Setter S M, Corbett C F, Campbell R K, White J R
College of Pharmacy, Washington State University, Spokane 99201-3899, USA.
Ann Pharmacother. 2000 Dec;34(12):1423-31. doi: 10.1345/aph.19414.
To examine the pharmacology, therapeutics, pharmacokinetics, dosing guidelines, adverse effects, and drug interactions of insulin aspart, and summarize the clinical trials of efficacy and safety in patients with type or type 2 diabetes mellitus.
A MEDLINE database search (1985-May 2000) was performed to identify all applicable published articles and abstracts; in some cases, Novo Nordisk unpublished information was also obtained. Review articles on insulin analogs were also identified, as well as review chapters in medical textbooks.
The majority of the studies identified were in abstract form. These studies reported information on the pharmacokinetics of insulin aspart in healthy volunteers and in those with diabetes, as well as the therapeutic utility, safety, and clinical efficacy in patients with diabetes. A limited number of randomized studies were reported as artices in the medical literature
All published clinical studies were reviewed.
Insulin aspart, the second Food and Drug Administration-approved rapid-acting insulin analog, is produced by recombinant technology that replaces the proline at position 28 on the B chain of insulin with negatively charged aspartic acid. Insulin aspart exists as hexamers that rapidly dissociate into monomers and dimers on subcutaneous injection. When administered immediately prior to a meal, insulin aspart is at least as effective as regular human insulin in control of postprandial blood glucose concentrations. Insulin aspart achieves higher peak insulin concentrations in less time and with a shorter duration of action than regular human insulin.
Insulin aspart is a convenient premeal insulin for use by patients requiring mealtime insulin. Furthermore, due to favorable pharmacokinetics, insulin aspart controls postprandial blood glucose concentrations at least as well as regular human insulin and contributes to improved quality of life.
研究门冬胰岛素的药理学、治疗学、药代动力学、给药指南、不良反应及药物相互作用，并总结其在1型或2型糖尿病患者中疗效和安全性的临床试验。
检索MEDLINE数据库（1985年至2000年5月）以识别所有适用的已发表文章和摘要；在某些情况下，还获取了诺和诺德公司未发表的信息。还识别了关于胰岛素类似物的综述文章以及医学教科书中的综述章节。
所识别的大多数研究为摘要形式。这些研究报告了门冬胰岛素在健康志愿者和糖尿病患者中的药代动力学信息，以及糖尿病患者的治疗效用、安全性和临床疗效。医学文献中作为文章报道的随机研究数量有限。
对所有已发表的临床研究进行了综述。
门冬胰岛素是第二种获美国食品药品管理局批准的速效胰岛素类似物，通过重组技术生产，该技术将胰岛素B链第28位的脯氨酸替换为带负电荷的天冬氨酸。门冬胰岛素以六聚体形式存在，皮下注射后迅速解离为单体和二聚体。在餐前立即给药时，门冬胰岛素在控制餐后血糖浓度方面至少与常规人胰岛素一样有效。与常规人胰岛素相比，门冬胰岛素能在更短时间内达到更高的胰岛素峰值浓度，且作用持续时间更短。
门冬胰岛素是需要餐时胰岛素的患者方便使用的餐前胰岛素。此外，由于其良好的药代动力学特性，门冬胰岛素在控制餐后血糖浓度方面至少与常规人胰岛素一样好，并有助于改善生活质量。
