Carprofen:

  • It is newly developed propionic acid derivative NSAID
  • Insoluble in water but soluble in ethanol

MOA:

  • It is principally COX-2 inhibitor with less interference with activity of COX-1 enzyme
  • Inhibition of phospholipase enzyme and impaired release of arachidonic acid

Pharmacological effects:

  • It exhibits analgesic, anti-inflammatory and anti-pyretic effects.

Pharmacokinetics:

  • It is well-absorbed following oral administration ~90% and peak serum levels occur between 1-3 hours post dosing in dogs
  • It is highly bound to plasma protein (90%) and has low volume of distribution.
  • It is metabolized mainly in liver by oxidation and glucuronide conjugation
  • It is excreted in feces (70-80%) and urine (10-20%)
  • Elimination half-life:
    • Dogs= 8-15 hrs
    • Horses = 22 hours
    • Cats = 15-20 hours
    • Man= 1-2 hours

Side effects/Adverse effects:

  • Few side effects than other NSAID
  • Hepatocellular damage, renal disease and GI disorder may occur rarely
  • Gastritis and ulcer formation in excess use

Drug Interactions:

  • It shouldnot be used along with other nephrotoxic drugs
  • Concurrent use of aspirin or other potent NSAID may enhance the ulcerogenic effect of carprofen
  • It also shows displacement drug interactions.

Clinical Uses:

  • For pain and inflammation in dogs
  • Osteoarthritis in dog
  • Control of surgical pain
  • Calf pneumonia in suppressing edema

Dose:

  • Dogs: 2-4 mg/kg, PO in divided dose for 7 days, then 2 mg/kg, OD
  • Dog and cats: 4 mg/kg, SC or IV as single dose
  • Cats: 0.5 mg/kg, PO, OD for long-term use
  • Horses: 0.7 mg/kg, PO, OD x 4-9 days, IV as single dose
  • Cattle: 1.4 mg/kg, SC or IV as single dose
  • Swine: 2-4 mg/kg, IV, OD

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