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艾塞那肽缓释长效缓释剂(EXENATIDE,Bydureon)

2012-02-29 16:37:00  作者:新特药房  来源:中国新特药网天津分站  浏览次数:1399  文字大小:【】【】【
简介:艾塞那肽的长效缓释剂型-Bydureon已经获得美国FDA的批准用于临床 BYDUREON制造商:Amylin和Alkermes公司 类药物:降糖药(胰高血糖素样肽-1 [GLP-1受体激动剂)。 活性成分(S):艾塞那肽缓释2毫克; PWD为SC ...

——长效缓释剂型艾塞那肽-Bydureon已经获得美国FDA的批准用于临床

商品名:BYDUREON,英文通用名:EXENATIDE,中文通用名:艾塞那肽,规格2mg,为长效注射剂,2012年1月27日获得FDA批准上市。本品用于改善2型糖尿病患者的血糖控制,适用于单用二甲双胍、磺酰脲类,以及二甲双胍合用磺酰脲类,血糖仍控制不佳的患者。

制造商:
Amylin和Alkermes公司

类药物:
降糖药(胰高血糖素样肽-1 [GLP-1受体激动剂)。

活性成分(S):
艾塞那肽缓释2毫克; PWD为SC注射后重建。

指示(S):
作为辅助饮食和运动,以改善2型糖尿病患者的血糖控制。不适用于第一线治疗不佳的饮食和运动控制的患者。

药理作用:
bydureon艾塞那肽,的GLP-1受体激动剂的缓释配方。艾塞那肽已被证明人类的GLP-1受体在体外结合并激活。这将导致两个葡萄糖依赖的胰岛素合成和体内胰岛β细胞胰岛素分泌增加,涉及环磷酸腺苷和/或其他细胞内的信号转导通路的机制。艾塞那肽也温和派胰高血糖素的分泌和降低胰高血糖素浓度高血糖期间,延缓胃排空,减少食物的摄入。

临床试验:
24周,随机,开放标签试验进行了比较Bydureon的安全性和有效性,在患者与2型糖尿病与饮食和运动,或口服降糖药治疗血糖控制不佳,包括二甲双胍,磺脲类Byetta的,使用Thiazolidinediones类,或结合这些疗法。

共有252例患者进行了研究。与饮食和运动(19%),单一口服降糖剂(47%),或结合治疗口服降糖药(35%)患者接受治疗。平均基线糖化血红蛋白为8.4%。患者被随机分配接受一次七天(每周)或Byetta的(10mcg每日两次),除了现有的口服抗糖尿病药物Bydureon 2毫克。两次分配5mcg Byetta的发起治疗的患者每天再增加剂量10mcg 4周后,每日两次。

主要终点是从基线到24周(或提前终止时的最后一个值)的糖化血红蛋白的变化。 24周的治疗后,患者服用Bydureon经历了1.6个百分点,从基线糖化血红蛋白统计学优越减少,比服用Byetta的病人减少了0.9个百分点。两个治疗组达到统计学显着的减肥,研究结束的2.3千克Byetta的病人(减肥是次要终点)的Bydureon患者和1.4千克平均损失。

法律分类:
RX

成人:
由SC注射给在腹部,大腿或上臂。混合后立即注入。 2毫克每7天一次(每周一次)。 Byetta的变化:停止,然后开始Bydureon。

儿童:
不推荐使用。

禁忌症(S):
甲状腺髓样癌的历史(个人或家庭)。多发性内分泌腺瘤病辨证分型2。

警告/注意事项:
不代替胰岛素。不用于治疗1型糖尿病或糖尿病酮症酸中毒。甲状腺C细胞肿瘤可能的风险。胰腺炎史;考虑其他降糖药。监测胰腺炎;如果怀疑,立即停止;如果得到证实,不重新启动。严重胃肠道疾病,肾功能​​不全(肌酐清除率<30ml/min者),终末期肾脏疾病:不建议。肾移植。怀孕(Cat.C)。哺乳的母亲。

互动(补):
胰岛素并发:不推荐。伴磺脲类,胰岛素或其他胰岛素促泌剂(如meglitinides)低血糖的风险增加;这些考虑减少剂量。口服药物可延缓吸收。监测华法林。

不良反应(S):
胃肠不适,便秘,头痛,注射部位反应可能形成抗体(血糖反应可能会减弱),胰腺炎(可能是致命的),过敏反应。


如何提供:
每个单剂量托盘-4(包含1瓶,1稀释剂的预充式注射器,小瓶连接器和针头)

欧盟已经批准 Bydureon® 每周注射一次的疗法上市,该药将在欧盟国家逐一推出。
Bydureon® 是2型糖尿病治疗中首个也是唯一的每周注射一次疗法,在欧盟获批也是世界首次

重要性:胰高糖素样肽1受体激动剂 Bydureon® 是2型糖尿病治疗中首个也是唯一的每周注射一次疗法,在欧盟获批也是世界首次,只需要每周一次注射就可以很好地控制血糖。

适应症:欧盟批准 Bydureon 与二甲双胍、磺脲类药物和噻唑烷二酮等单药或多药联合使用治疗2型糖尿病。

每周1次Bydureon获准用于2型糖尿病患者

2012年1月27日Amylin 制药 宣布美国食品药品管理局(FDA)已批准Bydureon(艾塞那肽缓释注射用混悬液)用于治疗成人2型糖尿病。Bydureon是一种胰高糖素样肽-1受体激动剂,可在饮食控制和运动的基础上改善这一人群的血糖控制情况。

