Metabolism of carprofen, a nonsteroidal anti-inflammatory agent, in rats, dogs, and humans

Influence of the Hydrophilicity of Suppository Bases on Rectal Absorption of Carprofen, a Lipophilic Nonsteroidal Anti-Inflammatory Drug

“…4 Enterohepatic circulation has been proposed as an explanation of the plateau in concentra-tions after carprofen administration and of the prolonged elimination of this NSAID. This observation has already been made previously in dogs.…”

In vitro effect of carprofen and meloxicam on the conductance and permeability to mannitol and the histologic appearance of the gastric mucosa of dogs

“…17 In dogs, biliary secretion predominates; following IV administration, 70% of a dose of carprofen is excreted in feces and 8% to 15% of that dose is excreted in urine. The 2 drugs have basic differences in their chemical composition.…”

“…10 The NSAID carprofen a is a propionic acid derivative. 17,18 The enolic acid NSAID meloxicam b is COX-2 selective and is 12 times as selective for COX-2 as it is for COX-1 in dogs. 15,16 Carprofen is highly protein bound in the blood and undergoes hepatic metabolism before being secreted in the bile into the duodenum, which allows enterohepatic recirculation.…”

In vitro stereoselective degradation of carprofen glucuronide by human serum albumin. Characterization of sites and reactive amino acids

“…4 rac-Carprofen [(±)-2-(6-chlorocarbazol-2-yl)-propionic acid] is a chiral nonsteroidal antiinflammatory drug (NSAID), mainly metabolized to the acyl glucuronide in man, dog, and rat. 14 Carprofen glucuronides were found in urine, accounting for 70% of the dose administered to man, 14 and in plasma their concentration approached that of carprofen. 15 Severe adverse reactions, such as photoallergic 16 and phototoxic reactions 17 have been reported with carprofen, but the pathogenesis of these side effects is still unknown.…”