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[酮色林急性给药对高血压患者血清素外周代谢及血流动力学指标的影响]

[The effect of acute administration of ketanserin on the peripheral metabolism of serotonin and hemodynamic indicators in hypertensive patients].

作者信息

Sebeková K, Raucinová M, Jurecková K

机构信息

Výskumného ústavu lekárskej bioniky Centra klinickej farmakológie v Bratislave.

出版信息

Bratisl Lek Listy. 1990 Nov;91(11):829-32.

PMID:2265368
Abstract

The effect of IV administration of ketanserin (Janssen Pharmaceutica, Beerse, Belgium) on peripheral serotonin (5HT) metabolism and on hemodynamic parameters was compared with the placebo effect. Ten hypertensive patients were infused placebo (400 ml of 5% glucose) or received 20 mg ketanserin IV followed by infusion of 20 mg ketanserin in 400 ml of 5% glucose. Increase in platelet 5HT consent without changes in plasma 5HT plasma levels, increase in urinary 5HT excretion and decrease in 5-hydroxyindole-acetic acid (5HIAA) excretion were observed under ketanserin administration compared to the placebo period. Blood pressure dropped effectively under ketanserin. Total peripheral resistance (TPR) decreased markedly in 2 patients with high initial TPR values. No changes in circulating volume, hematocrit and diuresis were observed. No correlation was found between the parameters of peripheral 5HT metabolism and water metabolism. The decrease in urinary 5HIAA excretion reflected presumably the decreased platelet turnover. The increase in urinary 5HT excretion may have resulted from increased 5HT availability for the proximal tubular cell transport system of organic cations or it may have been the consequence of altered renal 5HT metabolism caused by ketanserin. The concurrent increase in platelet 5HT content and decrease in platelet aggregation indicates a stabilizing effect of ketanserin on hyperactive platelets in hypertensive patients. The effect of ketanserin on platelet turnover is presumably involved in the mechanism of its antihypertensive and antiaggregatory action.

摘要

将酮色林(比利时贝尔泽杨森制药公司生产)静脉给药对周围血清素(5-羟色胺,5HT)代谢及血流动力学参数的影响与安慰剂效应进行了比较。10名高血压患者分别输注安慰剂(400毫升5%葡萄糖)或静脉注射20毫克酮色林,随后在400毫升5%葡萄糖中输注20毫克酮色林。与安慰剂期相比,酮色林给药时观察到血小板5HT含量增加而血浆5HT水平无变化,尿5HT排泄增加,5-羟吲哚乙酸(5HIAA)排泄减少。酮色林使血压有效下降。2名初始总外周阻力(TPR)值较高的患者TPR明显降低。未观察到循环血量、血细胞比容和尿量的变化。外周5HT代谢参数与水代谢参数之间未发现相关性。尿5HIAA排泄减少可能反映了血小板周转率降低。尿5HT排泄增加可能是由于近端肾小管细胞有机阳离子转运系统的5HT可用性增加,或者可能是酮色林引起的肾脏5HT代谢改变的结果。血小板5HT含量同时增加和血小板聚集减少表明酮色林对高血压患者过度活跃的血小板有稳定作用。酮色林对血小板周转率的影响可能参与了其降压和抗聚集作用的机制。

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