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当前位置:药品说明书与价格首页 >> 糖尿病 >> Ⅱ型糖尿病 >> 药物临床研究及应用 >> Cycloset(溴隐亭bromocriptine)速释片剂

Cycloset(溴隐亭bromocriptine)速释片剂

2009-09-17 14:12:00  作者:新特药房  来源:新特药网  浏览次数:24  文字大小:【】【】【
简介: 导读:溴隐亭速释片:不增加心血管危险糖尿病新药,近日美国FDA批准溴隐亭速释片用于治疗II型糖尿病,研究证实溴隐亭速释片单一治疗或辅助磺酰脲、二甲双胍加磺酰脲治疗,均可改善对广大糖尿病患者的血 ...

 导读:溴隐亭速释片:不增加心血管危险糖尿病新药,近日美国FDA批准溴隐亭速释片用于治疗II型糖尿病,研究证实溴隐亭速释片单一治疗或辅助磺酰脲、二甲双胍加磺酰脲治疗,均可改善对广大糖尿病患者的血糖控制,且不增加心血管疾病危险,为糖尿病患者提供了一条崭新的治疗途径。

美国FDA批准VeroScience公司与S2治疗公司合作开发的溴隐亭速释片(bromocriptine,Cycloset)治疗2型糖尿病,这是此类药物获准上市的第一个。溴隐亭速释片单一治疗或辅助磺酰脲、二甲双胍加磺酰脲治疗,均可改善对广大糖尿病患者的血糖控制。

临床前研究表明,增加多巴胺活性可改善糖尿病症状,白日增加多巴胺能活性也是重要的。对糖尿病动物研究显示,在白日特定的时间增加多巴胺能活性在生理学上是改善糖尿病代谢障碍最有效“重新设定”生物时钟神经化学。溴隐亭速释片一日1次早上用药,口服后不久可产生单一简短脉冲式多巴胺激动活性。溴隐亭上午改善膳食后的血糖而不增加血浆胰岛素浓度,在药物已基本从血液循环中清除后的许多小时还显示对2型糖尿病餐后(如午餐和晚餐)血糖控制的有效作用。

溴隐亭速释片代表了治疗2型糖尿病的新途径。对糖尿病患者来说是首个靶向人体多巴胺(神经系统内神经元或神经细胞的化学递质)活性的药物。多巴胺激动剂溴隐亭增加多巴胺活性。然而,溴隐亭速释片在人体内改善血糖控制的特异机制尚未清晰,溴隐亭治疗糖尿病的研发是基于临床前研究显示在代谢疾病状态时大脑多巴胺活性低,在2型糖尿病患者体内发现这些因素主要是诸如胰岛素抵抗性(人体丧失胰岛素降血糖作用的能力)等多种代谢功能障碍。而且,临床前以多巴胺激动剂溴隐亭治疗糖尿病动物显示,溴隐亭速释片作用于中枢神经系统启动重新设定和改善对外周代谢的控制。

溴隐亭速释片是美国FDA颁布“糖尿病治疗药需研究结果显示不增加心血管疾病危险”新准则后首个获准上市的药品。溴隐亭速释片纳入3000例患者的52周双盲安全性研究显示,其与安慰剂相比不加重下述心血管疾病:心肌梗塞、休克、因不稳定心绞痛住院、充血性心力衰竭和再次血管手术。

对新诊断的2型糖尿病或不能以目前已上市药物控制血糖的患者,溴隐亭速释片提供了治疗糖尿病的一条崭新途径。此外,2型糖尿病是心血管疾病高危人群,故溴隐亭速释片显示不增加诸如心脏病发作等心血管疾病危险的特点尤为引人注目。溴隐亭速释片纳入3000例患者为期一年的安全性研究显示,治疗2型糖尿病每日剂量高达4.8mg的安全性与安慰剂相媲美。

CYCLOSET

Indication(s):

Adjunct to diet and exercise, to improve glycemic control in type 2 diabetes.

