Lumiracoxib: Pharmacokinetic and Pharmacodynamic Profile When Coadministered with Fluconazole in Healthy Subjects

Journal of Clinical Pharmacology

Volumn 44, Issue 2, 2004, Pages 193-199

  Scott, Graham ^a   Yih, Linda ^b   Yeh, Ching Ming ^b   Milosavljev, Slavica ^b   Laurent, Aziz ^c   Rordorf, Christiane ^b  

^a Horsham Research Centre   (United Kingdom)

^b NOVARTIS PHARMA AG   (Switzerland)

^c Pharmaceutical Product Development   (United States)

Author keywords

COX 2 inhibitors; Drug interactions; Fluconazole; Lumiracoxib; Pharmacokinetics

Indexed keywords

CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITOR; CYTOCHROME P450 2C9; FLUCONAZOLE; LUMIRACOXIB; THROMBOXANE B2;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG SAFETY; DRUG TOLERABILITY; ENZYME INHIBITION; FEMALE; HEADACHE; HUMAN; MALE; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT;

ADULT; ANTIFUNGAL AGENTS; AREA UNDER CURVE; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; CYCLOOXYGENASE INHIBITORS; DICLOFENAC; DRUG INTERACTIONS; FEMALE; FLUCONAZOLE; HUMANS; ISOENZYMES; MALE; MEMBRANE PROTEINS; ORGANIC CHEMICALS; PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES; THROMBOXANE B2;

EID: 1642477736     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270003262110     Document Type: Article

References (31)

1. FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med 2001;345:433-442.
2. Kulkarni SK, Jain NK, Singh A: Cyclooxygenase isoenzymes and newer therapeutic potential for selective COX-2 inhibitors. Methods Find Exp Clin Pharmacol 2000;22:291-298.
3. Warner TD, Giuliano F, Vojnovic I, Bukasa A, Mitchell JA, Vane JR: Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci USA 1999;96:7563-7568.
4. Goldstein JL, Agrawal NM, Silverstein F, Kaiser J, Burr AM, Verburg KM, et al: Celecoxib is associated with a significantly lower incidence of clinically significant upper gastrointestinal events in osteoarthritis and rheumatoid arthritis patients as compared to NSAIDs [abstract]. Gastroenterology 1999;116:G0758.
5. Sigthorsson G, Crane R, Simon T, Hoover M, Quan H, Bolognese J, Bjarnason T: COX-2 inhibition with rofecoxib does not increase intestinal permeability in healthy subjects: a double blind crossover study comparing rofecoxib with placebo and indomethacin. Gut 2000;47:527-532.
6. Simon LS, Weaver AL, Graham DY, Kivitz AJ, Lipsky PE, Hubbard RC, et al: Anti-inflammatory and upper gastrointestinal effects of celecoxib in rheumatoid arthritis: a randomized controlled trial. JAMA 1999;282:1921-1928.
7. Langman MJ, Jensen DM, Watson DJ, Harper SE, Zhao PL, Quan H, et al: Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs. JAMA 1999;282:1929-1933.
8. Hawkey C, Laine L, Simon T, Beaulieu A, Maldonado-Cocco J, et al: Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: a randomized, double-blind, placebo-controlled trial. The Rofecoxib Osteoarthritis Endoscopy Multinational Study Group. Arthritis Rheum 2000;43:370-377.
9. Marshall PJ, Berry JC, Wasvary J, Van Duzer J, Scott G, Rordorf C, et al: The in vitro and in vivo selectivity of COX189, a new and highly selective inhibitor of COX-2 [abstract SAT0013]. Ann Rheum Dis 2002;61(Suppl. 1):259.
10. Scott G, Rordorf C, Blood P, Branson J, Milosavljev S, Greig G: Dose escalation study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of COX189 in healthy subjects [abstract FRI300]. Ann Rheum Dis 2002;61(Suppl. 1):242.
11. Tannenbaum H, Berenbaum F, Reginster JY, Zacher J, Robinson J, Poor G, et al: Lumiracoxib (Prexige™) is effective in the treatment of osteoarthritis of the knee: a 13-week, placebo-controlled, active-comparator, double-blind study [abstract 487]. Athritis Rheum 2002;46(Suppl. 9):S212.
12. Schnitzer TJ, Geusens P, Hasler P, Patel SK, Poor G, Senftleber I, Scott G: Efficacy and safety of COX189 in osteoarthritis: a multi-national study [abstract S336]. Arthritis Rheum 2000;43(Suppl. 9):1616.
13. Atherton C, Hayer R, Stevenson D, Jones JI, McKaig B, Cunliffe R, et al: No acute gastroduodenal erosive injury in a study of COX-189, a new highly selective COX-2 inhibitor [abstract M1730]. Gastroenterology 2002;122(4, Suppl. 1):A-344.
14. Rordorf C, Kellett N, Mair S, Ford M, Milosavljev S, Branson J, et al: Gastroduodenal tolerability of lumiracoxib vs. placebo and naproxen: a pilot endoscopic study in healthy male subjects. Aliment Pharmacol Ther 2003;18:533-541.
15. Hawkey C: Reduced cumulative incidence of gastroduodenal ulcers with two doses of a new coxib, COX189, compared with standard therapeutic doses of ibuprofen in osteoarthritis patients [abstract WED-G-553]. Gut 2002;51(Suppl. 3):A313.
16. Black DJ, Kunze KL, Wienkers LC, Gidal BE, Seaton TL, McDonnell ND, et al: Warfarin-fluconazole. II. A metabolically based drug interaction: in vivo studies. Drug Metab Dispos 1996;24:422-428.
17. Trapnell CB, Jamis-Dow C, Klecker RW, Collins JM: Metabolism of rifabutin and its 25-desacetyl metabolite, LM565, by human liver microsomes and recombinant human cytochrome P-450 3A4: relevance to clinical interaction with fluconazole. Antimicrob Agents Chemother 1997;41:924-926.
18. Kunze KL, Wienkers LC, Thummel KE, Trager WF: Warfarin-fluconazole. I. Inhibition of the human cytochrome P450-dependent metabolism of warfarin by fluconazole: in vitro studies. Drug Metab Dispos 1996;24:414-421.
19. Kantola T, Backman JT, Niemi M, Kivisto KT, Neuvonen PJ: Effect of fluconazole on plasma fluvastatin and pravastatin concentrations. Eur J Clin Pharmacol 2000;56:225-229.
20. Kaukonen KM, Olkkola KT, Neuvonen PJ: Fluconazole but not itraconazole decreases the metabolism of losartan to E-3174. Eur J Clin Pharmacol 1998;53:445-449.
21. Kunze KL, Trager WF: Warfarin-fluconazole. III. A rational approach to management of a metabolically based drug interaction. Drug Metab Dispos 1996;24:429-435.
22. Morita K, Konishi H, Shimakawa H: Fluconazole: a potent inhibitor of cytochrome P-450-dependent drug-metabolism in mice and humans in vivo. Comparative study with ketoconazole. Chem Pharm Bull (Tokyo) 1992;40:1247-1251.
23. Niemi M, Backman JT, Neuvonen M, Laitila J, Neuvonen PJ, Kivisto KT: Effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride. Clin Pharmacol Ther 2001;69:194-200.
24. Pfizer, Inc.: Diflucan U.S. prescribing information, revised June 1998. Accessed May 30, 2003, from http://www.pfizer.com/down-load/uspi_diflucan.pdf
25. World Medical Association Declaration of Helsinki: Recommendations guiding physicians in biomedical research involving human subjects. JAMA 1997;277:925-926.
26. De Caterina R, Giannessi D, Bernini W, Gazzetti P, Michelassi C, L'Abbate A, et al: Low-dose aspirin in patients recovering from myocardial infarction. Evidence for a selective inhibition of thromboxane-related platelet function. Eur Heart J 1985;6:409-417.
27. Garnett WR: Clinical implications of drug interactions with coxibs. Pharmacotherapy 2001;21:1223-1232.
28. Tang C, Shou M, Mei Q, Rushmore TH, Rodrigues AD: Major role of human liver microsomal cytochrome P450 2C9 (CYP2C9) in the oxidative metabolism of celecoxib, a novel cyclooxygenase-II inhibitor. J Pharmacol Exp Ther 2000;293:453-459.
29. Davies NM, McLachlan AJ, Day RO, Williams KM: Clinical pharmacokinetics and pharmacodynamics of celecoxib: a selective cyclo-oxygenase-2 inhibitor. Clin Pharmacokinet 2000;38:225-242.
30. Pharmacia Corporation: Celebrex U.S. prescribing information, revised August 2002. Accessed May 30, 2003, from http://www.pfizer.com/download/uspi_celebrex.pdf
31. Merck & Co., Inc.: Vioxx U.S. prescribing information, issued April 2002. Accessed May 30, 2003, from http://www.merck.com. product/usa/pi_circulars/v/vioxx/vioxx_pi.pdf