. The mean plasma concentrations on the 6th and 7th days of application were: 752.9 (Sx = 303.5) pg/ml for the i.v. route, 432.9 (Sx = 115.5) pg/ml for the tablets and 473.1 (Sx = 321.5) pg/ml for the elixir. The mean ratio between plasma concentrations with tablets and i.v. injection averaged 63%. It is concluded that the therapeutic activity of oral MP is about 60 to 70% that of the i.v. application.

Administration, Oral↗

PubMed1976

[Trial of a combination of proscillaridin A, thioridazine and Cori ester in the ambulatory treatment of some cardiopathies, especially senile types].

The effect of an association of proscillaridin A, thioridazine and Cori ester in ambulatory management of certain heart diseases, particularly in aged subjects, was assessed. Satisfactory results were observed in 58.3% of cases, with significant improvement of cardiac erethism, psychomotor instability and sleep disturbances, as well as cardiac frequency and signs of myocardial insufficiency. It is felt that the association is of assistance in the treatment of certain heart diseases unaccompanied by frank signs of insufficiency, especially in aged subjects.

Aged↗

PubMed1977

[Effect of proscillaridin-4'-methylether on pressure rise velocity in the left ventricle of patients with coronary heart disease (author's transl)].

In a randomized, controlled, double-blind study 2 groups of 7 patients each with coronary heart disease received either 1 mg methylproscillaridin (MP) a cardiac glycoside of the squill intravenously, or placebo to test the inotropic effect of MP. Pressures and dp/dt max were measured in the left ventricle before and after coronary angiography after an average of 62 min (60 to 70 min). There was a significant (p less than 0.05) increase of dp/dt max in the MP-group (Wilcoxon-Mann-Whitney test). Left ventricular enddiastolic pressure was decreased from 16.1 to 13.6 mm Hg in the MP-group, and increased in theplacebo group from 12 to 13.7 mm Hg (mean values). Thus, a positive inotropic effect of the glycoside may be assumed.

Angiography↗

PubMed1997