Trovik T S, Jaeger R, Jorde R, Ingebretsen O, Sager G
Department of Pharmacology, University of Tromsø, Norway.
Eur J Clin Pharmacol. 1992;43(3):265-8. doi: 10.1007/BF02333020.
In the present study equilibrium dialysis has been used to determine the degree of protein binding of the catecholamines adrenaline and noradrenaline and the adrenergic receptor blockers, prazosin and propranolol in diabetics. The binding of the catecholamines in plasma from Type I and II diabetic patients was not significantly different from that of healthy subjects. The ratio of the bound and free catecholamine concentrations was correlated with the level of albumin (HSA). Significantly reduced protein binding of prazosin was observed in Type I and II diabetic subjects compared to healthy volunteers. The binding of propranolol was significantly reduced in Type I patients. The ratios between the bound and unbound concentrations of prazosin and propranolol were significantly correlated with the levels of alpha 1-acid glycoprotein (AAG). The results suggest that non-enzymatic glycosylation of plasma proteins may increase the unbound fraction of the adrenergic blockers prazosin and propranolol.
在本研究中，已使用平衡透析法来测定糖尿病患者体内儿茶酚胺类物质肾上腺素和去甲肾上腺素以及肾上腺素能受体阻滞剂哌唑嗪和普萘洛尔的蛋白结合程度。I型和II型糖尿病患者血浆中儿茶酚胺类物质的结合情况与健康受试者并无显著差异。结合型和游离型儿茶酚胺浓度之比与白蛋白（HSA）水平相关。与健康志愿者相比，I型和II型糖尿病受试者中哌唑嗪的蛋白结合显著降低。I型患者中普萘洛尔的结合显著减少。哌唑嗪和普萘洛尔的结合型与未结合型浓度之比与α1-酸性糖蛋白（AAG）水平显著相关。结果表明，血浆蛋白的非酶糖基化可能会增加肾上腺素能阻滞剂哌唑嗪和普萘洛尔的游离部分。
