部分中文Metpure-XL处方资料（仅供参考）      【药物介绍】 药名：美托洛尔。美托洛尔属于2A类即无部分激动活性的β1-受体阻断药(心脏选择性β-受体阻断药)。它对β1-受体有选择性阻断作用，无PAA(部分激动活性)，无膜稳定作用。 【通用名称】酒石酸美托洛尔 　　 【英文名称】Metoprolol Tartrate 【化学名称为】(RS)1-异丙氨基-3-［对-(2-甲氧乙基)苯氧基］-2-丙醇L(+)-酒石酸盐。 　　 分子式：(C15H25NO3)2·C4H6O6 　　 分子量：684.82 【贮藏】遮光，密封保存。 【药理毒理】 其阻断β-受体的作用约与普萘洛尔（PP）相等，对β1-受体的选择性稍逊于阿替洛尔。美托洛尔对心脏的作用如减慢心率、抑制心收缩力、降低自律性和延缓房室传导时间等与普萘洛尔、阿替洛尔（AT）相似，其降低运动试验时升高的血压和心率的作用也与PP、AT相似。其对血管和支气管平滑肌的收缩作用较PP为弱，因此对呼吸道的影响也较小，但仍强于AT。美托洛尔也能降低血浆肾素活性。本品无致突变作用；对胎儿无影响；大鼠服用本品2年，800mg/天未发现良性及恶性新生物。 【药代动力学】 美托洛尔的脂溶性介于普萘洛尔（PP）与阿替洛尔（AT）之间。口服吸收迅速完全，吸收率大于90%，但肝脏代谢率达95%，首过效应为25～60%，故生物利用度仅为40～75%，与AT相近。血浆浓度达峰时间一般为1.5小时，最大作用时间为1～2小时。血压的降低与血药浓度不平行，而心率的降低则与血药浓度呈直线关系。体内分布容积为5.6L/kg，血浆蛋白结合率约12%，可透过血脑屏障和胎盘，也可从乳汁分泌。美托洛尔t1/2为3～5小时，肾功能不全时无明显改变。经肾排泄，尿内以代谢物为主，仅3～10%以原形经肾脏排出。不能经透析排出。 【适应症】 用于治疗高血压、心绞痛、心肌梗死、肥厚型心肌病、主动脉夹层、心律失常、甲状腺机能亢进、心脏神经官能症等。近年来尚用于心力衰竭的治疗，此时应在有经验的医师指导下使用。 【用法用量】 高血压：每次100～200mg，一日两次的疗效相当于阿替洛尔100mg/次，一日一次，在血液动力学稳定后立即使用。 稳定性心绞痛：也主张早期使用，用法与用量可参照急性心肌梗死。急性心肌梗死发生心房纤颤时若无禁忌可静脉使用美托洛尔，其方法同上。心肌梗死后若无禁忌应长期使用，因为已经证明这样做可以降低心性死亡率，包括猝死。一般50～100mg/次，一日2次。 在治疗高血压、心绞痛、心律失常、肥厚型心肌病、甲状腺机能亢进等症时一般25～50mg/次，一日2～3次，或100mg/次，一日两次。 心力衰竭：应在使用洋地黄和/或利尿剂等抗心衰的治疗基础上使用本药。起初6.25mg/次，一日2～3次，以后视临床情况每数日至一周增加6.25～12.5mg/次，一日2～3次，最大剂量可用至50～100mg/次，一日两次。最大剂量不应超过300～400mg/天。 【不良反应】 1.心血管系统：心率减慢、传导阻滞、血压降低、心衰加重、外周血管痉挛导致的四肢冰冷或脉搏不能触及、雷诺氏现象。 2.因脂溶性及较易透入中枢神经系统，故该系统的不良反应较多。疲乏和眩晕占10\%，抑郁占5\%，其他有头痛、多梦、失眠等。偶见幻觉。 3.消化系统：恶心、胃痛、便秘<,1\%、腹泻占5\%，但不严重，很少影响用药。 4.其他：气急、关节痛、瘙痒、腹膜后腔纤维变性、耳聋、眼痛等。 【禁忌】 低血压、显著心动过缓(心率<,45/分钟)、心源性休克、重度或急性心力衰竭、末梢循环灌注不良、Ⅱ度或Ⅲ度房室传导阻滞、病态窦房结综合征、严重的周围血管疾病。美托洛尔不可用于那些患有怀疑的急性心肌梗死，表现为心率＜45次/分钟，P-Q间期＞0.24秒或收缩压＜100mmHg的患者。对本品中任一成份过敏者禁用。 【注意事项】 1.普萘洛尔能延缓使用胰岛素后血糖水平的恢复，但选择性β1-受体阻断药的这一不良反应较小。须注意用胰岛素的糖尿病病人在加用β-受体阻滞剂时，其β-受体阻滞作用往往会掩盖低血糖的症状如心悸等，从而延误低血糖的及时发现。但在治疗过程中选择性β1-受体阻断药干扰糖代谢或掩盖低血糖的危险性要小于非选择性β-受体阻断药。 2.长期使用本品时如欲中断治疗，须逐渐减少剂量，一般于7～10天内撤除，至少也要经过3天。尤其是冠心病病人骤然停药可致病情恶化，出现心绞痛、心肌梗死或室性心动过速。 3.大手术之前是否停用β-阻滞剂意见尚不一致，β-受体阻滞后心脏对反射性交感兴奋的反应降低使全麻和手术的危险性增加，但可用多巴酚丁胺或异丙基肾上腺素逆转。尽管如此，对于要进行全身麻醉的病人最好停止使用本药，如有可能应在麻醉前48小时停用。 4.用于嗜铬细胞瘤时应先行使用α-受体阻断药。 　　 5.低血压、心脏或肝脏功能不全时慎用。 　　 6.慢性阻塞性肺部疾病与支气管哮喘病人如需使用美托洛尔亦应谨慎从事，以小剂量为宜，且剂量一般应小于同等效力的阿替洛尔。对支气管哮喘的病人应同时加用β2受体激动剂，剂量可按美托洛尔的使用剂量调整。 7.对心脏功能失代偿的病人应在使用洋地黄和/或利尿剂治疗的基础上使用美托洛尔，具体用法参见 [用法用量]。 8.不宜与异搏定同时使用，以免引起心动过缓、低血压和心脏停搏。 　　 9.在治疗胰岛素依赖型糖尿病(IDDM)患者时须小心观察。 孕妇及哺乳期妇女用药 妊娠期使用β-受体阻滞剂可引起各种胎儿问题，包括胎儿发育迟缓。β-受体阻滞剂对胎儿和新生儿可产生不利影响，尤其是心动过缓，因此在妊娠或分娩期间不宜使用。 【儿童用药】 儿童使用本品的经验有限。 老年患者用药 老年人的药代动力学与年轻人相比无明显变化，因而老年患者用量无需调整。 【药物相互作用】 若患者同时还使用交感神经节阻断剂、其它β受体阻滞剂（如滴眼剂）、或单胺氧化酶（MAO）抑制剂，则必须严密监视患者情况。 与利血平合用可增强本品作用，需注意低血压与心动过速。若计划终止与可乐定的联合用药，必须注意β受体阻滞剂的撤除应比可乐定的撤除提前几天。美托洛尔与维拉帕米和二氢吡啶类钙拮抗剂合用，可能会增加负性变力和变时作用。 服用β受体阻滞剂的患者，不可静脉注射维拉帕米类钙拮抗剂。 β受体阻滞剂会增加抗心律失常药（奎尼丁类和胺腆酮）的负性变力和负性变传导作用。接受β受体阻滞剂的患者，吸入麻醉增加心脏抑制作用。酶诱导和酶抑制物质会影响美托洛尔的血浆水平。 