Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide

European Journal of Clinical Pharmacology

Volumn 62, Issue 3, 2006, Pages 217-223

  Kajosaari, Lauri I ^a   Jaakkola, Tiina ^a   Neuvonen, Pertti J ^a   Backman, Janne T ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

Author keywords

CYP2C8; CYP3A4; Drug interaction; Pioglitazone; Repaglinide

Indexed keywords

AMODIAQUINE; ANTIDIABETIC AGENT; CLARITHROMYCIN; CYCLOSPORIN; CYTOCHROME P450 2C8; CYTOCHROME P450 3A4; ETHINYLESTRADIOL; GEMFIBROZIL; GLIBENCLAMIDE; GLIPIZIDE; GLUCOSE; ITRACONAZOLE; NORETHISTERONE; PACLITAXEL; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PIOGLITAZONE; PLACEBO; REPAGLINIDE; SIMVASTATIN; TOLBUTAMIDE; TRIMETHOPRIM; WARFARIN;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENTIATION; DRUG PROTEIN BINDING; FEMALE; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN EXPERIMENT; MALE; NON INSULIN DEPENDENT DIABETES MELLITUS; NORMAL HUMAN; PHARMACODYNAMICS; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; ARYL HYDROCARBON HYDROXYLASES; BLOOD GLUCOSE; CAPSULES; CARBAMATES; CHROMATOGRAPHY, LIQUID; CROSS-OVER STUDIES; CYTOCHROME P-450 ENZYME SYSTEM; DRUG ADMINISTRATION SCHEDULE; ENZYME INHIBITORS; FEMALE; GAS CHROMATOGRAPHY-MASS SPECTROMETRY; HALF-LIFE; HUMANS; HYPOGLYCEMIC AGENTS; MALE; PIPERIDINES; SUBSTRATE SPECIFICITY; THIAZOLIDINEDIONES;

EID: 33644817278     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00228-005-0093-8     Document Type: Article

References (28)

