部分中文盐酸考来维仑处方资料（仅供参考） 美国Sankyo Pharma公司宣布Colesevelam（商品名WelChol）作为一种新的降低胆固醇的药物已在全美国投放市场，可供医师和病人选用。 WelChol不但可以单独使用降低LDL胆固醇，而且还是唯一的经FDA批准的可与他汀类药物联合使用的降脂药。对以胆固醇升高为主的高脂血症，当饮食和锻炼不能很好达到效果时，WelChol单独使用或与他汀类合用可有效的降低血浆胆固醇。 WelChol的一个优点是它与其他常用的降低胆固醇的药物不同，它不被吸收入血而散布全身。美国芝加哥临床研究中心主席Michael Davidson教授在评价这种新药时说：“对于血浆胆固醇较高而正在服用其他降脂药的病人来说，WelChol是他们的福音，因为它不被吸收的特性决定了它无全身副作用，这些副作用在其他降脂药中很常见。这使得已经服药很久的病人可以在加服WelChol的同时继续服用其他降脂药。” 此外，WelChol与其他药之间的交叉反应也很小。在药物交叉反应研究中，WelChol没有明显的影响地高辛、洛伐他汀、奎尼丁和华法令等药的吸收，而这些药却与其他降脂药之间却有显著的反应。尽管如此，病人还是应该在服用WelChol之前将他们正在服用的药物告诉他们的医生。 一项调查显示，尽管国家胆固醇教育计划（NCEP）中列出了降低胆固醇的指导方针，但仅有54％的患有高胆固醇血症的被调查者知晓他们的降脂目标。另一项称为血脂治疗评估计划（L-TAP）的研究指出，在患有高胆固醇血症的被调查者中，仅有38％接受降脂治疗的病人达到了NCEP要求的胆固醇降低的目标水平。为此，Sankyo Pharma的负责人William L. Bailey说：“L-TAP研究表明对于难以达到降脂目标水平的病人来说，的确需要在现有药物治疗之上找到更好的辅助药物。我们临床试验表明，在降低LDL-c方面WelChol是有效的和安全的。特别是当WelChol与他汀类药物（如洛伐他汀、辛伐他汀等）联合使用时，WelChol能够很好的达到降低胆固醇的作用，且这种效果是单用其中一种药物所达不到的。”美国贝勒医学院的Peter H. Jones教授指出：“WelChol与他汀类药物合用可显著改善病人的血脂水平，以达到NCEP的目标水平。此外如果病人不能耐受他汀类药物，单独使用WelChol也能有很不错的效果。 分类名称 一级分类：循环系统药物 二级分类：调整血脂及抗动脉粥样硬化药物 三级分类：胆汁酸结合树脂    药品英文名 Colesevelam   药品别名 Welchol   药物剂型 片剂：每片含本品625mg。   药理作用 本品是新型的降低胆固醇的药物，能与胆酸及其主要成分甘氨胆酸相结合，加速其排清，阻断其重吸收，造成胆酸耗竭，肝脏胆固醇7-α-羟化酶上调，从而增加胆固醇向胆酸的转化。 本品可以降低原发性高胆固醇血症(primary hypercholesterolemia)患者体内的低密度脂蛋白胆固醇(LDLcholesterol，LDL-ch)浓度。临床试验结果显示，本品可以有效降低LDL-ch及总胆固醇浓度。 本品是以其非吸收性聚合体技术(non-absorbed polymer technology)为基础开发的新药，具有亲水性，为不溶于水的聚合物，而且不被消化酶水解，不被人体吸收，仅是通过人体，而后被排泄。   药动学 本品与其他常用的降低胆固醇的药物不同，该药物不被吸收进入血液而散布全身，不会导致全身性副作用，药动学性质简单。   适应证 本品可以单独使用以降低低密度脂蛋白胆固醇水平，用作原发性高胆固醇血症病人饮食和运动的辅佐治疗；另外，该药物还是惟一经FDA批准的可与他汀类药物联合使用的降脂药。对以胆固醇升高为主的高脂血症，当饮食和锻炼不能很好达到效果时，本品单独使用或与他汀类合用可有效的降低血浆胆固醇浓度。   禁忌证 本品禁用于肠功能紊乱者，以及对药物中任一组分过敏者。   注意事项 当患者总胆固醇水平高于7.8mmol/L时，一般不使用本品，如需使用应谨慎。非临床安全性研究显示，大鼠给予本品人体用药剂量的30倍可因维生素K缺乏而引起出血。   不良反应 本品可引起头痛、疼痛和无力等中枢神经系统不良反应；耳鼻喉方面常见有咽炎、鼻炎、鼻窦炎等不良反应；胃肠方面可引起腹痛、便秘、腹泻、消化不良、胃肠胀气和恶心等不良反应；骨骼肌肉系统的不良反应有肌痛和背痛；呼吸系统有咳嗽；皮肤方面可引起损伤、感染及感染综合征等。 本品因不被吸收而无全身副作用，本品与其他药之间的交叉反应也很小。   用法用量 口服，推荐起始剂量为3片/次，2次/d，或6片/次，1次/d。根据需要剂量可调整为7片/d。和HMG-COA还原酶抑制剂合用时，以4～6片/次较为安全和合适。   药物相应作用 本品与其他药物同服时，未见本品对地高辛、洛伐他汀、美托洛尔、奎尼丁、丙戊酸和华法林生物利用度有明显影响。本品可使丙戊酸缓释剂(Calan SR)的Cmax和AUC分别降低31%和11%。尽管临床丙戊酸的生物利用度具有较大的可变性，但原因目前尚不清楚。 