Pharmacokinetics, COX-2 specificity, and tolerability of supratherapeutic doses of rofecoxib in humans

European Journal of Clinical Pharmacology

Volumn 56, Issue 2, 2000, Pages 167-174

  Depre M ^a   Ehrich, E ^b   Van Hecken, A ^a   De Lepeleire, I ^b   Dallob, A ^b   Wong, P ^b   Porras, A ^b   Gertz, B J ^b   De Schepper, P J ^a  

^a UNIVERSITY HOSPITALS LEUVEN   (Belgium)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

COX 2 specificity; Pharmacokinetics; Rofecoxib

Indexed keywords

CYCLOOXYGENASE 1; CYCLOOXYGENASE 1 INHIBITOR; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITOR; IBUPROFEN; PLACEBO; PROSTAGLANDIN E2; ROFECOXIB; THROMBOXANE B2;

ADULT; ANALGESIA; ARTICLE; CLINICAL ARTICLE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; DRUG STRUCTURE; DRUG TOLERABILITY; ENZYME ACTIVITY; HUMAN; MALE; PRIORITY JOURNAL; PROSTAGLANDIN SYNTHESIS;

EID: 0034040719     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002280050736     Document Type: Article

References (27)

1. 1. Smith WL, Marnett LJ, Dewit DL (1991) Prostaglandin and thromboxane biosynthesis. Pharmacol Ther 49: 153-179
2. 2. Hla T, Neilson K (1992) Human cyclooxygenase-2 cDNA. Proc Natl Acad Sci USA 89: 7384-7388
3. 3. Holtzman MJ, Turk J, Shornick LP (1992) Identification of a pharmacologically distinct prostaglandin H synthase in cultured epithelial cells. J Biol Chem 267: 21438-21445
4. 4. Vane JR, Bakhe YS, Botting RM (1998) Cyclooxygenase 1 and 2. Annu Rev Pharmacol Toxicol 38: 97-120
5. 5. Seibert WW, Zhang Y, Leahy K, Hauser S, Masferrer J, Isakson P (1997) Distribution of COX-1 and COX-2 in normal and inflamed tissues. Adv Exp Med Biol 400A: 167-170
6. 6. Bjorkman DJ (1998) The effect of aspirin and nonsteroidal anti-inflammatory drugs on prostaglandins. Am J Med 105[suppl 1B]: 8S-12S
7. 7. Cryer B, Feldman M (1998) Cyclooxygenase-1 and cyclooxygenase-2. Selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med 104: 413-421
8. 8. Fenner H (1997) Differentiating among nonsteroidal anti-inflammatory drugs by pharmacokinetic and pharmacodynamic profiles. Semin Arthritis Rheum 26[suppl 1]: 28-33
9. 9. Vane JR, Botting RM (1997) Mechanism of action of aspirin-like drugs. Semin Arthritis Rheum 26[suppl 1]: 2-10
10. 10. Botten WW (1998) Scientific rationale for specific inhibition of COX-2. J Rheumatol 51: 2-7
11. 11. Vane JR (1994) Towards a better aspirin. Nature 367: 215-216
12. 12. Chan CC, Boyce S, Brideau C, Charleson S, Cromlish W, Ethier D, Evans J, Ford-Hutchinson AW, Forrest MJ, Gauthier JY, Gordon R, Gresser M, Guay J, Kargman S, Kennedy B, Leblanc Y, Leger S, Mancini J, O'Neill GP, Ouellet M, Patrick D, Percival MD, Perrier H, Prasit P, Rodger I, Tagari P, Therien M, Vickers P, Visco D, Wang Z, Webb J, Wong E, Xu LJ, Young RN, Zamboni R, Riendeau D (1999) Rofecoxib (VioxxTM, MK-0966, 4-(4′-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone): a potent, selective, and orally active cyclooxygenase-2 inhibitor - pharmacological and biochemical profiles. J Pharmacol Exp Ther 290: 551-560
13. 2 production in healthy subjects. Thromb Res 17: 317-327
