Sureshkumar Kalathil K, Vasudevan Sapna, Marcus Richard J, Hussain Sabiha M, McGill Rita L
Allegheny General Hospital, Division of Nephrology and Hypertension, 320 East North Avenue, Pittsburgh, PA 15212, USA.
Expert Opin Pharmacother. 2008 Apr;9(5):825-37. doi: 10.1517/14656566.9.5.825.
Aliskiren, the first renin inhibitor with sufficient bioavailability for oral use, is now available to clinicians treating hypertension.
The novel mechanism by which aliskiren works was used to provide understanding of its therapeutic and adverse effects.
After reviewing physiology and preclinical studies, human studies of aliskiren in hypertension were reviewed. Effects of aliskiren on serum levels and enzymatic activity of renin were explored.
RESULTS/CONCLUSIONS: Aliskiren has antihypertensive efficacy similar to existing medications such as thiazide diuretics, angiotensin-converting enzyme inhibitors and angiotensin receptor blockers, and can be used in drug combinations. Preclinical studies indicate possible cardioprotective and renoprotective effects, similar to other inhibitors of the renin-angiotensin cascade, but future studies are needed in humans.
阿利吉仑是首个口服生物利用度足够的肾素抑制剂，现已可供治疗高血压的临床医生使用。
利用阿利吉仑的新型作用机制来了解其治疗作用和不良反应。
在回顾生理学和临床前研究后，对阿利吉仑治疗高血压的人体研究进行了综述。探讨了阿利吉仑对肾素血清水平和酶活性的影响。
结果/结论：阿利吉仑具有与噻嗪类利尿剂、血管紧张素转换酶抑制剂和血管紧张素受体阻滞剂等现有药物相似的降压疗效，可用于联合用药。临床前研究表明，与肾素-血管紧张素级联反应的其他抑制剂类似，阿利吉仑可能具有心脏保护和肾脏保护作用，但仍需在人体中进行进一步研究。
