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人血清中塞来赞(咪唑水杨酸盐)的血药结合情况。

Blood binding of selezen (imidazole salicylate) in man.

作者信息

Zini R, Morin D, Acuto G C, Bianchini C, de Santis F, Tillement J P

机构信息

Laboratoire de pharmacologie UFR de Médecine de Paris XII, Créteil, France.

出版信息

Int J Clin Pharmacol Ther Toxicol. 1991 Jun;29(6):242-9.

PMID:1869346
Abstract

The interactions of selezen (imidazole salicylate) with human blood components were studied by equilibrium dialysis. These interactions were limited to the binding of salicylate to human serum albumin (HSA). The binding was saturable and involved several classes of binding sites with different association constants. A competition study indicated that salicylic acid at high concentration was able to displace warfarin and digitoxin but not glibenclamide from their HSA sites. On the other hand, selezen serum binding was decreased in renal impaired patients and this result was probably linked to the decreases in HSA concentration. So the use of small dosage regimens of selezen to these patients can be proposed. The same recommendation may be done for cirrhotic patients, where the decrease of selezen binding percentage was observed and due to both hypoalbuminemia and hyperbilirubinemia.

摘要

通过平衡透析研究了塞来赞(咪唑水杨酸盐)与人血液成分的相互作用。这些相互作用仅限于水杨酸盐与人血清白蛋白(HSA)的结合。这种结合是可饱和的,涉及几类具有不同缔合常数的结合位点。一项竞争研究表明,高浓度的水杨酸能够从HSA位点取代华法林和地高辛,但不能取代格列本脲。另一方面,肾功能受损患者的塞来赞血清结合率降低,这一结果可能与HSA浓度降低有关。因此,可以建议对这些患者使用小剂量的塞来赞。对于肝硬化患者也可以提出同样的建议,在肝硬化患者中观察到塞来赞结合百分比降低,原因是低白蛋白血症和高胆红素血症。

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