摘要
目的：观察国家二类新药－托拉塞米注射液在中国健康受试者中的安全性、耐受程度及利尿作用，为Ⅱ期临床试验给药剂量的确定提供依据。方法：本研究采用开放、随机的试验设计，将符合入选标准的３０名健康中国男性受试者随机分为 ５组，每组 ６名，分别注射托拉塞米注射液 ２．５，１０，２０，４０，８０ｍｇ，观察临床体征、实验室检查指标的变化及其尿量的变化。结果：在静脉注射托拉塞米注射液的所有剂量组，受试者都能耐受。４０ｍｇ组开始出现药物不良反应，其中２例头晕和１例恶心是中度的，其它均为轻度。８０ｍｇ组的１例肌肉痉挛是中度的，１例头晕和呕吐是重度的，但持续时间较短，其它均为轻度。在静脉注射托拉塞米注射液１０ ｍｇ后，已表现出利尿作用，在４０ｍｇ剂量组达最大，而且与８０ｍｇ组的利尿作用无显著差异。结论：在剂量２．５～８０ｍｇ范围内的所有剂量显示对健康受试者是安全和耐受的，临床推荐以不超过８０ｍｇ为宜。
OBJECTIVE: The tolerance and diuretic properties of torasemide after intravenous administration to healthy volunteers were studied. METHOD: The study was opened and randomized. Five groups, each of 6 subjects, were given single ascending i.v. doses ranging from 2.5 mg to 80 mg. The changes of vital signs and laboratory values were recorded. RESULTS: The subjects in all groups were well tolerated. There were 2 subjects complained of slight dizzy and 1 nausea at 40 mg dose group. At the highest dose (80mg) 1 volunteer complained of cramps in the knees calves and feet. There were no significant changes in other vital signs. Some significant drug-related changes were encountered in the within-study haematology and biochemistry assessments. Torasemide proved to be a potent diuretic 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. CONCLUSION: Torasemide was well tolerated from all perspectives studied. It showed a potent diuretic property.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第1期61-65,共5页
The Chinese Journal of Clinical Pharmacology
关键词
托拉塞米
耐受性
利尿作用
torasemide
tolerance
diuretic properties
