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部分盐酸二甲双胍缓释片中文处方资料（仅供参考）
英文药名: Glucophage XR(Metformin Extended Release Tablets)
中文药名: 格华止（盐酸二甲双胍缓释片）
药品名称
通用名：盐酸二甲双胍片
商品名：格华止(Glucophage)
英文名：Metformin Hydrochloride Tablets
性 状: 盐酸二甲双胍片为薄膜衣片，除去包衣后显白色或类白色。
药理毒理
药理作用：
1．盐酸二甲双胍片为双胍类降糖药。不是通过刺激胰岛β细胞增加胰岛素的浓度，而是直接作用于糖的代谢过程，促进糖的无氧酵解，增加肌肉、脂肪等外周组织对葡萄糖的摄取和利用，从而保护已受损的胰岛β细胞功能免受进一步损害，有利于糖尿病的长期控制。
2．盐酸二甲双胍片抑制肠道吸收葡萄糖，并抑制肝糖原异生，减少肝糖输出，可使糖尿病患者血糖及糖化血红蛋白降低。
3．本品无促使脂肪合成的作用，对正常人无明显降血糖作用。
4．盐酸二甲双胍片与磺酰脲类降糖药比较，不刺激胰岛素分泌，甚少引起低血糖症，而两者合用时可起到协同作用，以提高降血糖的疗效。
毒理研究：
动物实验提示，本品无致癌、致突变作用，对生育能力无影响。
药代动力学
口服二甲双胍主要在小肠吸收。空腹状态下口服二甲双胍0.5克的绝对生物利用度为50-60%。同时进食略减少药物的吸收速度和吸收程度。国内口服本品药代动力学试验结果表明，口服后中位达血药浓度时间为2小时，平均血浆药物清除半衰期约为4小时。二甲双胍几乎不与血浆蛋白结合，按照常用临床剂量和给药方案口服本品，可在24-48小时内达到稳态血浆浓度。本品主要经肾脏排泄，口服本品24小时内肾脏排泄90%。
适应症
1．盐酸二甲双胍片首选用于单纯饮食控制及体育锻炼治疗无效的2型糖尿病，特别是肥胖的2型糖尿病。
2．对于1型或2型糖尿病，本品与胰岛素合用，可增加胰岛素的降血糖作用，减少胰岛素用量，防止低血糖发生；
3．本品也可与磺脲类口服降糖药合用，具协同作用。
用法用量
应遵医嘱服药。本品应从小剂量开始使用，根据病人状况，逐渐增加剂量。通常本品的起始剂量为0.5克，每日二次；或0.85克，每日一次；随餐服用。可每周增加0.5克，或每2周增加0.85克，逐渐加至每日2克，分次服用。
成人最大推荐剂量为每日2550毫克。对需进一步控制血糖患者，剂量可以加至每日2550毫克(即每次0.85克，每天三次)。每日剂量超过2克时，为了更好的耐受，药物最好随三餐分次服用。
不良反应
盐酸二甲双胍片常见不良反应包括腹泻、恶心、呕吐、胃胀、乏力、消化不良、腹部不适及头痛。其他少见者为大便异常、低血糖、肌痛、头昏、头晕、指甲异常、皮疹、出汗增加、味觉异常、胸部不适、寒战、流感症状、潮热、心悸、体重减轻等。二甲双胍可减少维生素B12的吸收，但极少引起贫血。本品在治疗剂量范围内，引起乳酸性酸中毒罕见。
禁 忌
1．肾脏疾病或下列情况禁用本品：心力衰竭(休克)、急性心肌梗塞和败血症等引起的肾功能障碍(血清肌酐水平＞1.5毫克/分升(男性)，≥1.4毫克/分升(女性)或肌酐清除异常)。
2．需要药物治疗的充血性心衰，和其他严重心、肺疾患。
3．严重感染和外伤，外科大手术，临床有低血压和缺氧等。
4．已知对盐酸二甲双胍过敏。
5．急性或慢性代谢性酸中毒，包括有或无昏迷的糖尿病酮症酸中毒，和糖尿病酮症酸中毒需要用胰岛素治疗。
6．酗酒者。
7．接受血管内注射碘化造影剂者，可以暂时停用本品。
8．维生素B12、叶酸缺乏未纠正者。
注意事项
1．口服本品期间，定期检查肾功能，可以减少乳酸中毒的发生，尤其是老年患者更应定期检查肾功能。接受外科手术和碘剂X射线摄影检查前患者暂时停止口服本品。
2．肝功能不良：某些乳酸性酸中毒患者合并有肝功能损害，因此有肝脏疾病者应避免使用本品。
3．应激状态：在发热、感染和外科手术时，服用口服降糖药患者易发生血糖暂时控制不良，此时必须暂时停用本品，改用胰岛素。待应激状态缓解后恢复使用。
4．对1型糖尿病患者，不宜单独使用本品，而应与胰岛素合用。
5．应定期进行血液学检查。本品治疗引起巨幼红细胞性贫血罕见。如发生应排除维生素B12缺乏。