14. 14. Brideau C, Kargman S, Liu S, Dallob A, Ehrich E, Rodger I, Chan C (1996) A human whole blood assay for the clinical evaluation of biochemical efficacy of cyclooxygenase inhibitors. Inflamm Res 45: 68-74
15. 2 production. Inflamm Res 45: 246-253
16. 16. Patrignani P, Panara MR, Greco A, Fusco O, Natoli C, Iacobelli S, Cipollone J, Ganci A, Créminon C, Maclouf J, Patrono C (1994) Biochemical and pharmacological characterization of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases. J Pharmacol Exp Ther 271: 1705-1712
17. 17 Ehrich E, Dallob A, De Lepeleire I, Van Hecken A, Riendeau D, Yuan W, Porras A, Wittreich J, Seibold J, De Schepper PJ, Mehlisch D, Gertz B (1999) Characterization of rofecoxib as a cyclooxygenase-2 isoform inhibitor and demonstration of analgesia in the dental pain model. Clin Pharmacol Ther 65: 336-347
18. 18. Cannon G, Caldwell J, Holt P, Mclean B, Zeng Q, Ehrich E, Seidenberg B, Bolognese J, Daniels B (1998) MK-0966, A specific COX-2 inhibitor, has clinical efficacy comparable to diclofenac in the treatment of knee and hip osteoarthritis in a 26-week controlled clinical trial (abstract 983). Arthritis Rheum 41[suppl]: 196
19. 19. Saag K, Fisher C, McKay J, Ehrich E, Zhao PL, Seidenberg B, Bolognese J, Daniels B (1998) MK-0966, A specific COX-2 inhibitor, has clinical efficacy comparable to diclofenac in the treatment of knee and hip osteoarthritis in a 6-week controlled clinical trial (abstract 984). Arthritis Rheum 41[suppl]: 196
20. 20. Ged C, Rouillon JM, Pichard L, Combalbert J, Bressot N, Borres P, Michel H, Beaune P, Maurel P (1989) The increase in urinary excretion of 6 β-hydroxycortisol as a marker of human hepatic cytochrome P450IIIA induction. Br J Clin Pharmacol 28: 373-387
21. 21. Woolf E, Matuszewski B (1999) Determination of rofecoxib, a cyclooxygenase-2 specific inhibitor, in human plasma using high-performance liquid chromatography with post-column photochemical derivatization and fluorescence detection. J Chromatogr B Biomed Sci Appl 730: 221-227
22. 22. Whelton A (1995) Renal effects of over-the counter analgesics. J Clin Pharmacol 35: 454-463
23. 23. Murray MD, Brater DC (1993) Renal toxicity of non-steroidal anti-inflammatory drugs. Annu Rev Pharmacol 32: 435-465
24. 24. Venturi CM, Isakson P, Needleman P (1998) Non-steroidal anti-inflammatory drug-induced renal failure: a brief review of the role of cyclo-oxygenase isoforms. Curr Opin Nephrol Hypertens 7: 79-82
25. 25. Komhoff M, Grone HJ, Klein T, Seybert HW, Nusing RM (1997) Localisation of cyclo-oxygenase 1 and 2 in adult and fetal human kidney: implication for renal function. Am J Physiol 272: F460-F468
26. 26. Khan K, Venturini CM, Bunch RT, Brassard JA, Koki AT, Morris DL, Trump BF, Maziasz TJ, Alden CL (1998) Interspecies differences in renal localization of cyclooxygenase isoforms: implications in nonsteroidal antiinflammatory drug-related nephrotoxicity. Toxicol Pathol 26: 612-620
27. 27. Kovacs SJ, Martin DE, Everitt DE, Patterson SD, Jorkasky DK (1998) Urinary excretion of 6β-hydroxycortisol as an in vivo marker for CYP3A induction: applications and recommendations. Clin Pharmacol Ther 63: 617-622