Department of Medicine, University of Bristol.
Br J Clin Pharmacol. 1976 Aug;3(4):613-9. doi: 10.1111/j.1365-2125.1976.tb04884.x.
A double-blind, crossover trial has compared the diuretic response of ten normal male subjects to the oral administration of frusemide (40 mg) and bumetanide (1 mg). Both drugs gave a similar profile, with acute onset and cessation of response, and a marked peak effect. There was no significant difference between the times taken for each drug to produce its peak diuretic effect. The peak rate of diuretic response, and the total response for six hours after drug ingestion, were significantly greater after bumetanide, with respect to urinary volume and sodium excretion. The peak rate of magnesium excretion was greater after bumetanide. There was no difference between the drugs with respect to potassium, calcium or creatinine excretion or the urinary Na/K ratio. Following peak diuresis, potassium excretion did not show a linear return to its control value. At the time of peak diuresis, both drugs caused a significant reduction of euglobulin lysis time; levels of available plasmin were significantly lowered after frusemide, and levels of active plasmin were significantly raised after bumetanide. The significance of these findings in relation to the fibrinolytic mechanism is discussed. Estimations of plasma viscosity, serum total protein and magnesium concentrations showed that maximal haemoconcentration occurred several hours after diuresis.
一项双盲交叉试验比较了 10 名正常男性受试者口服呋塞米(40mg)和布美他尼(1mg)的利尿反应。两种药物的作用模式相似,具有急性起效和停止作用,并具有明显的峰值效应。两种药物达到峰值利尿效应的时间无显著差异。布美他尼的利尿反应峰值速率和药物摄入后 6 小时的总反应均显著大于呋塞米,在尿量和钠排泄方面。布美他尼的镁排泄峰值速率更高。两种药物在钾、钙或肌酐排泄或尿钠/钾比值方面没有差异。在达到峰值利尿作用后,钾排泄并没有线性恢复到对照值。在达到峰值利尿作用时,两种药物均导致优球蛋白溶解时间显著缩短;尿纤维蛋白溶酶原激活物(plasmin)的水平在呋塞米后显著降低,而布美他尼后尿纤维蛋白溶酶原(active plasmin)的水平显著升高。讨论了这些发现与纤维蛋白溶解机制的关系。对血浆粘度、血清总蛋白和镁浓度的估计表明,最大的血液浓缩发生在利尿作用后数小时。