Pharmacokinetic-pharmacodynamic correlations and biomarkers in the development of COX-2 inhibitors

Rheumatology

Volumn 44, Issue 7, 2005, Pages 846-859

  Huntjens, D R H ^a   Danhof, M ^a   Della Pasqua, O E ^a,b  

^a LEIDEN UNIVERSITY   (Netherlands)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

6 METHOXY 2 NAPHTHYLACETIC ACID; ACETYLSALICYLIC ACID; AUTACOID; BIOLOGICAL MARKER; CALCIUM CHANNEL BLOCKING AGENT; CELECOXIB; CYCLOOXYGENASE 1; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITOR; DICLOFENAC; DYFLOS; ETODOLAC; ETORICOXIB; FENOPROFEN; IBUPROFEN; INDOMETACIN; KETOPROFEN; MEFENAMIC ACID; MELOXICAM; NAPROXEN; NARCOTIC ANALGESIC AGENT; NIMESULIDE; OXAPROZIN; PIROXICAM; PROSTAGLANDIN E2; ROFECOXIB; SULINDAC SULFIDE; THROMBOXANE B2; UNINDEXED DRUG; VALDECOXIB; MEMBRANE PROTEIN; NONSTEROID ANTIINFLAMMATORY AGENT; PROSTAGLANDIN SYNTHASE; PROSTAGLANDIN SYNTHASE INHIBITOR; PTGS2 PROTEIN, HUMAN;

ANALGESIA; ANALGESIC ACTIVITY; BIOLOGICAL MODEL; CARDIOTOXICITY; CARDIOVASCULAR DISEASE; CHRONIC INFLAMMATION; CHRONIC PAIN; CLINICAL TRIAL; CONCENTRATION RESPONSE; CORRELATION FUNCTION; DISEASE COURSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG ELIMINATION; DRUG EXPOSURE; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG RESPONSE; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; ENZYME INHIBITION; GASTROINTESTINAL TOXICITY; HEART INFARCTION; HUMAN; IC 50; IN VITRO STUDY; LIVER TOXICITY; NEPHROTOXICITY; NEUROPATHIC PAIN; NONHUMAN; PATHOPHYSIOLOGY; PHARMACODYNAMICS; PHARMACOLOGICAL PARAMETERS; PHYSICAL CHEMISTRY; PREDICTION; PRIORITY JOURNAL; PROSTAGLANDIN BLOOD LEVEL; REVIEW; SIGNAL TRANSDUCTION; STROKE; ANIMAL; BLOOD; DISEASE MODEL; METHODOLOGY; PAIN; PAIN ASSESSMENT;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BIOLOGICAL MARKERS; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; CYCLOOXYGENASE INHIBITORS; DISEASE MODELS, ANIMAL; HUMANS; MEMBRANE PROTEINS; PAIN; PAIN MEASUREMENT; PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES; SIGNAL TRANSDUCTION;

EID: 22844452700     PISSN: 14620324     EISSN: 14620332     Source Type: Journal    
DOI: 10.1093/rheumatology/keh627     Document Type: Review

References (123)

1. Colburn WA. Optimizing the use of biomarkers, surrogate endpoints, and clinical endpoints for more efficient drug development. J Clin Pharmacol 2000;40:1419-27.
2. Rolan P, Atkinson AJ Jr, Lesko LJ. Use of biomarkers from drug discovery through clinical practice: Report of the Ninth European Federation of Pharmaceutical Sciences Conference on Optimizing Drug Development. Clin Pharmacol Ther 2003;73:284-91.
3. Biomarkers Definitions Working Group. Biomarkers and surrogate endpoints: Preferred definitions and conceptual framework. Clin Pharmacol Ther 2001;69:89-95.
4. Rolan P. The contribution of clinical pharmacology surrogates and models to drug development - a critical appraisal. Br J Clin Pharmacol 1997;44:219-25.
5. Vane JR. Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nat New Biol 1971;2131:232-5.
6. Vane JR, Botting RM. Formation and actions of prostaglandins and inhibition of their synthesis. In: Vane JR, Botting RM, eds. Therapeutic roles of selective COX-2 inhibitors. London: William Harvey Press, 2001;1-47.
7. Vane J. Towards a better aspirin. Nature 1994;367:215-16.
8. Martinez RV, Reval M, Campos MD, Terron JA, Dominguez R, Lopez-Munoz FJ. Involvement of peripheral cyclooxygenase-1 and cyclooxygenase-2 in inflammatory pain. J Pharm Pharmacol 2002; 54:405-12.
