Strub K M, Aeppli L, Müller R K
Eur J Rheumatol Inflamm. 1982;5(4):478-87.
Carprofen, a new non-steroidal anti-inflammatory agent, showed marked anti-inflammatory and analgesic effects in various relevant experimental models. The analgesic activity was restricted to conditions where pain was provoked by an inflammatory process. Induction of intestinal ulcers was the only side effect recognizable in animals and occurred only after high doses. Inhibition of prostaglandin (PG) synthesis by carprofen was slight in relation to its anti-inflammatory and analgesic potency. As ulcerogenicity of non-steroidal anti-inflammatory agents is correlated with inhibition of the PG-synthesis, the insignificant impairment of the PG-synthesis in therapeutically effective doses may explain the good gastrointestinal tolerance repeatedly reported for carprofen in clinical trials.
卡洛芬是一种新型非甾体抗炎药,在各种相关实验模型中显示出显著的抗炎和镇痛作用。其镇痛活性仅限于由炎症过程引发疼痛的情况。肠道溃疡的诱导是在动物中唯一可识别的副作用,且仅在高剂量后出现。与卡洛芬的抗炎和镇痛效力相比,其对前列腺素(PG)合成的抑制作用较弱。由于非甾体抗炎药的致溃疡作用与PG合成的抑制相关,治疗有效剂量下PG合成的轻微损害可能解释了临床试验中反复报道的卡洛芬良好的胃肠道耐受性。