For Oral Use In Dogs Only
DERAMAXX® (deracoxib) is a non-narcotic, non-steroidal anti-inflammatory drug of the coxib class. DERAMAXX® tablets are round, biconvex, chewable tablets that contain deracoxib formulated with beefy flavoring. The molecular weight of deracoxib is 397.38. The empirical formula is C17-H14-F3-N3-O3-S. Deracoxib is 4-[3-(difluoromethyl)-5-(3-fluoro-4-methoxyphenyl)-1H-pyrazole-1-yl] benzenesulfonamide, and can be termed a diaryl substituted pyrazole.
Parameter
Value
Tmaxa 2 hours
Oral Bioavailability (F)a > 90% at 2 mg/kg
Terminal elimination half-lifeb 3 hours at 2-3 mg/kg
19 hours at 20 mg/kg
Systemic Clearance b ~ 5 ml/kg/min at 2 mg/kg
~ 1.7 ml/kg/min at 20 mg/kg
Volume of Distributionc ~ 1.5 L/kg
Protein binding d > 90%
a Values obtained following a single 2.35 mg/kg dose
b Estimates following IV administration of deracoxib as an aqueous solution
c Based upon a dose of 2 mg/kg of deracoxib
d Based upon in vitro plasma concentrations of 0.1, 0.3, 1.0, 3.0, 10.0 µg/ml
Non-linear elimination kinetics are exhibited at doses above 8 mg/kg/day, at which competitive inhibition of constitutive COX-1 may occur.
Deracoxib is not excreted as parent drug in the urine. The major route of elimination of deracoxib is by hepatic biotransformation producing four major metabolites, two of which are characterized as products of oxidation and o-demethylation. The majority of deracoxib is excreted in feces as parent drug or metabolite.
Large intersubject variability was observed in drug metabolite profiles of urine and feces. No statistically significant differences between genders were observed.
Indications and Usage:
Osteoarthritis Pain and Inflammation:
DERAMAXX® Chewable Tablets are indicated for the control of pain and inflammation associated with osteoarthritis in dogs.
