英文药名:ONGLYZA(Saxagliptin Hydrate Tablets)
中文药名:沙格列汀片
生产厂家:协和发酵麒麟有限公司
オングリザ錠2.5mg/オングリザ錠5mg
治疗类别名称 选择性DPP-4抑制剂为2型糖尿病的药物的治疗 欧文商標名 ONGLYZA Tablets 2.5mg ONGLYZA Tablets 5mg 一般名 サキサグリプチン水和物[Saxagliptin Hydrate(JAN)] 化学名 (1S, 3S, 5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile monohydrate 構造式
分子式 C18H25N3O2・H2O 分子量 333.43 性状 是淡黄色或浅棕色粉末白色,还有包含海量的情形。乙醇(95),以容易地微溶,微溶于水。 操作注意事项 由于这种药物是通过观察在高温和高湿度的无包装状态受到影响,应特别注意在包装或小袋的情况进行说明。 适应症: II型糖尿病 用法与用量 成人,每天一次,每次为5mg口服给药。此外,也可以每天使用一次口服2.5mg的根据患者的病情。 药效药理 1.作用机制 胰高血糖素样肽-1(GLP-1)是从由一餐的摄取肠道分泌的一种激素,通过胰岛素分泌增强活性和胰高血糖素分泌抑制作用,起着体内葡萄糖稳态中起重要作用。这种药物通过抑制降解增加活性GLP-1的血中浓度的DPP-4活性的GLP-1,通过胰岛素分泌促进作用发挥降血糖作用。 2.药理作用 (1) DPP-4抑制活性和活性GLP-1浓度的增加作用 1) 人DPP-4(肾)抑制活性(体外),沙格列汀和主要的活性代谢物的Ki值,分别为1.3±0.31nmol/L和2.6±1.0nmol/L。 2) 在使用正常大鼠口服葡萄糖耐受性试验中,活性GLP-1的浓度在血浆中增加了这种药物的单次剂量。 3) 在2型糖尿病患者中,血浆中的DPP-4活性通过施用每日一次的这种药物5毫克抑制,活性GLP-1的浓度在血浆中升高。 (2) 葡萄糖耐受的改善和餐后血糖改善作用 1) 在肥胖和使用Zucker肥胖大鼠呈现糖耐量受损的口服葡萄糖耐量试验,血糖水平升高已经由这种药物的单次剂量的抑制。 2) 饮食方面,患者的2型糖尿病患者的血糖控制不良,每天一次14天的后和晚餐早餐此药为5mg,血糖水平升高早餐前进行运动疗法,由政府一直抑制。 包装规格 片剂为 2.5毫克:[PTP]100片(10片×10),140片(14片×10),500片(10片×50) 5毫克:[PTP]100片(10片×10),500片(10片×50),700片(14片×50)
制造厂商 协和发酵麒麟有限公司 产品特点: 沙格列汀是一种高效二肽基肽酶-4(Dipeptidyl Peptidase 4,DPP-4)抑制剂,通过选择性抑制DPP-4,可以升高内源性胰高血糖素样肽-1(GLP-1)和葡萄糖依赖性促胰岛素释放多肽(GIP)水平,从而调节血糖。 沙格列汀单药治疗2型糖尿病初治患者的一项临床Ⅲ期、多中心、平行、随机、双盲、安慰剂对照的临床研究结果表明,在主要治疗组,沙格列汀治疗可以较基线显著降低校正的平均HbA1c水平,校正的平均FPG水平和餐后葡萄糖曲线下面积也较基线显著降低,患者达标比例显著升高。开放标签组的各项血糖指标也较基线显著降低。各治疗组均与安慰剂组的不良事件发生率相似,未发现有症状的(手指血糖≤50 mg/dl)低血糖事件。沙格列汀治疗也没有使体重增加。因此,对于初治患者,沙格列汀每日1次单药治疗均有显著的血糖控制作用,安全性和耐受性良好。 完整资料附件: 1):http://meds.qlifepro.com/detail/622245601/ 2):http://di-pedia.com:808/DIC_GOOCO%5CAttach%5C3969017F1028_1_03.html Launch of Onglyza® Tablets 2.5mg, 5mg for Type 2 Diabetes Kyowa Hakko Kirin Co., Ltd. (President and CEO: Nobuo Hanai; "Kyowa Hakko Kirin") announced today that it will launch Onglyza® Tablets 2.5mg and 5mg (generic name: saxagliptin hydrate; referred to below as "Onglyza®") to treat type 2 diabetes in Japan July 9, 2013. Onglyza® was originated by Bristol-Myers Squibb. This oral hypoglycemic agent for diabetes acts by selectively inhibiting dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down glucagon-like peptide-1*1 (GLP-1) and gastric inhibitory peptide*2 (GIP). Once-daily dosing with 5mg of Onglyza® produces a blood glucose-dependent reduction in blood sugar levels. The efficacy and safety of Onglyza® were confirmed in clinical studies performed in accordance with the Guideline for Clinical Evaluation of Oral Hypoglycemic Agents (PFSB/ELD Notification No. 0709-1, July 9, 2010). Onglyza® can be administered in combination with existing oral hypoglycemic agents, such as sulfonylurea drugs, thiazolidines, biguanides, short-acting insulin secretagogues, and alpha-glucosidase inhibitors. Combination use of Onglyza® with insulin preparations is also included in the approved indication of type 2 diabetes. Onglyza® provides a new option in the treatment of type 2 diabetes and is therefore expected to help healthcare professionals and patients to manage type 2 diabetes. *1 About glucagon-like peptide-1 (GLP-1) GLP-1 is secreted soon after eating, stimulating the pancreatic beta cells and increasing insulin secretion. When DPP-4 is inhibited, blood levels of GLP-1 are maintained and rising blood sugar levels can be curbed. *2 About Gastric inhibitory peptide (GIP) Gastric inhibitory peptide (GIP) is a GI hormone found in the mucosa of the small intestine. Release of the hormone, mediated by the presence of glucose or fatty acids in the duodenum, results in the release of insulin by the pancreas and inhibition of gastric mobility acid secretion. Onglyza® product overview Product name Onglyza® Tablets 2.5 mg and 5 mg Generic name Saxagliptin hydrate Indication Type 2 diabetes Dosage and Administration Once-daily oral administration of 5 mg saxagliptin in adults. Once-daily oral administration of 2.5 mg is also possible, based on the condition of the individual patient. Approval Date March 25, 2013
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