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Expert Opin Pharmacother. 2010 Feb;11(2):269-79. doi: 10.1517/14656560903501544.
There is a large unmet need for new therapies to treat type 2 diabetes (T2DM) which reduce fasting and postprandial glucose without increasing insulin levels and which are not associated with weight gain or hypoglycemia. The quick-release formulation of bromocriptine (bromocriptine-QR; Cycloset) represents such a therapy.
Bromocriptine-QR's proposed mechanism of action, unique formulation and clinical efficacy and safety will be discussed. A Medline search was conducted using the terms: bromocriptine quick-release, circadian rhythms, treatment type 2 diabetes, insulin resistance, beta-cell dysfunction (years 1985 - 2009).
The reader will gain an understanding of the importance of the brain as a target for the treatment of type 2 diabetes. In addition the safety, efficacy and indication for use of a first-in-class dopamine agonist as a treatment option for type 2 diabetes are discussed.
Bromocriptine-QR is indicated to be used alone or in conjunction with all available treatments for type 2 diabetes. Although the mechanism of action is not fully understood, bromocriptine-QR's action points to a central target in the brain (hypothalamus) which may explain the observed peripheral improvements in metabolic parameters.
有一个巨大的未满足的需求,为治疗 2 型糖尿病(T2DM)的新疗法,降低空腹和餐后血糖,而不增加胰岛素水平,并且不与体重增加或低血糖有关。溴隐亭(溴隐亭-QR;Cycloset)的速释制剂代表了这样一种治疗方法。
溴隐亭-QR 的拟议作用机制、独特的配方和临床疗效和安全性将进行讨论。使用术语进行了 Medline 搜索:溴隐亭快速释放、昼夜节律、治疗 2 型糖尿病、胰岛素抵抗、β细胞功能障碍(1985 年-2009 年)。
读者将了解大脑作为治疗 2 型糖尿病的靶点的重要性。此外,还讨论了作为 2 型糖尿病治疗选择的一种首创多巴胺激动剂的安全性、疗效和使用适应症。
溴隐亭-QR 被指示单独使用或与所有可用的 2 型糖尿病治疗方法联合使用。虽然作用机制尚未完全了解,但溴隐亭-QR 的作用指向大脑(下丘脑)中的一个中枢靶点,这可能解释了观察到的代谢参数的外周改善。