Pharmacology:

Bromocriptine is a dopamine receptor agonist that acts on the central nervous system (CNS). Although the exact mechanism of action by which bromocriptine improves glycemic control is not known, it is likely mediated by its ability to increase dopaminergic activity in the CNS. Cycloset improves glycemic control in patients with type 2 diabetes without increasing plasma insulin concentrations.

Clinical Trials:

Four double-blind, placebo-controlled clinical studies were conducted to assess the safety and efficacy of Cycloset in the management of type 2 diabetes.

In a 24-week monotherapy trial, 159 type 2 diabetes patients with inadequate glycemic control (HbA1c 7.5–11%) were randomized to receive Cycloset or placebo. Cycloset improved HbA1c (adj. mean change from baseline: –0.1% for Cycloset vs. 0.3% for placebo) and fasting plasma glucose (adj. mean change from baseline: 0mg/dL for Cycloset vs. 23mg/dL for placebo) compared to placebo.

In two pooled 24-week trials, 494 type 2 diabetes patients with inadequate glycemic control (HbA1c 7.8–12.5%) on stable sulfonylurea therapy were randomized to an add-on therapy with either Cycloset or placebo. Cycloset improved HbA1c (adj mean change from baseline: Study K: –0.1% for Cycloset vs. 0.4% for placebo; Study L: –0.4% for Cycloset vs. 0.3% for placebo) and fasting blood glucose concentrations (adj. mean change from baseline: Study K: 10mg/dL for Cycloset vs. 28mg/dL for placebo; Study L: 3mg/dL for Cycloset vs. 23mg/dL for placebo) compared to placebo.

Lastly, a 52-week safety trial involving 3070 patients compared Cycloset and placebo as add-on therapy to 1–2 oral anti-diabetic medications, including a subgroup being treated with metformin + sulfonylurea only. Patients receiving Cycloset, compared to placebo, experienced a significant improvement in HbA1c when used as adjunctive therapy to 1–2 oral antidiabetic medications (adj. mean change from baseline: –0.4% for Cycloset vs. 0% for placebo), including the subgroup of patients treated only with background metformin + sulfonylurea (adj. mean change from baseline: –0.5% for Cycloset vs. 0% for placebo).

Legal Classification:

Rx

Adults:

Take with food in the AM, within 2 hours of waking. Usual range: 1.6–4.8mg/day. Initially 0.8mg once daily; may increase by 0.8mg per week as tolerated until max 4.8mg/day.

Children:

Not recommended.

Contraindication(s):

Syncopal migraines. Nursing mothers. Other ergot-related drugs.

Warnings/Precautions:

Not for treating type 1 diabetes or ketoacidosis. Monitor orthostatic vital signs initially and periodically during therapy. Severe psychotic disorders: not recommended. Renal or hepatic disease. Pregnancy (Cat.B).

Interaction(s):

Concomitant selective 5-HT1B agonists (eg, sumatriptan), sympathomimetic drugs >10 days, ergot-related drugs within 6 hours, other dopamine agonists and antagonists, including neuroleptics (eg, clozapine, olanzapine, ziprasidone) and metoclopramide: not recommended. Potentiates antihypertensives. May potentiate highly protein bound drugs (eg, salicylates, sulfonamides, chloramphenicol, probenecid). May potentiate or be potentiated by strong CYP3A4 inducers, inhibitors, or substrates (eg, azole antimycotics, HIV protease inhibitors).

Adverse Reaction(s):

GI upset, fatigue, dizziness, headache, hypotension, syncope somnolence, hypoglycemia.

How Supplied:

Tabs—200, 600

Manufacturer:

Santarus, Inc.

Pharmacological Class:

Dopamine agonist (ergot deriv).

Active Ingredient(s):

Bromocriptine (as mesylate) 0.8mg; tabs.

Cycloset(溴隐亭bromocriptine)速释片剂咨询

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