Pharmacotherapeutic group: Anti-inflammatory and Antirheumatic Products, Non- Steroids, Propionic acid derivatives,
ATC vet code: QM01AE03
Pharmacodynamic properties
Ketoprofen, 2-(phenyl 3-benzoyl) propionic acid is a non-steroidal anti-inflammatory drug belonging to the arylpropionic acid group. The primary mechanism of action for ketoprofen is considered to be inhibition of the cyclooxygenase pathway of arachidonic acid metabolism, leading to decreased production of inflammatory mediators, such as prostaglandins and thromboxanes. This mechanism of action results in its anti-inflammatory, anti-pyretic and analgesic activity. These properties are also attributed to its inhibiting effect on bradykinin and superoxide anions together with its stabilizing action on lysosomal membranes.
The antiinflammatory effect is enhanced by the conversion of the (R)-enantiomer to (S)-enantiomer. It is known that the (S)-enantiomer supports the ant-inflammatory effect of ketoprofen.
Pharmacokinetic particulars
After intramuscular administration of the product (single dose of 3 mg ketoprofen/kg body weight), ketoprofen is rapidly absorbed, and has a high bioavailability.
Ketoprofen binds extensively to plasma proteins (>90%).
The concentrations of Ketoprofen are more sustained in inflammatory exudates than in plasma. It reaches high concentrations and persists in inflamed tissue, due to the fact that Ketoprofen is a weak acid. Ketoprofen is metabolized in the liver to inactive metabolites and it is excreted mainly in urine (primarily as glucuroconjugated metabolites) and, to a lesser extent, in faeces. Small amounts of ketoprofen can be detected in the milk of treated animals.
In cattle, following the intramuscular administration of the product (single dose of 3 mg ketoprofen/kg body weight), the active drug substance is rapidly absorbed, reaching its average Cmax in plasma (mean value: 7.2 μg/ml) between 0.5 and 1 hour (tmax) after initiation of treatment. The fraction of dose absorbed is very high (92,51±10,9%)
Following the intravenous administration in cattle, elimination half-life (t1/2) is of 2.1 h. The distribution volume (Vd) of 0.41 L/kg, and plasma clearance (Cl) of 0.14 L/h/kg.
In pigs, following the intramuscular injection of a single dose of 3 mg/ketoprofen/kg body weight, the active drug substance is rapidly absorbed, reaching its average Cmax in plasma (mean value: 16 μg/ml) between 0.25 and 1.5h (tmax) after initiation of the treatment. The fraction of dose absorbed is 84.7±33%.
Following the intravenous administration in pigs, elimination half-life (t1/2) is of 3.6 h. The distribution volume (Vd) of 0.15 L/kg, and plasma clearance (Cl) of 0.03 L/h/kg.
Ketoprofen also shows a low volume of distribution when administered by the intravenous route in equine species.