利福平会降低美托洛尔的血药浓度，西咪替丁、乙醇、肼屈嗪和选择性的5-羟色胺重摄取抑制剂（SSRIs），如：帕罗西汀、氟西汀和舍曲林会升高美托洛尔的血药浓度。 预先使用奎尼丁也可增加美托洛尔的血药浓度。与吲哚美辛或其它前列腺素合成酶抑制剂合用会降低β受体阻滞剂的抗高血压作用。在某些情况下，使用β受体阻滞剂的患者使用肾上腺素，心脏选择性β受体阻滞剂对血压控制的影响比非选择性的β受体阻滞剂小很多。接受β受体阻滞剂治疗的患者，其口服降糖药的剂量必须调整。 【药物过量】 症状：美托洛尔过量可导致严重低血压、窦性心动过缓、房室传导阻滞、心衰、心源性休克、心脏停搏、支气管痉挛、意识损害/昏迷、恶心、呕吐和发绀。同时摄入乙醇、抗高血压药、奎尼丁或巴比妥类药物会加重病情。药物过量最初的临床表现会在药物摄入后20分钟至2小时出现。过量的治疗：给予活性炭，必要时洗胃。若发生严重的低血压、心动过缓、或即将发生心衰，隔2～5分钟静脉注射β1受体激动剂（如普瑞特罗）或静脉滴注，直至获得希望的效果。若无选择性的β1受体激动剂，也可用多巴胺，或用硫酸阿托品（iv）以阻滞迷走神经。若未获得满意的疗效，可用其它拟交感胺类药如多巴酚丁胺或去甲肾上腺素。也可给予1～10mg的胰高血糖素。可能需要起搏器。静脉注射β2受体激动剂可缓解支气管痉挛。治疗β受体阻滞剂过量所用的解毒剂的剂量比常规治疗中推荐剂量高很多，这是因为β受体被β受体阻滞剂占领着。另有一例急性中毒一次服用50mg/片200片后心音微弱、血压测不出，用间羟胺等抢救成功。 Ingredient Name: METOPROLOL (me-TOE-proe-lole) Common Uses: This medicine is a beta-adrenergic blocking agent (beta-blocker) used to treat high blood pressure, alone or with other medicines. It is also used for the long-term treatment of chest pain and to treat certain types of heart failure. It may also be used for other conditions as determined by your doctor. Before Using This Medicine: WARNING: Do not suddenly stop taking this medicine; sharp chest pain, irregular heartbeat, and sometimes heart attack may occur. The risk may be greater if you have certain types of heart disease. Your doctor should slowly lower your dose over several weeks if you need to stop taking it, even if you only take it for high blood pressure. Heart disease is common and you may not know you have it. Limit physical activity while you are lowering your dose. If new or worsened chest pain or other heart problems occur, contact your doctor right away. You may need to start taking this medicine again. TELL YOUR DOCTOR OR DENTIST that you take this medicine before you receive any medical or dental care, emergency care, or surgery. TELL YOUR DOCTOR if you have a history of diabetes or take medicine to lower your blood sugar (eg, glyburide, insulin). This medicine may hide signs of low blood sugar such as fast heartbeat. Tell your doctor right away if you notice other signs of low blood sugar such as anxiety, chills, dizziness, drowsiness, fainting, headache, tremor, unusual sweating, vision changes, or weakness. THIS MEDICINE SHOULD NOT USUALLY BE USED by patients who have a history of certain lung or breathing problems (eg, asthma) or a certain type of adrenal gland tumor (pheochromocytoma). It may worsen these conditions. Tell your doctor if you have a history of these conditions; your doctor may need to adjust your dose or prescribe additional medicine to reduce the risk of side effects. TELL YOUR DOCTOR if you have a history of overactive thyroid. This medicine may hide symptoms of overactive thyroid (eg, fast heartbeat). Do