Deracoxib Chewable: Product Information

DERACOXIB CHEWABLE- deracoxib tablet
DERACOXIB — deracoxib tablet
BUTLER ANIMAL HEALTH SUPPLY, LLC DBA COVETRUS NORTH AMERICA

Caution:

Federal Law (U.S.) restricts this drug to use by or on the order of a licensed veterinarian.

Description:

Deracoxib Chewable Tablets is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Deracoxib Chewable Tablets are round, light brown colored, 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. The structural formula is:

Clinical Pharmacology

Mode of Action:

Deracoxib Chewable Tablets are a member of the coxib class of non-narcotic, nonsteroidal, cyclooxygenase-inhibiting anti-inflammatory drugs for the control of postoperative pain and inflammation associated with orthopedic and dental surgery and for the control of pain and inflammation associated with osteoarthritis in dogs.

Data indicate that deracoxib inhibits the production of PGE1 and 6-keto PGF1 by its inhibitory effects on prostaglandin biosynthesis.¹ Deracoxib inhibited COX-2 mediated PGE2 production in LPS-stimulated human whole blood.²

Cyclooxygenase-1 (COX-1) is the enzyme responsible for facilitating constitutive physiological processes (e.g., platelet aggregation, gastric mucosal protection, renal perfusion).³ Cyclooxygenase-2 (COX-2) is responsible for the synthesis of inflammatory mediators.⁴ Both COX isoforms are constitutively expressed in the canine kidney.⁵ At doses of 2-4 mg/kg/day, deracoxib tablets do not inhibit COX-1 based on in vitro studies using cloned canine cyclooxygenase.⁶ The clinical relevance of this in vitro data has not been shown.

Although the plasma terminal elimination half-life for deracoxib tablets is approximately 3 hours, a longer duration of clinical effectiveness is observed.

Summary pharmacokinetics of deracoxib tablets are listed in Table 1.

Table 1: Pharmacokinetics of Deracoxib

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 Clearanceb	~ 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 bindingd	> 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:

Always provide “Information for Dog Owners” Sheet with prescription. Carefully consider the potential benefits and risk of Deracoxib Chewable Tablets and other treatment options before deciding to use Deracoxib Chewable Tablets. Use the lowest effective dose for the shortest duration consistent with individual response.

Osteoarthritis Pain and Inflammation:

Deracoxib Chewable Tablets are indicated for the control of pain and inflammation associated with osteoarthritis in dogs.

Dosage and Administration:
Osteoarthritis Pain and Inflammation: 0.45 – 0.91 mg/lb/day (1 to 2 mg/kg/ day) as a single daily dose, as needed.
Dogs needing a dose of less than 12.5 mg can only be accurately dosed through use of the 12 mg tablet, which can be broken in half to provide 6 mg. Do not attempt to accurately dose smaller dogs through the use of breaking larger tablets. Inaccurate dosing may result in adverse drug events (see Adverse Reactions, Animal Safety, and Post-Approval Experience).

Postoperative Orthopedic Pain and Inflammation:

Deracoxib Chewable Tablets are indicated for the control of postoperative pain and inflammation associated with orthopedic surgery in dogs.

Dosage and Administration:
Postoperative Orthopedic Pain and Inflammation: 1.4 – 1.8 mg/lb/day (3 to 4 mg/kg/day) as a single daily dose, as needed, not to exceed 7 days of administration.
Dogs needing a dose of less than 12.5 mg can only be accurately dosed through use of the 12 mg tablet, which can be broken in half to provide 6 mg. Do not attempt to accurately dose smaller dogs through the use of breaking larger tablets. Inaccurate dosing may result in adverse drug events (see Adverse Reactions, Animal Safety, and Post-Approval Experience).

Postoperative Dental Pain and Inflammation:

Deracoxib Chewable Tablets are indicated for the control of postoperative pain and inflammation associated with dental surgery in dogs.

Dosage and Administration:
Postoperative Dental Pain and Inflammation: 0.45 – 0.91 mg/lb/day (1 to 2 mg/kg/day) as a single daily dose, for 3 days.

The first dose should be given approximately 1 hour prior to dental surgery and subsequent doses should be given daily for up to two additional treatments.
Dogs needing a dose of less than 12.5 mg can only be accurately dosed through use of the 12 mg tablet, which can be broken in half to provide 6 mg. Do not attempt to accurately dose smaller dogs through the use of breaking larger tablets. Inaccurate dosing may result in adverse drug events (see Adverse Reactions, Animal Safety, and Post-Approval Experience). Since deracoxib tablet bioavailability is greatest when taken with food, postprandial administration is preferable. However, deracoxib tablets have been shown to be effective under both fed and fasted conditions; therefore, they may be administered in the fasted state if necessary. For postoperative orthopedic and dental pain, administer Deracoxib Chewable Tablets prior to the procedure. Tablets are scored and dosage should be calculated in half-tablet increments. In clinical practice it is recommended to adjust the individual patient dose while continuing to monitor the dog’s status until a minimum effective dose has been reached.

Contraindications:

Dogs with known hypersensitivity to deracoxib should not receive Deracoxib Chewable Tablets.

Warnings:

Not for use in humans. Keep this and all medications out of reach of children. Consult a physician in case of accidental ingestion by humans. For use in dogs only. Do not use in cats.

Dogs needing a dose of less than 12.5 mg can only be accurately dosed through use of the 12 mg tablet, which can be broken in half to provide 6 mg. Do not attempt to accurately dose smaller dogs through the use of breaking larger tablets. Inaccurate dosing may result in adverse drug events (see Adverse Reactions, Animal Safety, and Post-Approval Experience).

All dogs should undergo a thorough history and physical examination before the initiation of NSAID therapy. Appropriate laboratory tests to establish hematological and serum biochemical baseline data prior to, and periodically during, administration of any NSAID is recommended. Owners should be advised to observe for signs of potential drug toxicity (see Adverse Reactions, Animal Safety and Post-Approval Experience) and be given an “Information for Dog Owners” Sheet.

Keep Deracoxib in a secure location out of reach of dogs, cats, and other animals to prevent accidental ingestion or overdose.