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烧伤后血清药物结合与血清蛋白浓度

Postburn serum drug binding and serum protein concentrations.

作者信息

Bloedow D C, Hansbrough J F, Hardin T, Simons M

出版信息

J Clin Pharmacol. 1986 Feb;26(2):147-51. doi: 10.1002/j.1552-4604.1986.tb02923.x.

Abstract

The free fractions of diazepam, imipramine, lidocaine, meperidine, phenytoin, propranolol, and salicylic acid were determined in the serum of seven burn patients (25% to 80% of their skin surface burned) about one week after the burn and in three of the patients at about four weeks following the injury. Serum protein fractions were measured by electrophoresis, and alpha-1 acid glycoprotein levels were determined. For the drugs that bind predominantly to albumin, the serum free fractions were greater in patients one week after the burn incident than in control subjects (diazepam, 0.055 vs. 0.017; phenytoin, 0.24 vs. 0.16; and salicylic acid, 0.69 vs. 0.32). The increase in free fraction for these drugs was attributed to the postburn decrease in serum albumin levels (2.2 vs. 4.4 g/dL, control). Imipramine, lidocaine, meperidine, and propranolol bind primarily to alpha-1 acid glycoprotein. The free fractions for these drugs decreased one week following the burn (imipramine, 0.074 vs. 0.095; lidocaine, 0.17 vs. 0.35; meperidine, 0.37 vs. 0.48; and propranolol, 0.045 vs. 0.107), presumably in response to the increased alpha-1 acid glycoprotein concentration (222 vs. 83 mg/dL, control). Diazepam, lidocaine, propranolol, and salicylic acid free fractions were still different from control values at four weeks after the accident.

摘要

在七名烧伤患者(皮肤表面烧伤25%至80%)烧伤后约一周以及其中三名患者受伤后约四周时,测定了地西泮、丙咪嗪、利多卡因、哌替啶、苯妥英、普萘洛尔和水杨酸的血清游离分数。通过电泳测量血清蛋白组分,并测定α-1酸性糖蛋白水平。对于主要与白蛋白结合的药物,烧伤事件一周后患者的血清游离分数高于对照受试者(地西泮,0.055对0.017;苯妥英,0.24对0.16;水杨酸,0.69对0.32)。这些药物游离分数的增加归因于烧伤后血清白蛋白水平的下降(对照为2.2对4.4 g/dL)。丙咪嗪、利多卡因、哌替啶和普萘洛尔主要与α-1酸性糖蛋白结合。这些药物的游离分数在烧伤后一周下降(丙咪嗪,0.074对0.095;利多卡因,0.17对0.35;哌替啶,0.37对0.48;普萘洛尔,0.045对0.107),可能是对α-1酸性糖蛋白浓度增加的反应(对照为222对83 mg/dL)。事故发生四周后,地西泮、利多卡因、普萘洛尔和水杨酸的游离分数仍与对照值不同。

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