9. Anderson GD, Hauser SD, McGarity KL, Bremer ME, Isakson PC, Gregory SA. Selective inhibition of cyclooxygenase (COX)-2 reverses inflammation and expression of COX-2 and interleukin 6 in rat adjuvant arthritis. J Clin Invest 1996;97:2672-9.
10. Meagher EA. Balancing gastroprotection and cardioprotection with selective cyclo-oxygenase-2 inhibitors: Clinical implications. Drug Saf 2003;26:913-24.
11. Dirig DM, Isakson PC, Yaksh TL. Effect of COX-1 and COX-2 inhibition on induction and maintenance of carrageenan-evoked thermal hyperalgesia in rats. J Pharmacol Exp Ther 1998;285:1031-8.
12. Derendorf H, Lesko LJ, Chaikin P et al. Pharmacokinetic/pharmacodynamic modeling in drug research and development. J Clin Pharmacol 2000;40:1399-418.
13. Mogil JS. The genetic mediation of individual differences in sensitivity to pain and its inhibition. Proc Natl Acad Sci USA 1999;96:7744-51.
14. Dahl V, Raeder JC. Non-opioid postoperative analgesia. Acta Anaesthesiol Scand 2000;44:1191-203.
15. Woolf CJ, Allchorne A, Safieh-Garabedian B, Poole S. Cytokines, nerve growth factor and inflammatory hyperalgesia: The contribution of tumour necrosis factor alpha. Br J Pharmacol 1997;121: 417-24.
16. Safieh-Garabedian B, Dardenne M, Kanaan SA, Atweh SF, Jabbur SJ, Saade NE. The role of cytokines and prostaglandin-E(2) in thymulin induced hyperalgesia. Neuropharmacology 2000;39: 1653-61.
17. Kelly DJ, Ahmad M, Brull SJ. Preemptive analgesia I: Physiological pathways, and pharmacological modalitics. Can J Anaesth 2001;48: 1000-10.
18. Breimer DD, Danhof M. Relevance of the application of pharmacokinetic-pharmacodynamic modelling concepts in drug development. The "wooden shoe' paradigm. Clin Pharmacokinet 1997;32:259-67.
19. Yaksh TL. Spinal systems and pain processing: Development of novel analgesic drugs with mechanistically defined models. Trends Pharmacol Sci 199;20:329-37.
20. Walker K, Fox AJ, Urban LA. Animal models for pain research. Mol Med Today 19991;5:319-21.
21. Ito S, OkUda-Ashitaka E, Minami T. Central and peripheral roles of prostaglandins in pain and their interactions with novel neuropeptides, nociceptin and nocistatin. Neurosci Res 2001;41:299-332.
22. Mukherjee A, Hale VG, Borga O, Stein R. Predictability of the clinical potency of NSAIDs from the preclinical pharmacodynamics in rats. Inflamm Res 1996;45:531-40.
23. Bennett GJ, Xie YK. A peripheral mononeuropathy in rat that produces disorders of pain sensation like those seen in man. Pain 1988;33:87-107.
24. Seltzer Z, Dubner R, Shir Y. A novel behavioral model of neuropathic pain disorders produced in rats by partial sciatic nerve injury. Pain 1990;43:205-18.
25. Kim SH, Chung JM. An experimental model for peripheral neuropathy produced by segmental spinal nerve ligation in the rat. Pain 1992;50:355-63.
26. Ma W, Eisenach JC. Morphological and pharmacological evidence for the role of peripheral prostaglandins in the pathogenesis of neuropathic pain. Eur J Neurosci 2002;15:1037-47.
27. Dubinsky B, Gebre-Mariam S, Capetola RJ, Rosenthale ME. The antialgesic drugs: Human therapeutic correlates of their potency in laboratory animal models of hyperalgesia. Agents Actions 1987;20:5-60.
28. Patrignani P, Panara MR, Greco A et al. Biochemical and pharmacological characterization of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases. J Pharmacol Exp Ther 1994;271:1105-12.
29. Walker MC, Kurumbail RG, Kiefer JR et al. A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors. Biochem J 2001;347:709-18.
30. Smith CJ, Zhang Y, Koboldt CM et al. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci USA 1998;95:13313-18.
31. Riendeau D, Percival MD, Brideau C et al. Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. J Pharmacol Exp Ther 2001;296:558-66.
