部份中文盐酸二甲双胍处方资料（仅供参考）
英文名：Metformin Hydrochloride
商品名：GLUCOPHAGE XR
中文名：盐酸二甲双胍缓释片
生产商：MERCK
药品简介
药理作用：
1.格华止为双胍类降糖药。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.格华止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.格华止无促使脂肪合成的作用，对正常人无明显降血糖作用。
4.格华止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。
适应症
1) 格华止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，格华止与胰岛素合用，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) 格华止也可与磺脲类口服降血糖药合用，具协同作用。
用法用量
应遵医嘱服药。格华止应从小剂量开始使用，根据病人状况，逐渐增加剂量。通常格华止(盐酸二甲双胍片)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
格华止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吸收，但极少引起贫血。格华止在治疗剂量范围内，引起乳酸性酸中毒罕见。
禁忌
1.肾脏疾病或下列情况禁用格华止：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，可以暂时停用格华止。
8. 维生素B12、叶酸缺乏未纠正者。
注意事项
1.口服格华止期间，定期检查肾功能，可以减少乳酸酸中毒的发生，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线摄影检查前患者暂时停止口服格华止。
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格华止。
3.应激状态：在发热、昏迷、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，此时必须暂时停用格华止，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，不宜单独使用格华止，而应与胰岛素合用。
5.应定期进行血液学检查。格华止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、丙酮酸盐和二甲双胍水平，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(例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§-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，及时看医生。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
不推荐孕妇使用格华止。哺乳期妇女应慎用格华止，必须使用格华止时，应停止哺乳。
儿童用药
10-16岁2型糖尿病患者使用格华止的每日最高剂量为2000mg。不推荐10岁以下儿童使用格华止。
老年用药
65岁以上老年患者使用二甲双胍时，应谨慎，并定期检查肾功能。通常不用最大剂量。不推荐80岁以上的患者使用格华止，除非其肌酐清除率检查表明其肾功能未降低。 。



Glucophage XR (Metformin Hydrochloride)
INDICATIONS AND USAGE
GLUCOPHAGE (metformin hydrochloride) Tablets is indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 2 diabetes mellitus.
GLUCOPHAGE XR (metformin hydrochloride) Extended-Release Tablets is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
DOSAGE AND ADMINISTRATION
There is no fixed dosage regimen for the management of hyperglycemia in patients with type 2 diabetes with GLUCOPHAGE or GLUCOPHAGE XR or any other pharmacologic agent. Dosage of GLUCOPHAGE or GLUCOPHAGE XR must be individualized on the basis of both effectiveness and tolerance, while not exceeding the maximum recommended daily doses. The maximum recommended daily dose of GLUCOPHAGE is 2550 mg in adults and 2000 mg in pediatric patients (10-16 years of age); the maximum recommended daily dose of GLUCOPHAGE XR in adults is 2000 mg.
GLUCOPHAGE should be given in divided doses with meals while GLUCOPHAGE XR should generally be given once daily with the evening meal. GLUCOPHAGE or GLUCOPHAGE XR should be started at a low dose, with gradual dose escalation, both to reduce gastrointestinal side effects and to permit identification of the minimum dose required for adequate glycemic control of the patient.
During treatment initiation and dose titration (see Recommended Dosing Schedule), fasting plasma glucose should be used to determine the therapeutic response to GLUCOPHAGE or GLUCOPHAGE XR and identify the minimum effective dose for the patient. Thereafter, glycosylated hemoglobin should be measured at intervals of approximately 3 months. The therapeutic goal should be to decrease both fasting plasma glucose and glycosylated hemoglobin levels to normal or near normal by using the lowest effective dose of GLUCOPHAGE or GLUCOPHAGE XR, either when used as monotherapy or in combination with sulfonylurea or insulin.
Monitoring of blood glucose and glycosylated hemoglobin will also permit detection of primary failure, i.e., inadequate lowering of blood glucose at the maximum recommended dose of medication, and secondary failure, i.e., loss of an adequate blood glucose lowering response after an initial period of effectiveness.
