药理类别：
二肽基肽酶-4（DPP-4）抑制剂+双胍类。
活性成分（S）：
Alogliptin，二甲双胍（如盐酸）; 12.5mg/500mg，12.5mg/1000mg的标签。
公司
武田制药北美公司
指示（S）：
兼任饮食和运动改善血糖控制的同时的alogliptin和二甲双胍治疗成人2型糖尿病（T2DM）是合适的。
使用限制：不能用于治疗1型糖尿病或糖尿病酮症酸中毒。
药理作用：
alogliptin通过减慢肠降血糖素激素的失活，从而提高了他们的血液中的浓度，并在以葡萄糖依赖的方式降低空腹和餐后血糖浓度的行为。二甲双胍改善2型糖尿病患者的葡萄糖耐受性，降低基础和餐后血糖。二甲双胍降低肝葡萄糖生产和肠道对葡萄糖的吸收，增加外周葡萄糖的摄取和利用，改善胰岛素敏感性。
临床试验：
的alogliptin和二甲双胍合用已经研究饮食和运动，控制不佳的2型糖尿病患者，单用二甲双胍或二甲双胍+噻唑烷二酮。共2,095例患者被随机分配在3个双盲，安慰剂或主动控制研究，以评估对血糖控制的影响Kazano。在2型糖尿病患者，治疗用Kazano制作A1C与比较的临床意义和显着改进。由于是典型的试验剂治疗2型糖尿病，糖化血红蛋白平均减少与Kazano出现基线糖化血红蛋白升高的程度有关。
在所有研究的信息：见标签。
法律分类：
接收
成人：
个性化。整个吞下去，不拆标签。采取每天两次同食;逐渐增加剂量，以减少胃肠道的影响。最大25毫克alogliptin/2000mg的二甲双胍每天。
儿童：
不成立的。
禁忌（S）：
肾功能不全（血肌酐≥就是周边[男性]，≥1.4mg/dL [女性]或肌酐清除率异常）。代谢性酸中毒。糖尿病酮症酸中毒。
警告/注意事项：
开始之前确认肾功能正常的显示器（尤其是老年人）。停止如果发生乳酸性酸中毒，酮症酸中毒，肾功能损害，休克，急性心肌梗死，急性充血性心力衰竭，低氧血症，脱水，败血症，胰腺炎，或过敏反应。暂时中止在手术过程中，可能会重新启动时误服，肾功能恢复正常化。血管性水肿史与其他DPP-4抑制剂。开始治疗前获取肝功检查。避免肝脏疾病的临床或实验室证据。监视器血液（尤其是血清维生素B12在易感患者）。老年，衰弱，营养不良，肾上腺或垂体功能不足，或饮酒中毒：增加低血糖的风险。伴随血管内的碘造影剂（暂停期间和程序48小时后）。怀孕（B类）。哺乳期的母亲。
互动（补）
肾小管分泌（如阿米洛利，地高辛，吗啡，普鲁卡因胺，奎宁，奎尼丁，雷尼替丁，氨苯喋啶，甲氧苄啶，万古霉素），西咪替丁：消除阳离子药物可能会增加二甲双胍水平。避免过度的酒精摄入量（会加强二甲双胍对乳酸的影响）。注意伴随吡或其他碳酸酐酶抑制剂（例如，唑尼沙胺，乙酰唑胺，dichlorphenamide）;可能引起代谢性酸中毒。利尿剂，类固醇，雌激素，口服避孕药，吩噻嗪，苯妥英，甲状腺产品，烟酸，拟交感神经药，钙通道阻滞剂，异烟肼，其他可能导致高血糖。伴随磺脲类或胰岛素：可能需要降低磺脲类或胰岛素的剂量，以减少低血糖的风险。 β-受体阻滞剂可掩盖低血糖症。
不良反应（S）
上呼吸道感染，鼻咽炎，腹泻，高血压，头痛，腰痛，尿路感染。
如何提供：
标签-60，180，500
Pharmacological Class:
Dipeptidyl peptidase-4 (DPP-4) inhibitor + biguanide.
Active Ingredient(s):
Alogliptin, metformin (as HCl); 12.5mg/500mg, 12.5mg/1000mg; tabs.
Company
Takeda Pharmaceuticals North America, Inc.
Indication(s):
Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM) when treatment with both alogliptin and metformin is appropriate.
Limitations of use: not for treatment of type 1 diabetes mellitus or diabetic ketoacidosis.
Pharmacology:
Alogliptin acts by slowing the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner. Metformin improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production and intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
Clinical Trials:
The coadministration of alogliptin and metformin has been studied in patients with T2DM inadequately controlled on diet and exercise alone, on metformin alone, or metformin + thiazolidinedione. A total of 2,095 patients were randomized in 3 double-blind, placebo- or active-controlled studies to evaluate the effects of Kazano on glycemic control. In patients with T2DM, treatment with Kazano produced clinically meaningful and statistically significant improvements in A1C vs. comparator. As is typical for trials of agents to treat T2DM, the mean reduction in A1C with Kazano appears to be related to the degree of A1C elevation at baseline.