not suddenly stop taking this medicine; suddenly stopping this medicine could worsen your condition. Your doctor should slowly lower your dose over several weeks if you need to stop taking it. Check with your doctor for more information. Some medicines or medical conditions may interact with this medicine. INFORM YOUR DOCTOR OR PHARMACIST of all prescription and over-the-counter medicine that you are taking. DO NOT TAKE THIS MEDICINE IF you are taking mibefradil. ADDITIONAL MONITORING OF YOUR DOSE OR CONDITION may be needed if you are taking amiodarone, bupropion, certain HIV protease inhibitors (eg, ritonavir), certain selective serotonin reuptake inhibitors (SSRIs) (eg, fluoxetine, paroxetine), cimetidine, digoxin, diphenhydramine, disopyramide, flecainide, hormonal contraceptives (eg, birth control pills), hydralazine, hydroxychloroquine, ketanserin, mefloquine, phenothiazines (eg, thioridazine), propafenone, quinazolines (eg, imatinib), quinidine, terbinafine, propylthiouracil, verapamil, barbiturates (eg, phenobarbital), indomethacin, phenylpropanolamine, bupivacaine, disopyramide, flecainide, hydralazine, ketanserin, lidocaine, or clonidine. DO NOT START OR STOP any medicine without doctor or pharmacist approval. Inform your doctor of any other medical conditions including lung or breathing problems (eg, asthma, bronchitis, chronic obstructive pulmonary disease / COPD), diabetes, low blood pressure, thyroid problems, or adrenal gland tumor (pheochromocytoma). Tell your doctor if you have a history of heart attack, slow or irregular heartbeat, heart failure, or other heart problems; chest pain or angina; blood vessel or circulation problems; liver disease; or if you will be having surgery or receiving anesthesia. USE OF THIS MEDICINE IS NOT RECOMMENDED if you have a very slow heartbeat (eg, bradycardia), certain types of irregular heartbeat (eg, atrioventricular / AV block, sick sinus syndrome), moderate to severe heart failure, very low systolic blood pressure (less than 100 mm Hg), severe blood circulation problems, or if you are unable to urinate. This medicine should not be used in CHILDREN younger than 6 years old; safety and effectiveness in these children have not been confirmed. Contact your doctor or pharmacist if you have any questions or concerns about using this medicine. How to Use This Medicine: Follow the directions for taking this medicine provided by your doctor. TAKE THIS MEDICINE BY MOUTH EITHER ALWAYS WITH FOOD OR IMMEDIATELY FOLLOWING A MEAL, at the same time each day. THIS MEDICINE may be broken in half. Swallow the tablets or half tablets whole. Do not crush or chew before swallowing. STORE THIS MEDICINE