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Pharmacological particulars
Pharmacotherapeutic group: Anti-inflammatory and anti-rheumatic products, Propionic acid derivatives.
ATCvet code: QM01AE91
Pharmacodynamic properties
Carprofen (CPF), (±)-6-chloro-α-methylcarbazole-2-acetic acid, is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and anti-pyretic properties. It is a derivative of phenylpropionic acid and a member of the arylpropionic acid class of NSAIDs. As a representative of the 2-arylpropionic family, it contains a chiral center at C2 of the propionic moiety and therefore, exists in 2 sterioisomeric forms, the (+)-S and (-)-R enantiomers.
In vitro studies have shown carprofen to be a cyclo-oxygenase inhibitor. However, the inhibition of prostaglandin synthesis by carprofen is slight in relation to its anti-inflammatory and analgesic potency. The precise mode of action is unclear.
Studies have shown that carprofen has potent antipyretic activity and significantly reduces the inflammatory response in lung tissue in cases of acute, pyrexic infectious disease in cattle.
Pharmacokinetic properties
After a single subcutaneous administration of the product at 1.4 mg carprofen per kilogram bodyweight the maximum plasma concentration (Cmax) of 10.4 μg/ml was reached after (Tmax) 7.2 hours.
Carprofen is highly bound to plasma proteins. It is well distributed in the tissues with the highest concentrations found in kidney and liver followed by fat and muscle. Carprofen has a plasma elimination half-life of 70 hours. Carprofen is eliminated primarily in the faeces, indicating that the biliary secretion plays an important role.
Metabolism: Carprofen (parent) is the main component in all tissues. Carprofen (parent compound) is slowly metabolised primarily by ring hydroxylation, hydroxylation at the α-carbon and by conjugation of the carboxylic acid group with glucuronic acid. The 8-hydroxylated metabolite and unmetabolised carprofen predominate in the faeces. Bile samples are comprised of conjugated carprofen.