部份中文艾塞那肽处方资料（仅供参考）
商品名：Bydureon Subcutaneous Injection Pen
英文名：Exenatide
中文名：艾塞那肽缓释剂型注射笔
生产商：阿斯利康
药品简介
近日，Bydureon Pen（exenatide，艾塞那肽长效缓释注射悬液，2mg）获美欧及日本批准，作为一种辅助药物，结合饮食和运动，用于改善2型糖尿病成人患者的血糖控制。
ビデュリオン皮下注用2mgペン
药用类别名称
GLP-1受体激动剂2型糖尿病治疗剂
批准日期：2015年5月
欧文商標名
Bydureon Subcutaneous Injection Pen
一般名：エキセナチド（JAN）
Exenatide
分子式：C184H282N50O60S
分子量：4186.57
構造式：
性　状：
本产品为白色粉末。易溶于水, 几乎不溶于甲醇, 几乎不溶于乙醇(99.5)。它是吸湿的。
操作注意事项
1. 避免冷冻, 并将光屏蔽保持在2至8°c 冷藏。
2. 如果无法在室温下存储, 请将光屏蔽存放在30°c或更低的温度下, 并在4周内使用。不要储存在超过 30°c, 因为可能会发生针堵塞。
批准条件
制定药品风险管理计划并加以实施。
药用药理学
1. 作用机制
Exenatide是一种活性成分的制剂是一种化学合成的肽, 具有与蜥蜴相同的39个氨基酸序列, 即衍生的Exendin-4 (Exendin-4), 由于n-终末序列不同于人GLP-1, 表明二肽肽-4 是一种内源性肽降解酶对降解的抗性, 其作用持续存在。该制剂, 异丙酯可生物降解D, l-乳酸-乙酰苷共聚物(50:50), 通过嵌入微粒子(PLGA), 每周一次皮下给药, Exenatide是一种持续释放制剂, 旨在显示与每天两次皮下注射制剂相同的效果 (Baietta皮下说明)。
GLP-1 受体激动剂作用
Exenatide与GLP-1受体以及体外内源性GLP-1试验结合, 表明GLP-1激动剂活性可增加细胞内 cAMP。
2. 血糖升高的抑制作用
(1) 降血糖作用
在对日本2型糖尿病患者进行的为期10周的测试中, 0.8注)和2.0mg的制剂每周重复皮下注射一次。HbA1c从给药开始(基线)到10周给药(平均±standard差)的变化量, 在安慰剂组中-0.4±0.3%, 0.8毫克注释) 在Group-1.0±0.7%, 在此代理2.0mg组为-1.5±0.7%。空腹血糖水平变化量(平均±标准差) 在安慰剂组中的血糖水平变化量(平均±标准差)-20.5±20.4 mg/dl, 剂0.8mg注释) 在组-25.2±10.9MG/DL 中, 在该代理2.0mg 组-50.8±27.8 Mg dl 中。作为膳食负荷测试的结果, 安慰剂组进食后血糖水平变化2小时 (平均±障标准差)-8.8±26.9mg/dL, 本剂 0.8mg 注释) 组-50.0±41.1 mg/dL, 本剂2.0MG组-50.0±276.8mgn/DL。
在使用糖尿病模型ZDF大鼠 (Zucker 糖尿病脂肪 (Zdf)/gm-(fabe)) 进行的一次皮下给药试验中, 该制剂在一个月后空腹血糖水平和 HbA1c, 与溶剂对照组相比有显著改善, 行为被确认为持续存在。
(2) 葡萄糖依赖性降血糖活性
在使用糖尿病疾病模型MICE(DB/DB 和 OB/OB)进行体内试验时, Exenatide表现出低血糖作用, 与血糖浓度给药前后的变化量相关。
(3) 葡萄糖反应胰岛素分泌作用
在体外胰岛素分泌试验中, 使用大鼠胰岛细胞, 外显素在低血糖水平上没有显示出效果, 它是在高血糖水平观察到的强化胰岛素分泌。此外, 在使用糖尿病模型大鼠的体内重复给药试验中, 与对照组相比, 异种细胞重量与喂养量相等, 胰腺β细胞重量无明显变化, 显著提高了胰岛素敏感性, 胰腺β细胞重量和胰岛素敏感性 (胰岛素敏感性矫正胰腺β细胞量) 的产物显著增加。进一步在体内重复给药试验使用糖尿病模型大鼠, exenatide 相比, 溶剂对照组, 它是显著增加血浆C肽。同样, 在使用ZDF大鼠对现有制剂进行的单剂量试验中, 即使在给药一个月后, 胰岛素敏感性的改善和血浆C肽也有增加。
(4) 胰高血糖素分泌物的抑制作用
在大鼠体内高血糖夹检中, 与溶剂对照组相比, Exenatide显著抑制了胰高血糖素分泌。
(5) 胃内容物的延迟作用
在大鼠体内胃含量放电试验中, 异种显示了剂量依赖性胃含量放电延迟效应。
3. 作药作用
在体内反复给药试验中, 用大鼠, 外显素抑制喂养量, 与溶剂给药组相比, 体重明显下降。在使用ZDF大鼠的单剂量试验中, 即使是剂量依赖性喂养量也会降低, 10天给药后体重下降得到证实。
4. 改善胰岛素抵抗的效果
在体内正常血糖高胰岛素夹具试验后, 反复给大鼠服用外显素, 与溶剂对照组相比, 异丙基葡萄糖注射率/血浆胰岛素浓度比显著增加, 显示胰岛素抵抗改善效果。类似的效果, 在使用ZDF大鼠对现有制剂进行的单剂量试验中, 即使经过一个月的给药, 也得到了证实。
注) 此制剂的批准使用和剂量, 如Exenatide, 每周在皮下注射一次2mg。(请参阅 "剂量" 一节)
适应症
2型糖尿病
然而, 磺酰脲剂除了饮食和运动疗法, 大苯胺为基础的剂和噻唑烷基剂(包括每一种药物单独治疗或联合治疗)只有在治疗中无法获得足够的效果。
用法与用量
通常情况下, 成人, 作为外显子, 每周一次2毫克, 皮下注射。
包装
注射剂
皮下注射注2毫克笔: 1套件
[笔: 1瓶, 针: 1]
制造和销售元 (进口)
AstraZeneca Company
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：
https://www.info.pmda.go.jp/go/pack/2499411G4025_1_05/
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Important Safety Information for BYDUREON® (exenatide extended-release for injectable suspension)
