当前位置：药品说明书与价格首页 >> 糖尿病 >> Ⅱ型糖尿病 >> 药品目录 >> 溴隐亭速释片剂Cycloset（bromocriptine）

溴隐亭速释片剂Cycloset（bromocriptine）

2011-03-29 23:31:45 作者：新特药房来源：中国新特药网天津分站浏览次数：282 文字大小：【大】【中】【小】

简介： CYCLOSET 制造商： Santarus公司药理分类：多巴胺受体激动剂（麦角deriv）。活性成分（补）：溴隐亭（如甲磺酸）0.8mg;标签。指示（补）：配合饮食和锻炼，以改善2型糖尿病患者的血糖控制。药理 ...

CYCLOSET

制造商：
Santarus公司

药理分类：
多巴胺受体激动剂（麦角deriv）。

活性成分（补）：
溴隐亭（如甲磺酸）0.8mg;标签。

指示（补）：
配合饮食和锻炼，以改善2型糖尿病患者的血糖控制。

药理作用：
溴隐亭是一种多巴胺受体激动剂，对中枢神经系统（CNS）的行为。尽管所采取的行动的溴隐亭改善血糖控制不知道确切的机制，它可能是由它的能力，增加在中枢神经系统多巴胺介导的活动。 Cycloset提高了在不增加血浆胰岛素浓度与2型糖尿病患者的血糖控制。

临床试验：
四双盲，安慰剂对照临床研究进行了评估2型糖尿病的安全性和Cycloset疗效。

在24周的单一疗法试验中，159型不足的血糖控制（糖化血红蛋白7.5-11％）2型糖尿病患者随机接受Cycloset或安慰剂。 Cycloset改善糖化血红蛋白（形容词从基线的平均变化：-0.1％，服用安慰剂的对比为Cycloset 0.3％）和空腹血糖（形容词意味着从基线的变化：0mg/dL为Cycloset主场迎战23mg/dL的安慰剂）相比，安慰剂。

在两池24周的试验，494型血糖控制不够稳定磺脲类治疗（糖化血红蛋白7.8-12.5％）2型糖尿病患者被随机分配到一个附加的任何Cycloset或安慰剂治疗。 Cycloset改善糖化血红蛋白（形容词从基线的平均变化：研究K表：-0.1％的Cycloset对比安慰剂0.4％;研究李：对Cycloset对比安慰剂0.3％-0.4％）和空腹血糖浓度（形容词平均变化从基线：研究K教授：10mg/dL为Cycloset对比服用安慰剂的患者28mg/dL，研究李：对安慰剂3mg/dL为Cycloset主场迎战23mg/dL）相比，安慰剂。

最后，52周的安全试验，涉及3070和安慰剂的患者相比Cycloset作为附加的治疗，以1-2口服抗糖尿病药物，包括一个小组正在与二甲双胍+磺脲类药物治疗只。患者接受Cycloset，与安慰剂相比，经验丰富的糖化血红蛋白显着改善时，作为辅助治疗，以口服降糖药物使用1-2（形容词意味着从基线的变化：-0.4％比0的Cycloset为安慰剂％），包括分组治疗的患者只有背景二甲双胍+磺脲类（形容词从基线的平均变化：-0.5％，服用安慰剂的Cycloset主场迎战0％）。

法律分类：
接收

成人：
采取在上午的食物，醒后2小时。正常范围：1.6-4.8mg/day。最初0.8mg，每日一次，可能会增加为每周0.8mg，直至最大4.8mg/day不能容忍的。

儿童：
不推荐。

禁忌（补）：
晕厥偏头痛。哺乳的母亲。麦角其他相关药物。

警告/注意事项：
不适用于治疗1型糖尿病或酮症酸中毒。最初，并定期监测体位性治疗期间生命体征。严重的精神障碍：不推荐。肾或肝脏疾病。妊娠（Cat.B）。

互动（补）：
伴随选择性5 - HT1B受体激动剂（如舒马），拟交感神经药“10天，6小时内麦角有关的药品，其他多巴胺受体激动剂和拮抗剂，包括抗精神病药（如氯氮平，奥氮平，齐拉西酮）和胃复安：不推荐。 Potentiates抗高血压药。会增强高度蛋白结合药物（如水杨酸盐，磺胺类，氯霉素，丙磺舒）。会增强或受到强烈的CYP3A4的诱导剂，抑制剂或底物（如氮唑antimycotics，HIV蛋白酶抑制剂）增大。

不良反应（补）：
胃肠不适，乏力，头晕，头痛，低血压，晕厥嗜睡，低血糖。

如何提供：
制表- 200，600

Manufacturer:

Santarus, Inc.

Pharmacological Class:

Dopamine agonist (ergot deriv).

Active Ingredient(s):

Bromocriptine (as mesylate) 0.8mg; tabs.

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:

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-HT_1B 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).