Pharmacology of COX-2 inhibitors

Progress in Experimental Tumor Research

Volumn 37, Issue , 2003, Pages 25-51

  Isakson, Peter C ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITOR; ISOENZYME; MEMBRANE PROTEIN; NONSTEROID ANTIINFLAMMATORY AGENT; PROSTAGLANDIN SYNTHASE; PROSTAGLANDIN SYNTHASE INHIBITOR; PTGS2 PROTEIN, HUMAN;

ANIMAL; CARDIOVASCULAR SYSTEM; DIGESTIVE SYSTEM; DRUG ANTAGONISM; DRUG EFFECT; HUMAN; KIDNEY; KINETICS; REVIEW; THROMBOCYTE;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BLOOD PLATELETS; CARDIOVASCULAR SYSTEM; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; CYCLOOXYGENASE INHIBITORS; DIGESTIVE SYSTEM; HUMANS; ISOENZYMES; KIDNEY; KINETICS; MEMBRANE PROTEINS; PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES;

EID: 0042632597     PISSN: 00796263     EISSN: None     Source Type: Book Series    
DOI: 10.1159/000071366     Document Type: Article

References (131)

1. Vane JR: Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nat New Biol 1971;231:232-235.
2. Kujubu DA, Fletcher BS, Varnum BC, Lim RW, Herschman HR: TIS10, a phorbol ester tumor promoter-inducible mRNA from Swiss 3T3 cells, encodes a novel prostaglandin synthase/ cyclooxygenase homologue. J Biol Chem 1991;266:12866-12872.
3. Merlie JP, Fagan D, Mudd J, Needleman P: Isolation and characterization of the complementary DNA for sheep seminal vesicle prostaglandin endoperoxide synthase (cyclooxygenase). J Biol Chem 1988;263:3550-3553.
4. Xie WL, Chipman JG, Robertson DL, Erikson RL, Simmons DL: Expression of a mitogenresponsive gene encoding prostaglandin synthase is regulated by mRNA splicing. Proc Natl Acad Sci USA 1991;88:2692-2696.
5. Hay C, de Belleroche J: Carrageenan-induced hyperalgesia is associated with increased cyclooxygenase-2 expression in spinal cord. Neuroreport 1997;8:1249-1251.
6. Huang Z, Massey J: Differential regulation of cyclooxygenase-2 mRNA stability by interleukin-1β and tumor necrosis factor-α in human in vitro differentiated macrophages. Biochem Pharmacol 2000;59:187-194.
7. Porreca E, Reale M, Di Febbo CD, Di Gioacchino M, Barbacane R, Castellani M, Baccante G, Conti P, Cuccurullo F: Down-regulation of cyclooxygenase-2 by interleukin-receptor antagonist in human monocytes. Immunology 1996;89:424-429.
8. Kang RY, Freire-Moar, Sigal E, Chu CQ: Expression of cyclooxygenase-2 in human and an animal model of rheumatoid arthritis. Br J Rheumatol 1996;35:711-718.
9. Samad TA, Moore KA, Sapirstein A, Billet S, Allchorne A, Poole S, Bonventre JV, Woolf CJ: Interleukin-1β-mediated induction of COX-2 in the CNS contributes to inflammatory pain hypersensitivity. Nature 2001;410:471-475.
10. Seigle I, Klein T, Backman JT, Saal JG, Nusing RM, Fritz P: Expression of cyclooxygenase-1 and cyclooxygenase-2 in human synovial tissue: Differential elevation of cyclooxygenase in inflammatory joint disease. Arthritis Rheum 1998;41:122-129.
11. Vanegas H, Schaible HG: Prostaglandins and cyclooxygenases in the spinal cord. Prog Neurobiol 2001;64:327-363.
12. DuBois RN, Abramson SB, Crofford L, Gupta RA, Simon LS, Van De Putte LB, Lipsky PE: Cyclooxygenase in biology and disease. Faseb J 1998;12:1063-1073.
13. Harris R, McKanna J, Akai Y, Jacobson H, DuBois R, Breyer M: Cyclooxygense-2 is associated with the macula densa of rat kidney and increases with salt restriction. J Clin Invest 1994;94:504-2510.
