核准日期 : 盐酸二甲双胍肠溶胶囊说明书 请仔细阅读说明书并在医师指导下使用 药品名称 通用名称 : 盐酸二甲双胍肠溶胶囊 商品名称 : 君力达 英文名称 :Metformin Hydrochloride Enteric-Coated Capsules 汉语拼音 ;Yansuan Erjiashuanggua Changrong Jiaonang 成份 本品主要成分为 : 盐酸二甲双胍 化学名称 :1,1- 二甲基双胍盐酸盐 化学结构式 : CH 3 H H 2 N N N CH 3,HCl HN NH 分子式 :C4H11N5 HCl 分子量 :165.63 性状 本品为肠溶胶囊, 内容物为白色结晶性粉末 适应症 用于单纯饮食控制不满意的非胰岛素依赖型糖尿病人, 尤其是肥胖者 不但有降血糖作用, 还可能有减轻体重的作用 对某些磺酰脲类无效的病例有效 如与磺酰脲类降血糖药合用有协同作用, 较各自的效果更好 规格 0.25g 用法用量 口服, 餐前半小时服用 成人开始一次 0.25g(1 粒 ), 一日 2~3 次, 以后根据血糖和尿糖情况调整用量, 每日最大剂量不超过 2.0g(8 粒 ), 或遵医嘱 不良反应 1 部分病人口服片剂后有胃肠道反应, 表现为食欲不振 恶心 呕吐 腹泻 胃痛 口中金属味 肠溶胶囊可在不同程度上减轻以上的不良反应 2 有时有乏力 疲倦 体重减轻 头晕 皮疹 禁忌 下列情况禁用 : 1 非胰岛素依赖型糖尿病伴有酮症 酸中毒 肝肾功能不全 心力衰竭 急性心肌梗塞 严重感染和外伤 重大手术以及临床有低血压和缺氧情况禁用 2 过度饮酒者 脱水 痢疾 营养不良者对本品和双胍类药物过敏者禁用 注意事项 1 1 型糖尿病不应单独使用
2 定期检查血糖 尿糖 尿酮体. 3 既往有乳酸性酸中毒史者慎用 3 进行肾脏造影者应于前 3 天停用本品 孕妇及哺乳期妇女用药 孕妇及哺乳期妇女禁用 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 2.0g 不推荐 10 岁以下儿童使用本品 老年用药 70 岁以上患者可能出现乳酸性酸中毒, 宜慎用 药物相互作用 1 本药与胰岛素合用会加强降血糖作用, 应减少胰岛素剂量 2 可加强抗凝药( 如华法林等 ) 的抗凝血作用, 导致出血倾向 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性酸中毒 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 因此疑二甲双胍过量的患者, 血透可以清除蓄积的药物 临床试验 对盐酸二甲双胍肠溶胶囊 ( 试验组 ) 和盐酸二甲双胍片剂 ( 对照组 ) 治疗 2 型糖尿病的临床疗效 毒副作用及安全性进行比较 患有 2 型糖尿病的入选受试者随机分入试验组和对照组, 分别口服给予相应的试验药和对照药 0.5g, 每日 3 次 观察, 治疗 20 天后和治疗前空腹及餐后 2 小时血糖水平 ; 治疗 8 周后和治疗前糖化血红蛋白水平, 血 尿常规, 肝 肾功能 ; 不良反应与耐受性等 试验结果表明受试组及对照组用药 20 天后空腹血糖 餐后 2 小时血糖以及用药 8 周后糖化血红蛋白水平均有明显下降, 经统计学处理有显著性差异, 但 2 组间比较无显著性差异, 提示盐酸二甲双胍肠溶胶囊用于 2 型糖尿病治疗的疗效较好, 且与盐酸二甲双胍片剂的疗效无差别 试验过程中与试验药物有关的不良反应, 对照组主要表现为腹泻 恶心 ; 受试组主要表现为腹泻, 在试验期间未出现恶心等症状 表明盐酸二甲双胍肠溶胶囊上消化道反应较轻, 明显优于对照组 药理毒理 本品属双胍类降糖药, 不促进胰岛素的分泌, 其降血糖作用是促进组织无氧糖酵解, 使肌肉等组织利用葡萄糖的作用加强, 同时抑制肝糖原的异生, 减少肝糖的产生, 使血糖降低 药代动力学 本品口服后由小肠吸收, 与口服普通片剂相比达峰时间慢 1~2 小时, 峰浓度与片剂相近, 服用 1g 后, 峰浓度为 1.44±0.39 μg/ml, 主要以原形经肾排泄 贮藏 密封保存 包装 铝塑包装, 每板 12 粒 (1) 每盒 2 板 ;(2) 每盒 3 板 有效期 24 个月 执行标准 WS1-(X-022)-2004Z 批准文号 国药准字 H10980064 生产企业 企业名称 : 北京圣永制药有限公司生产地址 : 北京市通州区梨园
邮政编码 :101121 电话和传真号码 :010-60524472,67648098 网址 :www.junlida.com.cn
Approval date: 9 th Feb,1998 Revise on 10 th July,2002 16 th Aug,2005 Metformin Hydrochloride Enteric Capsules (read carefully the following and use under the physician s guidance) Drug Name Generic Name: Metformin hydrochloride enteric capsules Brand Name: JUNLIDA ( 君力达 ) Active Ingredients Chemical Name : Hydrochroride of 1,1- Metformin Chemical Structure: CH 3 H H 2 N N N CH3,HCl HN NH Molecular formula: C 4 H 11 N 5.HCl Molecular weight: 165.63 Description White crystalline powder contained in enteric capsules. Indications used for non-insulin dependent diabetes mellitus where diet control alone has been unsatisfactory, especially for the over-weighted patients. Metformin hydrochloride is effective not only in decreasing blood sugar, but reducing body weight as well. It is also effective in patients where sulphonylureas treatment was uneffective. Metformin hydrochloride may be used either alone or in combination with insulin or sulphonylureas. If it is used together with sulphonylureas, the effects may be better due to their synergistic effect.. Strength 0.25g/ capsule Dosage and Administration given orally before meal. Treatment for adult patients is recommended to start with 0.25g (p.o), 2-3 times daily; then gradually adjust the dosage according to the blood sugar and diabetic sugar levels. Maximum dosage should not exceed 2.0g, or as directed by the physician. Adverse Reactions 1. Some patients may show gastro-instestinal adverse reactions including anorexia, nausea, diarrhoea, stomach-ache and metal taste. Contained in enteric capsules,the adverse effects of the drug can be reduced to a certain extent. 2. Some patients may feel weakness, weariness, dizziness and loss of body weight. Some may have skin rashes.
