Products
Mavacoxib is commercially available in the form of chewable tablets for dogs (Trocoxil). It has been approved in many countries since 2009.
Structure and properties
Mavacoxib (C16H11F4N3O2S, Mr = 385.3 g/mol) is a pyrazole benzenesulfonamide that exists as a white to off-white powder. It is nearly insoluble in water at a pH between 1.2 and 6.8. It has a V-shaped structure like other COX-2 inhibitors, which allows it to bind to the Active Site of the enzyme. Mavacoxib is identical to celecoxib (Celebrex, both Pfizer) except for the fluorine group, which carries a methyl group at this site. Because of the fluorine, it is not metabolized, unlike celecoxib, and therefore has a very long duration of action.
Effects
Mavacoxib (ATCvet QM01AH92) has analgesic, anti-inflammatory, and antipyretic properties. The effects are due to selective inhibition of cyclooxygenase-2 and thus prostaglandin synthesis. Because of its very long half-life, it has a long-lasting effect.
Indications
For the treatment of pain and inflammation associated with degenerative joint disease in dogs when continuous treatment for more than one month is indicated.
Dosage
According to the SmPC. Dosage is based on body weight. Mavacoxib is administered immediately before or during the main feeding. It may not be applied daily. Two weeks after the administration of the first dose, another dose is given, then once a month. The maximum duration of treatment is 6.5 months, thus mavacoxib may be administered up to seven times. It has a very long half-life of up to 39 days (in rare cases up to 80 days) and therefore only needs to be given once a month. This represents an advantage in terms of adherence to therapy.
Contraindications
Mavacoxib is contraindicated in hypersensitivity (including to sulfonamides), gastrointestinal disorders, blood clotting disorders, enteropathies with blood or protein loss, impaired renal or hepatic function, congestive heart failure, in breeding, pregnant, or lactating animals. It must not be administered concomitantly with glucocorticoids and NSAIDs. Refer to the drug label for complete precautions.
Interactions
Increased adverse effects (eg, gastrointestinal ulcers) can be expected with concomitant administration of glucocorticoids or NSAIDs. Other interactions are possible with anticoagulants and other strong protein-binding drugs. Since mavacoxib is effective for 1-2 months after administration, attention should be paid to the risk of interactions during this period. Therefore, other NSAIDs should not be given within 1 month of the last administration of mavacoxib.
Adverse effects
Possible adverse effects include vomiting, diarrhea, loss of appetite, bloody diarrhea, tarry stools, apathy, and impaired renal function. Rarely, gastrointestinal ulcers have been reported. In the event of an overdose, symptoms are primarily of the digestive tract.