Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Comparison of Piroxicam Pharmacokinetics and Anti-Inflammatory Effect in Rats after Intra-Articular and Intramuscular Administration

  • Received : 2014.03.25
  • Accepted : 2014.05.15
  • Published : 2014.05.31
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Abstract

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin $E_2$ in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

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References

  1. Altman, R. D. and Moskowitz, R. (1998) Intra-articular sodium hyaluronate (Hyalgan) in the treatment of patients with osteoarthritis of the knee: a randomized clinical trial. J. Rheumatol. 25, 2203-2212.
  2. Ashraf, S., Mapp, P. I. and Walsh, D. A. (2011) Contributions of angiogenesis to inflammation, joint damage, and pain in a rat model of osteoarthritis. Arthritis Rheum. 63, 2700-2710. https://doi.org/10.1002/art.30422
  3. Blagojevic, M., Jinks, C., Jeffery, A. and Jordan, K. P. (2010) Risk factors for onset of osteoarthritis of the knee in older adults: a systematic review and meta-analysis. Osteoarthritis Cartilage 18, 24-33. https://doi.org/10.1016/j.joca.2009.08.010
  4. Buckland-Wright, C. (2004) Subchondral bone changes in hand and knee osteoarthritis detected by radiography. Osteoarthritis Cartilage 18(Suppla A), S10-S19.
  5. Caruso, I., Forcella, E. and Marcazzan, E. (1964) Behavior of the plasma level of indomethacin. Reumatismo 16, 393-403.
  6. Cialdai, C., Giuliani, S., Valenti, C., Tramontana, M. and Maggi, C. A. (2009) Effect of Intra-articular 4-(S)-amino-5-(4-{4-[2,4-dichloro- 3-(2,4-dimethyl-8-quinolyloxymethyl)phenylsulfonamido]-tetrahydro- 2H-4-pyranylcarbonyl} piperazino)-5-oxopentyl](trimethyl)ammonium chloride hydrochloride (MEN16132), a kinin B2 receptor antagonist, on nociceptive response in monosodium iodoacetateinduced experimental osteoarthritis in rats. J. Pharmacol. Exp. Ther. 331, 1025-1032. https://doi.org/10.1124/jpet.109.159657
  7. Colbert, S. T., Curran, E., O'Hanlon, D. M., Moran, R. and McCarroll, M. (1999) Intra-articular tenoxicam improves postoperative analgesia in knee arthroscopy. Can. J. Anaesth. 46, 653-657. https://doi.org/10.1007/BF03013953
  8. Cook, T. M., Tucker, J. P. and Nolan, J. P. (1997) Analgesia after daycase knee arthroscopy: double-blind study of intra-articular tenoxicam, intra-articular bupivacaine and placebo. Br. J. Anaesth. 78, 163-168. https://doi.org/10.1093/bja/78.2.163
  9. Deeks, J. J., Smith, L. A. and Bradley, M. D. (2002) Efficacy, tolerability, and upper gastrointestinal safety of celecoxib for treatment of osteoarthritis and rheumatoid arthritis: systematic review of randomised controlled trials. BMJ 325, 619. https://doi.org/10.1136/bmj.325.7365.619
  10. Elhakim, M., Fathy, A., Elkott, M. and Said, M. M. (1996) Intra-articular tenoxicam relieves post-arthroscopy pain. Acta Anaesthesiol. Scand. 40, 1223-1226. https://doi.org/10.1111/j.1399-6576.1996.tb05554.x
  11. Fernihough, J., Gentry, C., Malcangio, M., Fox, A., Rediske, J., Pellas, T., Kidd, B., Bevan, S. and Winter, J. (2004) Pain related behaviour in two models of osteoarthritis in the rat knee. Pain 112, 83-93. https://doi.org/10.1016/j.pain.2004.08.004
  12. Frean, S. P., Abraham, L. A. and Lees, P. (1999) In vitro stimulation of equine articular cartilage proteoglycan synthesis by hyaluronan and carprofen. Res. Vet. Sci. 67, 183-190. https://doi.org/10.1053/rvsc.1999.0328
  13. Gerwin, N., Hops, C. and Lucke, A. (2006) Intraarticular drug delivery in osteoarthritis. Adv. Drug Deliv. Rev. 58, 226-242. https://doi.org/10.1016/j.addr.2006.01.018
