Information on Glufast

Glufast is a drug for the treatment of type 2 diabetes .Glufast is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.
Glufast belongs to the meglitinide class of blood glucose-lowering drugs. It is approved for use in Japan but has not yet gained FDA approval.

Additional information about Glufast
Glufast Indication: For the treatment of type 2 diabetes.
Mechanism Of Action: Glufast is a novel antidiabetic agent for the treatment of type-2 diabetes mellitus. Its chemical structure is similar to that of sulphonylureas. Glufast exerts a hypoglycaemic effect with rapid onset and short duration of action, by transiently increasing insulin secretion. Glufast is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels (Kir6.2/SUR1 complex, KATP channels) in pancreatic beta-cells. Glufast may also activate ryanodine receptors.

New Product GLUFAST for the Treatment of Type II Diabetes
Glufast, which is close to market is an insulin secretagogue with a rapid onset and short duration of action, lowers post-meal glucose levels by improving the body's own ability to produce insulin. 
Mr. Mutsuo Kanzawa, President and Chief Executive Officer of Kissei Pharmaceutical, stated, "We are very pleased to have signed the Glufast agreement with Elixir Pharmaceuticals. Since its launch in Japan in May 2004, Glufast has steadily increased its domestic market share and attained an important position in the treatment regimen for patients with type II diabetes. In addition to Japan, the product is currently in development in China, South Korea and the Middle East as part of Kissei's program to address patient markets worldwide."

Type II diabetes is a serious and debilitating disease, affecting 14 million patients in the United States alone. While there has been significant progress in the treatment of type II diabetes, there is still an enormous unmet medical need worldwide.
Mr. Heiden added, "We believe that Glufast represents an important advance for physicians and their patients who are seeking optimal glucose control. The launch of Glufast in the United States will be carried out by an Elixir specialty sales force with a focus on metabolic disease, specifically targeting diabetologists and endocrinologists.

Glufast, an insulin secretagogue with a rapid onset and short duration of action, lowers post-meal glucose levels by improving the body's own ability to produce insulin. Clinical data have shown that reducing post-meal glucosesurges with Glufast decreases HbA1c levels (a standard means of assessing chronic elevated blood glucose levels). Epidemiological studies have demonstrated that uncontrolled surges in post-meal glucose levels are directly associated with negative long-term health outcomes in diabetics.
Glufast is a member of the meglitinide class of compounds; two currently marketed products in this class are expected to generate over $300 million in sales in the U.S. in 2006.