Contra-inducations Metformin is forbidden to be given to the following patients: 1. Non-insulin-dependent diabetes mellitus patrients with ketosis, acidosis, hepatic or renal dysfunctions, acute myocardial infarction, serious infection and injury, major surgery operation, hypotension and anoxia. 2. excess alcohol-drinker, patients suffered from dehydration or dysentery, as well as those patients who are allergic to Metformin or other biguanide drugs. Precautions 1. Metformin shoud not be used alone in insulin-dependent (type I) diabetes. 2. Examine blood sugar, diabetic sugar and urine ketone regularly. 3. Metformin shoud be used cautiously in patients with history of lactic acidosis. 4. Metformin shoud not be used within 3 days before renography. Pregnancy and lactation Metformin shoud not be given to pregnant women, nor during their lactation period. Children For children aged between 10 16 years, the daily dosage should not exceed 2.0 g.. For those younger than 10 years, it is not recommended to use Metformin. Elderly Patients In Elderly patients (over 70 years old), Metformin should be given with great care. For these aged patients, there is a greater potential for the ocurrence of lactic acidosis. Therfore, regular examination of renal function is necessary. Drug Interaction 1.When Metformin is used together with insulin, it may strengthen the effect of decreasing blood sugar. In this case, It is necessary to reduce the insulin dosage. 2. Metformin can strengthen the anticoagulative effect of such anticoagulant durgs as Warfarin etc., leading to the tendency of hemorrhage. Overdosage Even though an overdose of 85g Metformin will not induce hypoglycemia, it will cause lactic acidosis. Clinical tests have shown that, under good hemodynamic conditions, Metformin can be cleared away from the body through dialysis at a speed of 170ml/min. Hence, to a patient suspected to be overdosed with Metformin, hemodialysis may be useful to eliminate the accumulated drug. Clinical trial The therapeutic efficacy; adverse events and safety of Metformin hydrochloride enteric capsule (test group) was compared with that of the normal Metformin hydrochloride tablet (control group) in the treatment of non-insulin dependent diabetes mellitus. Patients were randomly assigned to receive 1 of 2 treatments: 0.5g Metformin hydrochloride enteric capsule (p.o.),t.i.d. or 0.5g Metformin hydrochloride tablet (p.o.),t.i.d. for 8 weeks. After 20 days of treatment, the levels of blood-glucose (both fasting and at 2 hours after breakfast) were compared with those before the treatment. After 8 weeks of treatment, the levels of glycosylated hemoglobin, hepatic and renal function, blood and urine routine examination, adverse reaction and tolerability etc were also compared with those before the treatment. The results of the study shows that: of all the patients in both the test and control groups, their blood-glucose (both fasting and at 2 hours after breakfast) measured after 20 days of treatment, and the levels of glycosylated
hemoglobin measured after 8 weeks of treatment had decreased with remarkable statistical significance, but there is no significant difference when compared between these two groups. This result suggests that the therapeutic efficacy of Metformin hydrochloride enteric capsule is as good as the Metformin hydrochloride tablet. So far as adverse reaction is concerned, the main manifestions in patients of the control group was diarrhoea and nausea, while those of the test group was diarrhoea only, suggesting that the test drug causes less gastro-instestinal adverse reaction than the contol. Clinical Pharmacology Metformin hydrochloride is a biguanide hypoglycemic agent which does not stimulate insulin secretion. Its hypoglycemic activity lies in the fact that it promotes the anaerobic glycolysis in tissues, thus enhancing the tissue s ability to utilize the glucose; and in the meantime, it can also inhibit the heteroplasia of hepatic glycogen, thus reducing the generation of liver sugar and blood sugar. Pharmacodynamics Metformin hydrochloride is given orally and absorbed via the gastro-instestinal tract. After given the enteric capsules, the plasma t 1/2 of Metformin hydrochloride is 1-2 hours longer than that of normal Metformin tablets. The peak plasma concentration of Metformin hydrochloride of both these two drugs are similar: the peak plasma concentration is 1.44 ±0.39 u g/ml. Metformin hydrochloride metabolizes manly in the liver, and is excreted via the kidneys. Storage seal airtight to preserve Package enclosed in an aluminum-plastic plate (12 capsules/plate). 1 2plates/pack, 2 3plates/pack. Validity 24 months Ratification Number 国药准字 H10980064 Manufacturing Firm Name of the firm: Shengyong Pharmaceutical Co.Ltd Address: Liyuan,Tongzhou,Beijing Postcode: 101121 Telephone and FAX: 010-60524472, 010-67648098 Netsite: www.junlida.com.cn