Drab Scott R, Philis-Tsimikas Athena
University of Pittsburgh School of Pharmacy, Pittsburgh, Pennsylvania; University Diabetes Care Associates, Pittsburgh, Pennsylvania.
Pharmacotherapy. 2014 Mar;34(3):291-302. doi: 10.1002/phar.1361. Epub 2013 Oct 17.
Basal insulin represents an essential tool in the treatment of diabetes mellitus; it can be prescribed with oral antidiabetic agents for the management of type 2 diabetes (T2D) or used as part of a basal-bolus regimen in type 1 diabetes (T1D) and more advanced T2D. The basal insulin products currently on the market, although improved, do not optimally mimic endogenous insulin secretion. It is therefore important to investigate how the action of a basal insulin can be improved to match the physiologic profile more precisely and consequently to examine the desired properties of an ideal new-generation basal insulin. Some of these characteristics would include stable pharmacokinetic (PK) and pharmacodynamic (PD) profiles, true 24-hour duration of action in all patients, low within-person variability in absorption and glucose-lowering action, more flexible dose timing, and low occurrence of hypoglycemia. A new-generation basal insulin, insulin degludec, currently approved in Japan, Mexico, and Europe, was designed to provide a more stable pharmacotherapeutic option with a lower risk of hypoglycemia than the currently available basal insulins while retaining an efficacious profile. The characteristics of an ideal basal insulin are reviewed, and the pharmacology and clinical attributes of insulin degludec are discussed.
基础胰岛素是糖尿病治疗的重要工具；它可与口服抗糖尿病药物联合使用，用于治疗2型糖尿病（T2D），或作为基础-餐时胰岛素方案的一部分，用于治疗1型糖尿病（T1D）和病情更严重的T2D。目前市场上的基础胰岛素产品虽有所改进，但仍无法最佳地模拟内源性胰岛素分泌。因此，研究如何改善基础胰岛素的作用，使其更精确地匹配生理特征，并进而考察理想的新一代基础胰岛素的理想特性，具有重要意义。这些特性包括稳定的药代动力学（PK）和药效学（PD）特征、在所有患者中真正达到24小时的作用持续时间、个体内吸收和降糖作用的低变异性、更灵活的给药时间以及低血糖发生率低。新一代基础胰岛素德谷胰岛素目前已在日本、墨西哥和欧洲获批，旨在提供一种更稳定的药物治疗选择，与现有基础胰岛素相比，低血糖风险更低，同时保持疗效。本文综述了理想基础胰岛素的特性，并讨论了德谷胰岛素的药理学和临床特性。