Short-term administration of GLUCOPHAGE or GLUCOPHAGE XR may be sufficient during periods of transient loss of control in patients usually well-controlled on diet alone.
GLUCOPHAGE XR tablets must be swallowed whole and never crushed or chewed. Occasionally, the inactive ingredients of GLUCOPHAGE XR will be eliminated in the feces as a soft, hydrated mass. (See Patient Information printed below.)
Recommended Dosing Schedule
Adults
In general, clinically significant responses are not seen at doses below 1500 mg per day. However, a lower recommended starting dose and gradually increased dosage is advised to minimize gastrointestinal symptoms.
The usual starting dose of GLUCOPHAGE (metformin hydrochloride) Tablets is 500 mg twice a day or 850 mg once a day, given with meals. Dosage increases should be made in increments of 500 mg weekly or 850 mg every 2 weeks, up to a total of 2000 mg per day, given in divided doses. Patients can also be titrated from 500 mg twice a day to 850 mg twice a day after 2 weeks. For those patients requiring additional glycemic control, GLUCOPHAGE may be given to a maximum daily dose of 2550 mg per day. Doses above 2000 mg may be better tolerated given 3 times a day with meals.
The usual starting dose of GLUCOPHAGE XR (metformin hydrochloride) Extended-Release Tablets is 500 mg once daily with the evening meal. Dosage increases should be made in increments of 500 mg weekly, up to a maximum of 2000 mg once daily with the evening meal. If glycemic control is not achieved on GLUCOPHAGE XR 2000 mg once daily, a trial of GLUCOPHAGE XR 1000 mg twice daily should be considered. If higher doses of metformin are required, GLUCOPHAGE should be used at total daily doses up to 2550 mg administered in divided daily doses, as described above. (See CLINICAL PHARMACOLOGY: Clinical Studies.)
In a randomized trial, patients currently treated with GLUCOPHAGE were switched to GLUCOPHAGE XR. Results of this trial suggest that patients receiving GLUCOPHAGE treatment may be safely switched to GLUCOPHAGE XR once daily at the same total daily dose, up to 2000 mg once daily. Following a switch from GLUCOPHAGE to GLUCOPHAGE XR, glycemic control should be closely monitored and dosage adjustments made accordingly (see CLINICAL PHARMACOLOGY: Clinical Studies).
Pediatrics
The usual starting dose of GLUCOPHAGE is 500 mg twice a day, given with meals. Dosage increases should be made in increments of 500 mg weekly up to a maximum of 2000 mg per day, given in divided doses. Safety and effectiveness of GLUCOPHAGE XR in pediatric patients have not been established.
Transfer From Other Antidiabetic Therapy
When transferring patients from standard oral hypoglycemic agents other than chlorpropamide to GLUCOPHAGE or GLUCOPHAGE XR, no transition period generally is necessary. When transferring patients from chlorpropamide, care should be exercised during the first 2 weeks because of the prolonged retention of chlorpropamide in the body, leading to overlapping drug effects and possible hypoglycemia.
Concomitant GLUCOPHAGE or GLUCOPHAGE XR and Oral Sulfonylurea Therapy in Adult Patients
If patients have not responded to 4 weeks of the maximum dose of GLUCOPHAGE or GLUCOPHAGE XR monotherapy, consideration should be given to gradual addition of an oral sulfonylurea while continuing GLUCOPHAGE or GLUCOPHAGE XR at the maximum dose, even if prior primary or secondary failure to a sulfonylurea has occurred. Clinical and pharmacokinetic drug-drug interaction data are currently available only for metformin plus glyburide (glibenclamide).
