Concentration-effect relations of glibenclamide and its active metabolites in man: Modelling of pharmacokinetics and pharmacodynamics

British Journal of Clinical Pharmacology

Volumn 43, Issue 4, 1997, Pages 373-381

  Rydberg, T ^a,b,e   Jonsson A ^b   Karlsson, M O ^c   Melander, A ^d  

^a CENTRAL HOSPITAL   (Sweden)

^b LUND UNIVERSITY   (Sweden)

^c UPPSALA UNIVERSITY   (Sweden)

^d Network for Pharmacoepidemiology Foundation   (Sweden)

^e Apoteksbolaget AB Region Syd   (Sweden)

Author keywords

Diabetes mellitus; Glibenclamide; Glucose; Metabolites; Non insulin dependent; Pharmacodynamic modelling; Pharmacodynamics; Pharmacokinetics; Sulphonylurea

Indexed keywords

DRUG METABOLITE; GLIBENCLAMIDE;

ADULT; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG METABOLISM; FEMALE; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE BLIND PROCEDURE; THEORETICAL STUDY;

EID: 0030947756     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.1997.00571.x     Document Type: Article

References (41)

1. Christ OE, Heptner W, Rupp W. Investigations on absorption, excretion and metabolism in man after administration of 14C-labelled HB 419 Horm Metab Res 1969; 1 (Suppl. 1): 51-54.
2. Peart GF, Boutagy J, Shenfield GM. The metabolism of glyburide in subjects of known debrisoquine phenotype. Clin Pharmacol Ther 1989; 45: 277-284.
3. Ko H, Royer ME, Molony BA. Relationships between circulating glyburide/metabolite concentrations, serum glucose lowering, and dose of glyburide in man. In Micronase: Pharmacological and clinical evaluation, eds Rifkin H, et al., Princeton, NJ, Excerpta Medica Foundation 1975; 20-30 (International Congres Series No. 382).
4. Kaiser DG, Forist AA. A review of glyburide metabolism in man and laboratory animals. In Micronase: Pharmacological and clinical evaluation, eds. Rifkin H, et al., eds. Princeton, NJ, Excerpta Medica Foundation 1975; 31-43 (International Congress Series No. 382).
5. Ferner RE, Alberti KG. Sulphonylureas in the treatment of non-insulin-dependent diabetes. Quart J Med 1989; 73: 987-995.
6. Balant L, Fabre J, Loutan L, Samimi H. Does 4-trans-hydroxy-glibenclamide show hypoclycemic activity? Arzneimittel-Forsch/Drug Res 1979; 29: 162-163.
7. Pearson JG, Antal EJ, Raehl CL. et al Pharmacokinetic disposition of 14C-glyburide in patients with varying renal function. Clin Pharmacol Ther 1986; 39: 318-324.
8. Rydberg T, Jönsson A, Melander A. Comparison of the kinetics of glyburide and its active metabolites in humans. J Clin Pharm Ther 1995; 20: 283-295.
9. Rydberg T, Jönsson A, Røder M, Melander A. Hypoglycemic activity of glyburide (glibenclamide) metabolites in humans. Diabetes Care 1994; 17: 1026-1030.
10. Ferner RE, Antsiferov ML, Kelman AW, Alberti KG, Rawlins MD. The relationships between dose and concentration of tolbutamide and insulin and glucose responses in patients with non-insulin-dependent diabetes. Eur J Clin Pharmacol 1991; 40: 163-168.
11. Beal SL, Sheiner LB (Eds.). NONMEM Users Guides. NONMEM Project Group, University of California at San Francisco, San Francisco. 1992.
12. Holford NH. Concepts and usefulness of pharmacokinetic-pharmacodynamic modelling, Fundam Clin Pharmacol 1990; 4 (Suppl. 2): 93s-101s.
13. van Boxtel CJ, Holford NH, Danhof M. The in vivo study of drug action. 1st ed. Amsterdam: Elsevier Science Publishers B.V., 1992; 1-111.
14. Gabrielsson JL, Weiner DL. Pharmacokinetic and pharmacodynamic data analysis: Concepts and applications. 1st ed. Stockholm: The Swedish Pharmaceutical Press, 1994; 64-87.
15. Sheiner LB, Stuart LB. Evaluation of methods for estimating population pharmacokinetic parameters II. Biexponential model and experimental pharmacokinetic data. J Pharmacokin Biopharm 1981; 9: 635-651.
16. Ette EI, Ludden TM. Population pharmacokinetic modeling: The importance of informative graphics. Pharm Res 1995; 12: 1845-1855.
