Skip to main content
SpringerLink
Log in

Comparison of the pharmacokinetics of glipizide and glibenclamide in man

  • Originals
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Summary

Four subjects received 5 mg14C-glipizide orally, 3 subjects 1 mg intravenously and 2 subjects 5 mg14C-glibenclamide orally. Plasma levels of radioactivity, and urinary and faecal excretion were measured. For both drugs the disappearance of radioactivity from plasma followed complex kinetics and the apparent half-lives increased steadily with time. The two sulfonylureas were extensively metabolized and were excreted in the urine as hydroxylated or conjugated metabolites. The effects of both drugs on blood glucose and immunoreactive insulin were comparable. The findings are compared with other published results.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Schmidt, H.A.E., Petrides, P.: Glukose- und HB-419-Konzentration im Blut sowie HB 419-Ausscheidung im Urin nach einmaliger oraler Applikation von HB 419 -14C. Arzneimittel-Forsch.19 1422 - 1428 (1969)

    Google Scholar 

  2. Rupp, W., Christ, O., Heptner, W.: Resorption, Ausscheidung und Metabolismus nach intra-venöser und oraler Gabe von HB 419 -14C an Menschen. Arzneimittel-Forsch.19 1428–1434 (1969)

    Google Scholar 

  3. Anderson, J., Stephenson, R.J., Tomlinson, R.W.S., Weinberg, A.L.: Studies with14C-labelled glibenclamide. Postgrad. med. J.46 (Dec. Suppl.), 42–45 (1970)

    Google Scholar 

  4. Rupp, W., Christ, O., Fülberth, W.: Unter-suchungen zur Bioavailability von Glibenclamid. Arzneimittel-Forsch.22 471–473 (1972)

    Google Scholar 

  5. Fucella, L.M., Tamassia, V., Valzelli, G.: Metabolism and kinetics of the hypoglycemic agent glipizide. Comparison with glibenclamide. J. clin. Pharmacol.13 68–75 (1973)

    Google Scholar 

  6. Ambrogi, V., Artini, D., Fucella, L.M., Goldaniga, G., Orsini, G., Ronchi, R., Tamassia, V., Valzelli, G., Angelucci, R.: Farmacocinetica e metabolismo in animali da esperimento e nell'uomo della N-{4-[β-(5-metilpirazina-2-carbossiamido)-etil]-benzensolfonil}-N'-cicloesil-urea (K 4024) Boll. chim. farm.3 251–264 (1972)

    Google Scholar 

  7. Taylor, J.A.: K 4024 (Glydiazinamide). I. Pharmacokinetic studies in man. Pfizer Inc. Groton, Conneticut, Internal communication

  8. Schmidt, H.A.E., Schoog, M., Schweer, K.H., Winkler, E.: Pharmacokinetics and pharmacodynamics as well as metabolism following orally and intravenously administered C14-glipizide, a new antidiabetic. Diabetologia9 (Suppl.) 320–330 (1973)

    Google Scholar 

  9. Balant, L., Zahnd, G., Gorgia, A., Schwarz, R., Fabre, J.: Pharmacokinetics of glipizide in man: influence of renal insufficiency. Diabetologia9 (Suppl.) 331–338 (1973)

    Google Scholar 

  10. Zender, R.: Une micromethode automatique pour l'analyse quantitative des aldohexoses dans les liquides biologiques par l'o-toluidine. Clin. chim. Acta8 351–358 (1963)

    Google Scholar 

  11. Hales, C.N., Randle, P.Y.: Immunoassay of insulin with insulin-antibody precipitate. Biochem. J.88 137–146 (1963)

    Google Scholar 

  12. Dost, F.H.: Grundlagen der Pharmakokinetik. Stuttgart: Georg Thieme Verlag 1968

    Google Scholar 

  13. Heptner, W., Kellner, H.N., Christ, O., Weihrauch, D.: Metabolismus von HB 419 im Tier. Arzneimittel-Forsch.19 1400–1404 (1969)

    Google Scholar 

  14. Dettli, L.: Dosierungstheorie für die repetierte Applikation reversibel wirkender Pharmaka bei Eliminationsinsuffizienz. In: Pharmacological and clinical significance of pharmacokinetics, pp. 31–41, Stuttgart: F.K. Schattauer Verlag 1970

    Google Scholar 

  15. Garrett, E.R.: The clinical significance of pharmacokinetics. In: Pharmacological and clinical significance of pharmacokinetics, pp. 5–21. Stuttgart: F.K. Schattauer Verlag 1970

    Google Scholar 

  16. Doluisio, J.T., Dittert, L.W.: Influence of repetitive dosing of tetracyclines on biological half-life in serum. Clin. Pharmacol. Ther.10 690–701 (1969)

    Google Scholar 

  17. Fabre, J., Kunz, J.P., Virieuy, C., Laurencet, J.L., Pitton J.S.: Le comportement de la doxycycline chez l'homme. Chemotherapy13 (Suppl.) 23–40 (1968)

    Google Scholar 

  18. Gibaldi, M.: Pharmacokinetic aspects of drug metabolism. Ann. N.Y. Acad. Sci.179 19–31 (1971)

    Google Scholar 

  19. Schmidt, F.H., Hrstka, V.E.: Radio-immunoassay of glibenclamide: minimum effective dose levels and pharmacodynamics. XIIeCongrès International de Thérapeutique, Genève 1973

  20. Fabre, J., Balant, L., Zahnd, G.: Pharmacocinétique des nouvelles sulfonylurées dans les conditions normales et pathologiques. XIIeCongrès International de Thérapeutique, Genève 1973

  21. Schulz, E., Koch, K., Schmidt, F.H.: Ursachen der Potenzierung der hypoglykämischen Wirkung von Sulfonylharnstoff-Derivaten durch Medikamente. II. Pharmakokinetik und Metabolismus von Glibenclamid (HB 419) in Gegenwart von Phenylbutazon. Europ. J. clin. Pharmacol.4 32–37 (1971)

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Policlinique de Médecine et Division de Diabétologie et de Biochimie Clinique, Département de Médecine, Université de Genève, Switzerland

    L. Balant, J. Fabre & G. R. Zahnd

Authors
  1. L. Balant
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. J. Fabre
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. G. R. Zahnd
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Balant, L., Fabre, J. & Zahnd, G.R. Comparison of the pharmacokinetics of glipizide and glibenclamide in man. Eur J Clin Pharmacol 8, 63–69 (1975). https://doi.org/10.1007/BF00616416

Download citation

  • Received:

  • Revised:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00616416

Key words

Search

Navigation