Pearson R M
Clin Pharmacokinet. 1977 May-Jun;2(3):198-204. doi: 10.2165/00003088-197702030-00004.
Diazoxide is given by rapid intravenous injection for the urgent reduction of high blood pressure in patients with all grades of renal function. Oral diazoxide produces less consistent effects. Protein binding of diazoxide is reduced in renal failure and this can be related to reduction of albumin concentration. There is a relation between impairment of renal function and the hypotensive effect of rapidly injected diazoxide. This is explicable in terms of the greater concentration of free (unbound) drug achieved after rapid injection in patients with renal failure. Renal clearance of diazoxide and its metabolites is impaired in renal failure but this is unlikely to affect its activity.
二氮嗪通过快速静脉注射给药,用于紧急降低各级肾功能患者的高血压。口服二氮嗪产生的效果不太稳定。肾衰竭时二氮嗪的蛋白结合率降低,这可能与白蛋白浓度降低有关。肾功能损害与快速注射二氮嗪的降压效果之间存在关联。这可以用肾衰竭患者快速注射后游离(未结合)药物浓度更高来解释。肾衰竭时二氮嗪及其代谢产物的肾清除率受损,但这不太可能影响其活性。