1. Chilcott J, Tappenden P, Jones ML, Wight JP (2001) A systematic review of the clinical effectiveness of pioglitazone in the treatment of type 2 diabetes mellitus. Clin Ther 23:1792-1823; discussion 1791
2. Sahi J, Black CB, Hamilton GA, Zheng X, Jolley S, Rose KA, Gilbert D, LeCluyse EL, Sinz MW (2003) Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition. Drug Metab Dispos 31:439-446
3. Walsky RL, Gaman EA, Obach RS (2005) Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol 45:68-78
4. Gromada J, Dissing S, Kofod H, Frøkjaer-Jensen J (1995) Effects of the hypoglycaemic drugs repaglinide and glibenclamide on ATP-sensitive potassium-channels and cytosolic calcium levels in beta TC3 cells and rat pancreatic beta cells. Diabetologia 38:1025-1032
5. Hatorp V, Oliver S, Su CA (1998) Bioavailability of repaglinide, a novel antidiabetic agent, administered orally in tablet or solution form or intravenously in healthy male volunteers. Int J Clin Pharmacol Ther 36:636-641
6. Hatorp V (2002) Clinical pharmacokinetics and pharmacodynamics of repaglinide. Clin Pharmacokinet 41:471-483
7. Bidstrup TB, Bjørnsdottir I, Sidelmann UG, Thomsen MS, Hansen KT (2003) CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol 56:305-314
8. Niemi M, Leathart JB, Neuvonen M, Backman JT, Daly AK, Neuvonen PJ (2003) Polymorphism in CYP2C8 is associated with reduced plasma concentrations of repaglinide. Clin Pharmacol Ther 74:380-387
9. Niemi M, Backman JT, Kajosaari LI, Leathart JB, Neuvonen M, Daly AK, Eichelbaum M, Kivistö KT, Neuvonen PJ (2005) Polymorphic organic anion transporting polypeptide 1B1 (OATP1B1) is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther 77:468-478
10. van Heiningen PN, Hatorp V, Kramer Nielsen K, Hansen KT, van Lier JJ, De Merbel NC, Oosterhuis B, Jonkman JH (1999) Absorption, metabolism and excretion of a single oral dose of (14)C-repaglinide during repaglinide multiple dosing. Eur J Clin Pharmacol 55:521-525
11. Niemi M, Kajosaari LI, Neuvonen M, Backman JT, Neuvonen PJ (2004) The CYP2C8 inhibitor trimethoprim increases the plasma concentrations of repaglinide in healthy subjects. Br J Clin Pharmacol 57:441-447
12. Niemi M, Neuvonen PJ, Kivistö KT (2001) The cytochrome P4503A4 inhibitor clarithromycin increases the plasma concentrations and effects of repaglinide. Clin Pharmacol Ther 70:58-65
13. Niemi M, Backman JT, Neuvonen M, Neuvonen PJ (2003) Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics and pharmacodynamics of repaglinide: potentially hazardous interaction between gemfibrozil and repaglinide. Diabetologia 46:347-351
14. Kajosaari LI, Niemi M, Neuvonen M, Laitila J, Neuvonen PJ, Backman JT (2005) Cyclosporine markedly raises the plasma concentrations of repaglinide. Clin Pharmacol Ther 78:388-399
15. Jovanovic L, Hassman DR, Gooch B, Jain R, Greco S, Khutoryansky N, Hale PM (2004) Treatment of type 2 diabetes with a combination regimen of repaglinide plus pioglitazone. Diabetes Res Clin Pract 63:127-134
16. Jaakkola T, Backman JT, Neuvonen M, Neuvonen PJ (2005) Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics of pioglitazone. Clin Pharmacol Ther 77:404-414
17. The Diabetes Control and Complications Trial Research Group (1995) The relationship of glycemic exposure (HbA1c) to the risk of development and progression of retinopathy in the diabetes control and complications trial. Diabetes 44:968-983
18. Kajosaari LI, Laitila J, Neuvonen PJ, Backman JT (2005) Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. Basic Clin Pharmacol Toxicol 97:249-256
19. Eckland DA, Danhof M (2000) Clinical pharmacokinetics of pioglitazone. Exp Clin Endocrinol Diabetes 108(Suppl 2):234-242
20. EMEA (2003) Actos scientific discussion [cited 2005 Aug 30]. Available from: URL: http://www.emea.eu.int
21. Hanefeld M (2001) Pharmacokinetics and clinical efficacy of pioglitazone. Int J Clin Pract 121(Suppl):19-25
22. Yamazaki H, Suzuki M, Tane K, Shimada N, Nakajima M, Yokoi T (2000) In vitro inhibitory effects of troglitazone and its metabolites on drug oxidation activities of human cytochrome P450 enzymes: comparison with pioglitazone and rosiglitazone. Xenobiotica 30:61-70
23. Walsky RL, Obach RS, Gaman EA, Gleeson JP, Proctor WR (2005) Selective inhibition of human cytochrome P4502C8 by montelukast. Drug Metab Dispos 33:413-418
24. Wen X, Wang JS, Backman JT, Laitila J, Neuvonen PJ (2002) Trimethoprim and sulfamethoxazole are selective inhibitors of CYP2C8 and CYP2C9, respectively. Drug Metab Dispos 30:631-635
25. Carey R, Liu Y (2000) Pioglitazone does not markedly alter oral contraceptive or hormone replacement pharmacokinetics. Diabetes 49 (Suppl 1):A340-A341
26. Gillies PS, Dunn CJ (2000) Pioglitazone. Drugs 60:333-343; discussion 344-335
27. Hatorp V, Huang WC, Strange P (1999) Repaglinide pharmacokinetics in healthy young adult and elderly subjects. Clin Ther 21:702-710
28. Lin JH, Lu AY (1997) Role of pharmacokinetics and metabolism in drug discovery and development. Pharmacol Rev 49:403-449