Correlation between in vitro and in vivo concentration-effect relationships of naproxen in rats and healthy volunteers

British Journal of Pharmacology

Volumn 148, Issue 4, 2006, Pages 396-404

  Huntjens, Dymphy R H ^a   Spalding, David J M ^b   Danhof, Meindert ^a   Della Pasqua, Oscar E ^a,b  

^a LEIDEN UNIVERSITY   (Netherlands)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Biomarkers PK PD modelling NONMEM; COX inhibitors; Naproxen; NSAIDs

Indexed keywords

NAPROXEN; PROSTAGLANDIN E2; PROSTAGLANDIN SYNTHASE INHIBITOR; THROMBOXANE B2;

ANIMAL EXPERIMENT; ARTICLE; BLOOD CLOTTING; CONCENTRATION RESPONSE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG RESPONSE; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; MALE; MEASUREMENT; NONHUMAN; NORMAL HUMAN; PRIORITY JOURNAL; RAT; SPECIES DIFFERENCE; VOLUNTEER;

ADULT; ANIMALS; BLOOD PROTEINS; CYCLOOXYGENASE 1; CYCLOOXYGENASE INHIBITORS; DINOPROSTONE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MALE; NAPROXEN; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; THROMBOXANE B2;

EID: 33745106368     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706737     Document Type: Article

References (27)

