Generic Name for EXFORGE
Amlodipine (as besylate), valsartan; 5mg/160mg, 5mg/320mg, 10mg/160mg, 10mg/320mg; tabs.

Legal Classification:
Rx

Pharmacological Class for EXFORGE
Calcium channel blocker (dihydropyridine) + angiotensin II receptor blocker.

Manufacturer of EXFORGE
Novartis Pharmaceuticals Corp
 

Indications for EXFORGE
Hypertension.

Adult dose for EXFORGE
Take once daily. Initial therapy and not volume depleted: Initially 5/160mg; may increase after 1–2 weeks up to max 10/320mg. Add-on therapy: may be used if not controlled on monotherapy; if inadequate response after 3–4 weeks, may titrate up to max 10/320mg. Replacement therapy: may be substituted for the titrated components. Maximum effects within 2 weeks after dose change.

Children's dosing for EXFORGE
Not recommended.

Warnings/Precautions for EXFORGE
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.D; avoid in 2nd and 3rd trimesters). Nursing mothers: not recommended.

Interactions for EXFORGE
Concomitant K+ supplements, K+ sparing diuretics, K+ containing salt substitutes may lead to hyperkalemia; increased serum creatinine in HF.

Adverse Reactions for EXFORGE
Peripheral edema, nasopharyngitis, upper respiratory infection, dizziness; rare: orthostatic hypotension, postural dizziness.

How is EXFORGE supplied?
Tabs—30, 90

Related Disease:
Hypertension

FDA批准治疗高血压的复方制剂Exforge HCT

2009年4月30日，诺华公司宣布美国食品药品管理局(US Food and Drug Administration, FDA)已经批准Exforge HCT用于治疗高血压。该药是同时含有三种抗高血压处方药物成分的复合制剂，这三种成分分别为钙通道拮抗剂/氨氯地平，血管紧张素受体拮抗剂/缬沙坦，和利尿剂/双氢克尿塞。制造商希望Exforge HCT成为那些应用两种类型抗高血压药物联合治疗后效果不佳患者一种重要的新选择。

Exforge HCT可有效治疗中重度高血压患者(例如，收缩压范围:145 mm Hg～200 mm Hg，舒张压范围:100 mm Hg～120 mm Hg)。一项临床试验显示，患者接受最高剂量的Exforge HCT(氨氯地平/缬沙坦/双氢克尿塞: 10mg/320mg/25mg)与采用相同剂量的所有上述两种药物联合治疗相比，收缩压可多下降18%~29%，舒张压可多下降19%~32%。Exforge HCT较缬沙坦/双氢克尿塞320mg/25mg使收缩压/舒张压分别多下降7.6/5.0 mmHg；较氨氯地平/缬沙坦10mg/320mg使收缩压/舒张压多下降6.2/3.3 mmHg；较氨氯地平/双氢克尿塞10mg/25mg使血压多下降8.2/5.3 mmHg。这些结果也包括一项未知样本大小的安慰剂效应。动态血压监测显示Exforge HCT的降压效果可持续24小时。

采用任何2种下列药物治疗后效果不理想的患者可改用单一复方制剂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。

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。”

关于高血压

高血压及其后果是世界头号死亡原因。它导致动脉损伤，加重心、脑、肾和其他重要器官的负担。如不加控制，高血压可引发心脏病，中风，心脏和肾脏衰竭，继而死亡。目前，成年人中至少有25%以上的人群患有高血压，全球近10亿人患病，预计到2025年，患病人数将升至15.6亿人。

高血压的治疗仍是一个重要问题。据估计，10个高血压患者中有7个不能将血压控制到推荐水平，而且在高风险患者中，如患糖尿病的患者，血压控制率就更低了。大多数患者需要两种或更多药物以使血压得到足够的控制。

美国食品药品监督管理局（FDA）已批准两个固定复方制剂，复代文®（缬沙坦和氢氯噻嗪）和Exforge®（氨氯地平和缬沙坦），作为一线用药，用于需要多种药物治疗以令血压达标的病人。

