2,4-二硝基苯酚、碘乙酸盐和丙磺舒对大鼠对氨基马尿酸、环戊噻嗪和磺胺甲氧哒嗪肾排泄的不同抑制作用。

Different inhibitory effects of 2,4-dinitrophenol, iodoacetate, and probenecid on renal excretion of p-aminohippurate, cyclopenthiazide, and sulfamethoxypyridazine in rats.

作者信息

Stopp M, Weise C, Mewes S, Bräunlich H

出版信息

Acta Biol Med Ger. 1976;35(6):787-92.

Abstract

The present study was undertaken to determine whether the renal excretion of drugs can be modified by inhibition of the carrier system for organic acids in vivo. The renal excretion of p-aminohippurate is not influenced by 2,4-dinitrophenol but is reduced by iodoacetate and probenecid. The renal excretion of cyclopenthiazide is decreased by all inhibitors. Rats excrete only a very small portion of the administered dose of sulfamethoxypyridazine. Renal sulfamethoxypyridazine excretion is 3 times higher when the tubular reabsorption is blocked by simultaneous administration of NaHCO3. However, even then only a small portion of the injected dose is excreted. Renal sulfamethoxypyridazine excretion is only reduced by probenecid. This finding can be explained by the reduction of the urine volume. It can be concluded that p-aminohippurate and cyclopenthiazide are renally excreted by tubular secretion, whereas sulfamethoxy-pyridazine is excreted by glomerular filtration.

摘要

本研究旨在确定体内有机酸载体系统的抑制是否会改变药物的肾排泄。对氨基马尿酸的肾排泄不受2,4-二硝基苯酚的影响，但会被碘乙酸盐和丙磺舒降低。所有抑制剂都会降低环戊噻嗪的肾排泄。大鼠排泄的磺胺甲氧嗪给药剂量仅占很小一部分。同时给予碳酸氢钠阻断肾小管重吸收时，肾磺胺甲氧嗪排泄量会增加3倍。然而，即便如此，注射剂量中也只有一小部分被排泄。肾磺胺甲氧嗪排泄仅被丙磺舒降低。这一发现可以通过尿量减少来解释。可以得出结论，对氨基马尿酸和环戊噻嗪通过肾小管分泌进行肾排泄，而磺胺甲氧嗪则通过肾小球滤过排泄。