---------------------------------------------------------------
 详细处方信息以本药内容附件PDF文件（20123518093123.pdf）的“原文Priscribing Information”为准
---------------------------------------------------------------
部分中文艾塞那肽处方资料（仅供参考）

欧洲批准Bydureon(exenatide缓释剂)用于糖尿病
    礼来公司、Amylin公司与Alkermes公司表示欧盟正式批准了2mg规格的 Bydureon（exenatide，艾塞那肽缓释注射混悬剂）与一定的口服药物联用于治疗2型糖尿病。该药设计为提高机体胰岛素的产生，Bydureon每周使用一次。
    Bydureon的作用包括轻到中度的恶心、呕吐、腹泻、便秘。Bydureon在美国还未获得批准，公司计划将于2011年末向美国FDA递交相关补充资料。Bydureon每周一次分别与二甲双胍、一种磺酰脲类、一种噻唑烷二酮药联用，或是与二甲双胍+一种磺酰脲类或二甲双胍+一种噻唑烷二酮药联用。

分类名称
一级分类：内分泌系统药物 二级分类：糖尿病及胰岛疾病用药物 
 
药品英文名
Exenatide
 
药物剂型
注射剂：250mg/ml，1.2ml/支(每个单剂量5mg，共60个单剂量)；250mg/ml，2.4ml/支(每个单剂量10mg，共60个单剂量)。
 
药理作用
肠降血糖素(incretin mimetics)从消化道进入血液循环后，能像胰高血糖素样肽1(GLP-1)一样促进胰岛素分泌而显示抗高血糖作用。本品为肠降血糖素类似物，其氨基酸序列与GLP-1部分重叠，能与GLP-1受体结合并使之活化，通过环磷酸腺苷或其他信号转导途径促进胰岛β细胞分泌胰岛素，降低2型糖尿病患者的空腹血糖和餐后血糖。本品可以模拟体内自然分泌的激素，从而帮助人体调节血糖水平，而且在患者不需要的时候，就会停止该作用。本品不但能够降低血糖，而且还能加强正在丧失功能的细胞机能。
 
药动学
2型糖尿病患者皮下注射本品10mg后，2.1h血浆药物浓度达峰值，平均血浆峰浓度(Cmax)为211pg/ml，药时曲线下面积(AUC)为1036pg/ml。在5～10mg剂量范围内，AUC与给药剂量成正比。表观分布容积(Vd)为28.3L。本品经肾小球滤过而消除，清除率(CL)为9.1L/h，消除半衰期(t1/2β)为2.4h。肾功能不全患者药物清除率降低，而肝功能不全对本品代谢无影响。
 
适应证
本品作为辅助治疗手段，用于β细胞机能尚好，暂不需要注射胰岛素，而二甲双胍或磺酰脲类药物无法充分控制的2型糖尿病患者。
 
禁忌证
1．对本品过敏者禁用。2．严重肾功能不全患者(肌酐清除率＜(30ml/min)不推荐使用。3．本品可引起恶心、呕吐等胃肠道不良反应，故不推荐用于严重胃肠道疾病患者。
 
注意事项
1．本品生殖毒性分级为C，孕妇使用本品应权衡利弊。尚不知本品是否经乳汁分泌，哺乳期妇女慎用。2．儿童用药疗效及安全性尚未评价。3．老年人用药不需调整剂量。4．本品过量可引起严重的恶心、呕吐及血糖迅速降低，一旦出现药物过量，应根据临床表现采取适当的支持治疗，必要时补充葡萄糖。5．2～8℃避光保存，避免冷冻。
 
