McKeage K, Goa K L
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2001;61(11):1599-624. doi: 10.2165/00003495-200161110-00007.
Insulin glargine is a recombinant human insulin analogue produced by DNA technology using a nonpathogenic strain of Escherichia coli. Two modifications of human insulin result in a stable molecule which is soluble in slightly acidic conditions (pH 4.0) and precipitates in the neutral pH of subcutaneous tissue. Because of these properties, absorption of insulin glargine is delayed and the analogue provides a fairly constant, basal insulin supply without peaks in plasma insulin levels for approximately 24 hours, similar to that achieved by a continuous subcutaneous insulin infusion. Insulin glargine is indicated as a once daily subcutaneous injection to provide basal glycaemic control in adults and children aged >6 years with type 1 diabetes mellitus and in adults with type 2 diabetes mellitus. Fasting plasma glucose and fasting blood glucose levels generally improved to a greater extent in patients with type 1 diabetes mellitus receiving insulin glargine than patients who administered Neutral Protamine Hagedorn (NPH) insulin. In patients with type 1 or 2 disease, glycosylated haemoglobin levels were slightly reduced and to a similar extent with insulin glargine and NPH insulin. Most clinical trials in patients with type 1 or 2 diabetes mellitus demonstrated a lower incidence of hypoglycaemia, especially nocturnal hypoglycaemia, compared with NPH insulin. One of the most common adverse events with insulin glargine treatment was injection site pain which, in some studies, occurred more frequently than in patients receiving NPH insulin. In all cases the symptoms were mild and treatment discontinuation was not required. Otherwise, the drug is well tolerated and does not appear to be immunogenic.
Insulin glargine once a day provides basal control of glycaemia for approximately 24 hours without inducing peaks in plasma insulin levels in patients with type 1 or 2 diabetes mellitus. In long term, well designed trials insulin glargine once daily improved glycaemic control at least as effectively as NPH insulin given once or twice daily. The drug was well tolerated and in most studies the incidence of nocturnal hypoglycaemia was significantly less in patients treated with insulin glargine compared with patients receiving NPH insulin. Therefore, insulin glargine is likely to be a useful addition to the armamentarium of insulin therapy by establishing basal glycaemic control with once daily administration and a reduced risk of nocturnal hypoglycaemia.
甘精胰岛素是一种通过DNA技术利用非致病性大肠杆菌菌株生产的重组人胰岛素类似物。对人胰岛素进行的两项修饰产生了一种稳定的分子，该分子在微酸性条件（pH 4.0）下可溶，在皮下组织的中性pH值下会沉淀。由于这些特性，甘精胰岛素的吸收延迟，该类似物可提供相当恒定的基础胰岛素供应，在大约24小时内血浆胰岛素水平无峰值，类似于持续皮下胰岛素输注所达到的效果。甘精胰岛素适用于1型糖尿病的成人和6岁以上儿童以及2型糖尿病的成人，每日一次皮下注射以提供基础血糖控制。与使用中性鱼精蛋白锌胰岛素（NPH）的患者相比，接受甘精胰岛素治疗的1型糖尿病患者的空腹血糖和空腹血糖水平通常改善程度更大。在1型或2型糖尿病患者中，糖化血红蛋白水平略有降低，甘精胰岛素和NPH胰岛素降低的程度相似。与NPH胰岛素相比，大多数针对1型或2型糖尿病患者的临床试验显示低血糖发生率较低，尤其是夜间低血糖。甘精胰岛素治疗最常见的不良事件之一是注射部位疼痛，在一些研究中，其发生率高于接受NPH胰岛素的患者。在所有情况下，症状均较轻，无需停药。否则，该药物耐受性良好，似乎无免疫原性。
对于1型或2型糖尿病患者，甘精胰岛素每日一次可提供约24小时的基础血糖控制，且不会引起血浆胰岛素水平峰值。在长期、精心设计的试验中，甘精胰岛素每日一次改善血糖控制的效果至少与每日一次或两次给予NPH胰岛素的效果相同。该药物耐受性良好，在大多数研究中，与接受NPH胰岛素的患者相比，接受甘精胰岛素治疗的患者夜间低血糖发生率显著更低。因此，通过每日一次给药建立基础血糖控制并降低夜间低血糖风险，甘精胰岛素可能是胰岛素治疗药物库中的一个有用补充。