at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. IF YOU MISS A DOSE OF THIS MEDICINE, take it if you remember the same day. If you do not remember until the next day, skip the missed dose. Do not take 2 doses at once. If you miss more than one dose, check with your doctor or pharmacist. Cautions: DO NOT USE THIS MEDICINE if you are allergic to any ingredient in this medicine or to another beta-blocker (eg, propranolol). IF YOU HAVE A HISTORY OF ANY SEVERE ALLERGIC REACTION, talk with your doctor. You may be at risk for an even more severe allergic reaction if you come into contact with the substance that caused your allergy. Some medicines used to treat severe allergies may also not work as well while you are using this medicine. LAB TESTS, including liver function tests and blood cholesterol levels, may be performed while you use this medicine. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments. THIS MEDICINE MAY CAUSE DROWSINESS, DIZZINESS, OR LIGHTHEADEDNESS. These effects may be worse if you take it with alcohol or certain medicines. Use this medicine with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it. This medicine may cause dizziness, lightheadedness, or fainting; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects. PATIENTS WHO TAKE MEDICINE FOR HIGH BLOOD PRESSURE often feel tired or run down for a few weeks after starting treatment. Be sure to take your medicine even if you may not feel "normal." Tell your doctor if you develop any new symptoms. DO NOT SUDDENLY STOP TAKING THIS MEDICINE without first consulting your doctor. If your doctor decides you should no longer use this medicine, you will need to stop this medicine gradually according to your doctor's instructions. IF YOUR DOCTOR HAS INSTRUCTED YOU TO CHECK YOUR BLOOD PRESSURE and heart rate regularly, be sure to do so. TELL YOUR DOCTOR OR DENTIST that you take this medicine before you receive any medical or dental care, emergency care, or surgery. BEFORE YOU BEGIN TAKING ANY NEW MEDICINES, either prescription or over-the-counter, check with your doctor or pharmacist. Do not take any medicines used to treat colds or congestion without first talking with your doctor or pharmacist. Check with your health care provider before you start, stop, or change the dose of any medicine. FOR WOMEN: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using this medicine while you are pregnant. This medicine is found in breast milk. If you are or will be breast-feeding while you use this medicine, check with your doctor. Discuss any possible risks to your baby. DIABETES PATIENTS: this medicine may hide signs of low blood sugar, such as rapid heartbeat. Be sure to watch for other signs or low blood sugar. Low blood sugar may make you anxious, sweaty, weak, dizzy, drowsy, or faint. It may also make your vision change; give you a headache, chills, or tremors; or make you more hungry. