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外周作用性镇痛药。

Peripherally acting analgesics.

作者信息

Amadio P

出版信息

Am J Med. 1984 Sep 10;77(3A):17-26. doi: 10.1016/s0002-9343(84)80099-6.

Abstract

The therapeutic effect of aspirin and the other nonsteroidal anti-inflammatory drugs derives from the peripheral inhibition of prostaglandin synthetase. Aspirin produces irreversible inhibition, whereas the inhibition triggered by the other nonsteroidal anti-inflammatory drugs is reversible. Despite proved analgesic efficacy, use of aspirin and the nonsteroidal anti-inflammatory drugs may be accompanied by a wide range of side effects of a potentially serious nature. For relief of pain, there appears to be no clear-cut superiority of one nonsteroidal anti-inflammatory drug over another, and patients who fail to respond to one class of nonsteroidal anti-inflammatory drugs may respond to a representative of another class. As with aspirin, it is difficult to demonstrate the superiority of higher doses of these agents over the lower doses. The side-effect profile of non-narcotic analgesics favors acetaminophen, presumably because its inhibition of prostaglandin synthetase occurs centrally. Acetaminophen does not appear to have the same potential for toxicity that is seen with aspirin and other nonsteroidal anti-inflammatory drugs. At dosages up to 4 g per day, acetaminophen compares favorably in analgesic potency to aspirin and other nonsteroidal anti-inflammatory drugs, and it should be considered the treatment of choice for mild-to-moderate pain. Safe conditions for the analgesic use of nonsteroidal anti-inflammatory drugs in children and pregnancy have not been established. Because it is virtually free of side effects, acetaminophen may be the mild analgesic of choice for the pregnant patient. It has been used safely for years in children. Only a limited number of analgesic studies have been conducted in children. The results of analgesic studies carried out in adults are generally recognized as applicable to pain relief in children.

摘要

阿司匹林和其他非甾体抗炎药的治疗效果源于对前列腺素合成酶的外周抑制作用。阿司匹林产生不可逆抑制,而其他非甾体抗炎药引发的抑制是可逆的。尽管已证实具有镇痛功效,但使用阿司匹林和非甾体抗炎药可能会伴随一系列潜在严重性质的副作用。对于缓解疼痛而言,一种非甾体抗炎药相对于另一种似乎并无明显优势,对一类非甾体抗炎药无反应的患者可能对另一类中的代表性药物有反应。与阿司匹林一样,很难证明这些药物高剂量比低剂量更具优势。非麻醉性镇痛药的副作用情况有利于对乙酰氨基酚,大概是因为其对前列腺素合成酶的抑制作用发生在中枢。对乙酰氨基酚似乎没有阿司匹林和其他非甾体抗炎药所见的相同毒性潜力。在每天剂量高达4克时,对乙酰氨基酚在镇痛效力上与阿司匹林和其他非甾体抗炎药相当,并且它应被视为轻至中度疼痛的首选治疗药物。儿童和孕妇使用非甾体抗炎药进行镇痛的安全条件尚未确立。由于对乙酰氨基酚几乎没有副作用,它可能是孕妇的首选轻度镇痛药。它已在儿童中安全使用多年。仅对有限数量的儿童进行了镇痛研究。在成人中进行的镇痛研究结果通常被认为适用于儿童的疼痛缓解。

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