不良反应
不良反应可见低血糖、恶心、呕吐、腹泻、紧张不安、头晕、头痛、消化不良、虚弱、食欲减退、食管反流性疾病、多汗等。
 
用法用量
皮下注射，起始剂量为每次5mg，每日2次，分别于早餐和晚餐前1h使用。一个月后，根据临床疗效，剂量可增加到每次10mg，每日2次。
 
药物相应作用
1．本品与地高辛或洛伐他汀合用，地高辛及洛伐他汀的Cmax略有降低，达峰时间(Tmax)轻度延迟。2．本品与赖诺普利合用，赖诺普利的Cmax和AUC不变，而Tmax延迟。3．本品能延缓胃排空时间，使口服药物的吸收速度和吸收程度降低，如果与口服避孕药和抗生素合用，应在本品注射前至少1h服用口服避孕药和抗生素。
 
Indication
BYDUREON is an injectable prescription medicine that may improve blood sugar (glucose) in adults with type 2 diabetes mellitus, and should be used along with diet and exercise. BYDUREON is not recommended as the first medication to treat diabetes.

BYDUREON is a long-acting form of the medication in BYETTA® (exenatide) injection so both drugs should not be used together. BYDUREON is not insulin and should not be taken instead of insulin. BYDUREON is not for people with type 1 diabetes or people with diabetic ketoacidosis. BYDUREON is not recommended for use in children. It is not known if BYDUREON is safe and effective in people with a history of pancreatitis or severe kidney problems.

Important Safety Information
•In animal studies, BYDUREON caused rats to develop tumors of the thyroid gland. Some of these tumors were cancer. It is not known if BYDUREON causes thyroid tumors or a type of thyroid cancer called medullary thyroid cancer (MTC) in people. Do not take BYDUREON if you or any of your family members have MTC or if you have Multiple Endocrine Neoplasia syndrome type 2. While taking BYDUREON, tell your doctor if you get a lump or swelling in your neck, hoarseness, trouble swallowing, or shortness of breath. These may be symptoms of thyroid cancer.
•Inflammation of the pancreas (pancreatitis) may happen, which may be severe and lead to death. Before taking BYDUREON, tell your healthcare provider if you have had pancreatitis, stones in your gallbladder (gallstones), a history of alcoholism, or high blood triglyceride levels. Stop taking BYDUREON and call your healthcare provider right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may happen with or without vomiting and may be felt going from your abdomen through to your back; this may be a symptom of pancreatitis.
•Your risk for getting low blood sugar is higher if you take BYDUREON with another medicine that can cause low blood sugar, such as a sulfonylurea. The dose of your sulfonylurea may need to be lowered while you use BYDUREON.
•BYDUREON may cause nausea, vomiting, or diarrhea, leading to loss of fluids (dehydration). Dehydration may cause kidney failure; this can happen in people who have never had kidney problems before. Tell your healthcare provider if you have or had kidney problems or a kidney transplant. Call your healthcare provider right away if you have nausea, vomiting, or diarrhea that will not go away or if you cannot drink liquids.
•Before you use BYDUREON, tell your healthcare provider if you have severe problems with your stomach, such as delayed emptying of your stomach (gastroparesis) or problems with digesting food.
•Do not use BYDUREON if you have had an allergic reaction to exenatide or any of the other ingredients in BYDUREON. Severe allergic reactions can happen with BYDUREON. Stop taking BYDUREON and get medical help right away.
•BYDUREON may affect the way some medicines work and some medicines may affect the way BYDUREON works. Tell your healthcare provider about the medicines you take, especially if you take any medicine by mouth or warfarin sodium (Coumadin® or Jantoven®).
•Tell your healthcare provider if you are pregnant or plan to become pregnant. It is not known if BYDUREON will harm your unborn baby. Talk to your healthcare provider first if you are breastfeeding or plan to breastfeed.
•The most common side effects with BYDUREON include nausea, diarrhea, headache, vomiting, constipation, itching at injection site, a small bump (nodule) at the injection site, and indigestion. Nausea most commonly happens when first starting BYDUREON, but may become less over time.

---------------------------------------------------------------
 详细处方信息以本药内容附件PDF文件（20123518093123.pdf）的“原文Priscribing Information”为准
---------------------------------------------------------------