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屈昔康的药理特性

Pharmacological profile of droxicam.

作者信息

Esteve J, Farré A J, Roser R

机构信息

Laboratorios Dr Esteve, Barcelona, Spain.

出版信息

Gen Pharmacol. 1988;19(1):49-54. doi: 10.1016/0306-3623(88)90004-3.

Abstract

In Studies of anti-inflammatory activity, droxicam has shown itself to be as active as piroxicam and much more active than phenylbutazone, isoxicam and suprofen, both in acute studies such as carrageenin oedema, nystatin oedema and ultraviolet erythema, and in longer-term tests such as that of the cotton pellet. In the studies of anti-arthritic activity, which require long-term treatment, droxicam was as effective as piroxicam, both on primary and on secondary lesions. The study of analgaesic activity, conducted by means of the tests of protective activity against writhing induced by phenylbenzoquinone and acetylcholine bromide in the mouse and by acetic acid in the rat, droxicam activity was superior to that of acetylsalicylic acid, dipyrone, isoxicam and phenylbutazone. Droxicam also showed antipyretic activity in the rat, greater than that of acetylsalicylic acid, dipyrone and 4-aminoantipyrine, in the brewer's yeast and Salmonella typhi tests. Droxicam also acts as an ex vivo platelet aggregation inhibitor in the dog. In the study of inhibition of peritoneal capillary permeability in the mouse, droxicam was considerably more potent than isoxicam or phenylbutazone. Studies of general pharmacology have demonstrated that droxicam, at high doses, has no cardiovascular or respiratory effects, and that neither does it modify behaviour in rats and mice, determined by the Irwin test. Gastrointestinal tolerance of droxicam has been compared with that of piroxicam, and it has been found that droxicam is far better tolerated. The study of induction of gastrointestinal lesions in the rat demonstrated that the gastrolesive potential of droxicam is 10 times inferior to that of piroxicam.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在抗炎活性研究中,在角叉菜胶性水肿、制霉菌素性水肿和紫外线红斑等急性研究以及棉球试验等长期试验中,屈昔康显示出与吡罗昔康活性相当,且比保泰松、异恶酰草胺和舒洛芬活性高得多。在需要长期治疗的抗关节炎活性研究中,屈昔康对原发性和继发性病变的疗效与吡罗昔康相当。通过小鼠苯醌和溴化乙酰胆碱以及大鼠乙酸诱导扭体的保护活性试验进行的镇痛活性研究表明,屈昔康的活性优于乙酰水杨酸、安乃近、异恶酰草胺和保泰松。在啤酒酵母和伤寒沙门氏菌试验中,屈昔康在大鼠中也显示出解热活性,大于乙酰水杨酸、安乃近和4-氨基安替比林。屈昔康在犬体内还具有体外血小板聚集抑制作用。在小鼠腹膜毛细血管通透性抑制研究中,屈昔康比异恶酰草胺或保泰松效力强得多。一般药理学研究表明,高剂量的屈昔康对心血管或呼吸系统无影响,通过欧文试验也未发现其改变大鼠和小鼠的行为。已将屈昔康的胃肠道耐受性与吡罗昔康进行了比较,发现屈昔康的耐受性要好得多。大鼠胃肠道损伤诱导研究表明,屈昔康的致胃肠损伤潜力比吡罗昔康低10倍。(摘要截短至250字)

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