中华临床医师杂志（电子版）
中華臨床醫師雜誌（電子版）
중화림상의사잡지（전자판）
CHINESE JOURNAL OF CLINICIANS(ELECTRONIC VERSION)
2015年
16期
2979-2984
,共6页
心力衰竭%脑啡肽酶%酶抑制剂%受体,血管紧张素
心力衰竭%腦啡肽酶%酶抑製劑%受體,血管緊張素
심력쇠갈%뇌배태매%매억제제%수체,혈관긴장소
Heart failure%Neprilysin%Enzyme inhibitors%Receptors,angiotensin
肾素血管紧张素系统（RAAS）长期的过度激活在心力衰竭（简称心衰）的病理生理机制中扮演着重要的角色，阻断 RAAS 的药物目前已然成为了心衰治疗的基石。血管紧张素Ⅱ（Ang-Ⅱ）具有强大的血管收缩及促进心肌细胞发生肥大、纤维化的作用，过多的Ang-Ⅱ与很多心血管疾病相关，血管紧张素酶抑制剂（ACEI）及血管紧张素受体拮抗剂（ARB）可以阻断这种作用。心房钠尿肽和B型脑钠肽通过利钠、利尿调节机体的血压系统，舒张血管、抗细胞增殖等作用。双重血管紧张素受体-脑啡肽酶抑制剂在高血压和心衰中的疗效及安全性日益受到重视，奥马曲垃在治疗心衰和高血压中显示出了良好的前景，但是该药口服生物利用度低、血管性水肿发生率高。LCZ-696是由缬沙坦和AHU-377以1∶1的比例组成的复方制剂，在临床试验中展现出了独特的优势。该新型药物有可能改变以往的心衰药物治疗框架。
腎素血管緊張素繫統（RAAS）長期的過度激活在心力衰竭（簡稱心衰）的病理生理機製中扮縯著重要的角色，阻斷 RAAS 的藥物目前已然成為瞭心衰治療的基石。血管緊張素Ⅱ（Ang-Ⅱ）具有彊大的血管收縮及促進心肌細胞髮生肥大、纖維化的作用，過多的Ang-Ⅱ與很多心血管疾病相關，血管緊張素酶抑製劑（ACEI）及血管緊張素受體拮抗劑（ARB）可以阻斷這種作用。心房鈉尿肽和B型腦鈉肽通過利鈉、利尿調節機體的血壓繫統，舒張血管、抗細胞增殖等作用。雙重血管緊張素受體-腦啡肽酶抑製劑在高血壓和心衰中的療效及安全性日益受到重視，奧馬麯垃在治療心衰和高血壓中顯示齣瞭良好的前景，但是該藥口服生物利用度低、血管性水腫髮生率高。LCZ-696是由纈沙坦和AHU-377以1∶1的比例組成的複方製劑，在臨床試驗中展現齣瞭獨特的優勢。該新型藥物有可能改變以往的心衰藥物治療框架。
신소혈관긴장소계통（RAAS）장기적과도격활재심력쇠갈（간칭심쇠）적병리생리궤제중분연착중요적각색，조단 RAAS 적약물목전이연성위료심쇠치료적기석。혈관긴장소Ⅱ（Ang-Ⅱ）구유강대적혈관수축급촉진심기세포발생비대、섬유화적작용，과다적Ang-Ⅱ여흔다심혈관질병상관，혈관긴장소매억제제（ACEI）급혈관긴장소수체길항제（ARB）가이조단저충작용。심방납뇨태화B형뇌납태통과리납、이뇨조절궤체적혈압계통，서장혈관、항세포증식등작용。쌍중혈관긴장소수체-뇌배태매억제제재고혈압화심쇠중적료효급안전성일익수도중시，오마곡랄재치료심쇠화고혈압중현시출료량호적전경，단시해약구복생물이용도저、혈관성수종발생솔고。LCZ-696시유힐사탄화AHU-377이1∶1적비례조성적복방제제，재림상시험중전현출료독특적우세。해신형약물유가능개변이왕적심쇠약물치료광가。
Based on accumulating evidence that chronic over-activity of the renin-angiotensin-aldosterone system (RAAS) plays a fundamental role in HF pathophysiology, drugs inhibiting key components of the RAAS have become a cornerstone of contemporary drug therapy. For example, angiotensin-converting enzyme inhibitors (ACEI) reduce biosynthesis of angiotensin-Ⅱ (Ang-Ⅱ), one of the strongest vasoconstrictors, pro-hypertrophic and pro-fibrotic hormones in man. Excessive levels of Ang-Ⅱ have been implicated in many cardiovascular diseases, and additional to ACEI, the detrimental actions of Ang-Ⅱ can be abrogated by direct angiotensin receptor blockers (ARB). Importantly the NPs, particularly ANP and BNP, represents the body's own blood pressure lowering system. Besides promoting vasodilation, NPs counteract pathological growth, fibrosis and dysfunction of heart, kidneys, brain and the vasculature. Dual-acting angiotensin receptor neprilysin inhibitors (ARNI) are under scientific scrutiny for the treatment of hypertension and HF. Early dual ARNI agents such as sampatrilat demonstrated promising effect in HF and hypertension but were discontinued because of poor oral bioavailability and increase in prevalence of angioedema. LCZ-696 is a fixed dose combination of valsartan and AHU-377 in a 1∶1 ratio and is the first and most clinically advanced compound in this new class. As well as, the novel therapeutic agents (LCZ696) currently being evaluated which maybe could change our pharmacological framework for HF.
