Pharmacodynamics and enantioselective pharmacokinetics of carprofen in the cat

The pharmacodynamics and enantioselective pharmacokinetics of the arylpropionic acid non-steroidal anti-inflammatory drug, carprofen, were investigated in cats after administration of the racemic mixture (rac-carprofen) at dose rates ranging from 0·7 to 4·0 mg kg −1 intravenously and subcutaneously....

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Veröffentlicht in:Research in veterinary science 1996-03, Vol.60 (2), p.144-151
Hauptverfasser: Taylor, P.M, Delatour, P, Landont, F.M, Deal, C, Pickett, C, Aliabadi, F.Shojaee, Foot, R, Lees, P
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Sprache:eng
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Zusammenfassung:The pharmacodynamics and enantioselective pharmacokinetics of the arylpropionic acid non-steroidal anti-inflammatory drug, carprofen, were investigated in cats after administration of the racemic mixture (rac-carprofen) at dose rates ranging from 0·7 to 4·0 mg kg −1 intravenously and subcutaneously. A low dose of rac-carprofen (0·7 mg kg −1) partially inhibited the rise in skin temperature at a site of acute inflammation but had no effect on the ex vivo synthesis of serum thromboxane (Tx) B 2. A higher dose (4·0 mg kg −1) inhibited oedematous swelling, although the response was statistically significant at only one time, and also reduced the ex vivo synthesis of serum TxB 2 for 12 hours after intravenous injection or 24 hours after subcutaneous injection. The main features of carprofen pharmacokinetics were a low distribution volume, a relatively long elimination half-life, the predominance of the R(−) enantiomer and a bioavailability (after subcutaneous dosing) of 100 per cent and 92 per cent, respectively, after doses of 0·7 and 4·0 mg kg −1. On the basis of these data, it is suggested that a dose of 4·0 mg kg −1 by both intravenous and subcutaneous routes should be evaluated in clinical subjects.
ISSN:0034-5288
1532-2661
DOI:10.1016/S0034-5288(96)90009-0