Department of Clinical Pharmacy Practice, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY 11439, USA.
Cardiol Rev. 2010 Jul-Aug;18(4):213-7. doi: 10.1097/CRD.0b013e3181daad5f.
Type 2 diabetes mellitus is a common chronic disease that causes significant morbidity and mortality worldwide. The primary goal of treatment is to target glycemic control by maintaining the glycosylated hemoglobin (HbA1c) level near 6% to 7% without predisposing patients to hypoglycemia. Currently available antidiabetic agents work by different mechanisms to lower blood glucose levels. Unfortunately, each of them has its tolerability and safety concerns that limit use and dose titration. Dipeptidyl peptidase-4 enzyme inhibitors are novel drugs that prolong the action of incretins, and lead to increased insulin secretion and reduced hepatic glucose production. Saxagliptin is another dipeptidyl peptidase-4 (after sitagliptin) that is approved for the management of type 2 diabetes. It can be used alone or in combination with metformin, sulfonylurea, or thiazolidinedione (pioglitazone or rosiglitazone) when treatment with one drug alone provides inadequate glucose control. The usual adult dose is 2.5 to 5 mg once daily regardless of meals. A daily dose of 2.5 mg is recommended for patients with moderate to severe renal impairment or those who are taking potent CYP 3A4 inhibitors. In randomized clinical trials, saxagliptin alone lowered HbA1c levels by about 0.5%; with better efficacy seen when combined with other agents. It is well tolerated with the most common side effects being upper respiratory tract infection, headache, and urinary tract infection. In summary, saxagliptin is an option as an adjunct to lifestyle modifications and other antidiabetic agents to target glycemic control. It is also an alternative therapy for patients who have contraindications or intolerability to other antidiabetic agents.
2 型糖尿病是一种常见的慢性疾病,在全球范围内导致了显著的发病率和死亡率。治疗的主要目标是通过将糖化血红蛋白(HbA1c)水平控制在接近 6%-7%来控制血糖,同时避免患者出现低血糖。目前可用的抗糖尿病药物通过不同的机制降低血糖水平。不幸的是,它们各自都有其耐受性和安全性问题,限制了它们的使用和剂量调整。二肽基肽酶-4 酶抑制剂是一种新型药物,可延长肠促胰岛素的作用,导致胰岛素分泌增加和肝葡萄糖生成减少。沙格列汀是另一种二肽基肽酶-4(继西格列汀之后)抑制剂,已被批准用于 2 型糖尿病的治疗。它可单独使用或与二甲双胍、磺酰脲类或噻唑烷二酮类(吡格列酮或罗格列酮)联合使用,当单独使用一种药物不能充分控制血糖时。通常的成人剂量为每天 2.5 至 5 毫克,无论进餐与否。对于中重度肾功能不全或正在服用强效 CYP3A4 抑制剂的患者,建议每天剂量为 2.5 毫克。在随机临床试验中,沙格列汀单独使用可使 HbA1c 水平降低约 0.5%;与其他药物联合使用时效果更好。它的耐受性良好,最常见的副作用是上呼吸道感染、头痛和尿路感染。总之,沙格列汀是生活方式改变和其他抗糖尿病药物辅助治疗控制血糖的选择。对于其他抗糖尿病药物有禁忌或不耐受的患者,它也是一种替代治疗方法。