14. Seibert K, Zhang Y, Leahy K, Hauser S, Masferrer J, Perkins W, Lee L, Isakson P: Pharmacological and biochemical demonstration of the role of cyclooxygenase-2 in inflammation and pain. Proc Natl Acad Sci USA 1994;91:12013-12017.
15. Smith WL, Garavito RM, DeWitt DL: Prostaglandin endoperoxide H synthases (cyclooxygenases)-1 and -2. J Biol Chem 1996;271:33157-33160.
16. Matsumoto H, Ma W, Smalley W, Trzaskos J, Breyer R, Dey S: Diversification of cyclooxygenase-2-derived prostaglandins in ovulation and implantation. Biol Reprod 2001;64:1557-1565.
17. Pall M, Frieden B, Brännström M: Induction of delayed follicular rupture in the human by the selective COX-2 inhibitor rofecoxib: A randomised double-blind study. Hum Reprod 2001;16:323-1328.
18. Lipsky LP, Abramson SB, Crofford L, DuBois RN, Simon LS, van de Putte LB: The classification of cyclooxygenase inhibitors. J Rheumatol 1998;25:2298-2303.
19. Crofford LJ, Wilder RL, Ristimaki AP, Sano H, Remmers EF, Epps HR, Hla T: Cyclooxygenase-1 and -2 expression in rheumatoid synovial tissues. Effects of interleukin-1β, phorbol ester and corticosteroids. J Clin Invest 1994;93:1095-1101.
20. Amin AR, Attur M, Patel RN, Thakker GD, Marshall PJ, Rediske J, Stuchin SA, Patel IR, Abramson SB: Superinduction of cyclooxygenase-2 activity in human osteoarthritis-affected cartilage. Influence of nitric oxide. J Clin Invest 1997;99:1231-1237.
21. 2, immunoreactive leukotriene and pain after periodontal surgery. J Periodontol 1996;67:1307-1316.
22. Cominelli F, Nast CC, Duchini A, Lee M: Recombinant interleukin-1 receptor antagonist blocks the proinflammatory activity of endogenous interleukin-1 in rabbit immune colitis. Gastroenterology 1992;103:65-71.
23. 4, and (S)-flurbiprofen following extraction of impacted third molars. Pain 1997;73:339-345.
24. Ji RR, Woolf CJ: Neuronal plasticity and signal transduction in nociceptive neurons: Implications for the initiation and maintenance of pathological pain. Neurobiol Dis 2001;8:1-10.
25. Woolf CJ, Costigan M: Transcriptional and posttranslational plasticity and the generation of inflammatory pain. Proc Natl Acad Sci USA 1999;96:7723-7730.
26. Woolf CJ, Salter MW: Neuronal plasticity: Increasing the gain in pain. Science 2000;288:1765-1768.
27. Smith CJ, Zhang Y, Koboldt CM, Muhammad J, Zweifel BS, Shaffer A, Talley JJ, Masferrer JL, Seibert K, Isakson PC: Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci USA 1998;95:13313-13318.
28. Mitchell JA, Akarasereenont P, Thiemermann C, Flower RJ, Vane JR: Selectivity of nonsteroidal anti-inflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci USA 1993;90:11693-11697.
29. Bensen WG, Fiechtner JJ, McMillen JI, Zhao WW, Yu SS, Woods EM, Hubbard RC, Isakson PC, Verburg KM, Geis GS: Treatment of osteoarthritis with celecoxib, a cyclooxygenase-2 inhibitor: A randomized controlled trial. Mayo Clin Proc 1999;74:1095-1105.
30. Bensen WG, Weaver A, Espinoza L, Zhao WW, Riley W, Paperiello B, Recker D: Efficacy and safety of valdecoxib in treating the signs and symptoms of rheumatoid arthritis: A randomised, controlled comparison with placebo and naproxen. Rheumatology 2002 (in press).
