英文药名：Lusefi  tab(Luseogliflozin Hydrate) 中文药名：鲁格列净片 生产厂家：大正制药 药品介绍 类别名称 -SGLT2抑制剂-2 II型糖尿病治疗药物- 欧文商標名 Lusefi tab. 一般名：ルセオグリフロジン水和物(Luseogliflozin Hydrate)(JAN) luseogliflozin(INN) 化学名：(2S, 3R, 4R, 5S, 6R)-2-{5-[(4-Ethoxyphenyl)methyl]-2-methoxy-4-methylphenyl}-6-(hydroxymethyl)thiane-3, 4, 5-triol hydrate 構造式： 分子式：C23H30O6S・xH2O 分子量：434.55（無水物として） 融点：159.0℃ 性状：它是一种白色粉末。 N，易溶于N-二甲基甲酰胺，乙腈，略微溶于甲醇或乙醇（99.5），并且几乎不溶于水。它由轻逐渐Biki白色。 药效药理 1.作用机序 肾近端小管重吸收葡萄糖的钠 - 葡萄糖共转运体2（钠葡萄糖共转运蛋白2; SGLT2）来抑制的活性，在血中过量葡萄糖的血糖水平通过排泄在尿中下降。 2.SGLT2阻害作用 选择性地抑制经由人SGLT2（SGLT2过度表达细胞）（Ki值：1.1nmol/ L）的葡萄糖摄取活性（体外）。 3.尿糖排泄作用 1）在肥胖的2型糖尿病模型（Zucker肥胖大鼠和db / db小鼠），尿葡萄糖排泄（给药后8或24小时）增加了单次口服。在非肥胖的2型糖尿病模型（GK大鼠），并增加尿葡萄糖排泄（24小时后剂量）通过20周的饮食给药。 2）用于例2型糖尿病，鲁塞小栗Furojin为2.5mg，一旦7天早餐前一天口服给药为5mg或安慰剂。诡计小栗Furojin增加高达24小时的尿葡萄糖排泄后施用相比，安慰剂。 4.降血糖作用 1）肥胖的2型糖尿病模型（Zucker肥胖大鼠），为葡萄糖负荷由单次口服给药后抑制血糖值升高。此外，在肥胖的2型糖尿病模型（的db / db小鼠），以及从基线糖化血红蛋白被一个每日口服给药4周减少变化量。此外，非肥胖的2型糖尿病模型（GK大鼠），并通过20周的饮食给药减少了糖化血红蛋白水平。 2）受到患者的2型糖尿病患者，鲁塞小栗Furojin为2.5mg，口服5毫克或安慰剂一次7天早餐前一天。诡计小栗Furojin早餐与安慰剂相比，得到了改善的血糖AUC的每一个餐四小时后午餐和晚餐的，以及空腹血糖水平。 适应症：2型糖尿病 用法用量 成人口服：1日1次（2.5mg）早餐前或早餐后。注意，当效果不足，可提高到一次5mg. 包装规格 2.5mg/片 PTP：100片，140片，500片，瓶：500片 5mg/片 PTP：100片，140片，瓶：500粒 生产商：大正制药有限责任公司 Brand name: Lusefi tab. 2.5mg 　Active ingredient: Luseogliflozin hydrate 　Dosage form: white tablet, diameter: 7.1 mm, thickness: 3.2 mm 　Print on wrapping: ルセフィ,2.5mg,糖尿病用薬,Lusefi tab.2.5mg ----------------------------- Brand name: Lusefi tab. 5mg 　Active ingredient: Luseogliflozin hydrate 　Dosage form: white tablet, diameter: 8.6 mm, thickness: 5.0 mm 　Print on wrapping: Effects of this medicine This medicine inhibits glucose reabsorption in the renal proximal tubule and excretes excess glucose in urine to reduce blood sugar level. It is usually used to treat type 2 diabetic mellitus. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you have ketosis, diabetic coma/precoma, infections, injury, pituitary gland malfunction, adrenal gland dysfunction, irregular eating habits, insufficient food intake, excessive alcohol intake, urinary tract infection or genital infection. If you are in a pre- of post-operative state, poor nutritional state, starvation state, debilitated state or performing intense muscular exercise. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •In general, for adults, take 2.5 mg of Luseogliflozin at a time once a day before or after breakfast. The dosage may be increased to 5 mg at a time once a day according to your symptoms. This preparation contains 5 mg of Luseogliflozin in 1 tablet. Strictly follow the instructions. •If you miss a dose, take the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. Precautions while taking this medicine •Follow the instructions on diet and exercise. •This medicine may cause hypoglycemia symptom. Pay attention when you work at heights or drive a car. •If hypoglycemia symptom occurs, take sugar (sugar, candy, juice, glucose, etc.) immediately. If you are taking alpha-glucosidase inhibitor (which delays absorption of glucose) with this medicine, be sure to take glucose when hypoglycemia symptom occurs. •Drink an adequate amount of water to avoid dehydration. Possible adverse reactions to this medicine The most commonly reported adverse reactions include frequent urination and hypoglycemia symptom. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •cold sweat, tremor in limbs, hungry feeling [hypoglycemia] •fever, flank/hip pain, nausea/vomiting [pyelonephritis] •thirst, decreased consciousness, hyperpnea [dehydration] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store away from direct sunlight, heat and moisture. •Discard the remainder. Do not store them. Taisho Toyama Pharmaceutical Co., Ltd.Internal Revised: 1/2015 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. www.oneyao.net http://www.kegg.jp/medicus-bin/japic_med?japic_code=00062721 http://medical.taishotoyama.co.jp/data/tenp/htm/lsf/tenpu.htm