32. Mitchell JA, Akarasereenont P, Thiemermann C, Flower RJ, Vane JR. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci USA 1993;90:11693-7.
33. Santini G, Sciulli MG, Panara MR et al. Effects of flurbiprofen and flurbinitroxybutylester on prostaglandin endoperoxide synthases. Eur J Pharmacol 1996;316:65-72.
34. Frolich JC. A classification of NSAIDs according to the relative inhibition of cyclooxygenase isoenzymes. Trends Pharmacol Sci 1997;18:30-4.
35. Pairet M, van Ryn J. Experimental models used to investigate the differential inhibition of cyclooxygenase-1 and cyclooxygenase-2 by non-steroidal anti-inflammatory drugs. Inflamm Res 1998; 47(suppl 2):S93-S101.
36. Fenner H. Differentiating among nonsteroidal antiinflammatory drugs by pharmacokinetic and pharmacodynamic profiles. Semin Arthritis Rheum 1997;26:28-33.
37. Blain H, Boileau C, Lapicque F et al. Limitation of the in vitro whole blood assay for predicting the COX selectivity of NSAIDs in clinical use. Br J Clin Pharmacol 2002;53:255-65.
38. Famaey JP. In vitro and in vivo pharmacological evidence of selective cyclooxygenase-2 inhibition by nimesulide: An overview. Inflamm Res 1997;46:431-46.
39. Giuliano F, Warner TD. Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs. Br J Pharmacol 1999;126:1824-30.
40. Carabaza A, Cabre F, Rotllan E et al. Stereoselective inhibition of inducible cyclooxygenase by chiral nonsteroidal antiinflammatory drugs. J Clin Pharmacol 1996;36:505-12.
41. Vane JR, Botting RM. Mechanism of action of aspirin-like drugs. Semin Arthritis Rheum 1997;26:2-10.
42. Lipsky LP, Abramson SB, Crofford L, Dubois RN, Simon LS, Van De Putte LB. The classification of cyclooxygenase inhibitors. J Rheumatol 1998;25:2298-303.
43. Lin JH, Cocchetto DM, Duggan DE. Protein binding as a primary determinant of the clinical pharmacokinetic properties of non-steroidal anti-inflammatory drugs. Clin Pharmacokinet 1987;12:402-32.
44. Brune K, Neubert A. Pharmacokinetic and pharmacodynamic aspects of the ideal COX-2 inhibitor: A pharmacologist's perspective. Clin Exp Rheumatol 2001;19:S51-S57.
45. Yamamoto K, Abe M, Katashima M, Yamada Y, Sawada Y, Iga T. Pharmacodynamic analysis of antiplatelet effect of aspirin in the literature-modelling based on inhibition of cyclooxygenase in the platelet and the vessel wall endothelium. Japan J Hosp Pharmacol 1998;22:133-41.
46. Gierse JK, Koboldt CM, Walker MC, Seibert K, Isakson PC. Kinetic basis for selective inhibition of cyclo-oxygenases. Biochem J 1999;339:607-14.
47. Chan PL, Holford NH. Drug treatment effects on disease progression. Annu Rev Pharmacol Toxicol 2001;41:625-59.
48. Melli M. Assessment of plasma leukotriene and prostaglandin levels during adjuvant arthritis and kaolin-induced paw oedema in rats. Prostaglandins Leukot Essent Fatty Acids 1988;33:173-8.
49. Goff JR, Burkey AR, Goff DJ, Jasmin L. Reorganization of the spinal dorsal horn in models of chronic pain: Correlation with behaviour. Neuroscience 1998;82:559-74.
50. Cryer B, Feldman M. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med 1998;104:413-21.
51. Allen EM, Buss DC, Williams J, Routledge PA. The effect of charcoal on mefenamic acid elimination. Br J Clin Pharmacol 1987; 24:834-2.
52. Bernareggi A. Clinical pharmacokinetics of nimesulide. Clin Pharmacokinet 1998;35:247-74.
53. Borga O, Borga B. Serum protein binding of nonsteroidal antiinflammatory drugs: A comparative study. J Pharmacokinet Biopharm 1997;25:63-77.
54. Brocks DR, Jamali F. Clinical pharmacokinetics of ketorolac tromethamine. Clin Pharmacokinet 1992;23:4152-27.
55. Brocks DR, Jamali F. Etodolac clinical pharmacokinetics. Clin Pharmacokinet 1994;26:259-74.
56. Davies NM. Clinical pharmacokinetics of flurbiprofen and its enantiomers. Clin Pharmacokinet 1995;28:104-14.
57. Helleberg L. Clinical pharmacokinetics of indomethacin. Chin Pharmacokinet 1981;6:245-58.
58. Jamali F, Brocks DR. Clinical pharmacokinetics of ketoprofen and its enantiomers. Clin Pharmacokinet 1990;19:197-217.
