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胰岛素类似物:当代事实与未来展望一瞥。

Insulin analogs: Glimpse on contemporary facts and future prospective.

机构信息

Department of Pharmacology, Amity Institute of Pharmacy, Amity University, Gurugram, Haryana 122051, India.

Fortis Healthcare Limited, UBP, 4rd Floor, Sector 41, Gurugram, Haryana 22001, India.

出版信息

Life Sci. 2019 Feb 15;219:90-99. doi: 10.1016/j.lfs.2019.01.011. Epub 2019 Jan 10.

Abstract

Insulin remains a predominant life-saving medication for type 1 and type 2 Diabetes Mellites. Natural insulin secretion limits the fluctuation of the narrow and high surge of blood glucose levels. However, imitating the same by external insulin remains a challenge as a variety of insulin analogs (rapid acting, short acting, intermediate acting and long-acting) have different pharmacokinetic (PK) and pharmacodynamic (PD) properties. Inconsistent reduction in overall hyperglycemia level and nocturnal hypoglycemia due to variable absorption time and time action profile predominantly highlights the need of revisiting the PK/PD of insulin analogs as single analog is not yet sufficed to replace internal insulin exogenously. Combination therapy with basal and prandial insulins or intensification of hypoglycemic therapy with premixed insulins are of prime importance in managing diabetes effectively, imitating the natural insulin secretion. Therefore, the knowledge of PK/PD properties might help a practitioner to design, implement and manage insulin replacement therapy effectively and averting adverse events. Present study reports the comparative analysis of PK/PD profile of various insulin analogs based on the concurrent information about clinical aspects. Moreover, study interlinks the major concerns of therapeutic efficacy of insulin analogs with their respective onset of action and duration of effectiveness and reported adverse drug reaction which explore the scope of improvement.

摘要

胰岛素仍然是 1 型和 2 型糖尿病患者主要的救命药物。天然胰岛素分泌可限制血糖水平的窄幅高频波动。然而,由于各种胰岛素类似物(速效、短效、中效和长效)具有不同的药代动力学(PK)和药效动力学(PD)特性,因此通过外部胰岛素模拟这种作用仍然具有挑战性。由于吸收时间和作用时间的变化,整体高血糖水平的降低不一致,以及夜间低血糖,主要强调需要重新审视胰岛素类似物的 PK/PD,因为单一类似物还不足以替代内源性胰岛素。基础胰岛素和餐时胰岛素的联合治疗或通过预混胰岛素强化低血糖治疗对于有效地控制糖尿病、模拟天然胰岛素分泌至关重要。因此,了解 PK/PD 特性可能有助于临床医生有效地设计、实施和管理胰岛素替代治疗,并避免不良反应。本研究报告了基于临床方面的相关信息,对各种胰岛素类似物的 PK/PD 特征进行的比较分析。此外,研究将胰岛素类似物的治疗效果的主要关注点与其各自的起效时间和作用持续时间以及已报道的药物不良反应联系起来,探讨了改进的范围。

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