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1-去氨基-8-D-精氨酸加压素(DDAVP)对人体的抗利尿作用。

The antidiuretic action of 1-deamino-8-D-arginine vasopressin (DDAVP) in man.

作者信息

Radó J P, Marosi J, Szende L, Borbély L, Takó J, Fischer J

出版信息

Int J Clin Pharmacol Biopharm. 1976 Apr;13(3):199-209.

PMID:950263
Abstract
  1. After administration of a new vasopressin analogue (DDAVP), a marked and prolonged antidiuresis occurred in 10 patients with pituitary diabetes insipidus. 2. The antidiuretic effects of single intravenous doses of 0.04--24 mug DDAVP and single intranasal doses of 5--320 mug DDAVP were investigated. Time curves of the antidiuretic responses expressed in changes of urine osmolality (Uosm) and free water clearance per 100 ml GFR (CH2O X 100/GFR) are described. 3. Maximal "peak" response was obtained after an intravenous dose of 1 mug within the first 12 hrs (Uosm was 7--800 mOsm/KgH2O). Further increase of dosage resulted only in prolongation of duration of action (up to 48 hrs) and peak ("plateau") effect (up to 24 hrs). 4. There was a linear relationship between the log dose and log osmolality of urine collected in the second 12 hours after administration of single intravenous and intranasal doses of DDAVP. 5. Comparison of the effects of 1 mug lysine-vasopressin and 1 mug DDAVP revealed only slight differences in peak effects, but extreme differences in duration of action. 6. It is concluded that in the evaluation of a synthetic vasopressin analogue the maximal antidiuretic ability and the prolongation of action have to be analysed separately.
摘要
  1. 给予一种新的加压素类似物(去氨加压素)后,10例垂体性尿崩症患者出现显著且持久的抗利尿作用。2. 研究了单次静脉注射0.04 - 24微克去氨加压素和单次鼻内给予5 - 320微克去氨加压素的抗利尿作用。描述了以尿渗透压(Uosm)变化和每100毫升肾小球滤过率(GFR)的自由水清除率(CH2O×100/GFR)表示的抗利尿反应的时间曲线。3. 静脉注射1微克后,在最初12小时内获得最大“峰值”反应(Uosm为7 - 800毫摩尔/千克H2O)。剂量进一步增加仅导致作用持续时间延长(长达48小时)和峰值(“平台期”)效应延长(长达24小时)。4. 单次静脉注射和鼻内给予去氨加压素后,在第二个12小时收集的尿液的对数剂量与对数渗透压之间存在线性关系。5. 比较1微克赖氨酸加压素和1微克去氨加压素的作用,发现峰值效应仅有轻微差异,但作用持续时间有极大差异。6. 得出结论,在评估合成加压素类似物时,必须分别分析最大抗利尿能力和作用延长情况。

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