Diabetologia

, Volume 18, Issue 1, pp 17–22

Serum glibenclamide in diabetic patients, and influence of food on the kinetics and effects of glibenclamide

  • G. Sartor
  • A. Melander
  • B. Scherstén
  • E. Wåhlin-Boll
Originals

DOI: 10.1007/BF01228296

Cite this article as:
Sartor, G., Melander, A., Scherstén, B. et al. Diabetologia (1980) 18: 17. doi:10.1007/BF01228296

Summary

The steady state concentrations of glibenclamide in serum were measured radioimmunologically in 37 diabetic patients after administration for at least a year. No other antidiabetic drugs had been given. The interindividual variation in glibenclamide concentrations was extremely large (0 to 1520 nmol/l), greatly exceeding the variation in dosage (2.5–25 mg daily). There was no relation between dose and serum concentration of glibenclamide. Only four (9%) patients had fasting blood glucose concentrations below 5.5 mmol/l, and fewer than half had values below 8 mmol/l. In most cases, therefore, the therapy was inadequate. Single-dose kinetics of glibenclamide was assessed in healthy volunteers. Food intake did not influence the bioavailability of a 5 mg dose of glibenclamide. There was no insulin increase in response to glibenclamide unless a meal was also given, and this increase was not significant until 1 h after administration of drug and meal, when the mean serum concentration of glibenclamide had reached 100nmol/l. Even in the fasting state, however, there was a progressive fall in blood glucose after glibenclamide administration, significant within 45 min and with a nadir at 2–2 1/2 h.

Key words

Diabetes mellitus sulphonylurea glibenclamide steady state levels bioavailability food intake plasma insulin blood glucose 

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Copyright information

© Springer-Verlag 1980

Authors and Affiliations

  • G. Sartor
    • 1
    • 2
    • 3
    • 4
  • A. Melander
    • 1
    • 2
    • 3
    • 4
  • B. Scherstén
    • 1
    • 2
    • 3
    • 4
  • E. Wåhlin-Boll
    • 1
    • 2
    • 3
    • 4
  1. 1.University of LundSweden
  2. 2.Department of MedicineLund University HospitalLundSweden
  3. 3.Department of Clinical PharmacologyMalmö General HospitalMalmöSweden
  4. 4.Department of Community Care SciencesDalbySweden

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