Cheng Hui-Fang, Harris Raymond C
Division of Nephrology, S 3322 MCN, Vanderbilt University School of Medicine, Nashville, TN 37232-2372, USA.
Hypertension. 2004 Mar;43(3):525-30. doi: 10.1161/01.HYP.0000116221.27079.ea. Epub 2004 Jan 19.
Selective cyclooxygenase (COX)-2 inhibitors that are in widespread clinical use were developed to avoid side effects of conventional NSAIDs, including gastrointestinal and renal toxicity. However, COX-2 is constitutively expressed in the kidney and is highly regulated in response to alterations in intravascular volume. COX-2 metabolites have been implicated in maintenance of renal blood flow, mediation of renin release, and regulation of sodium excretion. COX-2 inhibition may transiently decrease urine sodium excretion in some subjects and induce mild to moderate elevation of blood pressure. Furthermore, in conditions of relative intravascular volume depletion and/or renal hypoperfusion, interference with COX-2 activity can have deleterious effects on maintenance of renal blood flow and glomerular filtration rate. In addition to physiological regulation of COX-2 expression in the kidney, increased renal cortical COX-2 expression is seen in experimental models associated with altered renal hemodynamics and progressive renal injury (decreased renal mass, poorly controlled diabetes), and long-term treatment with selective COX-2 inhibitors ameliorates functional and structural renal damage in these conditions.
广泛应用于临床的选择性环氧化酶(COX)-2抑制剂是为避免传统非甾体抗炎药的副作用而研发的,这些副作用包括胃肠道和肾脏毒性。然而,COX-2在肾脏中组成性表达,并在血管内容量改变时受到高度调节。COX-2代谢产物与肾血流的维持、肾素释放的介导以及钠排泄的调节有关。COX-2抑制在某些受试者中可能会暂时降低尿钠排泄,并导致血压轻度至中度升高。此外,在相对血管内容量减少和/或肾灌注不足的情况下,干扰COX-2活性可能会对肾血流的维持和肾小球滤过率产生有害影响。除了肾脏中COX-2表达的生理调节外,在与肾血流动力学改变和进行性肾损伤(肾质量降低、糖尿病控制不佳)相关的实验模型中,肾皮质COX-2表达增加,并且在这些情况下,用选择性COX-2抑制剂进行长期治疗可改善肾脏的功能和结构损伤。