6．即往服用盐酸二甲双胍片治疗，血糖控制良好的2型糖尿病患者出现实验室化验异常或临床异常 (特别是乏力或难于言表的不适)，应当迅速寻找酮症酸中毒或乳酸酸中毒的证据，测定包括血清电解质、酮体、血糖、血酸碱度，乳酸盐、丙酮酸二甲双胍水平，存在任何类型的酸中毒都应立即停用，开始其他恰当的治疗方法。
7．单独接受盐酸二甲双胍片治疗的患者正常情况下不会产生低血糖，但当进食过少，或大运动量后没有补充足够的热量，与其他降糖药联合使用(如磺脲类药物和胰岛素)，饮酒等情况下会出现低血糖，须注意。
8．老年、衰弱或营养不良的患者，以及肾上腺和垂体功能低减、酒精中毒的患者更易发生低血糖。老年患者和服用β-肾上腺阻滞剂的患者的低血糖很难辨认，须注意。
9．患者应当了解盐酸二甲双胍片治疗的潜在危险和益处，以及选择治疗的方式。他们也应知道同时控制饮食、规律运动的重要性，以及规律检测血糖、糖化血红蛋白、肾脏功能和血液学参数的重要性。
10．须向患者解释乳酸酸中毒的危险性、症状和容易发生乳酸酸中毒的情况。当出现不能解释的过度呼气、肌痛、乏力、嗜睡或其他非特异性的症状时，应立即停药，及时医生。在二甲双胍治疗的初期常出现胃肠道症状，一旦患者坚持某一剂量治疗后出现胃肠道症状，通常与药物本身无关，随后出现的胃肠道症状可能是由于乳酸酸中毒或其他严重的疾病造成的。
孕妇及哺乳期妇女用药
不推荐孕妇使用本品。哺乳期妇女应慎用本品，必须使用本品时，应停止哺乳。
儿童用药
10-16岁2型糖尿病患者使用本品的每日最高剂量为2000毫克。不推荐10岁以下儿童使用本品。
老年患者用药
65岁以上老年患者使用本品时应谨慎，并定期检查肾功能。通常不用最大剂量。不推荐80岁以上的患者使用本品，除非其肌酐清除率检查表明其肾功能未降低。
药物相互作用
1．单剂联合使用二甲双胍和格列苯脲未发现二甲双胍的药代动力学参数改变。
2．二甲双胍与呋塞米(速尿)合用，二甲双胍的AUC增加，但肾清除无变化；同时呋塞米的Cmax和AUC均下降，终末半衰期缩短, 肾清除无改变。
3．经肾小管排泌的阳离子药物(例如氨氯吡咪、地高辛、吗啡、普鲁卡因胺、奎尼丁、奎宁、雷尼替丁、氨苯喋啶、甲氧苄氨嘧啶和万古霉素)理论上可能与二甲双胍竞争肾小管转运系统，发生相互作用，因此建议密切监测、调整本品及/或相互作用药物的剂量。
4．二甲双胍与西咪替丁合用，二甲双胍的血浆和全血AUC增加，但两药单剂合用，未见二甲双胍清除半衰期改变。西咪替丁的药代动力学未见变化。
5．如同时服用某些可引起血糖升高的药物，如噻嗪类药物或其他利尿剂、糖皮质激素、酚噻嗪、甲状腺制剂、雌激素、口服避孕药、苯妥英、烟碱酸、拟交感神经药、离子通道阻滞剂和异烟肼等时要密切监测血糖，而在这些药物停用后，要密切注意低血糖的发生。
6．二甲双胍不与血浆蛋白结合，因此与蛋白高度结合的药物例如水杨酸盐、氨苯磺胺、氯霉素、丙磺舒等与磺脲类药物相比不易发生相互作用，后者主要与血清蛋白结合。
7．除氯磺丙脲，患者从其他的口服降糖药转为用本品治疗时，通常不需要转换期。服用氯磺丙脲的患者在换用本品的最初2周要密切注意，因为氯磺丙脲在体内有较长滞留，易导致药物作用过量，发生低血糖。
8．二甲双胍有增加华法令的抗凝血倾向。
9．树脂类药物与本品同服，可减少二甲双胍吸收。
药物过量
即使二甲双胍服药量达到85克都没有发生低血糖，但在这种情况下会发生乳酸中毒。在良好的血液动力学的状况下二甲双胍可以以170毫升/分的速度透析清除。因此怀疑二甲双胍过量的患者，血透可以清除蓄积的药物。
格华止XR 24小时缓释片（Glucophage XR）—2型糖尿病经典治疗药物
Glucophage XR extended-release tablets
Generic Name: metformin (met-FOR-min)
Brand Name: Examples include Fortomet and Glucophage XR
Glucophage XR extended-release tablets is used for:
Treating type 2 diabetes. It is used along with diet and exercise. It may be used alone or with other antidiabetic medicines.
