Brunner H R, Christen Y, Munafo A, Lee R J, Waeber B, Nussberger J
Hypertension Division, University Hospital Center, Lausanne, Switzerland.
Am J Hypertens. 1992 Dec;5(12 Pt 2):243S-246S. doi: 10.1093/ajh/5.12.243s.
This series of studies was designed to assess in normal volunteers the relationships between various doses (5, 10, 20, 40, 80, and 120 mg) of the orally active angiotensin II antagonist losartan (DuP 753, MK-954) and their inhibitory effect on the pressure response to a given bolus of angiotensin I or II. It was found that the maximal inhibitory effect was reached with a dose of 80 mg. The minimal dose necessary for maximal efficacy would therefore be expected to be between 40 and 80 mg. The effect lasted for more than 24 h and was related almost exclusively to the circulating levels of the active metabolite EXP3174. It remains to be demonstrated in hypertensive patients that the same dose relationship holds for the antihypertensive effect, but preliminary data already suggest that this is the case.
本系列研究旨在评估正常志愿者口服活性血管紧张素II拮抗剂氯沙坦（DuP 753，MK - 954）的不同剂量（5、10、20、40、80和120毫克）与它们对给予一定剂量血管紧张素I或II后压力反应的抑制作用之间的关系。结果发现，80毫克剂量时达到最大抑制作用。因此，预计产生最大疗效所需的最小剂量在40至80毫克之间。该作用持续超过24小时，且几乎完全与活性代谢物EXP3174的循环水平有关。在高血压患者中，同样的剂量关系是否适用于降压作用仍有待证明，但初步数据已表明情况确实如此。
