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Pharmacodynamic properties were evaluated using a model of acute inflammation, comprising subcutaneously implanted tissue cages stimulated by intracaveal injection of carrageenan.<\/jats:p><jats:p>Chiral inversion of (R)\u2010KTP to the (S)\u2010antipode occurred. The R:S ratio in plasma was 33:15 min after administration, decreasing to 1:1 at 8 h. The calculated extent of inversion was 31 \u00b1 7%. The R:S ratio in inflammatory exudate was of the order 3:1 at all the sampling times and the ratio in transudate was approximately 2:1 for 6 h, declining to 1:1 at 30 h. Only (S)\u2010KTP was detected in biological fluids after administration of this enantiomer. Elimination half\u2010life was longer for the (S) (2.19 h) than the (R)\u2010enantiomer (1.30 h) and volume of distribution was also somewhat higher for the (S)\u2010enantiomer. Body clearance values were 0.119 1\/kg\/h for (S)\u2010KTP and 0.151 1\/kg\/h for the (R)\u2010antipode. For (R)\u2010KTP effects obtained were considered as a hybrid, since they potentially reflect the actions of both enantiomers. Concentrations of LTB<jats:sub>4<\/jats:sub>and the cytokines interleukin\u20101, interleukin\u20106, and tumor necrosis factor alpha, in exudate were not significantly affected by either (R)\u2010 or (S)\u2010KTP treatments. Inhibition of ex vivo thromboxane B<jats:sub>2<\/jats:sub>(TxB<jats:sub>2<\/jats:sub>) synthesis, exudate prostaglandin E<jats:sub>2<\/jats:sub>(PGE<jats:sub>2<\/jats:sub>) synthesis, \u03b2\u2010glucuronidase release (\u03b2\u2010glu), and bradykinin\u2010induced skin swelling was significant in both treated groups. PK\/PD modelling was applied to the (S)\u2010KTP treatment only. EC<jats:sub>50<\/jats:sub>values for inhibition of serum TxB<jats:sub>2<\/jats:sub>, exudate PGE<jats:sub>2<\/jats:sub>and \u03b2\u2010glu and BK\u2010induced swelling were 0.047, 0.042, 0.101, and 0.038 \u03bcg\/ml, respectively. It is concluded that the low EC<jats:sub>50<\/jats:sub>values for inhibition of TxB<jats:sub>2<\/jats:sub>and PGE<jats:sub>2<\/jats:sub>by (S)\u2010KTP are likely to explain the effects produced by (R)\u2010KTP administration, since concentrations of (S)\u2010KTP in exudate of these calves following chiral inversion were at least 5 times higher than the EC<jats:sub>50<\/jats:sub>at all sampling times. The data for \u03b2\u2010glu and bradykinin\u2010induced swelling inhibition indicate possible inhibitory actions of (R)\u2010KTP as well as (S)\u2010KTP. \u00a9 1995 Wiley\u2010Liss, Inc.<\/jats:p>","DOI":"10.1002\/chir.530070806","type":"journal-article","created":{"date-parts":[[2005,1,7]],"date-time":"2005-01-07T15:50:16Z","timestamp":1105113016000},"page":"586-597","source":"Crossref","is-referenced-by-count":47,"title":["Pharmacokinetics and pharmacodynamics of ketoprofen enantiomers in calves"],"prefix":"10.1002","volume":"7","author":[{"given":"Maria Fabiana","family":"Landoni","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Peter","family":"Lees","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2004,9,17]]},"reference":[{"key":"e_1_2_1_2_2","doi-asserted-by":"publisher","DOI":"10.3109\/00498258609043529"},{"key":"e_1_2_1_3_2","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(88)90762-9"},{"key":"e_1_2_1_4_2","doi-asserted-by":"publisher","DOI":"10.1016\/0163-7258(90)90069-E"},{"key":"e_1_2_1_5_2","doi-asserted-by":"publisher","DOI":"10.1002\/chir.530050805"},{"key":"e_1_2_1_6_2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1365-2125.1991.tb05500.x"},{"key":"e_1_2_1_7_2","doi-asserted-by":"publisher","DOI":"10.1002\/chir.530040805"},{"key":"e_1_2_1_8_2","doi-asserted-by":"crossref","first-page":"284","DOI":"10.1016\/S0034-5288(18)31948-9","article-title":"Tissue cage model for collection of inflammatory exudate in ponies","volume":"36","author":"Higgins A. 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