Uche Anadu Ndefo, Pharm.D., BCPS, is Assistant Professor, Department of Pharmacy Practice, Texas Southern University, Houston. Okwuchukwu Okoli, M.D., is Field Physician, Doctors Without Borders/Medecins Sans Frontieres, New York, NY. Goldina Erowele, Pharm.D., is Clinical Pharmacist III, Department of Pharmacy, Harris Health Systems, Houston.
Am J Health Syst Pharm. 2014 Jan 15;71(2):103-9. doi: 10.2146/ajhp130131.
The pharmacology, pharmacodynamics, pharmacokinetics, safety, efficacy, and place in therapy of alogliptin and its combinations for managing type 2 diabetes mellitus are reviewed.
Alogliptin is a selective, orally bioavailable inhibitor of the enzymatic activity of dipeptidyl peptidase-4 (DPP-4). It works by slowing the inactivation of the incretin hormones, thereby increasing their concentrations in the bloodstream and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin has a moderate degree of absorption, estimated to exceed 75%, and its absorption is not affected by food. No drug interactions are known to be associated with alogliptin monotherapy. It is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. The clinical efficacy and safety of alogliptin have been demonstrated in several clinical trials, reducing patients' glycosylated hemoglobin level by 0.4-1.0% in 26 weeks. Alogliptin does not require any dosage adjustment when coadministered with ketoconazole, fluconazole, gemfibrozil, warfarin, metformin, glyburide, and pioglitazone. Alogliptin selectively binds to and inhibits DPP-4 in vitro at concentrations approximating therapeutic exposures. The most common adverse events associated with alogliptin are nasopharyngitis, headache, and upper respiratory tract infection. As with the other DPP-4 inhibitors, use of alogliptin may be associated with the development of pancreatitis during therapy.
Alogliptin, a selective DPP-4 inhibitor, does not differ greatly from the other DPP-4 inhibitors currently available. It can be used as monotherapy or in combination with metformin for the management of type 2 diabetes.
综述阿格列汀及其联合用药治疗 2 型糖尿病的药理学、药效学、药代动力学、安全性、疗效和治疗地位。
阿格列汀是一种选择性、口服生物利用的二肽基肽酶-4(DPP-4)抑制剂。它通过减缓肠促胰岛素激素的失活来发挥作用,从而增加其在血液中的浓度,并以葡萄糖依赖的方式降低 2 型糖尿病患者的空腹和餐后血糖浓度。阿格列汀的吸收程度中等,估计超过 75%,且不受食物影响。目前已知与阿格列汀单药治疗相关的药物相互作用。它被指示与饮食和运动联合使用,以改善 2 型糖尿病成人的血糖控制。阿格列汀在几项临床试验中已证明其临床疗效和安全性,可使患者的糖化血红蛋白水平在 26 周内降低 0.4-1.0%。当与酮康唑、氟康唑、吉非贝齐、华法林、二甲双胍、格列本脲和吡格列酮联合使用时,阿格列汀不需要调整剂量。阿格列汀在接近治疗暴露浓度时,在体外选择性地结合并抑制 DPP-4。与阿格列汀相关的最常见不良事件是鼻咽炎、头痛和上呼吸道感染。与其他 DPP-4 抑制剂一样,阿格列汀的使用可能与治疗期间胰腺炎的发生有关。
作为一种选择性 DPP-4 抑制剂,阿格列汀与目前可用的其他 DPP-4 抑制剂没有太大区别。它可作为单药治疗或与二甲双胍联合用于 2 型糖尿病的治疗。