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題 名 | 新一代的降血壓藥物--Aliskiren=New Generation of Antihypertensive Drug--Aliskiren |
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作 者 | 顧曉耘; | 書刊名 | 藥學雜誌 |
卷 期 | 25:3=100 2009.09[民98.09] |
頁 次 | 頁122-128 |
分類號 | 418.221 |
關鍵詞 | 腎素-血管收縮素系統; 腎素抑制劑; 血管收縮素轉化酶抑制劑; 血管收縮素接受體阻斷劑; Renin-angiotension system; RAS; Renin inhibitor; Angiotension converting enzyme inhibitor; ACEI; Angiotension receptor blocker; ARB; |
語 文 | 中文(Chinese) |
中文摘要 | 2007年3月,美國 FDA核准新一代的降血壓藥物 aliskiren上市,有別於同樣作用在腎素 -血管收縮素系統 (renin angiotension system, RAS)的藥物 -血管收縮素轉化酶抑制劑 (angiotension converting enzyme inhibitor, ACEI)和血管收縮素接受體阻斷劑 (angiotension receptor blocker, ARB);此藥與腎素的酵素活性位置做專一可逆性的結合,於是對腎素 -血管收縮素系統抑制來產生降血壓的作用。 Aliskiren於口服之後一到三小時達到最大濃度,在體內主要經由 CYP450系統代謝,但是並不會誘導或是抑制 CYP450的酵素活性;另一方面, aliskiren為 p-glycoprotein的受質,因此其吸收會受到抑制 p-glycoprotein的藥物的影響。有別於其他作用在 RAS的藥物, aliskiren較少產生乾咳的副作用,主要常見的副作用為腹瀉和持續使用後會造成血鉀上升。 目前在 FDA認可上市的有 tekturna和 tekturna HCT,分別為 aliskiren hemifumarate和aliskiren hemifumarate + hydrochlorothiazide,並且其中的 aliskiren分別具有 150mg和300mg兩種劑量,因其半衰期超過 24小時建議一天一次使用,此藥透過全新的機轉來治療高血壓,並且目前只有兩大試驗 AVOID和 ALOFT借由 add-on therapy間接證實其具有末期器官保護 (end organ protection)的作用,因此其在臨床的效果仍有待更多的試驗結果來證實。 |
英文摘要 | On March 2007, FDA approved the new generation of antihypertensive drug for marketing, aliskiren. With a different mechanism from ACEI and ARB, this drug selectively reversibly binds with renin and therefore suppresses RAS to lower the blood pressure. Aliskiren achieves its maximal plasma concentration in 1-3 hours after oral intake and it is mainly metabolized via the CYP450 system, which does not inhibit or induce the CYP450 activity. On the other hand, as being the substrate of p-glycoprotein; therefore, aliskiren absorption was interrupted by the drugs which inhibit the p-glycoprotein activity. Aliskiren has fewer side effects such as dry cough in comparison with RASrelated drugs and its common adverse effects are diarrhea and hyperkalemia after prolonged use. FDA had approved aliskiren hemifumarate, with the dosage of 150 mg and 300 mg, and aliskiren hemifumarate with hydrochlorothiazide for marketing until now. Because of its over-24hour half-life, it is supposed to be taken once daily. Aliskiren lowers blood pressure via a brand-new mechanism, and there are only two large clinical trials, AVOID and ALOFT, indirectly proveing its effect on end organ protection by add-on therapy; therefore, what we expect most is more randomized clinical trials to be published. |
本系統中英文摘要資訊取自各篇刊載內容。