Advertisement

European Journal of Clinical Pharmacology

, Volume 16, Issue 1, pp 39–44 | Cite as

Plasma and urinary levels of triamterene and certain metabolites after oral administration to man

  • U. Gundert-Remy
  • D. von Kenne
  • E. Weber
  • H. E. Geißler
  • B. Grebian
  • E. Mutschler
Originals

Summary

The plasma and urinary levels of triamterene and two metabolites were measured using a specific method of analysis. Urinary excretion was completed after 48 h, which permitted a rough estimate of its half-life as longer than two hours. The areas under the curve were 672.5±160.3 and 1.311.3±399.1 µg/ml × h after the triameterene 150 mg and 300 mg p.o., respectively and correspondingly 4.2±1.4% and 3.7±0.6% of the dose were excreted as unchanged drug. The principal metabolite of triamterene found was the sulfate conjugate. The area under the curve of this metabolite amounted to 6.672±2.120 and 11.941±5.005 µg/ml × h after the of 150 mg and 300 mg triamterene doses, respectively. The urinary excretion of the metabolite varied between 25.0±4.0% and 17.5±3.5% of the dose after either dose. In healthy subjects an effect on sodium excretion was observed after a dose of 150 mg, whereas the potassium-retaining effect was observed only after the dose of 300 mg.

Key words

triamterene pharmacokinetics diuretic effects 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Andrasch, H., Fink, T., Schmid, E.: Über die Harnausscheidung des Antikaliuretikums Triamteren und seines phenolischen Metaboliten 2,4,7-Triamino-6-p-hydroxy-phenylpteridin bei Lebergesunden und Kranken mit Leberzirrhose. Z. Gastroenterol.9, 240–245 (1971)Google Scholar
  2. 2.
    Baba, W. J., Tudhope, G. R., Wilson, G. M.: Triamterene, a new diuretic drug. I. Studies in normal men and in adrenalectomized rats. Br. Med. J.,1962/II, 756–760Google Scholar
  3. 3.
    Badinand, A., Rondelet, J., Vallon, J. J., Chappuis, O.: Étude de l'élimination urinaire et du passage sanguin du Triamtérène. J. Med. (Lyon)1047, 19–26 (1964)Google Scholar
  4. 4.
    Dayton, P. G., Ansley, J., Pruitt, A. W., Winkel, J., Rudman, D.: Impairment of p-hydroxylation of triamterene in patients with cirrhosis. Pharmacologist18, 153 (1976)Google Scholar
  5. 5.
    Dettli, L., Spring, P.: Pharmakologisch-klinische Prüfung neuer Diuretika. Arzneim. Forsch.15, 1162–1168 (1965)Google Scholar
  6. 6.
    Grebian, B., Geißler, H. E., Mutschler, E.: Über die Bestimmung von Triamteren, Hydroxytriamteren und Hydroxy-triamteren-schwefelsäureester in biologischem Material durch direkte Auswertung von Dünnschichtchromatogrammen. Arzneim.-Forsch. (Drug Res.)26, 2125–2127 (1976)Google Scholar
  7. 7.
    Greeff, K., Köhler, E.: Tierexperimentelle Untersuchungen über den Einfluß von Triamteren und Amilord auf Herz, Kreislauf und Toxizität des Digoxins. Arzneim. Forsch. (Drug Res.)25, 1766–1769 (1975)Google Scholar
  8. 8.
    Gundert-Remy, U.: Biliary and renal elimination of 14-C-triamterene in the rat. Naunyn-Schmiedebergs Arch. Pharmacol.297, Suppl. II R 9 (1977)Google Scholar
  9. 9.
    Lassen, J. B., Nielsen, O. E., Investigation into diuretic effect and elimination of triamterene. Acta Pharmacol. Toxicol.20, 309–316 (1963)Google Scholar
  10. 10.
    Lehmann, K.: Isolierung und Identifizierung von Stoffwechselprodukten des Triamteren. Arzneim. Forsch. (Drug Res.)15, 812–816 (1965)Google Scholar
  11. 11.
    Pruitt, A. W., Winkel, J. S., Dayton, P. G.: Variations in the fate of triamteren. Clin. Pharmacol. Ther.21, 610–619 (1977)Google Scholar
  12. 12.
    Seller, R. H., Greco, J., Banach, St., Seth, R.: Increasing the inotropic effect and toxic dose of digitalis by the administration of antikaliuretic drugs — further evidence for a cardiac effect of diuretic agents. Am. Heart J.90, 56–67 (1975)Google Scholar
  13. 13.
    Siegel, S.: Non-parametric statistics, pp. 75–83. New York: McGraw-Hill 1956Google Scholar
  14. 14.
    Heh, B. K., Francis, J. S., Gosselin, A. J., Relias, R. A.: Antiarrhythmic activity of four pteridine compunds in ouabain intoxication. Clin. Pharmacol. Ther.17, 141–145 (1975)Google Scholar
  15. 15.
    Weber, D. J.: Intravenous triamterene in the treatment of acute digitalis intoxication. Clin. Pharmacol. Ther.13, 868–874 (1972)Google Scholar

Copyright information

© Springer-Verlag 1979

Authors and Affiliations

  • U. Gundert-Remy
    • 1
    • 3
  • D. von Kenne
    • 1
  • E. Weber
    • 1
  • H. E. Geißler
    • 2
  • B. Grebian
    • 2
  • E. Mutschler
    • 2
  1. 1.Department of Clinical PharmacologyUniversity of HeidelbergGermany
  2. 2.Pharmacological Institute, Department of Biochemistry and PharmacyUniversity of Frankfurt/MainGermany
  3. 3.Institut für Klinische PharmakologieHeidelbergGermany

Personalised recommendations