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吡罗昔康-β-环糊精治疗风湿性疾病急性疼痛

Piroxicam-beta-cyclodextrin in the treatment of acute pain of rheumatic disease.

作者信息

Reginster J Y, Franchimont P

机构信息

University of Liege, Belgium.

出版信息

Eur J Rheumatol Inflamm. 1993;12(4):38-46.

PMID:7805703
Abstract

Analgesics continue to be the mainstay of therapy in osteoarthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) play an important role, particularly where there is a significant inflammatory component to the osteoarthritis. Piroxicam-beta-cyclodextrin (PBC) is a new formulation in which piroxicam has been complexed with beta-cyclodextrin, a cyclic oligosaccharide. This results in an increase in the rate of absorption of the active compound and, consequently, in an earlier onset of analgesic action. PBC, like piroxicam, is administered once daily. PBC has been used in the treatment of osteoarthritis. In comparison with piroxicam, PBC showed a more rapid analgesic-anti-inflammatory action after the first administration in patients with active osteoarthritis. Subsequent evaluations at the second, fifth and last day of treatment demonstrated a comparable efficacy of the two drugs. The efficacy and tolerability of PBC was compared with other NSAIDs given intramuscularly, such as diclofenac and ketoprofen. The three compounds provided marked pain relief within thirty minutes and this increased progressively until the third to fourth hour. The efficacy of oral PBC was comparable to that of intramuscular diclofenac or ketoprofen. In comparison with metamisole PBC achieved a more rapid and sustained reduction in pain intensity during the first twelve hours of treatment. This rapid and marked reduction in pain intensity with PBC was also observed in patients with low-back pain when compared with etodolac. In view of its efficacy, tolerability and rapid onset of action, piroxicam-beta-cyclodextrin appears to be an useful analgesic and a prominent progress in the treatment of acute rheumatic pain.

摘要

镇痛药仍然是骨关节炎治疗的主要手段。非甾体抗炎药(NSAIDs)发挥着重要作用,尤其是在骨关节炎存在明显炎症成分的情况下。吡罗昔康-β-环糊精(PBC)是一种新制剂,其中吡罗昔康与环状寡糖β-环糊精形成了复合物。这导致活性化合物的吸收速率增加,从而使镇痛作用更早起效。PBC与吡罗昔康一样,每日给药一次。PBC已用于骨关节炎的治疗。与吡罗昔康相比,PBC在活动性骨关节炎患者首次给药后显示出更快的镇痛抗炎作用。在治疗的第二天、第五天和最后一天进行的后续评估表明,两种药物的疗效相当。将PBC的疗效和耐受性与肌肉注射的其他NSAIDs(如双氯芬酸和酮洛芬)进行了比较。这三种化合物在30分钟内提供了显著的疼痛缓解,并且这种缓解逐渐增加,直至第三至第四小时。口服PBC的疗效与肌肉注射双氯芬酸或酮洛芬相当。与甲巯咪唑相比,PBC在治疗的前12小时内疼痛强度降低得更快且更持久。与依托度酸相比,在腰痛患者中也观察到PBC能使疼痛强度迅速且显著降低。鉴于其疗效、耐受性和快速起效,吡罗昔康-β-环糊精似乎是一种有用的镇痛药,也是急性风湿性疼痛治疗中的一项显著进展。

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