Beyer K H, Gelarden R T
Arch Int Pharmacodyn Ther. 1978 Feb;231(2):180-95.
Salicylic acid and its principal metabolic product, salicyluric acid, are ultrafiltered at the glomeruli, secreted by the proximal segment and undergo back diffusion; the net effect being an accumulation of salicylates in the cortex. The back diffusion of salicylate is pH-sensitive (salicylurate is not) and its secretion is less sensitive than that of salicylurate to depression by probenecid. There was an increasing concentration gradient of these salicylates from outer cortex to innermost medulla. The clearance of salicyluric acid exceeded glomerular filtration rate even at very low urine flow and was not pH-dependent, so that total salicylate accumulation in the medulla was less affected by adjustment of urinary pH. Increasing perfusion of the nephron markedly reduced the inner medulla/cortical concentration ratios and segmental concentrations of salt and urea and reduced the cortical concentrations of salicylates. Diuresis may decrease the medullary concentration of salicylates, depending on the rate and duration of increased urine flow.
水杨酸及其主要代谢产物水杨尿酸在肾小球处被超滤,由近端小管分泌并发生逆向扩散;最终结果是水杨酸盐在皮质中蓄积。水杨酸盐的逆向扩散对pH敏感(水杨尿酸则不敏感),其分泌对丙磺舒抑制作用的敏感性低于水杨尿酸。这些水杨酸盐从外皮质到最内层髓质的浓度梯度逐渐增加。即使在尿流非常低的情况下,水杨尿酸的清除率也超过肾小球滤过率,且不依赖于pH,因此髓质中水杨酸盐的总蓄积量受尿液pH调节的影响较小。增加肾单位灌注可显著降低髓质内层/皮质的浓度比以及盐和尿素的节段浓度,并降低皮质中水杨酸盐的浓度。利尿作用可能会降低髓质中水杨酸盐的浓度,这取决于尿流增加的速率和持续时间。