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TOCOLYTIC EFFECT OF PARECOXIB, A NEW PARENTERAL CYCLO‐OXYGENASE‐2‐SPECIFIC INHIBITOR, ON THE SPONTANEOUS AND PROSTAGLANDIN‐INDUCED CONTRACTIONS OF RAT ISOLATED MYOMETRIUM
Author(s) -
Ayar A
Publication year - 2007
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.2007.04632.x
Subject(s) - myometrium , prostaglandin , tocolytic , parecoxib , tocolytic agent , anesthesia , medicine , chemistry , pharmacology , uterus , preterm labor , pregnancy , fetus , biology , analgesic , genetics
SUMMARY1 The present study was undertaken to elucidate the effects of parecoxib, a novel cyclo‐oxygenase (COX)‐2 inhibitor, on spontaneous and prostaglandin‐induced contractions of uterine smooth muscle. 2 Non‐pregnant adult Wistar rats were decapitated and dissected to isolate myometrial strips. The tissue was mounted in 5 mL organ baths filled with Krebs’ solution that was maintained at 37°C and bubbled continuously with a mixture of 95% O 2 –5% CO 2 to give pH 7.4. Contractions were recorded through transducers for isometric tension recording. The dose‐dependent effects of parecoxib on contractility were quantified by changes in the mean amplitude, frequency and area under the contractile curve (AUC; percentage of control conditions) of the isometric tension recordings, averaged over 5 min intervals. Statistical analyses were performed using anova . 3 Application of parecoxib (50–900 µmol/L) caused dose‐dependent decreases in mean amplitude, mean frequency and mean AUC of both spontaneous and prostaglandin‐induced contractions. Mean percentage inhibition of the AUC of spontaneous contractions was found to be 29, 56, 74 and 84% in the presence of 50, 150, 300 and 600 µmol/L parecoxib, resepctively ( n = 8). In the case of prostaglandin (PG) F 2α ‐induced contractions, 100, 300, 600 and 900 µmol/L parecoxib resulted in a 27, 43, 61 and 73% inhibition, respectively ( n = 9). Moreover, pretreatment with parecoxib (600 µmol/L) reduced the responsiveness and maximum contractility to PGF 2α compared with non‐treated strips. 4 The data from the present study indicate, for the first time, that parecoxib inhibits spontaneous and prostaglandin‐induced contractions of rat myometrium in vitro. These results raise the possibility that parecoxib may be of therapeutic use in the management of preterm labour and dysmenorrhoea.