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高血压药物Dutoprol近日在美国上市。Dutoprol含有利尿活性成分Toprol-XL（美托洛尔，用于治疗高血压，可以单独使用或者和其他药物配合使用），能够在24小时内降低患者血压。
阿斯利康公司相关人士表示，DUTOPROL一天仅服用一片，为高血压患者提供了新选择。
制造商：
阿斯利康制药公司
类药物：
心脏选择性β1受体阻滞剂+利尿剂。
活性成分（S）：
琥珀酸美托洛尔缓释，氢氯噻嗪; 25/12.5mg，50/12.5mg，100/12.5mg;片。
指示（S）：
高血压。
药理作用：
美托洛尔是1心脏选择性β1-肾上腺素受体阻断剂。在较高的血药浓度，美托洛尔也抑制β2-肾上腺素受体在支气管和血管的肌肉。美托洛尔有没有内在拟交感活性和膜稳定活动是探测在更大的血浆浓度仅比β-封锁的规定。临床研究已经证实，美托洛尔β-阻断活动（1）减少在休息和运动后的心率和心输出量，（2）因行使的收缩期血压降低，（3）抑制异丙肾上腺素引起的心动过速（4）减少反射性心动过速。
氢氯噻（氢氯噻嗪）是噻嗪类利尿剂。噻嗪类药物影响的电解质再吸收的的肾小管机制，直接增加钠和氯的排泄。间接，氢氯噻嗪利尿作用，降低血浆量，从而增加血浆肾素活性，醛固酮分泌增加，增加尿钾损失，血钾降低。
临床试验：
一项随机，双盲，安慰剂对照，为期8周的，不平衡因子研究（N = 1571）评价不同剂量的琥珀酸美托洛尔缓释的降压作用（25毫克，50毫克，100毫克和200毫克）和氢氯噻嗪（6.25mg， 12.5mg和25毫克），以及他们的组合9。建立审判，琥珀酸美托洛尔缓释和氢氯噻嗪的降压作用，从基线到8周坐位舒张压（P = 0.0015）和收缩压（P = 0.0006），血压的变化做出贡献。血压下降明显2个星期内，并保持整个8周的研究。保留24小时后剂量的降血压的高峰期（6小时后给药）效果约96％。
有没有审判的Dutoprol证明，在高血压患者的心血管疾病的危险减少，但美托洛尔和HCTZ组件已经证明这样的好处。
法律分类：
RX
成人：
个性化。采取每日一次。替代疗法：可取代各个组件。滴定，如果有必要，每2周最大200/25mg。严重肾功能不全：不推荐。中度肝功能损害：考虑启动低氢氯噻嗪组成部分。
儿童：
不成立的。
禁忌症（S）：
心源性休克。明显心脏衰竭。第二或第三度房室传导阻滞。窦性心动过缓。无尿。磺胺类药物过敏。
警告/注意事项：
缺血性心脏病。支气管痉挛疾病。嗜铬细胞瘤。大手术。肾脏或肝脏疾病。糖尿病和低血糖。甲状腺功能亢进（甲亢）。周围血管疾病。瑞士法郎。 SLE。急性近视。中学闭角型青光眼。痛风。后交感神经。避免突然停止。监测电解质。怀孕（Cat.C）。哺乳的母亲。
互动（补）：
添加剂消耗儿茶酚胺药物（如利血平，单胺氧化抑制剂）的影响。 Potentiated由CYP2D6抑制剂（如奎尼丁，氟西汀，帕罗西汀，普罗帕酮）。与洋地黄，可乐定，维拉帕米，地尔硫卓心动过缓的风险。 Potentiated由酒精，巴比妥，麻醉药品，其他抗高血压药物。低血钾与皮质类固醇，促肾上腺皮质激素。可能会增加锂中毒。拮抗非甾体抗炎药（显示器）。调整降糖药物。降低胆胺和考来替泊树脂的吸收。拮抗去甲肾上腺素。可能增加肌肉松弛剂（如筒箭毒碱）。可能会干扰甲状旁腺测试。
不良反应（S）：
鼻咽炎，乏力，头晕，背痛，恶心，支气管痉挛，心动过缓，充血性心力衰竭，心脏传导阻滞。
如何提供：
标签-30
最后更新：
2012年5月21日
Manufacturer:
AstraZeneca Pharmaceuticals
Pharmacological Class:
Cardioselective β1-blocker + diuretic.