59. Olkkola KT, Brunetto AV, Mattila MJ. Pharmacokinetics of oxicam nonsteroidal anti-inflammatory agents. Clin Pharmacokinet 1994;26:107-20.
60. 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; 96:7563-8.
61. US Department of Health and Human Services Food and Drug Administration. Challenge and opportunity on the critical path to new medical products. Washington, DC: US FDA, 2004;1-31.
62. Furberg CD, Psaty BM, FitzGerald GA. Parecoxib, valdecoxib, and cardiovascular risk. Circulation 2005;111:249.
63. Garcia Rodriguez LA, Varas-Loretizo C, Maguire A, Gonzalez-Perez A. Nonsteroidal antiinflammatory drugs and the risk of myocardial infarction in the general population. Circulation 2004; 109:3000-6.
64. Cheng Y, Austin SC, Rocca B et al. Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 2002;296: 539-41.
65. Simon LS, Strand V. A world without Vioxx: To COX-2 or not to COX-2? Cleveland Clin J Med 2004;71:849-50, 852, 854.
66. Lyseng-Williamson KA, Curran MP. Lumiracoxib. Drugs 2004;64: 2237-46.
67. Patrianani P. Lumiracoxib: A viewpoint by Paola Patrignani. Drugs 2004;64:2247-8.
68. Lashbrook JM, Ossipov MH, Hunter JC, Raffa RB, Tallarida RJ, Porreca F. Synergistic antiallodynic effects of spinal morphine with ketorolac and selective. Pain 1999;82:65-72.
69. Hurley RW, Chatterjea D, Rose FM, Taylor CP, Hammond DL. Gabapentin and pregabalin can interact synergistically with naproxen to produce antihyperalgesia. Anesthesiology 2002;97:1263-73.
70. Patel S, Naeem S, Kesingland A et al. The effects, of GABA(B) agonists and gabapentin on mechanical hyperalgesia in models of neuropathic and inflammatory pain in the rat. Pain 2001; 90:217-26.
71. Chan CC, Boyce S, Brideau C er al. 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;290:551-60.
72. Lu Y, Westlund KN. Gabapentin attenuates nociceptive, behaviors in an acute arthritis model in rats. J Pharmacol Exp Ther 1999; 290:214-19.
73. Hunter JC, Gogas KR, Hedley LR et al. The effect of novel anti-epileptic drugs in rat experimental models of acute and chronic pain. Eur J Pharmacol 1997;324:153-60.
74. Jett MF, Ramesha CS, Brown CD et al. Characterization of the analgesic and anti-inflammatory activities of ketorolac and its enantiomers in the rat. J Pharmacol Exp Ther 1999;288:1288-97.
75. Syriatowicz JP, Hu D, Walker JS, Tracey DJ. Hyperalpesia due to nerve injury: Role of prostaglandins. Neuroscience 1999;94:587-94.
76. Inoue K, Fujisawa H, Motonaga A et al. Anti-inflammatory effects of etodolac: Comparison with other non-steroidal anti-inflammatory drugs. Biol Pharm Bull 1994;17:1577-83.
77. Le Bars D, Gozariu M, Cadden SW. Animal models of nociception. Pharmacol Rev 2001;53:597-652.
78. Sandrini M, Vitale G, Pini LA. Effect of rofecoxib on nociception and the serotonin system in the rat brain. Inflamm Res 2002;51:154-9.
79. Torres-Lopez JE, Ortiz MI, Castaneda-Hernandez G, Alonso-Lopez R, Asomoza-Espinosa R, Granados-Soto V. Comparison of the antinociceptive effect of celecoxib, diclofenac and resveratrol in the formalin test. Life Sci 2002;70:1669-76.
80. Tonussi CR, Ferreira SH. Mechanism of diclofenac analgesia: Direct blockade of inflammatory sensitization. Eur J Pharmacol 1994;251:171-9.
81. Malmberg AB, Brandon EP, Idzerda RL, Liu H, McKnight GS, Basbaum AI. Diminished inflammation and nociceptive pain with preservation of neuropathic pain in mice with a targeted mutation of the type I regulatory subunit of cAMP-dependent protein kinase. J Neurosci 1997;17:7462-70.
