部份中文富马酸阿利吉仑处方资料（仅供参考）
aliskiren为第二代肾素抑制剂阿利吉仑是新一代非肽类肾素阻滞药，能在第一环节阻断RAS系统，降低肾素活性，减少AngII和醛固酮的生成，不影响缓激肽和前列腺素的代谢，起到降血压和治疗心血管疾病的作用。从目前研究来看阿利吉仑是强效的、高度选择性的、口服有效的、长效的新一代抗高血压药物。该药作用于肾素依赖性，因此加大剂量给药只会延长时间不会导致血压骤降，与ARB（氯沙坦、替米沙坦）相似，不良反应的发生率与安慰剂组相比无显著差异。
药理作用
ACEI和ARB减弱了AngⅡ抑制肾素合成和释放的负反馈，导致反应性血浆肾素活性(PRA)增高。而阿利吉仑能显著而持续地降低PRA、Ang I、Ang II，与剂量呈正相关。依那普利降低Ang II水平与阿利吉仑相似，但增加PRA 15倍。缬沙坦单药治疗增加PRA、Ang I、Ang II，而阿利吉仑+ARB(缬沙坦)联合治疗的PRA、Ang I和Ang II水平与安慰剂相似，表明阿利吉仑抵消了服用缬沙坦后引起的PRA和Ang II代偿性增高。有学者认为RI对PRA基础水平低的患者降压能力有限，从而限制了阿利吉仑作为单药降压的效用。但此观点目前仍有争论。
药代动力学特点
阿利吉仑相对分子质量小，理化性质稳定。阿利吉仑的亲脂性较低，可起到更好的抵抗肠降解的作用，口服后不会被肠道、血液及肝脏中的肽酶降解，口服生物利朋度大约2．5%，明显高于第l，2代药物。口服l一3 h达血浆峰浓度，广泛分布于血管外间隙，分布容积135 L，蛋白结合率50%。主要经粪便和尿液以原形排泄，几乎不被代谢，只有1．4%的口服剂量，经细胞色素P450同功酶cYP3A4代谢。清除半衰期24—40 h，阿利吉仑每天给药1次，7—8 d达到血药稳态水平。肝脏病病人、肾脏病病人、糖尿病病人或是老年人口服阿利吉仑不用调整剂量。
适应症
单纯性高血压、高血压肥胖、高血压伴糖尿病。
器官保护作用
肾脏保护作用、抗动脉粥样硬化作用、心脏保护作用。
安全性和耐受性
7000例高血压病人的数据分析显示，阿利吉仑每日75—600 mg口服的安全性和耐受性，与安慰剂和ARB相等同，不良事件发生率与安慰剂组相同。较为常见的不良反应是腹泻、腹痛、消化不良、胃食管返流、低血压、头痛、头昏、疲劳、背痛、咳嗽、皮疹、尿酸增加、痛风、肾结石、高钾血症和剂量相关性血红蛋白降低。罕见血管神经性水肿和癫痫发作。阿利吉仑治疗咳嗽发生率较ACEI低，水肿发生率较氨氯地平低。
药物之间相互作用
阿利吉仑与其他降压药物联用时病人耐受性良好，但低血压发生风险增加。与保钾利尿剂、钾补充剂和能够提高血清钾浓度的药物(如肝索、ARB、AcEI)联用，增加高钾血症发生率。阿利吉仑可降低速尿的血药浓度，速尿对阿利吉仑的药代动力学也有轻度影响。但联用时利尿剂引起的低钾血症发生率都有降低趋势。与厄贝沙坦联用，本药的血浓度降低。与阿托伐他汀和酮康唑联用，本药血浓度升高。利福平可降低阿利吉仑的血浆浓度和肾素抑制作用。[2] 
不良反应
治疗依从性差是目前抗高血压治疗的主要问题之一。Stanton和Nussberger等的研究均表明，阿利吉仑37．5，75，150，300mg，每天1次，服药4周，坚持率>95%，受试者能很好地耐受。并在单次给药和多次给药研究中，口服剂量达到640mg，服药8d后，血压正常健康受试者亦能很好地耐受，且没有明显的毒性反应。实验中各项临床实验检查，如血液学、生化和尿液分析，以及体格检查、心电图记录，在整个服药过程中绝大多数保持正常。
目前的观察阿利吉仑不良反应很少，类似于安慰药。最常见的不良反应为乏力、胃肠道反应或头痛。增加阿利吉仑的剂量，不良反应的发生率没有增加。在226例高血压患者服用阿利吉仑300mg/d组中l例出现胸痛和心电图示局部缺血改变，另1例出现低血压休克，经治疗后均得到康复。另外，Dieterle等研究了健康人群中阿利吉仑与华法林钠之间的相互作用，结果显示阿利吉仑基本不影响华法林钠的抗凝作用，不会改变PT、INR、aPTT。
优势
早在30年前，肾素-血管紧张素醛固酮（RAAS）系统在高血压及其并发症发生、发展过程中的重要作用已被认识。其中，肾素作为RAAS系统的起始步骤，可通过直接抑制其活性而阻断RAAS系统的病理作用。雷米吉仑（remikiren）、依那吉仑（enalkiren）等特异性肾素抗体以及肽类肾素拮抗药相继被开发出来，尽管这些制剂能够降低肾素水平，具有明显的降压作用，但因口服剂的生物利用度较低、作用维持时间短、合成费用高等缺点，最终未能成功应用于临床。
在这样的前提下，阿利吉仑的获准应用于临床具有了不寻常的意义。阿利吉仑是第二代肾素-血管紧张素受体抑制剂，虽然和血管紧张素转化酶抑制剂、血管紧张素Ⅱ受体拮抗剂和醛固酮受体阻断剂的作用机制一样，但所不同的是，阿利吉仑直接作用的部位是肾素。在爱尔兰进行的Ⅱ期临床试验证实，阿利吉仑能有效降低轻中度高血压患者的血压水平；在Ⅲ期临床试验中，受试者在开始治疗的2周内就出现了明显的降压效果。此外，阿利吉仑与厄贝沙坦的对比试验也证实了阿利吉仑对轻中度高血压患者的疗效。
尽管阿利吉仑显示出较好的降压作用，但Wright博士指出，降压治疗的主要目标是防止并发症，而现在还不能确切得知阿利吉仑能否防止产生心衰等并发症以及能否对肾起保护作用。 
RASILEZ table. 300mg. 28table
Qualitative and quantitative composition:
Each tablet contains 300mg aliskiren.
