部分中文KOMBIGLYZE XR处方资料（仅供参考）
英文商品名: KOMBIGLYZE XR
英文药品名: SAXAGLIPTIN HCL/METFORMIN HCL
中文药品名:盐酸沙格列汀/盐酸二甲双胍
阿斯利康和施贵宝糖尿病药Kombiglyze XR获FDA批准
近日，阿斯利康和百时美-施贵宝共同推出的药物Kombiglyze XR已获得FDA批准用于治疗2型糖尿病成人患者。
Kombiglyze XR每日用药一次，是一种复方制剂，同时含有缓释型甲福明二甲双胍和DPP-4抑制剂两种成分，可以控制血糖水平——包括糖化血蛋白水平(HbA1c)、空腹血糖水平和饭后血糖水平。
Kombiglyze XR主要是作为一种辅助药物，用于那些适合同时采用saxagliptin(商品名为Onglyza)和甲福明二甲双胍治疗的2型糖尿病患者，再结合饮食和运动帮助他们控制血糖水平。
这次获准的依据是该药在一系列临床实验中获取的数据，其中包括两项III期临床实验和一项生物等效性实验，后者从疗效和安全性对saxagliptin和甲福明二甲双胍IR两种单独药物合用和安慰剂+甲福明二甲双胍IR进行了检测。
Kombiglyze XR和saxagliptin+甲福明二甲双胍XR(两种单独药物联用)的生物等效性也在实验中得到了证实。
2007年1月份，百时美-施贵宝和阿斯利康达就达成了一份合作协议，双方将联手研究、开发并推广2型糖尿病治疗药。
Kombiglyze^TM被建议在欧盟获批
欧洲人用医疗产品委员会对批准Kombiglyze^TM的上市授权持积极意见。本品是一种含有saxagliptin和缓释盐酸二甲双胍（2．5／850m和2．5／1000mg）的膜衣片，计划用于治疗2型糖尿病患者。
规格：
KOMBIGLYZE XR 24小时片剂 (5-500)毫克/片 30片/瓶
KOMBIGLYZE XR 5/500
Manufacturer:
Bristol-Myers Squibb
Pharmacological Class:
Antidiabetic (dipeptidyl peptidase-4 (DPP4) inhibitor + biguanide).
Active Ingredient(s):
Saxagliptin 5mg, metformin HCl extended-release 500mg; tabs.
Also:
KOMBIGLYZE XR 5/1000
Saxagliptin 5mg, metformin HCl extended-release 1000mg; tabs.
KOMBIGLYZE XR 2.5/1000
Saxagliptin 2.5mg, metformin HCl extended-release 1000mg; tabs.
Indication(s):
Adjunct to diet and exercise in type 2 diabetes when treatment with both saxagliptin and metformin is appropriate.
Pharmacology:
Kombiglyze XR is an antidiabetic product that combines a DPP4 inhibitor and extended-release form of the biguanide, metformin. Saxagliptin slows the inactivation of incretin hormones, increasing their levels in the blood, leading to reduced fasting and postprandial glucose levels in a glucose-dependent manner. Metformin improves glucose tolerance in type 2 diabetes by decreasing hepatic glucose production, decreased intestinal absorption of glucose, and by improving insulin sensitivity; it generally does not cause hypoglycemia.
Kombiglyze XR has not been studied in combination with insulin.
Clinical Trials:
A study involving treatment-naive patients with type 2 diabetes who had inadequate glycemic control on diet and exercise was conducted to evaluate the safety and efficacy of saxagliptin + metformin immediate-release. The coadministration of saxagliptin 5mg/day plus metformin resulted in significant improvements in A1C, fasting plasma glucose, and 2-hour postprandial glucose compared to placebo plus metformin.
In another study, saxagliptin 2.5mg and 5mg was given as add-on therapy to patients with inadequate glycemic control on metformin immediate-release alone. This combination provided significant improvements in A1C, FPG, and PPG compared with placebo add-on to metformin immediate-release.
Legal Classification:
Rx
Adults:
Take once daily with evening meal. Swallow whole. Individualize; titrate based on response. Maximum saxagliptin 5mg/day and metformin extended-release 2000mg/day. Concomitant strong CYP3A4/5 inhibitors: maximum saxagliptin 2.5mg/day.
Children:
Not recommended.
Contraindication(s):
Renal impairment (serum creatinine ≥1.5mg/dL [men], ≥1.4mg/dL [women]). Metabolic acidosis, diabetic ketoacidosis. Concomitant intravascular iodinated contrast agents (suspend during and for 48 hours after use).
Warnings/Precautions:
Not for treating type 1 diabetes. Confirm normal renal function before starting; monitor (esp. in patients ≥80yrs). Avoid in hepatic disease. Discontinue if lactic acidosis, shock, acute MI, sepsis, or hypoxemia occurs. Suspend therapy if dehydration occurs or before surgery. Monitor hepatic function, hematology (especially serum Vitamin B12 in susceptible patients). Elderly, debilitated, uncompensated strenuous exercise, malnourished or deficient caloric intake, adrenal or pituitary insufficiency, or alcohol intoxication: increased risk of hypoglycemia. Pregnancy (Cat.B), nursing mothers: not recommended; consider using insulin instead.
Interaction(s):
Saxagliptin potentiated by strong CYP3A4/5 inhibitors (eg, ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin). Cationic drugs eliminated by renal tubular secretion (eg, amiloride, digoxin, morphine, procainamide, quinidine, quinine, triamterene, trimethoprim, ranitidine, vancomycin): may increase metformin levels. Avoid excessive alcohol intake (potentiates effects of metformin on lactate). Diuretics, steroids, phenothiazines, phenytoin, sympathomimetics, calcium channel blockers, isoniazid, niacin, others may cause hyperglycemia. Increased risk of hypoglycemia with alcohol, sulfonylureas. ß-blockers may mask hypoglycemia.
