Nakajima T, Yamada T, Setoguchi M
Research Laboratories, Yoshitomi Pharmaceutical Industries, Fukuoka, Japan.
J Cardiovasc Pharmacol. 1992 Jan;19(1):102-7. doi: 10.1097/00005344-199201000-00014.
Plasma and tissue angiotensin-converting enzyme (ACE) activities were measured in spontaneously hypertensive rats (SHR) after single or repeated oral (p.o.) treatment with a hypotensive dose (1 mg/kg) of quinapril and compared with those after administration of enalapril (1 mg/kg). The degree of ACE inhibition in response to quinapril varied in tissues; marked inhibition was observed in aorta, lung, and plasma by single treatment with quinapril, and inhibition in plasma and aorta caused by quinapril was more potent than that caused by enalapril. The prolonged ACE inhibition was observed in the aorta, a target organ, by repeated treatment with quinapril for 2 weeks. These results indicate that quinapril has a good pharmacokinetic profile, namely rapid absorption and easy penetration to the target organ. In addition, quinapril produced greater inhibition of cardiac ACE than did enalapril after either p.o. or intravenous (i.v.) administration, suggesting the beneficial effects of quinapril in treatment of congestive heart failure (CHF).
用降压剂量(1毫克/千克)的喹那普利单次或重复口服(p.o.)治疗自发性高血压大鼠(SHR)后,测定其血浆和组织中的血管紧张素转换酶(ACE)活性,并与给予依那普利(1毫克/千克)后的活性进行比较。喹那普利对ACE的抑制程度在不同组织中有所不同;单次给予喹那普利后,在主动脉、肺和血浆中观察到明显抑制,且喹那普利对血浆和主动脉的抑制作用比依那普利更强。通过用喹那普利重复治疗2周,在靶器官主动脉中观察到ACE抑制作用持续存在。这些结果表明喹那普利具有良好的药代动力学特征,即吸收迅速且易于渗透到靶器官。此外,无论是口服还是静脉注射(i.v.)给药后,喹那普利对心脏ACE的抑制作用都比依那普利更强,提示喹那普利在治疗充血性心力衰竭(CHF)方面具有有益作用。