Indications
Treatment of essential hypertension.
Dosage and administration:
The recommended dose of Rasilez is 300 mg once daily. In patients whose blood pressure is not adequately controlled, the dose may be increased to 300 mg once daily.
The antihypertensive effect occurs within two weeks after starting treatment with a dose of 300 mg once daily.
Rasilez may be used alone or in combination with other antihypertensive agents.
It should be taken once daily with a light meal, preferably at the same vreem every day. It should not be taken with grapefruit juice.
Renal impairment:
No adjustment of the initial dose pratsietni with mild to severe renal impairment
Hepatic impairment:
No adjustment of the starting dose in patients with mild to severe hepatic impairment
Elderly:
No adjustment of the initial dose in the elderly.
Paediatric/under 18/
Not recommended the use of Rasilez in children and adolescents below 18 years due to insufficient data on safety and efficacy.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. History of angioedema with aliksiren. Hereditary or idiopathic angioedema. Second and third trimesters of pregnancy. Concomitant use of aliskiren with cyclosporine or itraconazole, two highly potent - P-gp, or other potent inhibitors of P-gp is contraindicated.
Special warnings and precautions for use:
Patients taking other drugs that inhibit the renin-angiotensin system and / or those with reduced renal function and / or diabetes mellitus are at increased risk of hyperkalemia during treatment with aliskiren.
Aliskiren should be used with caution in patients with severe congestive heart failure functional class III-IV by NYHA.
If severe or persistent diarrhea Rosilez intake should be stopped.
Angioedema
As with other agents acting on the renin-angiotensin system in patients treated with aliskiren reported cases of angioedema or symptoms suggestive of angioedema.
A subset of these patients there is a history of angioedema or symptoms suggestive of angioedema due in some cases the use of other drugs capable of inducing angioedema, including RAS inhibitors or angiotensin receptor blockers.
Patients with a history of angioedema may be at increased risk of angioedema during treatment with aliskiren. Caution should be exercised when prescribing aliskiren in patients with a history of angioedema, and such patients should be carefully monitored during treatment and especially at the initiation of treatment.
If angioedema need immediate discontinuation of Rasilez, conducting appropriate therapy and monitoring provided until complete and sustained resolution of signs and symptoms.
Sodium and/or volume-depleted
Patients with marked volume-and/or salt-depletion can occur symptomatic hypotension following initiation of treatment with Rasilez. This condition should be corrected prior to administration of Rasilez, or the treatment should start under close observation medicine.
Renal impairment
As with other agents acting on the renin-angiotensin system, caution should be exercised when aliskiren in the presence of predisposing to kidney failure fektori such as hypovolemia, heart disease, liver disease or kidney disease. During post-marketing experience, cases of acute renal failure, reversible upon discontinuation of treatment in at-risk patients receiving aliskiren.
In the event of any signs of renal failure occur, aliskiren should be discontinued immediately.
Renal artery stenosis
No controlled clinical data on the use of Rasilez in patients with unilateral or bilateral renal artery stenosis or stenosis to a solitary kidney. Toda However, as with other agents acting on the renin-angiotensin system, there is an increased risk of renal insufficiency, including acute renal failure in patients with renal artery stenosis treated with aliskiren. Therefore, in these patients, caution is required. If renal failure occurs, treatment should be discontinued
Adverse reactions
Metabolism and nutrition disorders:
Uncommon - hyperkalemia
Gastrointestinal disorders:
Common - Diarrhea
Skin and subcutaneous tissue disorders:
Uncommon - rash
Rare - angioedema
Renal and urinary disorders:
Uncommon - acute renal failure, renal impairment
General disorders and administration site conditions:
Uncommon - peripheral edema
Investigations
Rare - Reduction in hemoglobin, decrease in hematocrit
Rare - Increase in serum creatinine.