Meloxicam
Clinical Particulars
Meloxicam, an NSAID that preferentially inhibits the COX-2 enzyme, is a piroxicam analogue in which the pyridyl group in the amidic part of the molecule was substituted with the 5-methylthiazole system.
Pharmacokinetics
Mechanism of Action
COX Inhibition: Meloxicam preferentially inhibits the COX-2 enzyme.
Clinical Applications
Meloxicam is used in veterinary presentations to alleviate inflammation and pain in acute and chronic musculoskeletal disorders and to reduce post-operative pain and inflammation.
Anti-inflammatory Alleviation of inflammation in both acute and chronic musculoskeletal disorders and the reduction of postoperative inflammation
Analgesia: Mild pain-relieving effects.
Perioperative Use: A component of multimodal analgesia suitable for relieving pain associated with surgery in ASA1, ASA2 and potentially some ASA3 patients of many species. Meloxicam provides effective analgesia, especially in combination with opiates.
Pharmacodynamics
Metabolism
Hepatic: Primarily metabolised by oxidation in the liver in most species. A significant amount of enterohepatic re-circulation occurs.
Species Differences: Rabbits metabolise meloxicam faster than dogs, humans and rats.
Elimination
Faecal | Inactive Metabolites: In dogs and cats, metabolites are generally excreted in faeces.
Precautions
Availability
Identifiers
Systematic Name: [IUPAC Name: 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide]
Formula: C14-H13-N3-O4-S2
Pharmacotherapeutic group: Antiinflammatory and antirheumatic products, non-steroids (oxicams)
ATCvet Code: QM01AC06; QM01AC56 (WHO),
ATC code: M01AC06; M01AC56 (WHO),
Evidence Base
Beretta, C., Garavaglia, G., Cavalli, M., 2005. COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis. Pharmacol. Res. 52, 302–306. https://doi.org/10.1016/j.phrs.2005.04.004
Blois, S.L., Allen, D.G., Wood, R.D., Conlon, P.D., 2010. Effects of aspirin, carprofen, deracoxib, and meloxicam on platelet function and systemic prostaglandin concentrations in healthy dogs. Am. J. Vet. Res. 71, 349–358. https://doi.org/10.2460/ajvr.71.3.349
Busch, U., Schmid, J., Heinzel, G., Schmaus, H., Baierl, J., Huber, C., Roth, W., 1998. Pharmacokinetics of meloxicam in animals and the relevance to humans. Drug Metab. Dispos. 26, 576–584.
Emery, P., 1999. Clinical aspects of COX-2 inhibitors. Drugs Today 35, 267. https://doi.org/10.1358/dot.1999.35.4-5.552202
Engelhardt, G., 1996. Pharmacology of meloxicam, a new non-steroidal anti-inflammatory drug with an improved safety profile through preferential inhibition of COX-2. Br. J. Rheumatol. 35 Suppl 1, 4–12. https://doi.org/10.1093/rheumatology/35.suppl_1.4
Eskafian, H., Shojaee Tabrizi, A., Ansari Lari, M., 2017. Gastroscopic Study of Meloxicam, Tramadol, and Their Combined Administration on the Development of Gastric Injuries in Dogs. Top Companion Anim Med 32, 109–113. https://doi.org/10.1053/j.tcam.2017.09.001
Euller-Ziegler, L., Vélicitat, P., Bluhmki, E., Türck, D., Scheuerer, S., Combe, B., 2001. Meloxicam: a review of its pharmacokinetics, efficacy and tolerability following intramuscular administration. Inflamm. Res. 50 Suppl 1, S5-9. https://doi.org/10.1007/PL00022377
Hawkins, M.G., Karriker, M.J., Wiebe, V., Taylor, I.T., Kass, P.H., 2006. Drug distribution and stability in extemporaneous preparations of meloxicam and carprofen after dilution and suspension at two storage temperatures. Journal of the American Veterinary Medical Association 229, 968–974. https://doi.org/10.2460/javma.229.6.968
Karateev, A.E., 2014. [Meloxicam: the golden mean of nonsteroidal anti-inflammatory drugs]. Ter. Arkh. 86, 99–105.
Morović-Vergles, J., 2008. [Meloxicam--the balance of efficacy and safety]. Reumatizam 55, 85–86.
Mullins, K.B., Thomason, J.M., Lunsford, K.V., Pinchuk, L.M., Langston, V.C., Wills, R.W., McLaughlin, R.M., Mackin, A.J., 2012. Effects of carprofen, meloxicam and deracoxib on platelet function in dogs. Vet Anaesth Analg 39, 206–217. https://doi.org/10.1111/j.1467-2995.2011.00684.x
Naruse, T., Nishida, Y., Ishiguro, N., 2007. Synergistic effects of meloxicam and conventional cytotoxic drugs in human MG-63 osteosarcoma cells. Biomed. Pharmacother. 61, 338–346. https://doi.org/10.1016/j.biopha.2007.02.011
Noble, S., Balfour, J.A., 1996. Meloxicam. Drugs 51, 424–430; discussion 431-432. https://doi.org/10.2165/00003495-199651030-00007
Ogino, K., Hatanaka, K., Kawamura, M., Katori, M., Harada, Y., 1997. Evaluation of Pharmacological Profile of Meloxicam as an Anti-Inflammatory Agent, with Particular Reference to Its Relative Selectivity for Cyclooxygenase-2 Over Cyclooxygenase-1. PHA 55, 44–53. https://doi.org/10.1159/000139511
Türck, D., Roth, W., Busch, U., 1996. A review of the clinical pharmacokinetics of meloxicam. Br. J. Rheumatol. 35 Suppl 1, 13–16. https://doi.org/10.1093/rheumatology/35.suppl_1.13