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呋塞米与BAY g 2821(莫唑胺)药效学作用比较及BAY g 2821(莫唑胺)药效学与药代动力学的相关性

Comparison of the pharmacodynamic effects of furosemide and BAY g 2821 and correlation of the pharmacodynamics and pharmacokinetics of BAY g 2821 (muzolimine).

作者信息

Loew D, Ritter W, Dycka J

出版信息

Eur J Clin Pharmacol. 1977 Dec 16;12(5):341-4. doi: 10.1007/BF00562448.

Abstract

In a biometrically planned, double-blind study on 12 Oedema-free male patients the saluretic effect of muzolimine 30 mg was compared with furosemide 40 mg. The plasma level of muzolimine was determined and correlated with its pharmacodynamics. In terms of excretion during the 12-hour observation period muzolimine 30 mg had as great a cumulative effect as furosemide 40 mg. There was a significant difference in the time-response curve. During the first gwo hours furosemide 40 mg had more saluretic effect than muzolimine 30 mg. Between two and four hours there was no significant difference between the two substances. Between four and six hours, however, muzolimine was somewhat more effective than furosemide, although the difference did not reach the level of significance. After 6 h there was no longer any difference between the two compounds. The half-life of the fall in concentration of muzolimine in plasma was 3.7 up to 10 h after its administration. The time-response curve of the increased urine excretion correlated well with the time course of the concentration of muzolimine in plasma.

摘要

在一项针对12名无水肿男性患者的生物计量学设计、双盲研究中,比较了30毫克莫唑胺与40毫克呋塞米的利钠作用。测定了莫唑胺的血浆水平,并将其与药效学进行关联。在12小时观察期内,就排泄情况而言,30毫克莫唑胺的累积效应与40毫克呋塞米相当。时间 - 反应曲线存在显著差异。在最初两小时内,40毫克呋塞米的利钠作用比30毫克莫唑胺更强。在两到四小时之间,两种药物之间没有显著差异。然而,在四到六小时之间,莫唑胺比呋塞米稍有效一些,尽管差异未达到显著水平。6小时后,两种化合物之间不再有差异。给药后,血浆中莫唑胺浓度下降的半衰期在3.7至10小时之间。尿量增加的时间 - 反应曲线与血浆中莫唑胺浓度的时间进程密切相关。

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