Routledge P A
Br J Clin Pharmacol. 1986 Nov;22(5):499-506. doi: 10.1111/j.1365-2125.1986.tb02927.x.
The plasma protein binding of basic drugs appears to vary more than was at first assumed and is related to the marked intra-and interindividual differences in one of the chief binding proteins, AAG. Changes in AAG concentrations will result in alterations in the distribution and metabolism of basic drugs which will complicate the interpretation of the relationship between total drug concentration and drug efficacy or toxicity. For some drugs, e.g. lignocaine, direct measurement of free concentrations may improve their clinical use but rapid and reliable techniques are as yet not readily available.
碱性药物的血浆蛋白结合情况似乎比最初设想的变化更大,这与主要结合蛋白之一——α1-酸性糖蛋白(AAG)显著的个体内和个体间差异有关。AAG浓度的变化会导致碱性药物的分布和代谢发生改变,这将使对总药物浓度与药物疗效或毒性之间关系的解读变得复杂。对于某些药物,如利多卡因,直接测定游离浓度可能会改善其临床应用,但快速且可靠的技术目前还不容易获得。