2011年10月7日,美国食品药品管理局(FDA)宣布批准Juvisync(西他列汀+辛伐他汀)用于治疗同时患有2型糖尿病和高脂血症的成人患者。Juvisync是一种固定剂量复方制剂,其所含的两种药物此前均已获准。只允许对同时具有这两种药物适应证的患者开具这种复方制剂的处方。 西他列汀是一种二肽基肽酶-4抑制剂,可增强人体自身的降糖能力,已被批准与饮食和运动疗法联合用于改善成人2型糖尿病患者的血糖控制水平。辛伐他汀是3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂或称他汀类药物的一种,已获准与饮食和运动疗法联合用于降低血液低密度脂蛋白胆固醇水平。 Juvisync已获准的剂量强度包括(西他列汀/辛伐他汀)100 mg/10 mg、100 mg/20 mg和100 mg/40 mg三种。生产商已开始研发含有50 mg西他列汀的药片,即Juvisync 50 mg/10 mg、50 mg/20 mg和50 mg/40 mg。在含有50 mg西他列汀的药片上市之前,需要使用该剂量药物的患者应服用单一成分的西他列汀药片。 Juvisync的最常见不良反应包括上呼吸道感染、鼻塞或流涕、咽痛、头痛、肌痛、腹痛、便秘和恶心。 制造商: 类药物: 活性成分(S): 药理: 临床试验: 法律分类: 成人: 儿童: 禁忌(S): 警告/注意事项: 相互作用(S): 不良反应(S): 如何提供: 最后更新: 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. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses. 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. In addition, simvastatin reduces VLDL and TG and increases HDL-C. 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 (>10x ULN), 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:11/3/2011 |