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine. Possible Side Effects: SIDE EFFECTS that may occur while taking this medicine include constipation, diarrhea, dizziness, dry mouth or eyes, gas, headache, heartburn, lightheadedness, nausea, stomach pain, stuffy or runny nose, tiredness, trouble sleeping, vomiting, or weakness. If they continue or are bothersome, check with your doctor. CONTACT YOUR DOCTOR IMMEDIATELY if you experience blue or unusually cold hands or feet; blurred vision or other vision changes; chest pain; chills, fever, or sore throat; fainting; hallucinations; mood or mental changes (eg, confusion, depression, short-term memory loss); pounding in the chest; ringing in the ears; severe dizziness or lightheadedness; shortness of breath; slow or irregular heartbeat; swelling of the arms, hands, and feet; unusual bruising or bleeding; unusual tiredness or weakness; wheezing; or yellowing of the skin or eyes. AN ALLERGIC REACTION to this medicine is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; or unusual hoarseness. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your healthcare provider. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. Overdose: If overdose is suspected, contact your local poison control center or emergency room immediately. Symptoms may include blue skin discoloration; difficult or slowed breathing; severe dizziness; very slow heart rate; vomiting; unusual weakness. Additional Information: DO NOT SHARE THIS MEDICINE with others for whom it was not prescribed. DO NOT USE THIS MEDICINE for other health conditions. KEEP THIS MEDICINE out of the reach of children and pets. IF USING THIS MEDICINE FOR AN EXTENDED PERIOD OF TIME, obtain refills before your supply runs out. CHECK WITH YOUR PHARMACIST about how to dispose of unused medicine. --------------------------------------------------------------- 原产地英文商品名: Metpure-XL 12.5mg/tab 100tabs/box 原产地英文药品名: Metoprolol Tartrate 中文参考商品译名: Metpure-XL 12.5毫克/片 100片/盒 中文参考药品译名: 酒石酸美托洛尔 中文参考化合物名称: (RS)1-异丙氨基-3-［对-(2-甲氧乙基)苯氧基］-2-丙醇L(+)-酒石酸盐 生产厂家中文参考译名: EMCURE PHARMACEUTICALS LIMITED 生产厂家英文名: EMCURE PHARMACEUTICALS LIMITED --------------------------------------------------------------- 原产地英文商品名: Metpure-XL 25mg/tab 100tabs/box 原产地英文药品名: Metoprolol Tartrate 中文参考商品译名: Metpure-XL 25毫克/片 100片/盒 中文参考药品译名: 酒石酸美托洛尔 中文参考化合物名称: (RS)1-异丙氨基-3-［对-(2-甲氧乙基)苯氧基］-2-丙醇L(+)-酒石酸盐 生产厂家中文参考译名: EMCURE PHARMACEUTICALS LIMITED 生产厂家英文名: EMCURE PHARMACEUTICALS LIMITED