Meloxicam SR 5ml - 2mg/ml
ZooPharm can provide extended release Meloxicam SR by prescription in a patented, sustained release system. Meloxicam SR releases and provides therapeutic blood levels for up to 72 hours
Meloxicam is used in dogs, rats, mice, rabbits, primates and other species for relief of inflammation and pain in both acute and chronic musculo-skeletal disorders. Meloxicam is often used to reduce postoperative pain and inflammation following orthopaedic, soft tissue and other surgical procedures.
Meloxicam is an NSAID of the oxicam class that acts by inhibiting prostaglandin synthesis and inducible COX-2, thereby exerting antiinflammatory, anti-exudative, analgesic and antipyretic effects.The molecule is highly plasma protein bound, when circulating in the body (95-99%). It has a long plasma half-life, enabling less frequent dosage schemes.4,5,6
Compared to several other NSAID´s tested, meloxicam was shown to be the most selective inhibitor of inducible cyclo-oxygenase activity. Primary pharmacological effects include anti-inflammatory, anti-pyretic and analgesic properties in several species including humans, probably due to inhibition of inducible cyclo-oxygenase.7
Tissue reactions after a single subcutaneous injection of meloxicam was studied in rats. The tolerance after i.v., i.m., and s.c. injection and after dermal, rectal, and eye-drop application of a meloxicam formulation was also studied in several laboratory animals (rats, guinea pigs and rabbits). The total composition of the formulation used is not given, but it is stated that the formulation was one intended for human use. The conclusions reported from these study data indicated that the meloxicam injectable formulation was well tolerated.7
Its chemical name is 4-Hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide
The pharmacokinetic behavior of meloxicam after a single dose was elucidated in an intravenous pilot study in calves with radiolabelled meloxicam and in a bioavailability study in calves with administration of 0.5% injectable meloxicam solution via the IV and SC route in a cross-over design. The Cmax of meloxicam from the SC administration was reached after 6 to 8 hours. The absolute availability was variable with values ranging from 44 to 154 % in individual animals. The mean elimination half-life of meloxicam from plasma was approximately 26 hours irrespective of the route of administration. Elimination of total radioactivity from plasma exhibited a terminal half-life of approximately 24 hours. Plasma protein binding ex vivo was found to be > 96.5 % and the same degree of binding was found in vitro.
At all sacrifice time points investigated in the pilot study, the liver contained the highest concentration followed by the kidney and bile. Comparatively low concentrations were found in skeletal muscle and fat. The proportions of radioactivity excreted in the urine and the feces were approximately equal (46%) and excretion was completed after 6 days. Only trace quantities of parent compound were found in the urine.7
Meloxicam SR is available from ZooPharm by prescription in vials containing 5 ml volume of the formulation, in a sustained release biodegradable matrix (at a concentration of 2 mg/ml).
Contraindications and Precautions:
Although meloxicam is COX-2 selective, at higher doses its specificity is diminished and more GI distress may be seen.1,5GI distress is usually transient and subsides with a dose decrease or termination of therapy.6 The use of meloxicam is contraindicated during pregnancy and lactation.6,7Meloxicam should not be used in dogs younger than 6 weeks of age.6Use is also contraindicated in animals suffering from GI disorders or impaired hepatic, cardiac, or renal function.1,5,6
Extreme caution should be used in animals that are dehydrated, hypovolemic, or hypotensive because there is an increased risk of renal toxicity.5,6
CONTRAINDICATIONS: Meloxicam SR is contraindicated for use in cats.
Meloxicam is highly protein bound; therefore, it can be displacedby other highly protein-bound drugs such as warfarin and phenylbutazone, resulting in toxicity.5,,6 Because meloxicam may inhibit platelet aggregation and also cause GI ulceration, it should not be used with other drugs that alter hemostasis or cause GI ulceration, including heparin, warfarin, aspirin, flunixin, phenylbutazone, and corticosteroids.5Meloxicam may antagonize the antihypertensive effects of angiotensin-converting enzyme inhibitors.5
- Ulrich Busch, Jochen Schmid, Gu¨ Nther Heinzel, Helmut Schmaus, Ju¨ Rgen Baierl, Claudia Huber, Willy Roth Pharmacokinetics of meloxicam in animals and the relevance to human. Drug Metabolism And Disposition, The American Society for Pharmacology and Experimental Therapeutics, 1998 Vol. 26, No. 6
- David Fowler, Kevin Isakow, Nigel Caulkett, Cheryl Waldner, An evaluation of the analgesic effects of meloxicam in addition to epidural morphine/mepivacaine in dogs undergoing cranial cruciate ligament repair. Can Vet J Volume 44, August 2003
- Laboratory Study: Pharmacokinetic Properties Of A Novel Sustained Release Meloxicam Formulation in Dogs. September 2012
- Friton GM, Philipp H, Schneider T & Kleemann R (2003), Berl Munch Tierärztl Woch, 116: 421-426
- Hirsch AC, Philipp H & Kleemann R (2003), J Vet Pharm Ther, 26: 355-360
- Papatsas I, Georgoulakis IE, Filiousis G, Alexopoulos G & Kyriakis SC (2004), Proc 18th IPVS Congress, p
- Meloxicam Report Committee of Veterinary Medicinal Products (CVMP), European Medicines Agency, 2010.
- Papich MG: Saunders Handbook of Veterinary Drugs. Philadelphia, WB Saunders,2002, p 318.
- Plumb DC: Veterinary Drug Handbook, ed 4. Ames, Iowa State University Press, 2002, pp 516–517.
- The European Agency for the Evaluation of Medicinal Products. Available at: www.emea.eu.int; accessed December 9, 2002.
- Stephane L Bourque,Michael A Adams,Kanji Nakatsu and Andrew Winterborn. Comparison of Buprenorphine and Meloxicam for Postsurgical Analgesia in Rats: Effects on Body Weight, Locomotor Activity and Hemodynamic Parameters. Journal of the American Association for Laboratory Animal Science Vol 49, No 5 September 2010
- Matthew T Rätsep, Valerie F Barrette, Andrew Winterborn, Michael A Adams, and B Anne Croy. Hemodynamic and Behavioral Differences after Administration of Meloxicam, Buprenorphine, or Tramadol as Analgesics for Telemeter Implantation in Mice. Journal of the American Association for Laboratory Animal Science. Vol 52, No 5. September 2013