Higuchi S, Otomo S, Aihara H
Nihon Yakurigaku Zasshi. 1985 May;85(5):343-6. doi: 10.1254/fpj.85.343.
Antiedema effects of basic nonsteroidal anti-inflammatory drugs that don't inhibit prostaglandin biosynthesis were investigated with carrageenin-induced hind paw edema in rats. Locally administered mepirizole, tiaramide.HCl and aminopyrine, the basic nonsteroidal anti-inflammatory drugs, didn't show any suppression against the edema formation. In the case of indomethacin, phenylbutazone and ketoprofen, inhibitors of prostaglandin biosynthesis, they inhibited the edema formation. Inhibitory effects of orally and subcutaneously administered basic nonsteroidal anti-inflammatory drugs such as tiaramide.HCl and benzydamine on the edema formation were more potent in fasted rats than in nonfasted rats. In the case of acidic nonsteroidal anti-inflammatory drugs such as indomethacin and ibuprofen, their inhibitory activities were almost the same in both the fasted rats and nonfasted rats. These results suggest that the site of action of the basic nonsteroidal anti-inflammatory drugs such as tiaramide.HCl and mepirizole is not the inflamed site, and certain systemic effects may contribute to the anti-edema effects.
利用角叉菜胶诱导大鼠后爪水肿,研究了不抑制前列腺素生物合成的碱性非甾体抗炎药的抗水肿作用。局部给予碱性非甾体抗炎药美吡唑、盐酸替拉米特和氨基比林,未显示出对水肿形成的任何抑制作用。而对于前列腺素生物合成抑制剂吲哚美辛、保泰松和酮洛芬,它们抑制了水肿形成。口服和皮下给予碱性非甾体抗炎药如盐酸替拉米特和苄达明对水肿形成的抑制作用在禁食大鼠中比在非禁食大鼠中更强。对于酸性非甾体抗炎药如吲哚美辛和布洛芬,它们在禁食大鼠和非禁食大鼠中的抑制活性几乎相同。这些结果表明,碱性非甾体抗炎药如盐酸替拉米特和美吡唑的作用部位不是炎症部位,某些全身作用可能有助于其抗水肿作用。