阿利吉仑的药理和临床研究

Pharmacology and Clinical Research of Aliskiren

阿利吉仑是有效、口服、低分子量肾素抑制剂,其是根据X-射线晶体学对肾素活性位点进行分子模拟开发出来的抗高血压新药,安全性和耐受性较好。比较研究中发现,阿利吉仑相当于常用降压药物如利尿剂、ACE抑制剂和ARBs。阿利吉仑具有药效持久,并且停药后无反弹,其单用或合用都能显著抑制血清肾素活性。

Aliskiren is an effective,oral,low molecular weight renin inhibitor. According to molecular modeling based upon X-ray crystallography of rennin active site,aliskiren is developed,its safety and tolerability profile is comparable to placebo. In comparison studies,Aliskiren is equivalent to commonly used antihypertensive drugs such as diuretics,ACE inhibitors and ARBs. Aliskiren has prolonged suppression of plasma renin activity and no rebound after aliskiren withdrawal. Aliskiren monotherapy or its combination with other antihypertensive drugs can significantly inhibit the serum renin activity.