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）

生产厂家: Not available
药品介绍
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。
包装规格
Product                                                 Manufacturer
Glucophage XR Tabs (Metformin) 500 mg 100's B M S 
Glucophage XR Tabs (Metformin) 750 mg 100's B M S

Glucophage Xr
Drug Name
Glucophage Xr is used to treat type 2 diabetes. It helps to control blood sugar. Treatment is combined with diet and exercise. This medicine can be used alone or with other medicines for diabetes.
How To Use
Take this medicine by mouth with a glass of water. Take it with meals. Swallow whole, do not crush or chew. Take your medicine at regular intervals. Do not take your medicine more often than directed. To be sure this medication is helping your condition, your blood will need to be tested on a regular basis. Your kidney function may also need to be tested. It is important that you not miss any scheduled visits to your doctor.
Possible Side Effects
Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue.
• breathing problems.
• feeling faint or lightheaded, falls.
• low blood sugar (ask your doctor or health care professional for a list of these symptoms).
• muscle aches or pains.
• slow or irregular heartbeat.
• unusual stomach pain or discomfort.
• unusually tired or weakness.
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• diarrhea.
• headache.
• heartburn.
• metallic taste in mouth.
• nausea.
• stomach gas, upset.
This list may not describe all possible side effects.
Precautions
Do not take this medicine if you have had an allergic reaction to it or are allergic to any ingredient in this product. Laboratory and/or medical tests such as liver and kidney function tests, fasting blood glucose, glycosylated hemoglobin, or complete blood counts, should be done to monitor your progress or to check for side effects. Regularly check your blood or urine sugar as directed by your doctor. If your blood sugars have been under control and suddenly are difficult to manage, contact your doctor as soon as possible. Before you have any medical or dental treatments, emergency care, laboratory tests, or surgery, tell the doctor or dentist that you are using this medicine. During times of stress such as fever, infection, injury, or surgery it may be more difficult to control your blood sugar. Consult your doctor, as a change in your medicine may be required. This medicine usually does not cause low blood sugar, or hypoglycemia, but this effect may occur if you do not consume enough calories from food, juices, fruit, or other sources. The symptoms of hypoglycemia include chills, cold sweat, dizziness, drowsiness, shaking, rapid heartbeat, weakness, headache, fainting, tingling of the hands or feet, or hunger. It is a good habit to carry glucose tablets or gel to treat low blood sugar. If you are in a situation where you don't have these reliable forms of glucose, eat a quick source of sugar such as table sugar, honey, candy, or drink a glass of orange juice or non-diet soda to quickly raise your blood sugar level. Tell your doctor immediately about the reaction. To help prevent hypoglycemia, eat meals on a regular schedule and do not skip meals. Symptoms of high blood sugar, or hyperglycemia, include thirst, increased urination, confusion, drowsiness, flushing, rapid breathing, or fruity breath odor. If these symptoms occur, tell your doctor immediately. Your medicine dosage may need to be increased. Limit alcohol intake while using this medicine. Before you begin taking any new medicine, either prescription or over-the-counter, check with your doctor or pharmacist. Caution is advised when using this medicine in the elderly since they may be more sensitive to the effects of this medicine. For women: this medicine can cause changes in the menstrual cycle of women with certain fertility problems, therefore increasing the risk of becoming pregnant. Consult your doctor or pharmacist about the use of reliable birth control while using this medicine. If you plan on becoming pregnant, discuss with your doctor the benefits and risks of using this medicine during pregnancy. It is unknown if this medicine is excreted in breast milk. Do not breast-feed while taking this medicine.
Overdos
Seek emergency medical attention if you think you have used too much of this medicine. You may have signs of low blood sugar, such as hunger, headache, confusion, irritability, drowsiness, weakness, dizziness, tremors, sweating, fast heartbeat, seizure (convulsions), fainting, or coma. An overdose of Glucophage Xr may cause a life-threatening condition called lactic acidosis. Get emergency medical help if you have any of these symptoms of lactic acidosis: weakness, increasing sleepiness, slow heart rate, cold feeling, muscle pain, shortness of breath, stomach pain, feeling light-headed, and fainting.
Missed dose
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
Storage
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light. Keep out of the reach of children.