Powell A M, Chan W Y
Prostaglandins Leukot Med. 1984 Feb;13(2):129-37. doi: 10.1016/0262-1746(84)90002-7.
In two independent studies, ibuprofen and naproxen sodium were found to be equi-effective in alleviating dysmenorrheic symptoms. However, the effects of these drugs on menstrual PG release were found to be dissimilar. Ibuprofen primarily inhibited menstrual PGF2 alpha release with little effect on PGE2 release, whereas, naproxen sodium inhibited both PGF2 alpha and PGE2 release equally. To verify these results, we determined the inhibitory potency, IC50, of ibuprofen and naproxen sodium on PGF2 alpha and PGE2 synthesis in the rat uterine homogenate system. The preferential PGF2 alpha inhibitory activity of ibuprofen was confirmed. These findings suggest that ibuprofen may, in addition to inhibiting fatty acid cyclooxygenase, also inhibit PGF2 alpha reductase, or some other PG metabolic pathways which affect PGF2 alpha and PGE2 synthesis differently. The significance of this differential PG synthesis inhibitory effect in dysmenorrheic therapy is discussed.
在两项独立研究中,发现布洛芬和萘普生钠在缓解痛经症状方面疗效相当。然而,发现这些药物对月经期间前列腺素(PG)释放的影响并不相同。布洛芬主要抑制月经期间PGF2α的释放,对PGE2的释放影响很小,而萘普生钠对PGF2α和PGE2的释放抑制作用相同。为了验证这些结果,我们在大鼠子宫匀浆系统中测定了布洛芬和萘普生钠对PGF2α和PGE2合成的抑制效力IC50。布洛芬对PGF2α的优先抑制活性得到了证实。这些发现表明,布洛芬除了抑制脂肪酸环氧化酶外,还可能抑制PGF2α还原酶或其他一些对PGF2α和PGE2合成有不同影响的PG代谢途径。本文讨论了这种不同的PG合成抑制作用在痛经治疗中的意义。