Julou L, Guyonnet J C, Ducrot R, Fournel J, Pasquet J
Scand J Rheumatol Suppl. 1976;1976(0):33-44.
Ketoprofen possesses the typical pharmacological properties of non-steroidal anti-inflammatory agents i.e. anti-inflammatory, analgesic and antipyretic activity, as well as antibradykinin activity and ability to inhibit prostaglandin synthesis. Ketoprofen is as potent as indomethacin in the tests for anti-inflammatory and analgesic activity, but its antipyretic and antibradykinin activities and its inhibitory activity against prostaglandin synthesis is respectively 4, 8 and 8 times greater than that of indomethacin. It seems very likely that the pituitary-adrenal axis is not involved in the mechanism of the anti-inflammatory action of ketoprofen, since in the carrageenan abscess test, the compound shows the same activity both in adrenalectomized and in normal rats and, when locally applied to the inflamed area, it is more active than when administered systemically. In the mouse the acute oral toxicity of ketoprofen is about one twentieth that of indomethacin. Like all powerful steroidal or non-steroidal antiinflammatory agents, ketoprofen shows some gastrointestinal toxicity, but its effect is mild and distinctly less than that of indomethacin. Pharmacokinetic studies in the rat, dog and monkey have shown that gastro-intestinal absorption of the drug is rapid and almost complete; the compound and its metabolites are excreted from the body fairly rapidly.
酮洛芬具有非甾体抗炎药的典型药理特性，即抗炎、镇痛和解热活性，以及抗缓激肽活性和抑制前列腺素合成的能力。在抗炎和镇痛活性测试中，酮洛芬与吲哚美辛的效力相当，但其解热、抗缓激肽活性以及对前列腺素合成的抑制活性分别是吲哚美辛的4倍、8倍和8倍。酮洛芬的抗炎作用机制似乎很可能与垂体-肾上腺轴无关，因为在角叉菜胶脓肿试验中，该化合物在肾上腺切除的大鼠和正常大鼠中表现出相同的活性，并且当局部应用于炎症部位时，其活性比全身给药时更高。在小鼠中，酮洛芬的急性口服毒性约为吲哚美辛的二十分之一。与所有强效甾体或非甾体抗炎药一样，酮洛芬也表现出一些胃肠道毒性，但其作用轻微，明显小于吲哚美辛。在大鼠、狗和猴子身上进行的药代动力学研究表明，该药物在胃肠道的吸收迅速且几乎完全；化合物及其代谢产物从体内排泄得相当快。
