Gibson T P
Ortho-McNeil Pharmaceutical, Raritan, New Jersey 08869, USA.
Am J Med. 1996 Jul 31;101(1A):47S-53S. doi: 10.1016/s0002-9343(96)00138-6.
Chronic pain remains a problem because it is often misdiagnosed and undertreated. Adverse effects and safety concerns associated with many analgesics have limited the use of these agents and contributed to the undertreatment of pain. With regard to the pharmacologic agents most commonly used to manage pain, centrally acting analgesics (e.g., morphine, codeine) are associated with respiratory depression, tolerance, and dependence, and most nonsteroidal anti-inflammatory drugs (NSAIDs) produce adverse gastrointestinal effects. New to the United States, tramadol HCl, which has been prescribed for almost 2 decades in Europe, is a single-entity, centrally acting analgesic that is effective for the management of moderate to moderately severe pain. Although the mechanism of action of this analgesic is not completely understood, animal models suggest that at least two complementary modes of action appear applicable: (1) binding of parent compound and mono-O-desmethyltramadol (M1 metabolite) to the mu-opioid receptor and (2) weak inhibition of norepinephrine and serotonin reuptake. Clinical experience suggests that tramadol appears to have a low potential for abuse or addiction. Results from clinical trials conducted in the United States as well as European postmarketing surveillance studies indicate that tramadol is an effective analgesic that may have a particularly important role in the management of chronic painful conditions.
慢性疼痛仍然是一个问题，因为它常常被误诊且治疗不足。许多镇痛药相关的不良反应和安全问题限制了这些药物的使用，并导致了疼痛治疗不足。就最常用于管理疼痛的药物而言，中枢性镇痛药（如吗啡、可待因）与呼吸抑制、耐受性和依赖性有关，而且大多数非甾体抗炎药（NSAIDs）会产生不良胃肠道影响。盐酸曲马多在美国是新药，在欧洲已被处方使用近20年，它是一种单一成分的中枢性镇痛药，对中度至中度重度疼痛的管理有效。尽管这种镇痛药的作用机制尚未完全了解，但动物模型表明至少有两种互补的作用模式似乎适用：（1）母体化合物和单-O-去甲基曲马多（M1代谢物）与μ阿片受体结合；（2）对去甲肾上腺素和5-羟色胺再摄取的微弱抑制。临床经验表明曲马多似乎滥用或成瘾的可能性较低。在美国进行的临床试验以及欧洲上市后监测研究的结果表明，曲马多是一种有效的镇痛药，在慢性疼痛病症的管理中可能具有特别重要的作用。