31. Day R, Morrison B, Luza A, Castaneda O, Strusberg A, Nahir M, Helgetveit KB, Kress B, Daniels B, Bolognese J, Krupa D, Seidenberg B, Ehrich E: A randomized trial of the efficacy and tolerability of the COX-2 inhibitor rofecoxib vs. ibuprofen in patients with osteoarthritis. Rofecoxib/Ibuprofen Comparator Study Group. Arch Intern Med 2000;160:1781-1787.
32. Emery P, Zeidler H, Kvien TK, Guslandi M, Naudin R, Stead H, Verburg KM, Isakson PC, Hubbard RC, Geis GS: Celecoxib versus diclofenac in long-term management of rheumatoid arthritis: A randomised double-blind comparison. Lancet 1999;354:2106-2111.
33. Kivitz AJ, Eisen G, Zhao WW, Bevirt T, Recker D: The COX-2-specific inhibitor valdecoxib is as effective as naproxen in treating symptomatic osteoarthritis of the knee and demonstrates reduced gastrointestinal ulceration. J Fam Pract 2002;51:530-537.
34. Schnitzer TJ, Truitt K, Fleischmann RM, Dalgin P, Block J, Zeng Q, Bolognese JA, Seidenberg B, Ehrich E: The safety profile, tolerability and effective dose range of rofecoxib in the treatment of rheumatoid arthritis. Phase II Rofecoxib Rheumatoid Arthritis Study Group. Clin Ther 1999;21:688-1702.
35. Bensen WG, Zhao SZ, Burke TA, Zabinski RA, Makuch RW, Maurath CJ, Agrawal NM, Geis GS: Upper gastrointestinal tolerability of celecoxib, a COX-2-specific inhibitor, compared to naproxen and placebo. J Rheumatol 2000;27:1876-1883.
36. Simon LS, Lanza FL, Lipsky PE, Hubbard RC, Talwalker S, Schwartz BD, Isakson PC, Geis GS: Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase-2 inhibitor: Efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects. Arthritis Rheum 1998;41:1591-1602.
37. Silverstein FE, Faich G, Goldstein JL, Simon LS, Pincus T, Whelton A, Makuch R, Eisen G, Agrawal NM, Stenson WF, Burr AM, Zhao WW, Kent JD, Lefkowith JB, Verburg KM, Geis GS: Gastrointestinal toxicity with celecoxib versus nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-Term Arthritis Safety Study. JAMA 2000;284:1247-1255.
38. Bombardier C, Laine L, Reicin AS, Shapiro A, Burgos-Vargas R, Davis B, Ferraz M, Hawkey C, Hochberg M, Kvien TK, Schnitzer TJ: Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. N Engl J Med 2000;343:1520-1528.
39. Watson DJ, Harper SE, Zhao PL, Quan H, Bolognese JA, Simon TJ: Gastrointestinal tolerability of the selective COX-2 inhibitor rofecoxib compared with nonselective COX-1 and COX-2 inhibitors in osteoarthritis. Arch Intern Med 2000;160:2998-3003.
40. Hawkey C: COX-2 inhibitors. Lancet 1999;353:307-314.
41. Vane JR, Bakhle Y, Botting R: Cyclooxygenases 1 and 2. Annu Rev Pharmacol Toxicol 1998;39:7-120.
42. Gierse JK, McDonald JJ, Hauser SD, Rangwala SH, Koboldt CM, Seibert K: A single amino acid difference between COX-1 and COX-2 reverses the selectivity of COX-2-specific inhibitors. J Biol Chem 1996;271:15810-15814.
43. Kurumbail RG, Stevens AM, Gierse JK, McDonald JJ, Stegeman RA, Pak JY, Gildehaus D, Miyashiro JM, Penning TD, Seibert K, Isakson PC, Stallings WC: Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents. Nature 1996;384:644-648.
44. Luong C, Miller A, Barnett J, Chow J, Ramesha CS, Browner MF: Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2. Nat Struct Biol 1996;3:927-933.
45. 2 synthase. Nature 1994;367:243-249.
46. Garavito RM: The three-dimensional structure of cyclooxygenases; in Vane JR, Botting J, Botting R (eds): Improved Non-Steroidal Anti-Inflammatory Drugs: COX-2 Enzyme Inhibitors. Dordrecht, Kluwer Academic, 1996, pp 29-43.