  14. Gupta, A., Axelsson, K., Allvin, R., Liszka-Hackzell, J., Rawal, N., Althoff, B. and Augustini, B. G. (1999) Postoperative pain following knee arthroscopy:the effects of intra-articular ketorolac and/or morphine. Reg. Anesth. Pain Med. 24, 225-230.
  15. Hart, F. D. and Huskisson, E. C. (1984) Non-steroidal anti-inflammatory drugs: Current status and rational therapeutic use. Drugs 27, 232-255. https://doi.org/10.2165/00003495-198427030-00004
  16. Hashizume, M. and Mihara, M. (2009) Desirable effect of combination therapy with high molecular weight hyaluronate and NSAIDs on MMP production. Osteoarthritis Cartilage 17, 1513-1518. https://doi.org/10.1016/j.joca.2009.04.018
  17. Haywood, L., McWilliams, D. F., Pearson, C. I., Gill, S. E., Ganesan, A., Wilson, D. and Walsh, D. A. (2003) Inflammation and angiogenesis in osteoarthritis. Arthritis Rheum. 48, 2173-2177. https://doi.org/10.1002/art.11094
  18. Izdes, S., Orhun, S., Turanli, S., Erkilic, E. and Kanbak, O. (2003) The effects of preoperative inflammation on the analgesic efficacy of intraarticular piroxicam for outpatient knee arthroscopy. Anesth. Analg. 97, 1016-1019.
  19. Janusz, M. J., Hookfin, E. B., Heitmeyer, S. A., Woessner, J. F., Freemont, A. J., Hoyland, J. A., Brown, K. K., Hsieh, L. C. Almstead, N. G., De, B., Natchus, M. G., Pikul, S. and Taiwo, Y. O. (2001) Moderation of iodoacetate-induced experimental osteoarthritis in rats by matrix metalloproteinase inhibitors. Osteoarthritis Cartilage 9, 751-760. https://doi.org/10.1053/joca.2001.0472
  20. Kang, Y., Eger, W., Koepp, H., Williams, J. M., Kuettner, K. E. and Homandberg, G. A. (1999) Hyaluronan suppresses fibronectin fragment- mediated damage to human cartilage explants cultures by enhancing proteoglycan synthesis. J. Orthop. Res., 17, 858-869. https://doi.org/10.1002/jor.1100170611
  21. Kawasaki, K., Ochi, M., Uchio Y, Adachi, N. and Matsusaki, M. (1999) Hyaluronic acid enhances proliferation and chondroitin sulfate synthesis in cultured chondrocytes embedded in collagen gels. J. Cell. Physiol. 179, 142-148. https://doi.org/10.1002/(SICI)1097-4652(199905)179:2<142::AID-JCP4>3.0.CO;2-Q
  22. Knight, A. D. and Levick, J. R. (1984) Morphometry of the ultrastructure of the blood-joint barrier in the rabbit knee. Q. J. Exp. Physiol. 69, 271-288. https://doi.org/10.1113/expphysiol.1984.sp002805
  23. Laake, K., Kjeldaas, L. and Borchgrevink, C. F. (1984) Side-effects of piroxicam (Feldenee). A one-year material of 103 reports from Norway. Acta Med. Scand. 215, 81-83.
  24. Larsen, N. E., Lombard, K. M., Parent, E. G. and Balazs, E. A. (1992) Effect of hylan on cartilage and chondrocyte cultures. J. Orthop. Res. 10, 23-32. https://doi.org/10.1002/jor.1100100104
  25. Lee, S. C., Rha, D. W. and Chang, W. H. (2011) Rapid analgesic onset of intra-articular hyaluronic acid with ketorolac in osteoarthritis of the knee. J. Back Musculoskelet. Rehabil. 24, 31-38.
  26. Magari, K., Miyata, S., Ohkubo, Y., Mutoh, S. and Goto, T. (2003) Calcineurin inhibitors exert rapid reduction of inflammatory pain in rat adjuvant-induced arthritis. Br. J. Pharmacol. 139, 927-934. https://doi.org/10.1038/sj.bjp.0705310
  27. Mihara, M., Higo, S., Uchiyama, Y., Tanabe, K. and Saito, K. (2007) Different effects of high molecular weight sodium hyaluronate and NSAID on the progression of the cartilage degeneration in rabbit OA model. Osteoarthritis Cartilage 15, 543-549. https://doi.org/10.1016/j.joca.2006.11.001
  28. Moreland, L. W. (2003) Intra-articular hyaluronan (hyaluronic acid) and hylans for the treatment of osteoarthritis: mechanisms of action. Arthritis Res. Ther. 5, 54-67.
