Farré A J, Colombo M, Fort M, Gutiérrez B, Rodríguez L, Roser R
Methods Find Exp Clin Pharmacol. 1986 Jul;8(7):407-22.
Droxicam showed high antiinflammatory activity in carrageenin-induced edema in rat. At doses of 0.25 and 0.5 mg/kg, droxicam was as active as piroxicam and more active than phenylbutazone given at 2.5 and 5 mg/kg. Against nystatin-induced edema, droxicam (ED50, p.o., 5, 6, 7, 8 h: 7.5, 12.9, 4.8, 8.4 mg/kg) was 4-11 times more active than phenylbutazone and more than 12 times more active than isoxicam. In cotton pellet-induced granuloma in rats, title compound was as active as suprofen. In U.V. light-induced erythema in guinea pigs, droxicam (ED50, p.o., 1, 2, 3, 4 h: 0.51, 0.94, 1.56, 4.88 mg/kg) was 5-9 times more active than phenylbutazone. At doses of 0.1, 0.33 and 1.0 mg/kg/day, droxicam, similar to piroxicam, showed good antiarthritic activity in rats injected with Mycobacterium butyricum against primary and secondary lesions. Droxicam demonstrated strong analgesic activity in protecting against writhings: induced by phenylbenzoquinone in mice: ED50: droxicam = 5.3, phenylbutazone = 61.5, acetylsalicylic acid = 90.7, dipyrone = 83.6, isoxicam = 88.3 mg/kg, p.o.; induced by acetylcholine bromide in mice: ED50: droxicam = 1.1, phenylbutazone = 32.1, acetylsalicylic acid = 32.2, isoxicam = 32.7 mg/kg, p.o.; induced by acetic acid in rat: ED50: droxicam = 0.94, acetylsalicylic acid = 8.72, isoxicam = 4.70 mg/kg, p.o. Antipyretic activity of title compound was demonstrated in rats with pyresis induced by brewer's yeast, being 4-13 times more active than dipyrone. In pyresis induced by Salmonella typhi, droxicam was more active than acetylsalicylic acid and 4-aminoantipyrine at all times and doses. In a study of protection against diarrhea induced by castor oil in rats, droxicam and piroxicam showed equal activity (ED50 = 0.081 and 0.079 mg/kg, p.o., respectively) and were 3.9 and 15.6 times more active than isoxicam and phenylbutazone, respectively. Droxicam significantly inhibited peritoneal capillary permeability in mice at a dose of 5 mg/kg, p.o., while isoxicam and phenylbutazone required 100 and 200 mg/kg, p.o., respectively. Droxicam did not exhibit uricosuric activity in rats. It did not show cardiovascular or respiratory effects in anesthetized cats, nor modify their response to administration of acetylcholine, norepinephrine and histamine. In the Irwin's test, droxicam did not alter rat behavior (80 mg/kg, i.p.) nor that of mice (160 mg/kg, p.o.). Induction of gastrointestinal injuries in rats by droxicam was 10 times less than by piroxicam (UD50: droxicam, 57 mg/kg, p.o.; piroxicam, 5.6 mg/kg, p.o.). The potentiation of gastric injuries induced by stress through cold in rats was also studied.(ABSTRACT TRUNCATED AT 400 WORDS)
屈昔康在角叉菜胶诱导的大鼠水肿中显示出高抗炎活性。在0.25和0.5mg/kg剂量下，屈昔康的活性与吡罗昔康相当，且比2.5和5mg/kg剂量的保泰松活性更强。在制霉菌素诱导的水肿模型中，屈昔康（口服给药，5、6、7、8小时的ED50分别为7.5、12.9、4.8、8.4mg/kg）的活性比保泰松高4 - 11倍，比异恶酰胺高12倍以上。在棉球诱导的大鼠肉芽肿模型中，该受试化合物的活性与舒洛芬相当。在紫外线诱导的豚鼠红斑模型中，屈昔康（口服给药，第1、2、3、4小时的ED50分别为0.51、0.94、1.56、4.88mg/kg）的活性比保泰松高5 - 9倍。在每天0.1、0.33和1.0mg/kg的剂量下，屈昔康与吡罗昔康相似，在注射丁酸分枝杆菌的大鼠中，对原发性和继发性病变均显示出良好的抗关节炎活性。屈昔康在保护小鼠免受苯醌诱导的扭体反应中表现出强烈的镇痛活性：ED50：屈昔康=5.3，保泰松=61.5，乙酰水杨酸=90.7，安乃近=83.6，异恶酰胺=88.3mg/kg，口服；在溴化乙酰胆碱诱导的小鼠扭体反应中：ED50：屈昔康=1.1，保泰松=32.1，乙酰水杨酸=32.2，异恶酰胺=32.7mg/kg，口服；在乙酸诱导的大鼠扭体反应中：ED50：屈昔康=0.94，乙酰水杨酸=8.72，异恶酰胺=4.70mg/kg，口服。受试化合物在啤酒酵母诱导发热的大鼠中表现出解热活性，比安乃近高4 - 13倍。在伤寒沙门氏菌诱导的发热模型中，屈昔康在所有时间和剂量下均比乙酰水杨酸和4 - 氨基安替比林活性更强。在一项保护大鼠免受蓖麻油诱导腹泻的研究中，屈昔康和吡罗昔康表现出同等活性（口服给药的ED50分别为0.081和0.079mg/kg），分别比异恶酰胺和保泰松高3.9倍和15.6倍。屈昔康在口服剂量为5mg/kg时能显著抑制小鼠腹腔毛细血管通透性，而异恶酰胺和保泰松分别需要口服100和200mg/kg才能达到相同效果。屈昔康在大鼠中未表现出促尿酸尿活性。在麻醉猫中，它未显示出心血管或呼吸效应，也未改变它们对乙酰胆碱、去甲肾上腺素和组胺给药的反应。在欧文氏试验中，屈昔康（腹腔注射80mg/kg）未改变大鼠行为，（口服160mg/kg）也未改变小鼠行为。屈昔康诱导大鼠胃肠道损伤的程度比吡罗昔康小10倍（UD50：屈昔康，口服57mg/kg；吡罗昔康，口服5.6mg/kg）。还研究了冷应激诱导大鼠胃损伤的增强作用。（摘要截断于400字）