47. Wong E, Bayly C, Waterman H, Riendeau D, Mancini J: Conversion of prostaglandin G/H synthase-1 into an enzyme sensitive to PGHS-2-selective inhibitors by a double His513-Arg and Ile523-Val mutation. J Biol Chem 1997;272:9280-9286.
48. Walker M, Kurumbail RG, Kiefer J, Moreland K, Koboldt C, Isakson PC, Seibert K, Gierse JK: A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors. Biochem J 2001;357:709-718.
49. Chan CC, Boyce S, Brideau C, Charleson S, Cromlish E, Ethier D, Evans J, Ford-Hutchison AW, Forrest M, Gauthier J, Gordon R, Gresser M, Guay J, Kargman S, Kennedy B, Leblanc Y, Leger S, Mancini J, O'Niell G, Ouellet M, Patrick D, Percival MD, Perrier H, Prasit P, Rodger IW, Tagari P, Therien M, Vickers PJ, Visco D, Wang Z, Webb JK, Wong E, Xu LJ, Young R, Zamboni R, Riendeau D: Rofecoxib (Vioxx, MK-0966; 4-(4_-methylsulfonylphenyl)-3-phenyl-2(5H)furanone): a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. J Pharmacol Exp Ther 1999;290:551-560.
50. Copeland RA, Williams JM, Giannaras J, Nurnberg S, Covington M, Pinto D, Pick S, Trzaskos JM: Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase. Proc Natl Acad Sci USA 1994;91:11202-11206.
51. Gierse JK, Koboldt CM, Walker MC, Seibert K, Isakson PC: Kinetic basis for selective inhibition of cyclo-oxygenases. Biochem J 1999;339:607-614.
52. Rome LH, Lands WE: Structural requirements for time-dependent inhibition of prostaglandin biosynthesis by anti-inflammatory drugs. Proc Natl Acad Sci USA 1975;72:4863-4865.
53. Patrignani P, Panara MR, Greco A, Fusco O, Natoli C, Iacobelli S, Cipollone F, Ganci A, Creminon C, Maclouf J: Biochemical and pharmacological characterization of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases. J Pharmacol Exp Ther 1994;271:1705-1712.
54. Masferrer JL, Zweifel BS, Manning PT, Hauser SD, Leahy KM, Smith WG, Isakson PC, Seibert K: Selective inhibition of inducible cyclooxygenase 2 in vivo is anti-inflammatory and nonulcerogenic. Proc Natl Acad Sci USA 1994;91:3228-32.
55. Davies NM, McLachlan AJ, Day RO, Williams KM: Clinical pharmacokinetics and pharmacodynamics of celecoxib: A selective cyclooxygenase-2 inhibitor. Clin Pharmacokinet 2000;38:225-242.
56. Karim A, Tolbert D, Piergies A, Hubbard RC, Harper K, Wallemark CB, Slater M, Geis GS: Celecoxib does not significantly alter the pharmacokinetics or hypoprothrombinemic effect of warfarin in healthy subjects. J Clin Pharmacol 2000;40:655-663.
57. Scott LJ, Lamb HM: Rofecoxib. Drugs 1999;58:499-505.
58. Karim A, Schwartz L, Boynton J, Slater M, Snabes MC, Piergies A: Multiple dose pharmacokinetics and tolerability of parecoxib sodium, a prodrug of the COX-2-specific inhibitor, following intravenous and intramuscular administration. American Society of Health-System Pharmacists Annual Meeting. Am J Health-System Pharmacy 2001;36:abstr P-456E.
59. McKenna F, Weaver A, Fiechtner JJ, Bello AE, Fort JG: COX-2-specific inhibitors in the management of osteoarthritis of the knee: A placebo-controlled, randomized, double-blind study. J Clin Rheumatol 2001;7:151-159.
60. McKenna F, Borenstein D, Wendt H, Wallemark C, Lefkowith JB, Geis GS: Celecoxib versus diclofenac in the management of osteoarthritis of the knee. Scand J Rheumatol 2001;30:11-18.