Glucophage XR extended-release tablets is a biguanide antidiabetic. It works by decreasing the amount of sugar that the liver produces and the intestines absorb. It also helps to make your body more sensitive to the insulin that you naturally produce.
Do NOT use Glucophage XR extended-release tablets if:
you are allergic to any ingredient in Glucophage XR extended-release tablets
you have a severe infection, low blood oxygen levels, kidney or liver problems, high blood ketone or acid levels (eg, diabetic ketoacidosis), or dehydration
you have had a stroke or a recent heart attack, or you are in shock
you are 80 years or older and have not had a kidney function test
you will be having surgery or certain lab procedures
Contact your doctor or health care provider right away if any of these apply to you.
Before using Glucophage XR extended-release tablets:
Some medical conditions may interact with Glucophage XR extended-release tablets. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
if you are pregnant, planning to become pregnant, or are breast-feeding
if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
if you have allergies to medicines, foods, or other substances
if you have heart failure, especially heart failure that is treated by medicine
if you have a history of heart problems, lung or breathing problems, thyroid problems, stomach or bowel problems (eg, paralysis, blockage),adrenalorpituitary problems, or lactic acidosis
if you have vomiting, diarrhea, poor health or nutrition, low blood calcium or vitamin B12 levels, or anemia, or if you are dehydrated
if you have an infection, fever, recent injury, or moderate to severe burns
if you drink alcohol or have a history of alcohol abuse
if you will be having surgery or certain lab procedures
if you are taking a beta-blocker (eg, propranolol)
Some MEDICINES MAY INTERACT with Glucophage XR extended-release tablets. Tell your health care provider if you are taking any other medicines, especially any of the following:
Calcium channel blockers (eg, nifedipine), corticosteroids (eg, prednisone), diuretics (eg, furosemide, hydrochlorothiazide), estrogen, hormonal contraceptives (eg, birth control pills), insulin, isoniazid, nicotinic acid, phenothiazine (eg, chlorpromazine), phenytoin, sulfonylureas (eg, glipizide), sympathomimetics (eg, albuterol, pseudoephedrine), or thyroid hormones (eg, levothyroxine) because the risk of high or low blood sugar may be increased
Amiloride, cimetidine, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin, or medicines that may harm the kidney (eg, aminoglycoside antibiotics [eg, gentamicin], amphotericin B, tacrolimus) because they may increase the risk of Glucophage XR extended-release tablets's side effects. Ask you doctor if you are unsure if any of your medicines might harm the kidney
This may not be a complete list of all interactions that may occur. Ask your health care provider if Glucophage XR extended-release tablets may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.
How to use Glucophage XR extended-release tablets:
Use Glucophage XR extended-release tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.
An extra patient leaflet is available with Glucophage XR extended-release tablets. Talk to your pharmacist if you have questions about this information.
Take Glucophage XR extended-release tablets by mouth with the evening meal unless your doctor tells you otherwise.
Swallow Glucophage XR extended-release tablets whole. Do not break, crush, or chew before swallowing.
Take Glucophage XR extended-release tablets on a regular schedule to get the most benefit from it. Taking Glucophage XR extended-release tablets at the same time each day will help you remember to take it.