FDA approves Exforge HCT® - the only high blood pressure treatment to combine three medications in a single pill

• Exforge HCT combines in one pill a calcium channel blocker, angiotensin receptor blocker and diuretic (amlodipine, valsartan, hydrochlorothiazide)
• In a clinical trial, Exforge HCT demonstrated significantly greater reductions in systolic and diastolic BP, compared to all dual combinations of its components1
• Up to 85% of patients may need multiple medications to help control their blood pressure2 and many need three or more1
• Exforge HCT can help appropriate patients reach BP goals; offers convenienceand potential cost savings by reducing up to three co-payments to one

Basel, 30 April, 2009 — The US Food and Drug Administration (FDA) has approved Exforge HCT, the only single pill to combine the three most prescribed high blood pressure treatments in their classes in the US3: the calcium channel blocker amlodipine, the angiotensin receptor blocker valsartan, and the diuretic hydrochlorothiazide. Exforge HCT is an important new option for patients who have tried taking dual combinations of these classes of blood pressure medications without success.

“The majority of people with hypertension will require more than one medication to control their blood pressure and it’s not uncommon for patients with severe hypertension and/or patients requiring stricter blood pressure control to need three or more medications,” said David A. Calhoun, MD, Professor of Medicine, Vascular Biology and Hypertension Program, University of Alabama at Birmingham. “With a triple combination option, appropriate patients may experience a simpler routine of a convenient, once-daily pill to help them control their high blood pressure.”

Exforge HCT provides proven efficacy in patients with moderate to severe hypertension (MSDBP 100 mmHg and <120 mmHg, MSSBP 145 mmHg and <200 mmHg)1. In a clinical trial, the maximum dose of Exforge HCT (amlodipine/valsartan/hydrochlorothiazide 10 mg/320 mg/25 mg) demonstrated additional reductions of 18-29% in systolic blood pressure and 19-32% in diastolic blood pressure when compared to all dual combinations of its components at the same doses1,4. The reductions in systolic/diastolic blood pressure with Exforge HCT were 7.6/5.0 mmHg greater than with valsartan/hydrochlorothiazide 320mg/25 mg; 6.2/3.3 mmHg greater than with amlodipine/valsartan 10mg/320 mg; and 8.2/5.3 mmHg greater than with amlodipine/hydrochlorothiazide 10 mg/25 mg4. These results also include a placebo effect of unknown size. Ambulatory blood pressure monitoring showed that the blood pressure lowering effect of Exforge HCT was maintained throughout the 24-hour period4.

High blood pressure affects approximately 74 million adults in the US and one in four adults worldwide5. If high blood pressure is not treated, it can lead to heart attack and stroke. Exforge HCT is not indicated for the treatment or prevention of heart attack or stroke.2/3 Research suggests that up to 85% of patients may need multiple medications2 and many need three or more1 to help control their blood pressure. Patients may find treatment more convenient with one single pill rather than separate pills.

Exforge HCT contains three effective medicines that work in three different ways1. A patient may be switched to the single pill combination Exforge HCT if blood pressure is not adequately controlled on any two of the following anti-hypertensive classes: calcium channel blockers, angiotensin receptor blockers, and diuretics4. The full blood pressure lowering effect was achieved two weeks after being on the maximal dose of Exforge HCT.

“This approval of Exforge HCT as the only single blood pressure pill combining the efficacy of three of the most-prescribed treatments in their classes represents a significant milestone toward reducing the burden of unmet need in hypertension,” said Trevor Mundel, MD, Global Head of Development at Novartis Pharma AG. “Novartis remains confident in the important role of single pill combination medications to help appropriate patients achieve their blood pressure targets, while providing physicians with a range of powerful yet flexible combinations of doses to effectively manage high blood pressure in different patients.”

Exforge and Exforge HCT will be offered at the same price in the US on a doseequivalent basis, essentially providing the added diuretic in Exforge HCT at no additionalcost. Since Exforge HCT combines three medications in a single pill, patients may benefit from reduced insurance co-payments.