Fornes P, Richer C, Vacher E, Bruneval P, Giudicelli J F
Département de Pharmacologie, Faculté de Médecine Paris-Sud, France.
J Cardiovasc Pharmacol. 1993 Aug;22(2):305-13. doi: 10.1097/00005344-199308000-00021.
The effects of long-term oral administration of losartan on the occurrence of stroke and on mortality were investigated in young salt-loaded stroke-prone spontaneously hypertensive rats (SHR-SPs) during the treatment period (5-20 weeks of age) and up to 8 weeks thereafter. Two doses of losartan, 1 and 10 mg/kg/day, were investigated, which afforded no and only moderate antihypertensive effects, respectively. During the treatment period, losartan at both doses completely suppressed stroke and mortality and strongly opposed (low dose) or abolished (high dose) the increases in saline intake, diuresis, and proteinuria observed in controls. It markedly limited (low dose) or abolished (high dose) vascular fibrinoid necrosis formation in the brain, kidneys, and heart. Finally, losartan, especially at the high dose, reduced arterial thickening and glomerular and tubulo-interstitial lesions in the kidneys, as well as arterial thickening, infarction, and fibrosis in the heart. Eight weeks after treatment discontinuation, all animals but one (low dose) were still alive. Vascular fibrinoid necrosis development remained strongly prevented (low dose) or fully suppressed (high dose) in all investigated organs. Finally, cardiac and renal lesions tended to worsen, and proteinuria was noted only in the low-dose group. We conclude that in SHR-SPs, angiotensin II, through AT1 receptor stimulation, most likely plays a major role in fibrinoid necrosis formation, vascular proliferative changes, and stroke occurrence and that losartan, most likely independently of its effect on blood pressure, affords a full and long-lasting protection against stroke and mortality both during and after the treatment period.
在年轻的盐负荷易卒中自发性高血压大鼠(SHR-SPs)的治疗期(5至20周龄)及此后长达8周的时间内,研究了长期口服氯沙坦对卒中发生及死亡率的影响。研究了两种剂量的氯沙坦,分别为1和10 mg/kg/天,其中低剂量无降压作用,高剂量仅有中度降压作用。在治疗期间,两种剂量的氯沙坦均完全抑制了卒中和死亡率,并强烈对抗(低剂量)或消除(高剂量)了对照组中观察到的盐摄入量、尿量和蛋白尿的增加。它显著限制(低剂量)或消除(高剂量)了脑、肾和心脏中的血管纤维样坏死形成。最后,氯沙坦,尤其是高剂量时,减少了肾脏的动脉增厚以及肾小球和肾小管间质病变,以及心脏的动脉增厚、梗死和纤维化。停药8周后,除一只(低剂量组)外所有动物均存活。在所有研究器官中,血管纤维样坏死的发展仍受到强烈抑制(低剂量)或完全抑制(高剂量)。最后,心脏和肾脏病变有恶化趋势,仅在低剂量组观察到蛋白尿。我们得出结论,在SHR-SPs中,血管紧张素II通过刺激AT1受体,很可能在纤维样坏死形成、血管增殖性变化和卒中发生中起主要作用,并且氯沙坦很可能独立于其对血压的影响,在治疗期间及治疗后均能提供全面且持久的预防卒中和降低死亡率的保护作用。