Continue to take Glucophage XR extended-release tablets even if you feel well. Do not miss any doses.
If you miss a dose of Glucophage XR extended-release tablets, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Glucophage XR extended-release tablets.
Important safety information:Glucophage XR extended-release tablets may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Glucophage XR extended-release tablets with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
Follow the diet and exercise program given to you by your health care provider.
Do not drink large amounts of alcohol while you take Glucophage XR extended-release tablets. Talk to your doctor or health care provider before you drink alcohol while you take Glucophage XR extended-release tablets.Tell your doctor or dentist that you take Glucophage XR extended-release tablets before you receive any medical or dental care, emergency care, or surgery.Be careful not to become dehydrated, especially during hot weather or while you are being active. Dehydration may increase the risk of Glucophage XR extended-release tablets's side effects.
If vomiting or diarrhea occurs, you will need to take care not to become dehydrated. Contact your doctor for instructions.
You may notice undissolved parts of Glucophage XR extended-release tablets in your stool. This is normal and not a cause for concern.
Carry an ID card at all times that says you have diabetes. Check your blood sugar levels as directed by your doctor. If they are often higher or lower than they should be and you take Glucophage XR extended-release tablets exactly as prescribed, tell your doctor.
Glucophage XR extended-release tablets does not usually cause low blood sugar. Low blood sugar may be more likely to occur if you skip a meal, exercise heavily, or drink alcohol. It may also be more likely if you take Glucophage XR extended-release tablets along with certain medicines for diabetes (eg, sulfonylureas, insulin). Tell your doctor right away if you experience symptoms of low blood sugar (eg, fast heartbeat, headache, chills, sweating, tremors, increased hunger, vision changes, nervousness, weakness, dizziness, drowsiness, fainting).
It is a good idea to carry a reliable source of glucose (eg, tablets or gel) to treat low blood sugar.
If this is not available, you should eat or drink a quick source of sugar like table sugar, honey, candy, orange juice, or non-diet soda.
This will raise your blood sugar level quickly. Tell your doctor right away if this happens. To prevent low blood sugar, eat meals at the same time each day and do not skip meals.
Fever, infection, injury, or surgery may increase your risk of high or low blood sugar levels.
If any of these occur, check your blood sugar level closely and tell your doctor right away.
Glucophage XR extended-release tablets may commonly cause stomach upset, indigestion, nausea, vomiting, or diarrhea at the beginning of treatment.
If you develop unusual or unexpected stomach problems, or if you develop stomach problems later during treatment, contact your doctor at once. This may be a sign of lactic acidosis.
Lab tests, including kidney function, fasting blood glucose, hemoglobin A1c, and complete blood cell counts, may be performed while you take Glucophage XR extended-release tablets. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.
Use Glucophage XR extended-release tablets with caution in the ELDERLY; they may be more sensitive to its effects. Low blood sugar levels may also be more difficult to recognize in the elderly.
Glucophage XR extended-release tablets should not be used in CHILDREN younger than 17 years; safety and effectiveness in these children have not been confirmed.
PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Glucophage XR extended-release tablets while you are pregnant. It is not known if Glucophage XR extended-release tablets is found in breast milk. Do not breast-feed while taking Glucophage XR extended-release tablets.
When used for long periods of time, Glucophage XR extended-release tablets may not work as well.
If your blood sugar has been under control and then becomes hard to manage, contact your doctor. Do not change the dose of your medicine without checking with your doctor.
Possible side effects of Glucophage XR extended-release tablets:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Diarrhea; gas; headache; indigestion; nausea; stomach pain or upset; temporary metallic taste; vomiting.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); chest pain or discomfort; dizziness or light-headedness; fast or difficult breathing; feeling of being unusually cold; fever, chills, or persistent sore throat; general feeling of being unwell; muscle pain or weakness; slow or irregular heartbeat; unusual drowsiness; unusual or persistent stomach pain or discomfort; unusual tiredness or weakness.
This is not a complete list of all side effects that may occur.
If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.
If OVERDOSE is suspected:
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include dizziness or light-headedness; fast or difficult breathing; feeling of being unusually cold; general feeling of being unwell; muscle pain or tenderness; slow or irregular heartbeat; unusual drowsiness; unusual stomach discomfort; unusual weakness or tiredness.
