Carprofen

Carprofen belongs to the non-steroidal anti-inflammatory drugs and shows anti-inflammatory, analgesic and antipyretic effects. In veterinary medicine, it is used as an adjuvant in treatment to relieve (inflammatory) joint disease and pain following surgery.

Previously, it was also used in human medicine until 1995, but for commercial reasons it was withdrawn and is no longer marketed for human use.

Pharmacodynamics

The effect of the drug is based on the inhibition of the enzyme cyclooxygenase (COX), which catalyzes the metabolization of arachidonic acid to prostaglandins and other eicosanoids. These eicosanoids, particularly prostacyclin and thromboxane, are significantly involved in inflammatory processes.

In mammals, two cyclooxygenases are of considerable importance. COX-1 is responsible for synthesizing prostaglandins, which are important for normal gastrointestinal and renal function, whereas COX-2 produces prostaglandins, which are pro-inflammatory. Thus, inhibition of COX-1 produces gastrointestinal and renal toxicity, while inhibition of COX-2 produces anti-inflammatory effects.
Es wird davon ausgegangen, dass die Hemmung der COX-2 nur ca. 1,75-fach stärker ist als die der COX-1.

Furthermore, carprofen exerts a direct beneficial effect on canine cartilage cells by stimulating the formation of glycosaminoglycans (important components of connective tissue).

Pharmacokinetics

Orally administered carprofen is more than 90% bioavailable and is rapidly and almost completely absorbed by the organism. The drug circulates in a 99% protein-bound manner and has a half-life of approximately 8 hours (in dogs).
Nach der Verstoffwechselung in der Leber wird der Großteil mit dem Kot und der Rest mit dem Urin ausgeschieden.

Interactions

Avoid concomitant administration of other agents that are also highly protein-bound, such as phenytoin, anticoagulants, salicylates, sulfonamides, ACE inhibitors, and antidiabetics.

Side effects

Mainly, side effects such as gastrointestinal pain and nausea, renal and hepatic disorders occur after the administration of carprofen.

Toxicological data

Overdose of non-steroidal anti-inflammatory drugs may cause dizziness and uncontrollable rhythmic eye movements.
LD50 (Maus, oral): 282 mg/kg
LD50 (Ratte, oral): 149 mg/kg