Summary
The plasma concentration of proscillaridin was measured by a modified86Rd method during treatment with multiple doses of a commercial preparation of proscillaridin. Despite high doses, very low plasma levels were found, and there were only minute amounts of glycoside activity in urine and faeces. Administration of an enteric-coated proscillaridin preparation gave higher plasma levels, which raises the possibility of inactivation of the glycoside by acid gastric juice. The results suggest that proscillaridin has low biological availability when given orally, and that it is extensively metabolised in the body.
Similar content being viewed by others
References
Andersson, K.-E., Bertler, A., Redfors, A.: In vitro stability of proscillaridin A. Europ. J. clin. Pharmacol.8 135–139 (1975a)
Andersson, K.-E., Bergdahl, B., Bertler, A., Redfors, A.: Plasma and urine activities after single oral doses of proscillaridin A. In preparation 1975b
Belz, G.G.: Klinisch-experimentelle Untersuchungen mit dem Herzglykosid Proscillaridin unter besonderer Berücksichtigung seiner enteralen Resorptionsquote. Med. Klin.63 96–102 (1968)
Belz, G.G., Stauch, M., Rudolfsky, G.: Plasma levels after a single dose of proscillaridin. Europ. J. clin. Pharmacol.7 95–97 (1974)
Bertler, A., Redfors, A.: An improved method of estimation digoxin in human plasma. Clin. Pharmacol. Ther.11 665–673 (1970)
Butzengeiger, K.H., Graeber, U., Lange, J., Schumacher, R.: Therapeutische Prüfung von Proscillaridin A. Dtsch. med. Wschr.92 2212–2214, 2217 (1967)
Doherty, J.E., Perkins, W.H.: Studies with tritiated digoxin in human subjects after intravenous administration. Amer. Heart J.63 528–536 (1962)
Hansel, J.: Klinische Untersuchungen mit dem neuen Herzglykosid Proscillaridin A (Sandoscill®). Med. Klin.63 919–922 (1968)
Hänel, J., Meiffert, G.: Klinisch-experimentelle Studie zur Charakterisierung eines Herzglykosids. Med. Welt26 1404–1408 (1966)
Löschhorn, N.: Probleme der quantitativen Prüfung von Herzglykosiden, dargestellt an Proscillaridin. Therapiewoche19 1529 (1969)
Meier, G., Wagner, G.: Therapeutische Erfahrungen mit einem neuen Herzglykosid: Proscillaridin A. Med. Welt35 1995–2002 (1965)
Redfors, A.: Plasma digoxin concentrations — its relation to digoxin dosage and clinical effects in patients with atrial fibrillation. Brit. Heart J.34 383–391 (1972)
Redfors, A., Bertler, A.: Estimation of plasma digoxin and its diagnostic use in suspected digitalis induced arrhythmias. Symposium on Cardiac Arrhythmias, pp. 601–612. (Eds. Sandøe, E., Flensted-Jensen, E., Olesen, K.H.). Denmark: Elsinore 1970
Repke, K.: Metabolism of cardiac glycosides. Proc. First Int. Pharmacological Meeting, Vol. 3, pp. 47–73, New Pergamon Press 1963
Smith, T.W., Haber, E.: Digitalis. Clinical value of the radioimmunoassay of the digitalis glycosides. Pharmacol. Rev.25 219–228 (1973)
Smith, T.W., Butler, V.P., Haber, E.: Determination of therapeutic and toxic serum digoxin concentrations by radioimmunoassay. New Engl. J. Med.281 1212–1216 (1969)
Wülfing von der Heyden, D.: Beitrag zur quantitativen und qualitativen Prüfung des Reinglykosids Proscillaridin. Med. Welt13 738–743 (1969)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Andersson, K.E., Bertler, Å. & Redfors, A. On the pharmacokinetics of proscillaridin A in man. Eur J Clin Pharmacol 8, 421–425 (1975). https://doi.org/10.1007/BF00562316
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00562316