Proper storage of Glucophage XR extended-release tablets:
Store Glucophage XR extended-release tablets at room temperature, between 68 and 77 degrees F (20 and 25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Glucophage XR extended-release tablets out of the reach of children and away from pets.
Bristol-Myers施贵宝公司周一称，他们治疗2型糖尿病的一种新型二甲双胍(Glucophage XR)获美国食品和药物管理局批准。
这种被命名为Glucophage XR的新药是盐酸二甲双胍缓释胶囊，只需一天一次服用，它被获准做为饮食控制和运动失败后治疗2型糖尿病的首选药物，也可与磺脲类药物和胰岛素合并使用。
Bristol-Myers施贵宝公司周一称，他们治疗2型糖尿病的一种新型二甲双胍(Glucophage XR)获美国食品和药物管理局批准。公司称，1200例病人的临床试验结果显示，在降低病人血糖水平方面，新型二甲双胍与普通二甲双胍效果相当。
Bristol-Myers施贵宝公司周一称，他们治疗2型糖尿病的一种新型二甲双胍(Glucophage XR)获美国食品和药物管理局批准。公司估计60%接受口服降糖治疗的2型糖尿病病人每天要服多种药物，该公司世界医药部负责人Lane说：“这种新型二甲双胍为2型糖尿病病人提供了一种每天一次的简单用药方法。”该公司发言人Shapero告诉路透社医学新闻，他们计划在11月份早些时候推出这种新型二甲双胍。
FDA最近还批准了Bristol-Myers公司的一种复方降糖药Glucovance，它是格列本脲(glyburide)和盐酸二甲双胍的复方制剂，这两种降糖药共同作用以增进2型糖尿病病人血糖的控制。Shapero说，Glucophage
XR与普通二甲双胍有相同的安全性。二甲双胍的副作用有不规则的心慌、严重的胃部不适和低血糖（如与其它降糖药合用）。
Bristol-Myers公司指出，在极少的情况下，Glucophage XR、Glucovance和普通二甲双胍可能会引起乳酸性酸中毒，并有可能会致命，主要发生于肾功能较差的病人。接受心脏药物治疗、肾脏有问题、有肝脏疾病或80岁以上的病人建议不使用这种降糖药。
国外的研究人员近期进行了一项为期24周的双盲研究，评估了新型缓释二甲双胍治疗2型糖尿病的有效性和安全性。
将新诊断的、单纯饮食控制和运动干预及既往只服用口服降糖药的2型糖尿病患者随机分为三种缓释二甲双胍剂量组（1500mg qd组、1500mg bid组、2000mg qd组）及短效二甲双胍组（1500mg bid）。结果显示，治疗12周时，所有治疗组患者的平均HbA1c均有显著下降(P < 0.001)。与治疗基线相比，缓释二甲双胍1500mg qd组、1500mg bid组和短效二甲双胍组患者的A1C分别下降了0.73%、0.74%和0.70%，不具有统计学意义；而缓释二甲双胍2000mg组患者的A1C平均下降了1.06%，与短效二甲双胍组相比具有统计学差异。治疗1~8周时，患者血糖的下降最为明显，并持续至研究结束。
各治疗组的副反应相似，但缓释二甲双胍治疗组中患者因为恶心而自行停药的比例要低于短效二甲双胍组。研究人员指出，每日1次或2次应用缓释二甲双胍与每日2次服用短效二甲双胍一样安全、有效，且能满意控制血糖达24周.
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注：以下产品不同规格和不同价格。购买以咨询为准！
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产地国家: 美国
原产地英文商品名:
GLUCOPHAGE XR TAB SR 24H 500MG/tablet 100Tabs/box
原产地英文药品名:
METFORMIN HYDROCHLORIDE
中文参考商品译名:
格华止XR24小时缓释片 500毫克/片 100片/盒
中文参考药品译名:
盐酸二甲双胍
生产厂家中文参考译名:
百时美施贵宝美国制药
生产厂家英文名:
Bristol-Myers Squibb
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产地国家: 美国
原产地英文商品名:
GLUCOPHAGE XR TAB SR 24H 750MG/tablet 100Tabs/box
原产地英文药品名:
METFORMIN HYDROCHLORIDE
中文参考商品译名:
格华止XR24小时缓释片 750毫克/片 100片/盒
中文参考药品译名:
盐酸二甲双胍
生产厂家中文参考译名:
百时美施贵宝美国制药
生产厂家英文名:
Bristol-Myers Squibb |
