欧盟的批准是基于涵盖5000多名患者的临床试验，其结果表明，与氨氯地平相比，Exforge疗效更好且水肿发生率更低
诺华公司日前宣布，欧盟已授予Exforge作为治疗高血压的高效、单片新药的上市批准Exforge是在单片里结合了两种最常处方的高血压品牌药物—代文（缬沙坦）和络活喜（苯磺酸氨氯地平）。Exforge适用于那些接受氨氯地平或缬沙坦单一药物治疗而血压不能完全得以控制的患者。
Exforge即将在德国上市，随后取决于络活喜专利保护到期的情况还将在今年陆续在大部分其他欧盟国家上市。继获得美国的临时批准和瑞士的批准之后，Exforge又获得了欧盟的批准决定，该决定适用于所有27个欧盟成员国以及冰岛和挪威的是的。
“高血压是一个严重的卫生问题，如不加以控制，可引发心脏病，中风，心脏和肾脏衰竭，继而死亡，”德国波恩大学内科Rainer Dusing教授说，“将这两种著名的、强效的抗高血压药物合二为一，可帮助患者血压达标并得以保持，且耐受性良好。”
涵盖5000多名患者的临床试验表明，Exforge可使10个患者中有9个达标（即舒张压低于90毫米汞柱，或基线降低超过10毫米汞柱）。试验显示，Exforge可使血压降低36毫米汞柱或在某些人群中降低43毫米汞柱。
总而言之，临床试验表明Exforge具有高效、良好耐受等品质，且副作用方面比单独使用氨氯地平要有显著提高。尤其是，与氨氯地平单一治疗相比，Exforge可降低周围水肿的发生。
“Exforge有望成为吸引患者的治疗选择，因为它将两种最强的作用机制结合到一种药物中，”诺华制药公司全球药品开发总裁James Shannon博士说，“将两种成份复合成一片药物可提高患者的依从性。研究表明，提高高血压患者的依从性可降低医疗成本，降低住院的风险，且降低门诊病人的资源占用。”
FDA批准治高血压的复方制剂Exforge HCT
FDA已批准诺华公司出品的Exforge HCT，该药是唯一同时含有三种抗高血压处方药物成分的复合制剂，这三种成分分别为Exforge (氨氯地平+缬沙坦)和双氢克尿塞。
诺华表示，有研究结果显示，85%的高血压患者需要多种药物——其中多数人需要3种以上抗压药联合治疗控制血压才能达到预定效果。
至此，采用任何两种下列药物治疗后效果不理想的患者可转用Exforge HCT，这些抗压药包括：钙通道阻滞剂、血管紧张素受体阻滞剂和利尿剂。实验表明，患者使用最高剂量的Exforge HCT治疗2周之后，降压效果非常理想。
有专家表示，这种药物为患者带来了一种便利的治疗方式，它每天仅用药一次，在减轻高血压患者治疗负担上具有重要意义。
同等剂量的Exforge和Exforge HCT在美国地区的售价相同。目前，该药也正在接受欧盟委员会的审批。
Pharmacology
Exforge combines two anti-hypertensive drugs that have complementary mechanisms of action: amlodipine, a calcium (Ca+) channel blocker, and valsartan, an angiotensin II (Ang II) antagonist. Amlodipine blocks the influx of Ca+ into vascular smooth muscle and cardiac muscle, with a greater effect on vascular smooth muscle. It is a peripheral artery vasodilator that causes a reduction in peripheral vascular resistance and a reduction in blood pressure. Valsartan blocks the vasoconstrictive and aldosterone-secreting effects of Ang II by blocking its receptor sites in vascular smooth muscle and the adrenal gland.
Clinical Trials
In a placebo-controlled study, 1018 patients with mild-to-moderate hypertension were given three combinations of amlodipine + valsartan, or amlodipine alone (5mg), valsartan alone (80, 160, or 320mg), or placebo. At week 8, the combination treatments (doses of 5/80, 5/160, 5/320mg) were significantly better than their monotherapy components in the reduction of diastolic BP and systolic BP.
In a placebo-controlled study, 1250 patients with mild-to-moderate hypertension were given treatments of two combinations of amlodipine + valsartan (10/160 or 10/320mg), amlodipine alone (10mg), valsartan alone (160 or 320mg), or placebo. At week 8, the combination treatments were shown to be significantly better than their monotherapy components in reducing diastolic and systolic BP.
Adverse Reactions
Peripheral edema, nasopharyngitis, upper respiratory infection, dizziness; rare: orthostatic hypotension, postural dizziness.
Adults
Usual maintenance: 1 tab daily. May switch from both components taken separately to same dose in Exforge. Dose-limiting effects of either component taken separately: may switch to Exforge with a lower dose of that component; if inadequate response after 3–4 weeks, may titrate to max 10/320mg per day. May switch patients not controlled on any dihydropyridine CCB alone or ARB alone to Exforge.
Children
Not recommended.
Precautions
Correct hypovolemia before starting (may need to reduce diuretic) or monitor closely for hypotension. Severe heart failure (HF) (if renal function depends on renin-angiotensin-aldosterone system). Severe obstructive coronary disease. Recent MI. Severe aortic stenosis. Hepatic or severe renal impairment. Renal artery stenosis. Dialysis. Surgery. Pregnancy (Cat. C in 1st trimester, Cat. D in 2nd and 3rd trimesters). Nursing mothers: not recommended.
Interactions
Concomitant K+ supplements, K+ sparing diuretics, K+ containing salt substitutes may lead to hyperkalemia and, in HF patients, increased serum creatinine.
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