For information on all studies conducted: see full labeling.
Legal Classification:
Rx
Adults:
Individualize. Swallow whole; do not split tabs. Take twice daily with food; increase dose gradually to reduce GI effects. Max 25mg alogliptin/2000mg metformin per day.
Children:
Not established.
Contraindication(s):
Renal impairment (Scr ≥1.5mg/dL [men], ≥1.4mg/dL [women] or abnormal CrCl). Metabolic acidosis. Diabetic ketoacidosis.
Warnings/Precautions:
Confirm normal renal function before starting; monitor (esp. in elderly). Discontinue if lactic acidosis, ketoacidosis, renal impairment, shock, acute MI, acute CHF, hypoxemia, dehydration, sepsis, pancreatitis, or hypersensitivity reactions occur. Temporarily suspend during surgery; may restart when oral intake is resumed and renal function normalized. History of angioedema with other DPP-4 inhibitors. Obtain LFTs before starting therapy. Avoid if clinical or lab evidence of hepatic disease. Monitor hematology (esp. serum Vit. B12 in susceptible patients). Elderly, debilitated, malnourished, adrenal or pituitary insufficiency, or alcohol intoxication: increased risk of hypoglycemia. Concomitant intravascular iodinated contrast agents (suspend during and for 48hrs after procedure). Pregnancy (Category B). Nursing mothers.
Interaction(s)
Cationic drugs eliminated by renal tubular secretion (eg, amiloride, digoxin, morphine, procainamide, quinine, quinidine, ranitidine, triamterene, trimethoprim, vancomycin), cimetidine: may increase metformin levels. Avoid excessive alcohol intake (potentiates effects of metformin on lactate). Caution with concomitant topiramate, or other carbonic anhydrase inhibitors (eg, zonisamide, acetazolamide, dichlorphenamide); may induce metabolic acidosis. Diuretics, steroids, estrogens, oral contraceptives, phenothiazines, phenytoin, thyroid products, nicotinic acid, sympathomimetics, calcium channel blockers, isoniazid, others that may cause hyperglycemia. Concomitant sulfonylurea or insulin: may need lower dose of sulfonylurea or insulin to reduce risk of hypoglycemia. β-blockers may mask hypoglycemia.
Adverse Reaction(s)
Upper respiratory tract infection, nasopharyngitis, diarrhea, hypertension, headache, back pain, UTI.
How Supplied:
Tabs—60, 180, 500
WARNING: LACTIC ACIDOSIS—for KAZANO
Lactic acidosis is a rare, but serious complication that can occur due to metformin accumulation. The risk increases with conditions such as sepsis, dehydration, excess alcohol intake, hepatic impairment, renal impairment, and acute congestive heart failure. The onset is often subtle,accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, increasing somnolence, and nonspecific abdominal distress. Laboratory abnormalities include low pH, increased anion gap, and elevated blood lactate. If acidosis is suspected, KAZANO should be discontinued and the patient hospitalized immediately.
NESINA, KAZANO, and OSENI are contraindicated in
NESINA, KAZANO, and OSENI are contraindicated in patients with a history of serious hypersensitivity reaction to any of the components of these products, such as anaphylaxis, angioedema, or severe cutaneous adverse reactions. KAZANO is contraindicated in patients with renal impairment (e.g., serum creatinine levels =1.5 mg/dL for men, =1.4 mg/dL for women or abnormal creatinine clearance), which may also result from conditions such as cardiovascular collapse (shock), acute myocardial infarctions, and septicemia. KAZANO is contraindicated in patients with acute or chronic metabolic acidosis, including diabetic ketoacidosis. Do not initiate OSENI in patients with established NYHA Class III or IV heart failure.
Warnings and Precautions—for KAZANO
Lactic acidosis: Warn against excessive alcohol intake. KAZANO is not recommended in hepatic impairment and is contraindicated in renal impairment. Ensure normal renal function before initiating and at least annually thereafter. Temporarily discontinue in patients undergoing radiologic studies with intravascular iodinated contrast materials or any surgical procedures necessitating restricted intake of food and fluids. Lactic acidosis due to metformin accumulation during therapy is fatal in approximately 50% of cases. The risk increases in patients with renal impairment, congestive heart failure requiring drug treatment, and with increasing age.
Vitamin B12 deficiency: Metformin may lower Vitamin B12 levels. Monitor hematologic parameters annually.
Warnings and Precautions—for OSENI
Congestive heart failure: Fluid retention may occur and can exacerbate or lead to congestive heart failure. Combination use with insulin and use in congestive heart failure NYHA Class I and II may increase risk. Monitor patients for signs and symptoms.
Edema: Dose-related edema may occur. Use with caution in patients with edema.