Beaver W T
Department of Pharmacology, School of Medicine, Georgetown University, Washington, D.C. 20007.
Am J Med. 1988 May 20;84(5A):3-15. doi: 10.1016/0002-9343(88)90471-8.
Of the four categories of oral analgesics, three have been available since the 19th century. Although adequate doses of the more potent oral opioids such as morphine and methadone are effective even in severe pain, the commonly used "weak" narcotics such as codeine and propoxyphene are no more effective than usual doses of aspirin or acetaminophen. Furthermore, the opioids produce gastrointestinal and central nervous system adverse effects, and, during long-term administration, tolerance may develop and there is a risk of drug dependence. Aspirin and acetaminophen are the traditional agents of choice for oral analgesic therapy; until 10 years ago, there were no single-entity, oral analgesics--with the exception of large doses of oral narcotics--that were more effective than usual doses of aspirin or acetaminophen. However, there is a ceiling on the analgesic effect attainable with safe doses of these drugs, which may in part be overcome through the use of the third category of oral analgesics, combinations of aspirin or acetaminophen with oral opioids. The fourth category of oral analgesics constitutes the most important recent development in pain management with analgesic drugs: the newer peripherally acting, nonsteroidal anti-inflammatory analgesics, some of which are clearly more efficacious than aspirin or acetaminophen and compare favorably not only with full doses of narcotic combination products but even, in some cases, with strong injectable opioids. On repeated dosing, some nonsteroidal anti-inflammatory drugs are better tolerated than aspirin and some have a much longer duration of analgesic effect than aspirin or acetaminophen. Further study is needed to compare nonsteroidal anti-inflammatory drugs among themselves and to determine their value in chronic pain and in combination therapy.
在四类口服镇痛药中，有三类自19世纪以来就已存在。尽管使用足够剂量的强效口服阿片类药物，如吗啡和美沙酮，即使在剧痛情况下也有效，但常用的“弱”麻醉药，如可待因和丙氧芬，并不比常规剂量的阿司匹林或对乙酰氨基酚更有效。此外，阿片类药物会产生胃肠道和中枢神经系统不良反应，而且在长期用药过程中，可能会产生耐受性，并有药物依赖的风险。阿司匹林和对乙酰氨基酚是口服镇痛治疗的传统首选药物；直到10年前，除了大剂量口服麻醉药外，没有哪种单一成分的口服镇痛药比常规剂量的阿司匹林或对乙酰氨基酚更有效。然而，这些药物的安全剂量所能达到的镇痛效果存在上限，部分可以通过使用第三类口服镇痛药，即阿司匹林或对乙酰氨基酚与口服阿片类药物的组合来克服。第四类口服镇痛药是镇痛药在疼痛管理方面最重要的最新进展：新型外周作用的非甾体抗炎镇痛药，其中一些明显比阿司匹林或对乙酰氨基酚更有效，不仅与全剂量的麻醉药复方制剂相比具有优势，而且在某些情况下，甚至与强效注射用阿片类药物相比也具有优势。反复给药时，一些非甾体抗炎药比阿司匹林耐受性更好，一些药物的镇痛作用持续时间比阿司匹林或对乙酰氨基酚长得多。需要进一步研究以比较不同的非甾体抗炎药，并确定它们在慢性疼痛和联合治疗中的价值。
