年龄和吸烟对利多卡因及地西泮血浆蛋白结合率的影响。
The effects of age and smoking on the plasma protein binding of lignocaine and diazepam.
作者信息
Davis D, Grossman S H, Kitchell B B, Shand D G, Routledge P A
出版信息
Br J Clin Pharmacol. 1985 Feb;19(2):261-5. doi: 10.1111/j.1365-2125.1985.tb02641.x.
In 63 healthy ambulant subjects 18 to 88 years of age, the plasma protein binding of diazepam (principally bound to albumin) decreased with age. Diazepam binding in plasma correlated positively with plasma albumin concentration which also decreased with age. In contrast, the plasma protein binding of the basic drug, lignocaine (predominantly bound to alpha 1-acid glycoprotein [AAG]), tended to increase slightly with age. Lignocaine binding in plasma correlated positively with plasma AAG concentration which also increased slightly with age. Smoking did not affect the plasma protein binding of diazepam or lignocaine or the plasma concentrations of albumin, AAG or nonesterified fatty acids. These results suggest that age-related changes in plasma protein binding of lignocaine and diazepam are determined in part by age-related changes in the concentrations of the binding proteins in plasma. The ageing process alone causes only small changes in the plasma protein binding of these drugs compared with the effect of disease states, however.
在63名年龄在18至88岁之间的健康能走动的受试者中，地西泮的血浆蛋白结合率（主要与白蛋白结合）随年龄增长而降低。血浆中的地西泮结合与血浆白蛋白浓度呈正相关，而血浆白蛋白浓度也随年龄增长而降低。相比之下，碱性药物利多卡因的血浆蛋白结合率（主要与α1 -酸性糖蛋白[AAG]结合）则随年龄增长略有升高。血浆中的利多卡因结合与血浆AAG浓度呈正相关，而血浆AAG浓度也随年龄增长略有升高。吸烟并不影响地西泮或利多卡因的血浆蛋白结合率，也不影响白蛋白、AAG或非酯化脂肪酸的血浆浓度。这些结果表明，利多卡因和地西泮血浆蛋白结合的年龄相关变化部分是由血浆中结合蛋白浓度的年龄相关变化所决定的。然而，与疾病状态的影响相比，衰老过程本身仅导致这些药物的血浆蛋白结合发生微小变化。
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