新型降糖药Juvisync(西格列汀与辛伐他汀合剂）上市
对成千上万同时患有糖尿病和高胆固醇的患者来说，他们的生活将掀开崭新的一页。10月7日，第一只供这些人群使用的组合药丸Juvisync获得美国FDA的批准。Juvisync由默沙东负责开发，Juvisync是将默沙东生产的2型糖尿病药(辛伐他汀)Januvia与舒降之(辛伐他汀)的组合产品，该药为第一个2型糖尿病治疗药物与降脂药的复方制剂。
Juvisync是一种含有两种既往获批药物（西格列汀和辛伐他汀）的复合制剂，西格列汀可降低血糖，辛伐他汀则可降低血液中的低密度脂蛋白。FDA批准的Juvisync剂型由100mg磷酸西格列汀和10、20及40mg辛伐他汀组成。生产商承诺将制备更多的组合剂型。在新组合剂型上市前，需要服用50mg西格列汀的患者仍需继续服用单一成分磷酸西格列汀片剂。
FDA药品评价和研究中心主管Park博士指出，为了确保该产品的有效性和安全性，包含不同剂量西他列汀和辛伐他汀的固定剂量复合剂已被研发，以满足个体患者的不同需要。
Juvisync的最常见副作用包括上呼吸道感染、鼻塞、流涕、咽痛、头痛、肌肉疼痛和胃痛、便秘及恶心。
制造商：
默克制药公司
类药物：
二肽基肽酶-4（DPP - 4）抑制剂+ HMG - CoA还原酶抑制剂。
活性成分（S）：
西他列汀，辛伐他汀; 100mg/10mg，100mg/20mg，100mg/40mg;选项卡。
指示（S）：
患者对他们来说，西他列汀和辛伐他汀治疗是适当的。西他列汀作为辅助饮食和运动改善血糖控制与2型糖尿病的成年人表示。辛伐他汀作为辅助治疗，在饮食上表示：，减少冠心病死亡，总死亡率降低风险和减少非致命性心肌梗塞，中风和冠脉事件的高风险患者的血管重建手术的需要的危险;降低升高的总减少血症患者载脂蛋白B，C，LDL - C的，TG和增加HDL - C的原发性高脂血症（杂合子家族性和nonfamilial）和混合血脂异常患者;升高TG和降低TG和VLDL - C dysbetalipoproteinemia患者;减少纯合子家族性高胆固醇血症患者的总- C和LDL - C水平。
药理：
西他列汀是一个DPP - 4抑制剂，这被认为是施加其行动与2型糖尿病患者肠促胰岛素激素的灭活减慢。辛伐他汀是一种HMG - CoA还原酶，酶催化的HMG - CoA转化为甲羟戊酸，早期和速率限制步骤中的胆固醇的生物合成途径的特异性抑制剂。
临床试验：
西他列汀和辛伐他汀的安全性和有效性进行了研究，在多个临床研究。
法律分类：
接收
成人：
燕子整体。给单剂量为每日的下午。最初100mg/40mg每天。已经在辛伐他汀的患者：每天开始西格列汀100毫克剂量辛伐他汀已经上当受骗。如果需要≥4个星期后调整剂量。同时服用维拉帕米，地尔硫卓：最大每一天100mg/10mg。同时服用胺碘酮，氨氯地平，雷诺嗪：每天最大100mg/20mg。纯合子家族性高胆固醇血症：每一天100mg/40mg。中国患者服用降脂修改剂量含烟酸产品（≥1g/day烟酸）：谨慎100mg/40mg剂量;肌病的风险增加。
儿童：
<18yrs：不推荐。
禁忌（S）：
伴随强CYP3A4抑制剂（如酮康唑，伊曲康唑，泊沙康唑，红霉素，克拉霉素，泰利霉素，HIV蛋白酶抑制剂，奈法唑酮）。同时服用吉非贝齐，环孢素，达那唑。活动性肝病。怀孕（Cat.X）。哺乳的母亲。
警告/注意事项：
不适用于治疗1型糖尿病或糖尿病酮症酸中毒。中度至重度肾功能不全或终末期肾病：不推荐。开始治疗前评估肾功能并在此后定期。监测胰腺炎，肌酸激酶显着升高（> 10xULN），肌病;停止，如果发生。暂时截留的剂量，如果发生急性或严重的条件下诱发肾功能衰竭，继发横纹肌溶解的发展。监测肝功能基线，然后根据需要。肝脏疾病的历史。大量的酒精消费。血管性水肿的历史与其他DPP - 4抑制剂。老人。
相互作用（S）：
见禁忌。同时磺脲类或胰岛素：这些减少剂量，以减少低血糖的风险。减少最大辛伐他汀剂量胺碘酮，维拉帕米，地尔硫，氨氯地平，雷诺嗪，伏立康唑，必须使用。注意与其他贝特类药物，秋水仙碱。避免大量葡萄柚汁（> 1夸脱每天）。监测地高辛，香豆素类抗凝血剂。
不良反应（S）：
上呼吸道感染，头痛，腹痛，便秘，恶心，鼻咽炎;胰腺炎，肌病，横纹肌溶解症，过敏反应（终止如果发生），糖化血红蛋白和空腹血糖水平增加。
如何提供：
标签- 30，90，1000
最后更新：
2011年11月28日
JUVISYNC
Manufacturer:
Merck & Co., Inc.