61. Saag K, Van der Heijde D, Fisher C, Samara A, DeTora L, Bolognese J, Sperling R, Daniels B: Rofecoxib, a new cyclooxygenase-2 inhibitor, shows sustained efficacy, comparable with other nonsteroidal anti-inflammatory drugs. Arch Fam Med 2000;9:1124-1134.
62. Makarowski W, Zhao W, Bevirt T, Recker D: Efficacy and safety of the COX-2-specific inhibitor valdecoxib in the management of osteoarthritis of the hip: A randomized, double-blind, placebocontrolled comparison with naproxen. Osteoarthritis Cartilage 2002;10:290-296.
63. Dougados M, Behier JM, Jolchine I, Calin A, Van der Heijde D, Olivieri I, Zeidler H, Herman H: Efficacy of celecoxib, a cyclooxygenase 2-specific inhibitor, in the treatment of ankylosing spondylitis. Arthritis Rheum 2001;44:180-185.
64. Morrison BW, Daniels S, Kotey P, Cantu N, Seidenberg B: Rofecoxib, a specific cyclooxygenase-2 inhibitor, in primary dysmenorrhea: A randomized controlled trial. Obstet Gynecol 1999;94:04-508.
65. Daniels S, Talwalker S, Torri S, Kuss M, Snabes MC, Recker D, Verburg KM: Valdecoxib, a COX-2-specific inhibitor, is effective and well tolerated in treating women with primary dysmenorrhea. Obstet Gynecol 2001 (in press).
66. Chang D, Desjardins PJ, Chen E, Polis A, McAvoy M, Mockoviack S, Geba G: Comparison of the analgesic effects of rofecoxib and enteric-coated diclofenac sodium in the treatment of postoperative dental pain: A randomized, placebo-controlled clinical trial. Clin Ther 2002;24:490-503.
67. Chang D, Fricke J, Bird S, Bohidar N, Dobbins T, Geba G: Rofecoxib versus codeine/acetaminophen in postoperative dental pain: A double-blind, randomized, placebo- and active comparator-controlled clinical trial. Clin Ther 2001;23:1446-1455.
68. Daniels SE, Desjardins PJ, Talwalker S, Kuss M, Recker D, Verburg KM: Single oral doses of valdecoxib are as effective as oxycodone/acetaminophen in reducing pain following oral surgery: Results of two randomized, double-blind trials. J Am Dent Assoc 2002;133:611-621.
69. Gimbel JS, Brugger A, Zhao W, Verburg KM, Geis GS: Efficacy and tolerability of celecoxib versus hydrocodone/acetaminophen in the treatment of pain after ambulatory orthopedic surgery in adults. Clin Ther 2001;23:228-241.
70. Fricke J, Varkalis J, Zwillich S, Adler R, Forester E, Recker D, Verburg KM: Valdecoxib is more efficacious than rofecoxib in relieving pain associated with oral surgery. Am J Ther 2002;9:89-97.
71. Malmstrom K, Daniels S, Kotey P, Seidenberg BC, Desjardins PJ: Comparison of rofecoxib and celecoxib, two cyclooxygenase-2 inhibitors, in postoperative dental pain: A randomized, placebo and active comparator-controlled clinical trial. Clin Ther 1999;21:1653-1663.
72. Reuben SS, Fingeroth R, Krushell R, Maciolek H: Evaluation of the safety and efficacy of the perioperative administration of rofecoxib for total knee arthroplasty. J Arthroplast 2002;17:26-31.
73. Desjardins P, Talwalker S, Recker D, Verburg K, Woolf C: A single pre-operative oral dose of valdecoxib, a long-acting COX-2-specific inhibitor, relieves post-oral surgery or bunionectomy pain. Anesthesiology 2002 (in press).
74. Hamilton GR, Baskett TF: In the arms of Morpheus, the development of morphine for postoperative pain relief. Can J Anaesth 2000;47:367-374.
75. Kehlet H, Rung GW, Callesen T: Postoperative opioid analgesia: Time for a reconsideration? J Clin Anesth 1996;8:441-445.
76. Mulroy MF: Monitoring opioids. Reg Anesth 1996;21:89-93.
77. Wheeler M, Oderda G, Ashburn M, Lipman A: Adverse events associated with postoperative opioid analgesia: A systematic review. J Pain 2002;3:159-180.