82. Wang JJ, Ho ST, Hu OY, Chu KM. An innovative cold tail-flick test: The cold ethanol tail-flick test. Anesth Analg 1995;80:102-7.
83. Miranda HF, Sierralta F, Pinardi G. Neostigmine interactions with non steroidal anti-inflammatory drugs. Br J Pharmacol 2002; 135:1591-7.
84. Yamamoto T, Nozaki-Taguchi N. The role of cyclooxygenase-1 and -2 in the rat formalin test. Anesth Analg 2002;94:962-7.
85. Masue T, Dohi S, Asano T, Shimonaka H. Spinal antinociceptive effect of epidural nonsteroidal antiinflammatory drugs on nitric oxide-induced hyperalgesia in rats. Anesthesiology 1999;91:198-206.
86. Ossipov MH, Jerussi TP, Ren K, Sun H, Porreca F. Differential effects of spinal (R)-ketoprofen and (S)-ketoprofen against signs of neuropathic pain and tonic nociception: Evidence for a novel mechanism of action of (R)-ketoprofen against tactile allodynia. Pain 2000;87:193-9.
87. Laird JM, Martinez-Caro L, Garcia-Nicas E, Cervero F. A new model of visceral pain and referred hyperalgesia in the mouse. Pain 2001;92:335-42.
88. Kouya PF, Hao JX, Xu XJ. Buprenorphine alleviates neuropathic pain-like behaviors in rats after spinal cord and peripheral nerve injury. Eur J Pharmacol 2002;450:49-53.
89. Pertovaara A, Wei H. A dissociative change in the efficacy of supraspinal versus spinal morphine in the neuropathic rat. Pain 2003;101:237-50.
90. Huang P, Kehner GB, Cowan A, Liu-Chen LY. Comparison of pharmacological activities of buprenorphine and norbuprenorphine: Norbuprenorphine is a potent opioid agonist. J Pharmacol Exp Ther 2001;297:688-95.
91. Gilbert AK, Franklin KB. The role of descending fibers from the rostral ventromedial medulla in opioid analgesia in rats. Eur J Pharmacol 2002;449:75-84.
92. Lattanzi R, Negri L, Schmidhammer H, Giannini E. Antinociceptive activity of a novel buprenorphine analogue. Life Sci 2002;70:2177-85.
93. Tejwani GA, Rattan AK. The role of spinal opioid receptors in antinociceptive effects produced by intrathecal administration of hydromorphone and buprenorphine in the rat. Anesth Analg 2002;94:1542-6.
94. Klamt JG. Effects of intrathecally administered lamotrigine, a glutamate release inhibitor, on short- and long-term models of hyperalgesia in rats. Anesthesiology 1998;88:487-94.
95. Laughlin TM, Tram KV, Wilcox GL, Birnbaum AK. Comparison of antiepileptic drugs tiagabine, lamotrigine, arid gabapentin in mouse models of acute, prolonged, and chronic nociception. J Pharmacol Exp Ther 2002;302:1168-15.
96. Boyce S, Wyatt A, Webb JK et al. Selective NMDA NR2B antagonists induce antinociception without motor dysfunction: Correlation with restricted localisation of NR2B subunit in dorsal horn. Neuropharmacology 1999;38:611-23.
97. Feng Y, Cui M, Willis WD. Gabapentin markedly reduces acetic acid-induced visceral nociception. Anesthesiology 2003;98:729-33.
98. Chen SR, Eisenach JC, McCaslin PP, Pan HL. Synergistic effect between intrathecal non-NMDA antagonist and gabapentin on allodynia induced by spinal nerve ligation in rats. Anesthesiology 2000;92:500-6.
99. Cheng JK, Pan HL, Eisenach JC (2000) Antiallodynic effect of intrathecal gabapentin and its interaction with clonidine in a rat model of postoperative pain. Anesthesiology 2000;92:1126-31.
100. Dolezal T, Krsiak M. Augmentation of analgesic effect of ibuprofen by alprazolam in experimental model of pain. Physiol Res 2002;51:179-84.
101. Pinardi G, Sierralta F, Miranda HF. Atropine reverses the antinociception of nonsteroidal anti-inflammatory drugs in the tail-flick test of mice. Pharmacol Biochem Behav 2003;74:603-8.