Bydureon的获准是基于一项临床试验项目的安全性和有效性数据。这项试验的结果显示,每周1次Bydureon治疗可改善血糖控制情况。FDA做出批准Bydureon的决定,还参考了每日注射2次百泌达(艾塞那肽)的临床经验。

在一项“头对头”临床研究中,患者接受了Bydureon或百泌达治疗,两组患者最常报告的不良事件均为恶心,但Bydureon组少于百泌达组(14% vs. 35%)。Bydureon组的其他常见治疗相关不良事件包括腹泻、上呼吸道感染和注射部位结节。未发生主要低血糖事件。

动物研究显示,注射Bydureon的大鼠发生了甲状腺肿瘤,其中部分为恶性。尚不清楚人类使用Bydureon是否也可导致甲状腺肿瘤或甲状腺髓样癌(MTC)。对有MTC或2型多发性内分泌肿瘤综合征个人史或家族史的患者,应避免使用Bydureon。

如果同时使用磺酰脲类药物和Bydureon,应减少磺酰脲类药物的剂量。不得对有严重肾脏问题的患者使用Bydureon。

Bydureon采用单剂注射器包装,由患者自行皮下注射,每周注射1次。在临床研究中,患者和医生均愿意使用这种给药系统。

Manufacturer:
Amylin and Alkermes

Pharmacological Class:
Antidiabetic (glucagon-like peptide-1 [GLP-1] receptor agonist).

Active Ingredient(s):
Exenatide extended-release 2mg; pwd for SC inj after reconstitution.

Indication(s):
As adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes. Not for first-line therapy in patients inadequately controlled on diet and exercise.

Pharmacology:
Bydureon is an extended-release formulation of exenatide, a GLP-1 receptor agonist. Exenatide has been shown to bind and activate the human GLP-1 receptor in vitro. This leads to an increase in both glucose-dependent synthesis of insulin and in vivo secretion of insulin from pancreatic beta cells, by mechanisms involving cyclic AMP and/or other intracellular signaling pathways. Exenatide also moderates glucagon secretion and lowers glucagon concentrations during periods of hyperglycemia, slows gastric emptying, and decreases food intake.

Clinical Trials:
A 24-week, randomized, open-label trial was conducted to compare the safety and efficacy of Bydureon to Byetta in patients with type 2 diabetes and inadequate glycemic control with diet and exercise alone or with oral antidiabetic therapy, including metformin, a sulfonylurea, a thiazolidinedione, or combination of two of those therapies.

A total of 252 patients were studied. Patients were treated with diet and exercise alone (19%), a single oral antidiabetic agent (47%), or combination therapy of oral antidiabetic agents (35%). The mean baseline HbA1c was 8.4%. Patients were randomly assigned to receive Bydureon 2mg once every seven days (weekly) or Byetta (10mcg twice-daily), in addition to existing oral anti-diabetic agents. Patients assigned to Byetta initiated treatment with 5mcg twice-daily then increased the dose to 10mcg twice-daily after 4 weeks.

The primary endpoint was change in HbA1c from baseline to Week 24 (or the last value at time of early discontinuation). After 24 weeks of treatment, patients taking Bydureon experienced a statistically superior reduction in HbA1c of 1.6 percentage points from baseline, compared to a reduction of 0.9 percentage points for patients taking Byetta. Both treatment groups achieved statistically significant weight loss by the end of the study, with an average loss of 2.3kg for Bydureon patients and 1.4kg for Byetta patients (weight loss was a secondary endpoint).

Legal Classification:
Rx

Adults:
Give by SC inj in abdomen, thigh, or upper arm. Inject immediately after mixing. 2mg once every 7 days (weekly). Changing from Byetta: discontinue, then start Bydureon.

Children:
Not recommended.

Contraindication(s):
History (personal or family) of medullary thyroid carcinoma. Multiple endocrine neoplasia syndrome type 2.

Warnings/Precautions:
Not a substitute for insulin. Not for treating type 1 diabetes or diabetic ketoacidosis. Risk of thyroid C-cell tumors possible. History of pancreatitis; consider other antidiabetics. Monitor for pancreatitis; if suspected, promptly discontinue; if confirmed, do not restart. Severe GI disorders, renal impairment (CrCl <30mL/min), end-stage renal disease: not recommended. Renal transplantation. Pregnancy (Cat.C). Nursing mothers.

Interaction(s):
Concurrent insulin: not recommended. Increased risk of hypoglycemia with concomitant sulfonylurea, insulin, or other insulin secretagogues (eg, meglitinides); consider reducing dose of these. May delay absorption of oral drugs. Monitor warfarin.

Adverse Reaction(s):
GI upset, constipation, headache, inj site reactions; possible antibody formation (glycemic response may be attenuated), pancreatitis (may be fatal), hypersensitivity reactions.

How Supplied:
Single-dose trays—4 (each contains 1 vial, 1 prefilled syringe with diluent, vial connector and needles)


Last Updated:
2/24/2012

责任编辑:admin


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