78. Kehlet H, Dahl JB: The value of 'multimodal' or 'balanced analgesia' in postoperative pain treatment. Anesth Analg 1993;77:1048-1056.
79. Rawal N: Management of Acute and Chronic Pain. London, BMJ Books, 1998.
80. Rawal N: Ten years of acute pain services - Achievements and challenges. Reg Anesth Pain Med 1999;24:68-73.
81. Camu F, Beecher T, Recker D, Verburg KM: Valdecoxib, a COX-2-specific inhibitor, is an efficacious, opioid-sparing analgesic in patients undergoing hip arthroplasty. Am J Ther 2002;9:43-51.
82. Reuben SS, Connelly NR: Postoperative analgesic effects of celecoxib or rofecoxib after spinal fusion surgery. Anesth Analg 2000;91:1221-1225.
83. Reynolds L, Brill R, Recker D, Sainati S, Verburg KM: The COX-2-specific inhibitor, valdecoxib, is an effective, opioid-sparing analgesic in patients undergoing total knee arthroplasty. J Pain Sympt Manag 2002 (in press).
84. Singh G, Ramey DR: NSAID-induced gastrointestinal complications: The ARAMIS perspective 1997. Arthritis, Rheumatism and Aging Medical Information System. J Rheumatol 1998; 51(suppl):8-16.
85. Singh G, Ramey DR, Morfeld D, Shi H, Hatoum HT, Fries JF: Gastrointestinal tract complications of nonsteroidal anti-inflammatory drug treatment in rheumatoid arthritis. A prospective observational cohort study. Arch Intern Med 1996;156:1530-1536.
86. Verburg KM, Maziasz TJ, Weiner E, Loose L, Geis GS, Isakson PC: COX-2-specific inhibitors: Definition of a new therapeutic concept. Am J Ther 2001;8:49-64.
87. Barrier C, Hirschowitz B: Controversies in the detection and management of nonsteroidal anti-inflammatory drug-induced side effects in the upper gastrointestinal tract. Arthitis Rheum 1989;32:926-932.
88. Scholes D, Stergachis A, Penna P, Normand E, Hansten P: Nonsteroidal anti-inflammatory drug discontinuation in patients with osteoarthritis. J Rheumatol 1995;22:708-712.
89. Fries JF: NSAID gastropathy: Epidemiology. J Musculoskel Med 1991;8:21-28.
90. Singh G: Recent considerations in nonsteroidal anti-inflammatory drug gastropathy. Am J Med 1998;105:31S-38S.
91. Blower AL, Brooks A, Fenn GC, Hill A, Pearce MY, Morant S, Bardhan KD: Emergency admissions for upper gastrointestinal disease and their relation to NSAID use. Aliment Pharmacol Ther 1997;11:283-291.
92. Gabriel SE, Jaakkimainen L, Bombardier C: Risk for serious gastrointestinal complications related to use of nonsteroidal anti-inflammatory drugs. A meta-analysis. Ann Intern Med 1991;115:787-796.
93. Paulus H: FDA Arthritis Advisory Committee Meeting: Risks of agranulocytosis/aplastic anemia, flank pain and adverse gastrointestinal effects with nonsteroidal anti-inflammatory drugs. Arthitis Rheum 1987;30:593-595.
94. Langman MJ, Weil J, Wainwright P, Lawson DH, Rawlins MD, Logan RF, Murphy M, Vessey MP, Colin-Jones DG: Risks of bleeding peptic ulcer associated with individual non-steroidal anti-inflammatory drugs. Lancet 1994;343:1075-1078.
95. Garcia Rodriguez LA, Jick H: Risk of upper gastrointestinal bleeding and perforation associated with individual nonsteroidal anti-inflammatory drugs. Lancet 1994;343:769-772.
96. Langman MJ, Jensen DM, Watson DJ, Harper SE, Zhao PL, Quan H, Bolognese JA, Simon TJ: Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs. JAMA 1999;282:929-1933.