Active Ingredient(s):
Metoprolol succinate extended-release, hydrochlorothiazide; 25/12.5mg, 50/12.5mg, 100/12.5mg; tablets.
Indication(s):
Hypertension.
Pharmacology:
Metoprolol is a cardioselective β1-adrenergic receptor-blocking agent. At higher plasma concentrations, metoprolol also inhibits β2-adrenoreceptors in the bronchial and vascular musculature. Metoprolol has no intrinsic sympathomimetic activity, and membrane-stabilizing activity is detectable only at plasma concentrations much greater than required for beta-blockade. Clinical studies have confirmed the beta-blocking activity of metoprolol as shown by (1) reduction in heart rate and cardiac output at rest and upon exercise, (2) reduction of systolic blood pressure upon exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia.
Hydrochlorothiazide (HCTZ) is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of sodium and chloride. Indirectly, the diuretic action of HCTZ reduces plasma volume, with consequent increases in plasma renin activity, increases in aldosterone secretion, increases in urinary potassium loss, and decreases in serum potassium.
Clinical Trials:
A randomized, double-blind, placebo-controlled, 8-week, unbalanced factorial study (N=1571) evaluated the antihypertensive effects of various doses of metoprolol succinate extended release (25mg, 50mg, 100mg and 200mg) and HCTZ (6.25mg, 12.5mg and 25mg), and 9 of their combinations. The trial established that metoprolol succinate extended release and HCTZ both contribute to the antihypertensive effect, change from baseline to week 8 in sitting diastolic (p=0.0015) and systolic (p=0.0006) blood pressure. Blood pressure declines were apparent within 2 weeks and were maintained throughout the 8-week study. The blood pressure lowering 24hrs post dosing retained approximately 96% of the peak (6hrs post dosing) effect.
There are no trials of Dutoprol demonstrating reductions in cardiovascular risk in patients with hypertension, but both the metoprolol and HCTZ components have demonstrated such benefits.
Legal Classification:
Rx
Adults:
Individualize. Take once daily. Replacement therapy: may be substituted for individual components. Titrate, if necessary, every 2 weeks up to max 200/25mg. Severe renal impairment: not recommended. Moderate hepatic impairment: consider initiating with lower HCTZ component.
Children:
Not established.
Contraindication(s):
Cardiogenic shock. Overt heart failure. 2nd- or 3rd-degree AV block. Sinus bradycardia. Anuria. Sulfonamide allergy.
Warnings/Precautions:
Ischemic heart disease. Bronchospastic disease. Pheochromocytoma. Major surgery. Renal or hepatic disease. Diabetes and hypoglycemia. Thyrotoxicosis (hyperthyroidism). Peripheral vascular disease. CHF. SLE. Acute myopia. Secondary angle-closure glaucoma. Gout. Post-sympathectomy. Avoid abrupt cessation. Monitor electrolytes. Pregnancy (Cat.C). Nursing mothers.
Interaction(s):
Additive effects with catecholamine-depleting drugs (eg, reserpine, MAOIs). Potentiated by CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone). Risk of bradycardia with digitalis, clonidine, diltiazem, verapamil. Potentiated by alcohol, barbituates, narcotics, other antihypertensives. Hypokalemia with corticosteroids, ACTH. May increase lithium toxicity. Antagonized by NSAIDs (monitor). Adjust antidiabetic drugs. Decreased absorption with cholestyramine and colestipol resins. Antagonizes norepinephrine. Possible increased response to muscle relaxants (eg, tubocurarine). May interfere with parathyroid tests.
Adverse Reaction(s):
Nasopharyngitis, fatigue, dizziness, back pain, nausea; bronchospasm, bradycardia, CHF, heart block.
How Supplied:
Tabs—30
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