英文药名：Xigduo XR(Dapagliflozin and Metformin HCl Extended-release Tablets) 中文药名：达帕格列净/盐酸二甲双胍复方缓释片 生产厂家：阿斯利康（AstraZeneca） 药品介绍 2014年10月30日，FDA批准阿斯利康（AstraZeneca）旗下糖尿病复方新药Xigduo XR（达格列净/缓释型盐酸二甲双胍）在美国上市，用于治疗2型糖尿病。 Xigduo XR首次将钠-葡萄糖协同转运蛋白2（SGLT2）抑制剂达格列净（dapagliflozin，商品名Forxiga ）和缓释型盐酸二甲双胍相结合；对于需要达格列净联合二甲双胍治疗的2型糖尿病成人患者，该药可作为辅助药物，配合饮食和运动来控制血糖。此前，Xigduo（达格列净/速释盐酸二甲双胍）已于2014年1月获欧盟批准，是欧盟上市的首个SGLT2抑制剂和二甲双胍复方产品。 Xigduo XR不推荐用于1型糖尿病或糖尿病酮症酸中毒患者。其标签上还带有乳酸酸中毒的黑框警告（治疗期间二甲双胍在体内的蓄积可造成乳酸酸中毒）。 该复方新药的禁忌症包括，中度到重度肾损伤、对达格列净或二甲双胍严重过敏史、合并糖尿病酮症酸中毒等代谢性酸中毒。 FDA基于4项3期临床试验结果批准了Xigduo XR的申请，这些临床试验不仅证实了达格列净IR或XR片剂的安全性和有效性，还将其与格列吡嗪联合二甲双胍的治疗方案进行了对比。 尽管没有Xigduo XR复方片剂应用的临床研究，但在健康成人中，Xigduo XR与达格列净和二甲双胍两种单方片剂的联合治疗方案具有生物等效性。 Xigduo XR（达格列净/缓释型盐酸二甲双胍）的多个剂量规格目前均已获得FDA批准，包括5 mg/500 mg、5 mg/1000mg、10mg/500mg和10mg/1000 mg，应根据患者当前的治疗方案决定起始用药剂量。 Xigduo XR的用法是，每日1次，在清晨进餐时服用。缓释型制剂逐量释放药物成分可减少二甲双胍带来的胃肠道不良反应。每日最大推荐剂量为达格列净10 mg/缓释型盐酸二甲双胍2000mg）。 XIGDUO XR Rx Pharmacological Class: Sodium-glucose co-transporter 2 inhibitor (SGLT2) + biguanide. Active Ingredient(s): Dapagliflozin, metformin HCl ext-rel; 5mg/500mg, 5mg/1000mg, 10mg/500mg, 10mg/1000mg; tablets. Company AstraZeneca Pharmaceuticals Indication(s): Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both ­dapagliflozin and metformin is appropriate. Limitations of use: not for treating type 1 diabetes or diabetic ketoacidosis. Pharmacology: Dapagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, thereby increasing urinary glucose excretion. Metformin HCl decreases hepatic glucose production, intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Clinical Trials: There have been no clinical efficacy studies conducted with Xigduo XR combination tablets to characterize its effect on HbA1c reduction. Xigduo XR is considered to be bioequivalent to coadministered dapagliflozin and metformin HCl extended-release (XR) tablets. The coadministration of dapagliflozin + metformin XR tablets has been studied in treatment-naive patients inadequately controlled on diet and exercise alone; and in patients with type 2 diabetes inadequately controlled on metformin. Treatment with dapagliflozin + metformin at all doses produced clinically and statistically significant improvements in HbA1c and fasting plasma glucose vs. placebo plus metformin as initial or add-on therapy. For more clinical trial data, see full labeling. Legal Classification: Rx Adults: Individualize. Swallow whole. Take once daily in the AM with food; increase dose gradually. Maximum daily dose: 10mg/2000mg. Children: <18 years: not established. Contraindication(s): Moderate-to-severe renal impairment (SCr ≥1.5mg/dL [men], ≥1.4mg/dL [women] or eGFR <60mL/min/1.73m2). Metabolic acidosis, diabetic ketoacidosis. Warnings/Precautions: Confirm normal renal function before starting and monitor thereafter (esp. in elderly). Discontinue if lactic acidosis (dehydration, sepsis), hypoxemia (shock, acute MI or CHF), renal impairment, or hypersensitivity reactions occur. Avoid in hepatic impairment. Correct volume depletion before initiating. Monitor for symptomatic hypotension after starting therapy (esp. elderly, renal impairment, or on loop diuretics). Elderly, debilitated, uncompensated strenuous exercise, malnourished or deficient caloric intake, adrenal or pituitary insufficiency, or alcohol intoxication: increased risk of hypoglycemia. Temporarily suspend for surgery; restart once oral intake resumes and renal function normalized. Discontinue prior to any intravascular radiocontrast study; withhold for 48 hours after procedure. Monitor for genital mycotic infections, hematology (esp. serum Vit. B12), increases in LDL-C; treat if occur. Active bladder cancer: do not use. Pregnancy (Category C). Nursing mothers: not recommended. Interaction(s) Cationic drugs eliminated by renal tubular secretion (eg, amiloride, cimetidine, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin); may increase metformin levels; monitor. Diuretics, steroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, CCBs, and isoniazid may cause hyperglycemia. Avoid excessive alcohol. Concomitant drugs that may affect renal function or metformin disposition; monitor and adjust dose. Concomitant insulin or insulin secretagogue: consider a lower dose of insulin/insulin secretagogue to reduce risk of hypoglycemia. Beta-blockers may mask hypoglycemia. May cause false (+) urine glucose tests or unreliable measurements of 1, 5-AG assay; use alternative methods to monitor glycemic control. Adverse Reaction(s) Female genital mycotic infections, nasopharyngitis, UTI, diarrhea, headache, influenza, nausea, vomiting. How Supplied: XR tabs 5mg/ 500mg, 10mg/500mg—30, 500; 5mg/1000mg—30, 60, 90, 400; 10mg/1000mg—30, 90, 400 LAST UPDATED: 3/2/2015