97. Goldstein JL, Kent JD, Zhao W, Recker D, Verburg KM: Reduced incidence of gastroduodenal ulcers with valdecoxib compared to ibuprofen and diclofenac in patients with rheumatoid arthritis: A multicenter trial (abstract). Am J Gastroenterol 2001;96(suppl):9.
98. Goldstein JL, Stenson WF, Agrawal N, Eisen G, Omachi J, Kent JD, Recker D, Verburg KM: Valdecoxib is associated with a significantly lower incidence of ulcer complications and symptomatic ulcers in arthritis patients as compared to NSAIDs (Abstract - Digestive Disease Week). Gastroenterology 2002;122(suppl 1):5.
99. Schror K: Aspirin and platelets: The antiplatelet action of aspirin and thrombosis treatment and prophylaxis. Semin Thromb Hemost 1997;23:349-356.
100. Cheng JC, Siegel L, Katari B, Traynoff S, Ro J: Nonsteroidal anti-inflammatory drugs and aspirin: A comparison of the antiplatelet effect. Am J Ther 1997;4:62-65.
101. Nadell J, Bruno J, Varaday J, Segre E: Effect of naproxen and of aspirin on bleeding time and platelet aggregation. J Clin Pharmacol 1974;14:176-182.
102. Roth G, Majerus PW: The mechanism of the effect of aspirin on human platelets. J Clin Invest 1975;56:624-632.
103. Roth G, Stanford N, Majerus PW: Acetylation of prostaglandin synthase by aspirin. Biochemistry 1975;72:3073-3076.
104. Patrono C, Coller B, Dalen J, Fitzgerald G, Fuster V, Gent M, Hirsh J, Roth G: Platelet-active drugs: The relationship among dose, effectiveness and side effects. Chest 2001;119:39S-63S.
105. Leese PT, Hubbard RC, Karim A, Isakson PC, Yu SS, Geis GS: Effects of celecoxib, a novel cyclooxygenase-2 inhibitor, on platelet function in healthy adults: A randomized, controlled trial. J Clin Pharmacol 2000;40:124-132.
106. Leese P, Recker D, Kuss M: A double-blind, placebo-controlled study to evaluate the effects of valdecoxib, a novel COX-2-specific inhibitor, on platelet function in the elderly. Ann Rheum Dis 2001;60(suppl 10):abstr SAT0057.
107. Leese P, Talwalker S, Recker D, Kent J: Valdecoxib, a novel COX-2-specific inhibitor, does not impair platelet function in healthy adults: results of a randomized controlled trial. Am J Emerg Med 2002 (in press).
108. Greenberg H, Gottesdiener K, Huntington M, Wong P, Larson P, Wildonger L, Gillen L, Dorval E, Waldman S: A new cyclooxygenase-2 inhibitor, rofecoxib (VIOXX), did not alter the antiplatelet effect of low-dose aspirin in healthy volunteers. J Clin Pharmacol 2000;40:1509-1515.
109. Antiplatelet Trialists' Collaboration: Collaborative overview of randomised trials of antiplatelet therapy-I: Prevention of death, myocardial infarction and stroke by prolonged antiplatelet therapy in various categories of patients. BMJ 1994;308:81-106.
110. Fitzgerald G, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med 2001;345:433-442.
111. Catella-Lawson F, McAdam B, Morrison BW, Kapoor SC, Kujubu DA, Antes L, Lasseter K, Quan H, Gertz BJ, Fitzgerald GA: Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics and vasoactive eicosanoids. Pharmacology 1999;289:735-741.
112. McAdam B, Catella-Lawson F, Mardini I, Kapoor SC, Lawson J, Fitzgerald G: Systemic biosynthesis of prostacyclin by COX-2: The human pharmacology of a selective inhibitor of COX-2. Proc Natl Acad Sci USA 1999;96:2722-277.
113. White W, Faich G, Whelton A, Maurath C, Ridge N, Verburg K, Geis G, Lefkowith J: Comparison of thromboembolic events in patients treated with celecoxib, a cyclooxygenase-2 specific inhibitor, versus ibuprofen and diclofenac. Am J Cardiol 2002;89:425-430.