  29. Morris, E. A., Wilcon, S. and Treadwell, B. V. (1992) Inhibition of interleukin 1-mediated proteoglycan degradation in bovine articular cartilage explants by addition of sodium hyaluronate. Am. J. Vet. Res. 53, 1977-1982.
  30. Okuyama, S. and Aihara, H. (1984) The mode of action of analgesic drugs in adjuvant arthritic rats as an experimental model of chronic inflammatory pain: possible central analgesic action of acidic nonsteroidal antiinflammatory drugs. Jpn. J. Pharmacol. 35, 95-103. https://doi.org/10.1254/jjp.35.95
  31. Owen, S. G., Francis, H. W. and Roberts, M. S. (1994) Disappearance kinetics of solutes from synovial fluid after intra-articular injection. Br. J. Clin. Pharmacol. 38, 349-355. https://doi.org/10.1111/j.1365-2125.1994.tb04365.x
  32. Oztuna, V., Eskandari, M., Bugdayci, R. and Kuyurtar, F. (2007) Intraarticular injection of tenoxicam in osteoarthritic knee joints with effusion. Orthopedics 30, 1039-1042.
  33. Pendleton, A., Arden, N., Dougados, M., Doherty, M., Bannwarth, B., Bijlsma, J. W. J., Cluzeau, F., Cooper, C., Dieppe, P. A., GHYPERL, K. P., Hauselmann, H. J., Herrero-Beaumont, G., Kaklamanis, P. M., Leeb, B., Lequesne, M., Lohmander, S., Mazieres, B., Mola, E. M., Pavelka, K., Serni, U., Swoboda, B., Verbruggen, A. A., Weseloh, G. and Zimmermann-Gorska, I. (2000) EULAR recommendations for the management of knee osteoarthritis: report of a task force of the Standing Committee for International Clinical Studies Including Therapeutic Trials (ESCISIT). Ann. Rheum. Dis. 59, 936-944. https://doi.org/10.1136/ard.59.12.936
  34. Peyron, J. G. (1993) Intrarticular hyaluronan injections in the treatment of osteoarthritis: state of the art review. J. Rheumatol. Suppl. 39,10-15.
  35. Richardson, C. J., Blocka, K. L., Ross, S. G. and Verbeeck, R. K. (1985) Effects of age and sex on piroxicam disposition.Clin. Pharmacol. Ther. 37, 13-18. https://doi.org/10.1038/clpt.1985.4
  36. Sarzi-puttini, P., Cimmino, M. A., Scarpa, R., Caporali, R., Parazzin, F., Zaninelli, A., Atzeni, F. and Canesi, B. (2005) Osteoarthritis: an overview of the disease and its treatment strategies. Semin. Arthritis Rheum. 35, 1-10.
  37. Shimazu, A., Jikko, A., Iwamoto, M., Koike, T., Yan, W., Okada, Y., Shinmei, M., Nakamura, S. and Kato, Y. (1993) Effects of hyaluronic acid on the release of proteoglycan from the cell matrix in rabbit chondrocyte cultures in the presence and absence of cytokines. Arthritis Rheum. 36, 247-253. https://doi.org/10.1002/art.1780360217
  38. Sonoda, M., Harwood, F. L., Wada, Y, Moriya, H. and Amiel, D. (1997) The effects of hyaluronan on the meniscus and on the articular cartilage after partial meniscectomy. Am. J. Sports Med. 25, 755-762. https://doi.org/10.1177/036354659702500606
  39. Unlu, Z., Ay, K. and Tuzun, C. (2006) Comparison of intra-articular tenoxicam and oral tenoxicam for pain and physical functioning in osteoarthritis of the knee. Clin. Rheumatol. 25, 54-61. https://doi.org/10.1007/s10067-005-1136-3
  40. Williams J. A. and Thonar, E. J. M. (1989) Early osteophyte formation after chemically induced articular cartilage injury. Am. J. Sports Med. 17, 7-15. https://doi.org/10.1177/036354658901700102
  41. Yoshimi, E., Kumakura, F., Hatori, C., Hamachi, E., Iwashita, A., Ishii, N., Terasawa, T., Shimizu, Y. and Takeshita, N. (2010) Antinociceptive effects of AS1892802, a novel rho kinase inhibitor, in rat models of inflammatory and noninflammatory arthritis. J. Pharmacol. Exp. Ther. 334, 955-963. https://doi.org/10.1124/jpet.110.167924

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