•POSSIBLE THYROID TUMORS, INCLUDING CANCER: 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 use BYDUREON if you or any of your family members have MTC or if you have Multiple Endocrine Neoplasia syndrome type 2. While using BYDUREON, tell your healthcare provider if you get a lump or swelling in your neck, hoarseness, trouble swallowing, or shortness of breath. These may be symptoms of thyroid cancer.
•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. Symptoms of a severe allergic reaction to BYDUREON are severe rash or itching, swelling of your face, lips, and throat that may cause difficulty breathing or swallowing, feeling faint or dizzy, and very rapid heartbeat. If you have any symptoms of a severe allergic reaction, stop using BYDUREON and call your healthcare provider right away.
•Inflammation of the pancreas (pancreatitis) may happen, which may be severe and lead to death. Before using 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 using 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, occurs with or without vomiting, or is felt going from your stomach area through to your back. These may be symptoms of pancreatitis.
•Your risk for getting low blood sugar (hypoglycemia) is higher if you use 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. Signs and symptoms of low blood sugar may include shakiness, headache, drowsiness, weakness, dizziness, confusion, irritability, hunger, fast heartbeat, sweating, and feeling jittery.
•Tell your healthcare provider if you have or had kidney problems or a kidney transplant. 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. Call your healthcare provider right away if you have nausea, vomiting, or diarrhea that will not go away or if you cannot drink liquids.
•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.
•Serious injection-site reactions, with or without bumps (nodules), have happened in some people who use BYDUREON. Some of these injection-site reactions have required surgical intervention. Call your healthcare provider right away if you have severe pain, swelling, blisters, an open wound, or a dark scab at your injection site.
•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.
•Before using BYDUREON, tell your doctor about all the medicines you use, as using them with BYDUREON may affect how each medicine works. Tell your healthcare provider if you use other diabetes medicines, especially insulin or a sulfonylurea, 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.
Approved Uses
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 a substitute for insulin and has not been studied in combination with insulin. BYDUREON is not for people with type 1 diabetes or people with diabetic ketoacidosis (a condition caused by very high blood sugar). 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.