114. Konstam M, Weir M, Reicin AS, Shapiro D, Sperling R, Barr E, Gertz BJ: Cardiovascular thrombotic events in controlled clinical trials of rofecoxib. Circulation 2001;104:2280-2288.
115. Reicin A, Shapiro D, Sperline R, Barr E, Yu Q: Comparison of cardiovascular thrombotic events in patients with osteoarthritis treated with rofecoxib versus nonselective nonsteroidal antiinflammatory drugs (ibuprofen, diclofenac and nambutone). Am J Cardiol 2002;89:204-209.
116. White W, Recker D, Kent JD, Verburg KM, Whelton A: The COX-2-specific inhibitor, valdecoxib, is not associated with an increased risk of serious thrombotic events in arthritis patients (abstract). Am Coll Cardiol 2002 (submitted).
117. Whelton A, Kent JD, Recker D: No difference in thrombotic events in rheumatoid arthritis patients: Valdecoxib vs. naproxen and placebo (abstract). Am Coll Rheumatol. Arthritis Rheum 2002 (submitted).
118. Smith WL, Bell T: Immunohistochemical localization of the prostaglandin-forming cyclooxygenase in renal cortex. Am J Physiol 1978;235:F451-F457.
119. Guan Y, Chang M, Cho W, Zhang Y, Redha R, Davis L, Chang S, DuBois R, Hao C, Breyer M: Cloning, expression, and regulation of rabbit cyclooxygenase-2 in renal medullary interstitial cells. Am J Physiol 1997;273:F18-F26.
120. Harris R: The macula densa: Recent developments. J Hypertens 1996;14:815-822.
121. Whelton A, Hamilton C: Nonsteroidal anti-inflammatory drugs: Effects on kidney function. J Clin Pharmacol 1991;31:588-598.
122. Clive D, Stoff J: Renal syndromes associated with nonsteroidal anti-inflammatory drugs. N Engl J Med 1984;310:563-572.
123. Murray M, Lazaridis E, Brizendine E, Haag K, Becker P, Brater D: The effect of nonsteroidal anti-inflammatory drugs on electrolyte homeostasis and blood pressure in young and elderly persons with and without renal insufficiency. Am J Med Sci 1997;314:80-88.
124. Perneger T, Whelton P, Klag M: Risk of kidney failure associated with the use of acetaminophen, aspirin and nonsteroidal anti-inflammatory drugs. N Engl J Med 1994;331:1675-1679.
125. Whelton A: Nephrotoxicity of nonsteroidal anti-inflammatory drugs: Physiologic foundations and clinical implications. Am J Med 1999;106:13S-24S.
126. Murray M, Black P, Kuzmik D, Haag K, Manatunga A, Mullin M, Hall S, Brater D: Acute and chronic effects of nonsteroidal anti-inflammatory drugs on glomerular filtration rate in elderly patients. Am J Med Sci 1995;310:188-197.
127. Whelton A, Schulman G, Wallemark C, Drower EJ, Isakson PC, Verburg KM, Geis GS: Effects of celecoxib and naproxen on renal function in the elderly. Arch Intern Med 2000;160:1465-1470.
128. Whelton A, Maurath CJ, Verburg KM, Geis GS: Renal safety and tolerability of celecoxib, a novel cyclooxygenase-2 inhibitor. Am J Ther 2000;7:159-175.
129. Gertz B, Krupa D, Bolognese JA, Sperling R, Reicin A: A comparison of adverse renovascular experiences among osteoarthritis patients treated with rofecoxib and comparator nonselective nonsteroidal anti-inflammatory agents. Curr Med Res Opin 2002;18:82-91.
130. Whelton A, Fort JG, Puma JA, Normandin D, Bello AE, Verburg KM: Cyclooxygenase-2-specific inhibitors and cardiorenal function: A randomized, controlled trial of celecoxib and rofecoxib in older hypertensive osteoarthritis patients. Am J Ther 2001;8:85-95.
131. Whelton A, White W, Recker D, Kent JD, Verburg KM: Valdecoxib is associated with an incidence of renal effects similar to nonselective NSAIDs (abstract). Am Coll Rheumatol. Arthritis Rheum 2001 (submitted).