Adverse Reaction(s):
GI upset, URI, UTI, headache, nasopharyngitis, hypersensitivity reactions; lactic acidosis (rare, half the cases are fatal).
How Supplied:
Tabs 5/500—30
5/1000—30, 90, 500
2.5/1000—60, 500
Last Updated:
6/16/2011
Generic Name: metformin and saxagliptin (met FOR min and SAX a GLIP tin)
Brand Names: Kombiglyze XR
What is Kombiglyze XR?
Kombiglyze XR contains a combination of metformin and saxagliptin. Metformin and saxagliptin are oral diabetes medicines that help control blood sugar levels. Metformin works by decreasing glucose (sugar) production in the liver and decreasing absorption of glucose by the intestines. Saxagliptin works by regulating the levels of insulin your body produces after eating.
Kombiglyze XR is used to treat type 2 diabetes. Kombiglyze XR is not for treating type 1 diabetes.
Kombiglyze XR may also be used for purposes not listed in this medication guide.
Important information about Kombiglyze XR
You should not use Kombiglyze XR if you are allergic to metformin (Actoplus Met, Avandamet, Fortamet, Glucophage, Riomet) or saxagliptin (Onglyza), if you have kidney disease, or if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin).
If you need to have surgery or any type of x-ray or CT scan using a dye that is injected into your veins, you will need to temporarily stop taking Kombiglyze XR.
Some people develop lactic acidosis while taking metformin. Early symptoms may get worse over time and this condition can be fatal. Get emergency medical help if you have: muscle pain or weakness, numb or cold feeling in your arms and legs, trouble breathing, stomach pain, nausea with vomiting, slow or irregular heart rate, dizziness, or feeling very weak or tired.
Kombiglyze XR Oral Warnings
Metformin can rarely cause a serious (sometimes fatal) condition called lactic acidosis. Stop taking this product and get medical help right away if you develop any of the following symptoms of lactic acidosis: unusual tiredness, dizziness, severe drowsiness, feeling cold (especially in your arms and legs), muscle pain, fast/difficult breathing, slow/irregular heartbeat, stomach pain with nausea, vomiting, or diarrhea.
Lactic acidosis is more likely to occur in patients who have certain medical conditions, including kidney or liver disease, recent surgery, a serious infection, conditions that may cause a low level of oxygen in the blood or poor circulation (such as congestive heart failure, recent heart attack, recent stroke), heavy alcohol use, a severe loss of body fluids (dehydration), or X-ray or scanning procedures that require an injectable iodinated contrast drug. Tell your doctor immediately if any of these conditions occur or if you notice a big change in your overall health. You may need to stop taking this medication temporarily. The elderly are also at higher risk, especially those older than 80 years who have not had kidney tests. (See also Side Effects and Precautions sections.)
Kombiglyze XR is a combination of 2 medicines in one tablet. It works in 4 different ways to help control blood sugar. Kombiglyze XR works for 24 hours. Kombiglyze XR is believed to work in the following 4 different ways:
IMPORTANT SAFETY INFORMATION for KOMBIGLYZE XR (saxagliptin and metformin HCI extended-release) tablets
Lactic Acidosis: Metformin hydrochloride, one of the medicines in KOMBIGLYZE XR, can cause a rare, but serious, side effect called lactic acidosis (a build-up of lactic acid in the blood) that can cause death. Lactic acidosis is a medical emergency and must be treated in a hospital. Stop taking KOMBIGLYZE XR and call your doctor right away if you get any of the following symptoms of lactic acidosis: feel very weak and tired, unusual (not normal) muscle pain, trouble breathing, unusual sleepiness or sleep longer than usual, unexplained stomach or intestinal problems with nausea and vomiting or diarrhea, feel cold (especially in your arms and legs), dizzy or lightheaded, or have a slow or irregular heartbeat.
You have a higher chance of getting lactic acidosis if you have kidney or liver problems, have congestive heart failure that requires treatment with medicines, drink a lot of alcohol (very often or short-term “binge” drinking), get dehydrated (lose a large amount of body fluids), have certain x-ray tests with injectable dyes or contrast agents, have surgery, have a heart attack, severe infection, or stroke, or are 80 years of age or older and have not had your kidney function tested.
Do not take KOMBIGLYZE XR if you have kidney problems, have a condition called metabolic acidosis or diabetic ketoacidosis (increased ketones in the blood or urine), or are allergic to metformin hydrochloride, saxagliptin, or any of the ingredients in KOMBIGLYZE XR. Serious allergic reactions can occur with KOMBIGLYZE XR and may include swelling of the face, lips or throat, difficulty swallowing or breathing, swelling of the skin, hives, rash, itching, flaking, or peeling. If you have these symptoms, stop taking KOMBIGLYZE XR and contact your doctor right away.
Serious side effects can happen to people taking KOMBIGLYZE XR, including inflammation of the pancreas (pancreatitis) which may be severe and lead to death. Before taking KOMBIGLYZE XR, tell your doctor if you ever had pancreatitis, gallstones, history of alcoholism, or high triglyceride levels. Stop taking KOMBIGLYZE XR and contact your doctor right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen through to your back. The pain may happen with or without vomiting. These may be symptoms of pancreatitis.
Your doctor should do blood tests to check how well your kidneys are working before and during your treatment with KOMBIGLYZE XR.
If you take KOMBIGLYZE XR with another medicine that can cause low blood sugar (hypoglycemia), such as sulfonylureas or insulin, you have a higher risk of having low blood sugar. Symptoms of low blood sugar include, shaking, sweating, rapid heartbeat, change in vision, hunger, headache and change in mood. Follow your doctor's instructions for treating low blood sugar.
