Brune K
Eur J Rheumatol Inflamm. 1987;8(1):18-23.
Only recently have the pharmacokinetic characteristics of nonsteroidal anti-inflammatory drugs (NSAIDs) been recognized as decisive factors in understanding the effects and side effects of these drugs. The accumulation of NSAIDs in inflamed tissue is central to the anti-inflammatory action, whereas high drug concentrations in the gastrointestinal tract wall, kidneys, blood, and liver may be major contributing factors to the incidence and severity of side effects. Also, variations in pharmacokinetic handling of NSAIDs by different patients may contribute considerably to differences in therapeutic response. An evaluation of the response-related pharmacokinetics of the three most widely used NSAIDs, diclofenac, indomethacin, and piroxicam, shows some obvious reasons for these differences: The onset of absorption and the bioavailability of diclofenac can vary considerably, and relevant inter-patient differences are found in the terminal plasma half-life of indomethacin and piroxicam. The variability in these parameters may contribute significantly to the observed variations in clinical response and to the incidence of unwanted drug effects.
直到最近，非甾体抗炎药（NSAIDs）的药代动力学特性才被认为是理解这些药物的疗效和副作用的决定性因素。NSAIDs在炎症组织中的蓄积是其抗炎作用的核心，而胃肠道壁、肾脏、血液和肝脏中的高药物浓度可能是副作用发生率和严重程度的主要促成因素。此外，不同患者对NSAIDs药代动力学处理的差异可能在很大程度上导致治疗反应的差异。对三种最常用的NSAIDs（双氯芬酸、吲哚美辛和吡罗昔康）与反应相关的药代动力学进行评估，揭示了这些差异的一些明显原因：双氯芬酸的吸收起始和生物利用度可能有很大差异，并且在吲哚美辛和吡罗昔康的终末血浆半衰期方面发现了患者间的相关差异。这些参数的变异性可能在很大程度上导致观察到的临床反应差异以及不良药物效应的发生率。