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详细处方信息以本药内容附件PDF文件（2009122809271014.pdf）的“原文Priscribing Information”为准
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                          部分中文 Glufast 处方信息（仅供参考）
通用名：米格列奈钙片
本品主要由米格列奈钙组成，其化学名：双〔（2s）-2-苄基-3- (顺-六氢异吲哚-2-羰基)丙酸〕单钙二水合物。
适应症：本品可以单独用于经饮食和运动疗法不能有效控制高血糖的Ⅱ型糖尿病病人。
国外研究：
该化合物由日本橘生药品工业株式会社合成，2002年12月申请用于Ⅱ型糖尿病患者控制餐后血糖，2004年4月在日本上市。橘生制药在2003年3月已将该药授权给南韩的Choongwae公司、法国的Servier公司和日本的武田公司，分别处于临床前、Ⅲ期临床和注册阶段。同时，其在美国、加拿大、墨西哥以及授权法国Servier公司在欧洲、非洲和其他一些地区进行的该药Ⅲ期实验也已全面展开。
米格列奈钙的优点：
米格列奈是继瑞格列奈、那格列奈后第三个美格列脲类药物，是苯丙氨酸的衍生物。据文献报道，米格列奈与瑞格列奈、那格列柰以及传统磺酰脲类药物相比，具有以下优势：
⑴ 作用机制新颖，起效更快，作用持续时间更短
本品通过关闭胰腺β细胞膜上的ATP依赖性K通道，造成Ca内流，使细胞内Ca浓度增加而使细胞外含胰岛素的囊泡脱粒，从而刺激胰岛素的分泌。但是，米格列奈只是在进餐时才会迅速而短暂的刺激胰腺分泌胰岛素，起效快，作用持续时间短；而传统的的口服糖尿病药则持续刺激胰岛素分泌，且刺激过度，特别是在两餐之间，常使患者感到饥饿，用磺酰脲类药物时甚至要鼓励患者在两餐之间服用点心，使过多的胰岛素有所代谢。这种额外的进食使患者的体重增加；而他们在开始时就常常是肥胖者。米格列奈不同于传统的磺酰脲类药物之处在于该药给药后起效迅速而作用时间短，抑制Ⅱ型糖尿病特征性的餐后高血糖，避免了低血糖反应的发生。
⑵ 疗效更强
米格列奈体内体外都可以刺激双相胰岛素分泌，而且效果逆转迅速。最近研究人员利用轻度、中度和重度链脲素诱导的大鼠模型比较了米格列奈、那格列奈和伏格列波糖对降低餐后血糖的效果。在餐前向试验动物给药米格列奈（0.1和3mg/kg）、那格列奈（25、50和100mg/kg）或伏格列波糖（0.03、0.1和0.3mg/kg）。结果证明米格列奈的降糖效果最显著。在轻度和中度动物模型中，米格列奈显著而且迅速降低了血糖水平和血糖AUC。在严重糖尿病模型中，也观察到了米格列奈抑制进食诱导的血糖水平升高的趋势。该试验表明米格列奈可以预防2型糖尿病出现的餐后高血糖。利用糖尿病狗模型比较了米格列奈和格列齐特的降糖效果和促胰岛素分泌作用。结果米格列奈降低血糖的效力较格列齐特更强，而且不象后者那样容易产生低血糖。同时米格列条显示了迅速的促胰岛素分泌作用。
⑶ 给药灵活
每次于餐前服药，少进一餐则少服一剂，多加一餐则多服一剂，这种灵活的给药方式对于经常出差、旅游、赴宴等生活饮食不规律的患者来讲不必严格遵守就餐之间，十分方便。国外对2500多例患者使用后的跟踪调查表明，患者对米格列奈给药的灵活性非常满意，有77％的患者感到能推迟或少吃一餐正是减轻了负担，95％以上的患者选择要继续服用此类降糖药。
⑷ 有“体外胰腺”之美称
米格列奈作用主要集中于降低餐后高血糖，血糖可促进米格列奈刺激胰岛素释放，在有葡萄糖存在时，米格列奈促进胰岛素分泌量比无葡萄糖时约增加 50％，故其作用就象是一个“体外胰腺”，只是在需要时提供胰岛素。
⑸ 早期及轻度糖尿病患者的一线治疗药物
对于单纯依靠限制饮食或运动不能控制血糖水平的轻度患者，往往需要辅助用其他抗糖尿病药，而一旦用药，极易诱发低血糖，因米格列奈具有以上特点，作为一线治疗药物是最佳选择，对此类患者可作为常备降糖药。对于单纯依靠限制饮食或者运动来控制血糖水平的患者，面对各种美味的诱惑，经常因害怕血糖升高而不敢进食或过度节食，对身体造成不同程度的危害。对此类患者，可适时服用米格列奈避免上述情况发生。
⑹ 安全性高，耐受性好
米格列奈与磺酰脲类药物的对比研究表明，服用米格列奈低血糖的发生率约比后者低50％，发生低血糖的时间也不同。米格列奈发生低血糖主要在白天，而格列本脲则多在午夜以后，夜间发生低血糖症特别危险，因病人对它的发生不能及时察觉。长期使用米格列奈也不会产生因药物蓄积而致的药源性低血糖。米格列奈的不良反应发生率与空白一致，因不良反应中断治疗者仅0.3％。因此，米格列奈的耐受性好，患者的依从性高。

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详细处方信息以本药内容附件PDF文件（2009122809271014.pdf）的“原文Priscribing Information”为准
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