Clostre F, Etienne A
Henri Beaufour Institute, Le Plessis-Robinson, France.
Drugs Exp Clin Res. 1988;14(2-3):73-82.
Cicletanine is a new antihypertensive molecule which acts directly on vascular smooth muscle by increasing prostacyclin synthesis and interacting with various agents which mobilize intracellular Ca2+ ions. General pharmacological studies have shown that in the anaesthetized normotensive dog, cicletanine does not induce tachycardia (even at high doses) and does not modify aortic, femoral or coronary blood flow. Moreover, cicletanine shows a protective effect on vascular permeability and capillary hyperpermeability. This protective action on the vascular wall is of importance, since one of the direct vascular consequences of arterial hypertension is a fragilisation of vessel walls, tissue oedema and even vascular rupture. Cicletanine slows down the thrombogenic process initiated by electric arterial stimulation. Retardation of the thrombogenic process by the drug may be explained by the stimulation that cicletanine exerts on the synthesis and production of prostacyclin. Behavioural studies in mice, rats and primates have shown that cicletanine has no sedative effects, even at very high doses. General pharmacological studies have demonstrated that both cardiovascular function and the central nervous system are equally tolerant to cicletanine. Cicletanine is an antihypertensive agent which has no effect on cardiovascular haemodynamics and is able to prevent some rheological and vascular-linked cardiac risks of hypertension.
西氯他宁是一种新型抗高血压分子，它通过增加前列环素的合成并与各种动员细胞内钙离子的因子相互作用，直接作用于血管平滑肌。一般药理学研究表明，在麻醉的正常血压犬中，西氯他宁不会诱发心动过速（即使在高剂量时），也不会改变主动脉、股动脉或冠状动脉血流量。此外，西氯他宁对血管通透性和毛细血管高通透性具有保护作用。这种对血管壁的保护作用很重要，因为动脉高血压的直接血管后果之一是血管壁脆弱、组织水肿甚至血管破裂。西氯他宁可减缓由动脉电刺激引发的血栓形成过程。药物对血栓形成过程的延缓作用可能是由于西氯他宁对前列环素合成和产生的刺激。在小鼠、大鼠和灵长类动物中的行为学研究表明，西氯他宁即使在非常高的剂量下也没有镇静作用。一般药理学研究表明，心血管功能和中枢神经系统对西氯他宁的耐受性相同。西氯他宁是一种抗高血压药物，对心血管血液动力学没有影响，并且能够预防一些高血压相关的流变学和血管方面的心脏风险。
