药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201181501352938.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文Entocort EC处方资料(仅供参考)
FDA批准Entocort EC治疗Crohn病 阿斯特拉捷利康公司(AstraZeneca)2001年10月3日宣布,该公司成分为布地奈德的Entocort EC胶囊获得了FDA的批准。所批准的适应证为累及回肠和升结肠的轻到中度活动性Crohn病。 Crohn病是一种慢性炎症性疾病,病变主要累及肠,目前还不清楚此病的确切病因。主要的症状包括腹泻、腹部绞痛、发热和直肠出血等。治疗此病一般会耗费包括诊疗、检查和药物等大量的医疗资源,而且,目前临床上很难控制这种疾病。 布地奈德是一种合成的皮质激素,主要起糖皮质激素的作用,也有微弱的盐皮质激素作用。Entocort EC是一种新型的局部起效的布地奈德制剂,它可以明显缓解多数患者通常难以治疗的症状。由于Crohn病是一种急需新治疗药物的疾病,FDA对此药的批准可以被认为是Crohn病治疗方面的一个重要进展。Entocort EC不仅具有很好的疗效,而且也能很好地被患者耐受,所以此药是治疗Crohn病时一种不错的选择。 约1000名患者参与了评价Entocort EC的5项临床试验,他们均为轻到中度的回肠和升结肠活动性Crohn病患者。在这些试验中,48~69%的用Entocort EC 9mg每日一次治疗的患者在用药8周后病情缓解。试验规定“病情缓解”的标准为CDAI(Corhn病活动指标)评分低于或等于150。而这些患者治疗前的CDAI评分在272~290之间。 Entocort EC的另一个优势在于其有效成分在肠内释放,而此部位正是Crohn病主要累及的部位。此药在肠内迅速而充分的代谢,因此防止了大量药物被吸收入血。 Entocort EC最常见的不良反应是头痛、呼吸道感染、恶心和肾上腺功能亢进样症状。与Crohn病的系统治疗用糖皮质激素氢化泼尼松相比,在相当剂量下,此药较少引起糖皮质激素通常引起的不良反应。 Entocort EC不宜用于对布地耐德过于敏感的患者。另外,糖皮质激素能减弱下丘脑—垂体—肾上腺轴的应激能力,所以使用Entocort EC的患者在手术等应激情况发生前应系统性地补充糖皮质激素。接受系统性糖皮质激素治疗的患者改用Entocort EC治疗时,需监测肾上腺皮质功能。使用皮质激素的患者还应注意预防水痘、麻疹等感染性疾病。
英文药名: Entocort (Budesonide Capsules)
中文药名: 布地奈德胶囊
药品简介 轻-中度远端结肠炎的治疗:病变累及结肠远端30~40cm称远端溃疡性结肠炎,也称直乙状结肠炎。多有血性大便,轻中度患者一般无全身症状或轻微。 对表现为直肠炎或远端结肠炎的患者来说,采用口服或局部作用的治疗方式一般均可奏效,其治疗方案在一定程度上取决于患者本身的选择(如是否愿意经口服药,是否能适应局部给药,或经济承受力如何等)。 布地奈德(Budesonide,商品名为Entocort,即盐酸丁地松灌肠剂)保留灌肠。具有极高的首过效应,因此几乎无全身作用。当应用2mg剂量时,可相当于20~30mg泼尼松(或100mg氢化可的松)的作用。反复多个疗程使用布地奈德灌肠剂治疗后并不具有抑制机体下丘脑-垂体-肾上腺轴的不良作用。因此,长期使用布地奈德具有较好的安全性。其标准剂量为9mg,加大至15mg并不增加疗效,且有抑制肾上腺皮质的作用,出现晨间血浆皮质醇浓度减低。18mg的剂量不良反应增多,但仍低于全身用药。
生产厂家 AstraZeneca
药理作用 布地奈德是一具有高效局部抗炎作用的糖皮质激素。它能增强内皮细胞、平滑肌细胞和溶酶体膜的稳定性,抑制免疫反应和降低抗体合成,从而使组胺等过敏活性介质的释放减少和活性降低,并能减轻抗原抗体结合时激发的酶促过程,抑制支气管收缩物质的合成和释放而减轻平滑肌的收缩反应。急性、亚急性和长期毒性研究发现,布地奈德的全身作用,如体重下降、淋巴组织及肾上腺皮质萎缩,比其他糖皮质激素弱或者与其他糖皮质激素相当。经过六个不同的试验测试系统评价,布地奈德无致突变作用,亦无致癌作用。
药动学 吸入给药后,约10%~15%在肺部吸收,吸入单剂布地奈德1mg,约10分钟后达最大血药浓度2nmol/L。经气雾剂吸入布地奈德的全身生物利用度约为26%,其中2/5来自经口吞咽的部分。分布容积(Vd)约3L/kg,平均血浆蛋白结合率为85%~90%。本品主要经肝首过代谢(约90%),代谢物的糖皮质激素活性较低。主要代谢物6β-羟布地奈德和16α-羟泼尼松龙的活性不到布地奈德的1%。布地奈德的代谢物以其原形或结合的形式经肾排泄。尿中检测不到原型布地奈德。
What is Entocort EC? Entocort EC is used to treat mild to moderate Crohn's disease involving the ileum and/or the ascending colon. Entocort EC is a nonsystemic corticosteroid that is released into the intestine and works to reduce inflammation. Because 90% of the drug is released in the intestine and not into the bloodstream, it causes fewer side effects than other corticosteroids (i.e., prednisone).
How is Entocort EC taken? Entocort EC is normally taken in capsue form in the morning with or without food. Entocort EC should be swallowed whole and should never be crushed, chewed or broken in half.
Why is Entocort EC prescribed? Even though Entocort EC belongs to the class of drugs known as corticosteroids, it may be more efffective and have fewer side effects than other medications in this category.
What do I do if I miss a dose? If you miss a dose, take it as soon as you remember. If your next dose should be taken soon, just take that dose. Don't double up, or take more than one dose at a time.
Who should not take Entocort EC? Tell your doctor if you have ever had any of the following conditions: •Any condition that supresses the immune system •Cataracts •Diabetes (or a family history) •Glaucoma (or a family history) •High blood pressure •Liver disease •Osteoporosis •Tuberculosis •Ulcers
What are the side effects? Common side effects of Entocort EC include headache, respiratory infection, and nausea.
Are there any sexual side effects? Entocort EC is not known to cause any sexual side effects in either men or women.
What medications can Entocort EC interact with? Ketoconazole can intefere with the way the liver processes Entocort EC.
Are there any food interactions? Grapefruit or grapefruit juice can interact with Entocort EC and cause more of it to be released into the bloodstream.
Is Entocort EC safe during pregnancy? The FDA has classified Entocort EC as a type C drug. The effect that Entocort EC has on an unborn child has not been studied extensively. Entocort EC should only be used during pregnancy if clearly needed. Notify the prescribing doctor if you become pregnant while taking Entocort EC. Entocort EC does pass into breast milk and can affect a nursing infant.
How long is it safe to use Entocort EC? Entocort EC has been approved for use for up to 8 weeks.
Is there anything else I should know about Entocort EC? People taking Entocort EC should avoid exposure to anyone who has chickenpox or the measles or who has been vaccinated with a live virus. Entocort may also suppress the response of the hypothalamus-pituitary-adrenal (HPA), and therapy may be necessary before surgery (including dental surgery) or other stressful events.
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201181501352938.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- |