17. Vozeh S, Steimer J-L, Rowland M, et al. The use of population pharmacokinetics in drug development. Clin Pharmacokinet 1996; 30: 81-93.
18. Rydberg T, Wåhlin-Boll E, Melander A. Determination of glibenclamide and its two major metabolites in human serum and urine by column liquid chromatography. J Chromatogr 1991; 564: 223-233.
19. Andersen L, Dinesen B, Jorgensen PN, Poulsen F, Roder ME. Enzyme immunoassay for intact human insulin in serum or plasma. Clin Chem 1993; 39: 578-582.
20. Kroboth PD, Smith RB, Juhl RP. Pharmacokinetics and pharmacodynamics. Volume 2. Current problems, potential solutions. 1st ed. Cincinnati: Harvey Whitney books company, 1988; 1-89.
21. Lalonde RL, Straka RJ, Pieper JA, Bottorff MB, Mirvis DM. Propranolol pharmacodynamic modeling using unbound and total concentrations in healthy volunteers. J Pharmacokin Biopharm 1987; 15: 569-582.
22. Wagner JG. Kinetics of pharmacologic response. J Theoret Biol 1968; 20: 173-201.
23. Holford NH, Sheiner LB, Understanding the Dose-Effect Relationship: Clinical application of pharmacokinetic-pharmacodynamic models. Clin Pharmacokinet 1981; 6: 429-453.
24. Holford NH, Sheiner LB. Kinetics of pharmacologic response. Pharmac Ther 1982; 16: 143-166.
25. Reiter MJ, Shand DG, Pritchett EL. Comparison of intravenous and oral verapamil dosing. Clin Pharmacol Ther 1982; 32: 711-720.
26. Sheiner LB, Stanski DR, Vozeh S, Miller RD, Ham J. Simultaneous modeling of pharmacokinetics and pharmacodynamics: Application to d-tubocurarine. Clin Pharmacol Ther 1979; 25: 358-371.
27. Colburn WA. Simultaneous pharmacokinetic and pharmacodynamic modeling. J Pharmacokin Biopharm 1981; 9: 367-388.
28. Unadkat JD, Bartha F, Sheiner LB. Simultaneous modeling of pharmacokinetics and pharmacodynamics with nonparametric kinetic and dynamic models. Clin Pharmacol Ther 1986; 40: 86-93.
29. Whiting B, Holford NH, Sheiner LB. Quantitative analysis of the disopyramide concentration-effect relationship. Br J Clin Pharmacol 1980; 9: 67-75.
30. Colburn WA, Brazzell RK, Holazo AA. Verapamil pharmacodynamics after intravenous and oral dosing: Theoretic consideration. J Clin Pharmacol 1986; 26: 71-73.
31. Holazo AA, Brazzell RK, Colburn WA. Pharmacokinetic and pharmacodynamic modeling of cibenzoline plasma concentrations and antiarrhythmic effect. J Clin Pharmacol 1986; 26: 336-345.
32. Brown SA, Nelson RW, Bottoms GD. Models for the pharmacokinetics and pharmacodynamics of insulin in alloxan-induced diabetic dogs. J Pharm Sci 1987; 76: 295-299.
33. Jonsson EN, Karlsson MO. Manual for Xpose version 1.1. 1996. Internet: http://www.biof.uu.se/Xpose.
34. Statistical Sciences, Inc. S-PLUS Reference Manual, version 3.3, Seattle: StatSci, a division of Mathsoft, Inc., 1993.
35. van Boxtel CJ, Holford NH, Danhof M. The in vivo study of drug action, 1th ed. Amsterdam: Elsevier Science Publishers B.V., 1992; 97-101.
36. Schwinghammer T, Antal EJ, Kubacka RT, Hackimer ME, Johnston JM. Pharmacokinetics and pharmacodynamics of glyburide in young and elderly nondiabetic adults, Clin Pharm 1991; 10: 532-538.
37. Jönsson A, Rydberg T, Ekberg G, Hallengren B, Melander A. Slow elimination of glyburide in NIDDM subjects. Diabetes Care 1994; 17: 142-145.
38. Balant L, Zahnd GR, Weber F, Fabre J. Behaviour of glibenclamide on repeated administration to diabetic patients. Eur J Clin Pharmacol 1977; 11: 19-25.
39. Jaber LA, Antal EJ, Slaughter RL, Welshman IR. The pharmacokinetics and pharmacodynamics of 12 weeks of glyburide therapy in obese diabetes. Eur J Clin Pharmacol 1993; 45: 459-463.
40. Jaber LA, Antal EJ, Slaughter RL, Welshman IR. Comparison of pharmacokinetics and pharmacodynamics of short- and long-term glyburide therapy in NIDDM. Diabetes Care 1994; 11: 1300-1306.
41. Groop LC, Barzilai N, Ratheiser K, et al. Dose-dependent effects of glyburide on insulin secretion and glucose uptake in humans. Diabetes Care 1991; 14: 724-727.