Sharma S, Prasad A, Anand K S
Department of Neuropsycho-Pharmacology, Institute of Human Behaviour and Allied Sciences, Delhi, India.
Am J Ther. 1999 Jan;6(1):3-11. doi: 10.1097/00045391-199901000-00002.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a group of agents with similar action but diverse chemical structures and mechanism of action. There is considerable interpatient variability in the pain relief obtained from NSAIDs even when these agents belong to the same chemical family. The reasons for this interpatient variability include pharmacodynamic actions, pharmacokinetic parameters, or a combination of both. Furthermore, two distinct forms of the key enzyme cyclo-oxygenase (COX) have been identified. The constitutive enzyme COX-1 is found in most tissues and is believed to confer gastric mucosal protective action, and COX-2, the inducible enzyme, is implicated in pain and inflammation. Selective inhibition of COX-1 and COX-2 may allow prediction of drugs' major effects. By definition, NSAIDs are expected to modulate synovial inflammation present in the arthritic joints. Whether NSAIDs can positively influence the progression of arthritic disorders by modifying the underlying pathology remains to be answered. This review provides guidelines on how to choose NSAIDs rationally keeping in view the mechanism of tissue injury, the mode of action of NSAIDs, and their adverse effects.
非甾体抗炎药(NSAIDs)是一类作用相似但化学结构和作用机制各异的药物。即使这些药物属于同一化学家族,患者从NSAIDs获得的疼痛缓解程度仍存在很大的个体差异。这种个体差异的原因包括药效学作用、药代动力学参数或两者的结合。此外,已鉴定出关键酶环氧化酶(COX)的两种不同形式。组成型酶COX-1存在于大多数组织中,被认为具有胃黏膜保护作用,而诱导型酶COX-2则与疼痛和炎症有关。对COX-1和COX-2的选择性抑制可能有助于预测药物的主要作用。根据定义,NSAIDs有望调节关节炎关节中存在的滑膜炎症。NSAIDs是否能通过改变潜在病理来积极影响关节炎疾病的进展仍有待解答。本综述提供了关于如何根据组织损伤机制、NSAIDs的作用方式及其不良反应合理选择NSAIDs的指导原则。