1. BORGA, O. & BORGA, B. (1997). Serum protein binding of nonsteroidal antiinflammatory drugs: a comparative study. J. Pharmacokinet. Biopharm., 25, 63-77.
2. DERENDORF, H., LESKO, L.J., CHAIKIN, P., COLBURN, W.A., LEE, P., MILLER, R., POWELL, R., RHODES, G., STANSKI, D. & VENITZ, J. (2000). Pharmacokinetic/pharmacodynamic modeling in drug research and development. J. Clin. Pharmacol., 40, 1399-1418.
3. EGAN, K.M., WANG, M., LUCITT, M.B., ZUKAS, A.M., PURE, E., LAWSON, J.A. & FITZGERALD, G.A. (2005). Cyclooxygenases, thromboxane, and atherosclerosis: plaque destabilization by cyclooxygenase-2 inhibition combined with thromboxane receptor antagonism. Circulation, 111, 334-342.
4. ETTE, E.I., WILLIAMS, P.J., KIM, Y.H., LANE, J.R., LIU, M.J. & CAPPARELLI, E.V. (2003). Model appropriateness and population pharmacokinetic modeling. J. Clin. Pharmacol., 43, 610-623.
5. FELDMAN, M., SHEWMAKE, K. & CRYER, B. (2000). Time course inhibition of gastric and platelet COX activity by acetylsalicylic acid in humans Am. J. Physiol. Gastrointest. Liver Physiol., 279, G1113-G1120.
6. GABAY, C. & KUSHNER, I. (1999). Acute-phase proteins and other systemic responses to inflammation. N. Engl. J. Med., 340, 448-454.
7. GIERSE, J.K., KOBOLDT, C.M., WALKER, M.C., SEIBERT, K. & ISAKSON, P.C. (1999). Kinetic basis for selective inhibition of cyclooxygenases. Biochem. J., 339 (Part 3), 607-614.
8. GIULIANO, F. & WARNER, T.D. (2002). Origins of prostaglandin E2: involvements of cyclooxygenase (COX)-1 and COX-2 in human and rat systems. J. Pharmacol. Exp. Ther., 303, 1001-1006.
9. HASSAN-ALIN, M., NAESDAL, J., NILSSON-PIESCHL, C., LÅNGSTRÖM, G. & ANDERSSON, T. (2005). Lack of pharmacokinetic interaction between esomeprazole and the nonsteroidal antiinflammatory drugs naproxen and rofecoxib in healthy subjects. Clin. Drug Invest., 25, 731-740.
10. HUNTJENS, D.R., DANHOF, M. & DELLA PASQUA, O.E. (2005). Pharmacokinetic-pharmacodynamic correlations and biomarkers in the development of COX-2 inhibitors. Rheumatology (Oxford), 44, 846-859.
11. JOSA, M., URIZAR, J.P., RAPADO, J., DIOS-VIEITEZ, C., CASTANEDA-HERNANDEZ, G., FLORES-MURRIETA, F., RENEDO, M.J. & TROCONIZ, I.F. (2001). Pharmacokinetic/pharmacodynamic modeling of antipyretic and anti-inflammatory effects of naproxen in the rat. J. Pharmacol. Exp. Ther., 297, 198-205.
12. LEE, Y., RODRIGUEZ, C. & DIONNE, R.A. (2005). The role of COX-2 in acute pain and the use of selective COX-2 inhibitors for acute pain relief. Curr. Pharm. Des., 11, 1737-1755.
13. LIN, J.H., COCCHETTO, D.M. & DUGGAN, D.E. (1987). Protein binding as a primary determinant of the clinical pharmacokinetic properties of non-steroidal anti-inflammatory drugs. Clin. Pharmacokinet., 12, 402-432.
14. MANCINI, J.A., BLOOD, K., GUAY, J., GORDON, R., CLAVEAU, D., CHAN, C.C. & RIENDEAU, D. (2001). Cloning, expression, and up-regulation of inducible rat prostaglandin e synthase during lipopolysaccharide-induced pyresis and adjuvant-induced arthritis. J. Biol. Chem., 276, 4469-4475.
15. MARTINEZ, R.V., REVAL, M., CAMPOS, M.D., TERRON, J.A., DOMINGUEZ, R. & LOPEZ-MUNOZ, F.J. (2002). Involvement of peripheral cyclooxygenase-1 and cyclooxygenase-2 in inflammatory pain. J. Pharm. Pharmacol., 54, 405-412.
16. PANARA, M.R., PADOVANO, R., SCIULLI, M.G., SANTINI, G., RENDA, G., ROTONDO, M.T., PACE, A., PATRONO, C. & PATRIGNANI, P. (1998). Effects of nimesulide on constitutive and inducible prostanoid biosynthesis in human beings. Clin. Pharmacol. Ther., 63, 672-681.
17. PANARA, M.R., RENDA, G., SCIULLI, M.G., SANTINI, G., DI GIAMBERARDINO, M., ROTONDO, M.T., TACCONELLI, S., SETA, F., PATRONO, C. & PATRIGNANI, P. (1999). Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects. J. Pharmacol. Exp. Ther., 290, 276-280.
18. PATRIGNANI, P., PANARA, M.R., SCIULLI, M.G., SANTINI, G., RENDA, G. & PATRONO, C. (1997). Differential inhibition of human prostaglandin endoperoxide synthase-1 and -2 by nonsteroidal anti-inflammatory drugs. J. Physiol. Pharmacol., 48, 623-631.
19. PATRIGNANI, P., TACCONELLI, S., SCIULLI, M.G. & CAPONE, M.L. (2005). New insights into COX-2 biology and inhibition. Brain Res. Brain Res. Rev., 48, 352-359.
20. PATRONO, C., CIABATTONI, G., PATRIGNANI, P., PUGLIESE, F., FILABOZZI, P., CATELLA, F., DAVI, G. & FORNI, L. (1985). Clinical pharmacology of platelet cyclooxygenase inhibition. Circulation, 72, 1177-1184.
21. SATTERWHITE, J.H. & BOUDINOT, F.D. (1988). High-performance liquid chromatographic determination of ketoprofen and naproxen in rat plasma. J. Chromatogr., 431, 444-449.
22. SATTERWHITE, J.H. & BOUDINOT, F.D. (1991). Age- and dose-dependent naproxen disposition in Fischer 344 rats. J. Gerontol., 46, B222-B227.
23. SATTERWHITE, J.H. & BOUDINOT, F.D. (1995). Effects of age on the pharmacodynamics of naproxen in the rat. Exp. Gerontol., 30, 505-515.
24. VANE, J. (1994). Towards a better aspirin. Nature, 367, 215-216.
25. VANE, J.R. (1971). Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nat. New Biol., 231, 232-235.
26. VANE, J.R. & BOTTING, R.M. (2001). Formation and actions of prostaglandins and inhibition of their synthesis. In: Therapeutic Roles of Selective COX-2 Inhibitors, eds. Vane, J.R. & Botting, R.M. pp. 1-47. London: Willian Harvey Press.
27. WARNER, T.D., GIULIANO, F., VOJNOVIC, I., BUKASA, A., MITCHELL, J.A. & VANE, J.R. (1999). Nonsteroid drug selectivities for cyclooxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc. Natl. Acad. Sci. U.S.A. 96, 7563-7568.