With concomitant GLUCOPHAGE or GLUCOPHAGE XR and sulfonylurea therapy, the desired control of blood glucose may be obtained by adjusting the dose of each drug. In a clinical trial of patients with type 2 diabetes and prior failure on glyburide, patients started on GLUCOPHAGE 500 mg and glyburide 20 mg were titrated to 1000/20 mg, 1500/20 mg, 2000/20 mg, or 2500/20 mg of GLUCOPHAGE and glyburide, respectively, to reach the goal of glycemic control as measured by FPG, HbA1c, and plasma glucose response (see CLINICAL PHARMACOLOGY: Clinical Studies). However, attempts should be made to identify the minimum effective dose of each drug to achieve this goal. With concomitant GLUCOPHAGE or GLUCOPHAGE XR and sulfonylurea therapy, the risk of hypoglycemia associated with sulfonylurea therapy continues and may be increased. Appropriate precautions should be taken. (See Package Insert of the respective sulfonylurea.)
If patients have not satisfactorily responded to 1 to 3 months of concomitant therapy with the maximum dose of GLUCOPHAGE or GLUCOPHAGE XR and the maximum dose of an oral sulfonylurea, consider therapeutic alternatives including switching to insulin with or without GLUCOPHAGE or GLUCOPHAGE XR.
Concomitant GLUCOPHAGE or GLUCOPHAGE XR and Insulin Therapy in Adult Patients
The current insulin dose should be continued upon initiation of GLUCOPHAGE or GLUCOPHAGE XR therapy. GLUCOPHAGE or GLUCOPHAGE XR therapy should be initiated at 500 mg once daily in patients on insulin therapy. For patients not responding adequately, the dose of GLUCOPHAGE or GLUCOPHAGE XR should be increased by 500 mg after approximately 1 week and by 500 mg every week thereafter until adequate glycemic control is achieved. The maximum recommended daily dose is 2500 mg for GLUCOPHAGE and 2000 mg for GLUCOPHAGE XR. It is recommended that the insulin dose be decreased by 10% to 25% when fasting plasma glucose concentrations decrease to less than 120 mg/dL in patients receiving concomitant insulin and GLUCOPHAGE or GLUCOPHAGE XR. Further adjustment should be individualized based on glucose-lowering response.
Specific Patient Populations
GLUCOPHAGE or GLUCOPHAGE XR are not recommended for use in pregnancy. GLUCOPHAGE is not recommended in patients below the age of 10 years. GLUCOPHAGE XR is not recommended in pediatric patients (below the age of 17 years).
The initial and maintenance dosing of GLUCOPHAGE or GLUCOPHAGE XR should be conservative in patients with advanced age, due to the potential for decreased renal function in this population. Any dosage adjustment should be based on a careful assessment of renal function. Generally, elderly, debilitated, and malnourished patients should not be titrated to the maximum dose of GLUCOPHAGE or GLUCOPHAGE XR.
Monitoring of renal function is necessary to aid in prevention of lactic acidosis, particularly in the elderly. (See WARNINGS.)
HOW SUPPLIED
GLUCOPHAGE® (metformin hydrochloride) Tablets
GLUCOPHAGE 500 mg tablets are round, white to off-white, film-coated tablets debossed with "BMS 6060" around the periphery of the tablet on one side and "500" debossed across the face of the other side.
GLUCOPHAGE 850 mg tablets are round, white to off-white, film-coated tablets debossed with "BMS 6070" around the periphery of the tablet on one side and "850" debossed across the face of the other side.
GLUCOPHAGE 1000 mg tablets are white, oval, biconvex, film-coated tablets with "BMS 6071" debossed on one side and "1000" debossed on the opposite side and with a bisect line on both sides.
GLUCOPHAGE® XR (metformin hydrochloride) Extended-Release Tablets
GLUCOPHAGE XR 500 mg tablets are white to off-white, capsule shaped, biconvex tablets, with "BMS 6063" debossed on one side and "500" debossed across the face of the other side.
GLUCOPHAGE XR 750 mg tablets are capsule shaped, biconvex tablets, with "BMS 6064" debossed on one side and "750" debossed on the other side. The tablets are pale red and may have a mottled appearance.
Storage
Store at 20°—25° C (68°—77° F); excursions permitted to 15°—30° C (59°—86° F). [See USP Controlled Room Temperature.]