102. Yamamoto T, Nozaki-Taguchi N. Analysis of the effects of cyclooxygenase (COX)-1 and COX-2 in spinal nociceptive transmission using indomethacin, a non-selective COX inhibitor, and NS-398, a COX-2 selective inhibitor. Brain Res 1996;739:104-10.
103. Alsalameh S, Burian M, Mahr G, Woodcock BG, Geisslinger G. Review article: The pharmacological properties and clinical use of valdecoxib, a new cyclo-oxygenase-2-selective inhibitor. Aliment Pharmacol Ther 2003;17:489-501.
104. Ma W, Du W, Eisenach JC. Intrathecal lidocaine reverses tactile allodynia caused by nerve injuries and potentiates the antiallodynic effect of the COX inhibitor ketorolac. Anesthesiology 2003; 98:203-8.
105. Penning TD, Talley JJ, Bertenshaw SR et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of
106. Gupta SK, Bansal P, Bhardwaj RK, Velpandian T. Comparative anti-nociceptive, anti-inflammatory and toxicity profile of nimesulide vs nimesulide and piperine combination. Pharmacol Res 2000;41:657-62.
107. Bianchi M, Panerai AE. Effects of lornoxicam, piroxicam, and meloxicam in a model of thermal hindpaw hyperalgesia induced by formalin injection in rat tail. Pharmacol Res 2002;45:101-5.
108. Jourdan D, Alloui A, Eschalier A. Pharmacological validation of an automated method of pain scoring in the formalin test in rats. J Pharmacol Toxicol Methods 1999;42:163-70.
109. Machado SG, Miller R, Hu C. A regulatory perspective on pharmacokinetic/ pharmacodynamic modelling. Stat Methods Med Res 1999;8:217-45.
110. Niemegeers CJ, Van Bruggen JA, Janssen PA. Suprofen, a potent antagonist of acetic acid-induced writhing in rats. Arzneimittelforschung 1975;25:1505-9.
111. Santos AR, Vedana EM, De Freitas GA. Antinociceptive effect of meloxicam, in neurogenic and inflammatory nociceptive models in mice. Inflamm Res 1998;47:302-7.
112. Domer F. Characterization of the analgesic activity of ketorolac in mice. Eur J Pharmacol 1990;177:127-35.
113. Van Ree JM, Leys A. Behavioral effects of morphine and phencyclidine in rats: The influence of repeated testing before and after single treatment. Eur J Pharmacol 1985;113:353-62.
114. O'Callaghan JP, Holtzman SG. Quantification of the analgesic activity of narcotic antagonists by a modified hot-plate procedure. J Pharmacol Exp Ther 1975;192:497-505.
115. Cowan A, Doxey JC, Harry E.J. The animal pharmacology of buprenorphine, an oripavine analgesic agent. Br J Pharmacol 1977; 60:547-54.
116. Pong SF, Demuth SM, Kinney CM, Deegan P. Prediction of human analgesic dosages of nonsteroidal anti-inflammatory drugs (NSAIDs) from analgesic ED50 values in mice. Arch Int Pharmacodyn Ther 1985;273:212-20.
117. Vitale G, Sandrini M, Pini LA. Lack of activity of ketorolac in hot-plate test and serotonin binding capacity of brain membranes in rats. Agents Actions 1994;41:184-7.
118. Koehn GL, Henderson G, Karczmar AG. Di-isopropyl phospho-fluoridate-induced antinociception: Possible role of endogenous opioids. Eur J Pharmacol 1980;61:167-73.
119. Nakamura H, Shimizu M. Site of analgesic action of a nonsteroidal, anti-inflammatory drug, tolmetin sodium, in rats. Br J Pharmacol 1981;73:779-85.
120. Binder W, Scott C, Walker JS. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline and tire NK1 antagonist GR205171. Eur J Neurosci 1999;11:2065-72.
121. Calza L, Pozza M, Zanni M, Manzini CU, Manzini E, Hokfelt T. Peptide plasticity in primary sensory neurons and spinal cord during adjuvant-induced arthritis in the rat: An immunocytochemical and in situ hybridization study. Neuroscience 1998;82:575-89.
122. Silva JC, Rocha MF, Lima AA, Brito GA, de Menezes DB, Rao VS. Effects of pentoxifylline and nabumetone on the serum levels of IL-1beta and TNFalpha in rats with adjuvant arthritis. Inflamm Res 2000;49:14-19.
123. Panara MR, Padovano R, Sciulli MG et al. Effects of nimesulide on constitutive and inducible prostanoid biosynthesis in human beings. Clin Pharmacol Ther 1998;63:672-81.