Pharmacological Class:
Dipeptidyl peptidase-4 (DPP-4) inhibitor + HMG-CoA reductase inhibitor.
Active Ingredient(s):
Sitagliptin, simvastatin; 100mg/10mg, 100mg/20mg, 100mg/40mg; tabs
Indication(s):
In patients for whom treatment with both sitagliptin and simvastatin is appropriate. Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Simvastatin is indicated as an adjunctive therapy to diet to: reduce risk of total mortality by reducing CHD deaths and reduce risk of non-fatal MI, stroke, and the need for revascularization procedures in patients at high risk of coronary events; reduce elevated total-C, LDL-C, Apo B, TG and increase HDL-C in patients with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia; reduce elevated TG in patients with hypertriglyceridemia and reduce TG and VLDL-C in patients with primary dysbetalipoproteinemia; reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia.
Pharmacology:
Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate limiting step in the biosynthetic pathway for cholesterol.
Clinical Trials:
The safety and efficacy of sitagliptin and simvastatin have been studied in multiple clinical studies.
Legal Classification:
Rx
Adults:
Swallow whole. Give as single daily dose in the PM. Initially 100mg/40mg per day. Patients already on simvastatin: start with sitagliptin 100mg daily and the dose of simvastatin already being taken. Adjust dose if needed after ≥4 weeks. Concomitant verapamil, diltiazem: max 100mg/10mg per day. Concomitant amiodarone, amlodipine, ranolazine: max 100mg/20mg per day. Homozygous familial hypercholesterolemia: 100mg/40mg per day. Chinese patients taking lipid-modifying doses (≥1g/day niacin) of niacin-containing products: caution with 100mg/40mg dose; increased risk of myopathy.
Children:
<18yrs: not recommended.
Contraindication(s):
Concomitant strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, nefazodone). Concomitant gemfibrozil, cyclosporine, danazol. Active liver disease. Pregnancy (Cat.X). Nursing mothers.
Warnings/Precautions:
Not for treating type 1 diabetes or diabetic ketoacidosis. Moderate-to-severe renal impairment or ESRD: not recommended. Assess renal function prior to starting therapy and periodically thereafter. Monitor for pancreatitis, markedly elevated creatine kinase (>10xULN), myopathy; discontinue if occurs. Temporarily withhold dose if experiencing acute or serious condition predisposing to development of renal failure secondary to rhabdomyolysis. Monitor liver function at baseline, then as needed. History of liver disease. Substantial alcohol consumption. History of angioedema with other DPP-4 inhibitors. Elderly.
Interaction(s):
See Contraindications. Concomitant sulfonylurea or insulin: reduce dose of these to reduce risk of hypoglycemia. Reduce max simvastatin dose if amiodarone, verapamil, diltiazem, amlodipine, ranolazine, voriconazole must be used. Caution with other fibrates, colchicine. Avoid large quantities of grapefruit juice (>1 quart daily). Monitor digoxin, coumarin anticoagulants.
Adverse Reaction(s):
Upper respiratory infection, headache, abdominal pain, constipation, nausea, nasopharyngitis; pancreatitis, myopathy, rhabdomyolysis, hypersensitivity reactions (discontinue if occurs), increased A1C and fasting serum glucose levels.
How Supplied:
Tabs—30, 90, 1000
Last Updated:
11/28/2011
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