Lambe R, Kennedy O, Kenny M, Darragh A
Eur J Clin Pharmacol. 1986;31 Suppl:9-14. doi: 10.1007/BF00541461.
The tolerance and diuretic properties of torasemide after oral or intravenous administration to healthy volunteers were studied. Six groups, each of 6 subjects, were given single rising oral doses ranging from 10 to 100 mg; 8 subjects received ascending i.v. doses on alternate days, ranging from 2.5 to 80 mg. At the highest oral doses investigated (80 mg and 100 mg) a number of volunteers complained of cramps in the knees, calves and feet. These symptoms were generally of short duration. Similar effects were not encountered during the intravenous study. There were no significant changes in ECG. Some significant drug-related changes were encountered in the within-study biochemistry and haematology assessments. Torasemide proved to be a potent diuretic following oral administration at all the doses investigated and following intravenous administration at all doses except 2.5 mg. A linear relationship existed between the urine output and the logarithm of the dose, and both sodium and chloride excretion were linearly correlated with urine volume. The rate of potassium excretion was markedly lower than that of sodium and chloride and was linearly correlated with the logarithm of the urine volume. Torasemide was well tolerated from all perspectives studied. It showed a potent diuretic property, and was equally effective by the oral and intravenous routes.
研究了口服或静脉注射托拉塞米后健康志愿者的耐受性和利尿特性。将6组，每组6名受试者，给予10至100毫克的单次递增口服剂量；8名受试者每隔一天接受2.5至80毫克的递增静脉注射剂量。在研究的最高口服剂量（80毫克和100毫克）下，一些志愿者抱怨膝盖、小腿和脚部抽筋。这些症状通常持续时间较短。在静脉注射研究中未遇到类似影响。心电图无显著变化。在研究中的生物化学和血液学评估中遇到了一些与药物相关的显著变化。在所有研究剂量下口服托拉塞米以及除2.5毫克外的所有静脉注射剂量下，托拉塞米都被证明是一种强效利尿剂。尿量与剂量的对数之间存在线性关系，钠和氯的排泄与尿量呈线性相关。钾排泄率明显低于钠和氯，且与尿量的对数呈线性相关。从所研究的所有方面来看，托拉塞米耐受性良好。它显示出强效利尿特性，口服和静脉注射途径同样有效。