本品与阿托伐他汀、洛伐他汀或辛伐他汀同服不会影响他汀类药物的降脂作用。但尚未在其他药物中进行有关研究。当与可能干扰药物血浓度的其他药物同服时，药物的安全性和有效性可能受到影响，用药时应考虑进行药物浓度监测。本品在与其他药物联用时虽不易产生副作用，但患者还是应该在服用本品前告诉医生是否正在服用的其他药物。 如果患者不能耐受他汀类药物，单独使用本品也可以达到很好的效果。本品由于不被吸收，使用时的安全性将比目前被广泛使用的其他降血脂药物如他汀类药物显著增高。   专家点评 临床试验表明，在降低LDL胆固醇方面本品是有效的和安全的。特别是当本品与他汀类药物联合使用时，能够很好的达到降低胆固醇的作用。 临床研究显示，对于原发性高胆固醇血症患者，本品无论单用或与他汀类药物(如洛伐他汀、辛伐他汀等)合用均可降低其总胆固醇、LDL-ch和载脂蛋白B(Apo B)水平，同时升高HDL胆固醇水平，且这种效果是单用其中任一种药物所达不到的。约有1400例患者参与为期分别为4～50周的8项研究，其中除1项长程研究外，其余均为多中心随机双盲安慰剂对照研究。研究显示，本品用药后2周可达最大疗效，且这1疗效在整个长程研究中始终保持。 LDL-ch水平在3.38～5.72mmol/L(平均4.12mmol/L)的患者中进行的研究显示，在早餐和晚餐分别给予本品3.8g和4.5g，用药24周可使LDL-ch平均降低15%和18%；总胆固醇平均分别降低7%和10%；而Apo B两组均平均降低12%。本品2种剂量均使HDL胆固醇升高3%，两组甘油三酯轻度升高，与安慰剂组相比未见有统计学意义的明显差异。 98例LDL-ch在3.77～6.50mmol/L(平均4.39mmol/L)的患者中进行的研究显示，本品3.8g分别与早餐、晚餐同服或与早餐或晚餐分开服用，治疗6周后3种给药方案分别使平均LDL-ch降低18%，15%和18%，三组间无明显差异。本品与他汀类药物如阿托伐他汀(atorvastin)、洛伐他汀(lovastatin)或辛伐他汀(simvastatin)联合使用的3项临床研究显示，联合用药可使LDL-ch进一步降低。 Generic Name for WELCHOL Colesevelam HCl 625mg; tabs. Legal Classification: Rx Pharmacological Class for WELCHOL Bile acid sequestrant. Manufacturer of WELCHOL Daiichi Sankyo Indications for WELCHOL Adjunct to diet and exercise: to reduce elevated LDL-C in adults with primary hypercholesterolemia (Type IIa), alone or with a statin, when response to nondrug therapy is inadequate; to reduce LDL-C in boys and postmenarchal girls 10–17yrs of age with heterozygous familial hypercholesterolemia, alone or with a statin after failing an adequate trial of diet therapy. Adults and Children: <10yrs: not recommended. Take with a meal and liquid. ≥10yrs: Susp: one 1.875g pkt twice daily or one 3.75g pkt once daily. Empty contents into a glass or cup, add 4–8oz of water, stir and drink. Do not take susp in its dry form. >17yrs: 3 tabs twice daily or 6 tabs once daily. With a statin: may be dosed at the same time or dosed apart. Also: WELCHOL FOR ORAL SUSPENSION Contraindications for WELCHOL Bowel obstruction. Serum TG>500mg/dL. History of hypertriglyceridemia-induced pancreatitis. Precautions for WELCHOL TG levels >300mg/dL. Monitor lipids, TG, and non-HDL-C levels prior to therapy and periodically thereafter. Susceptibility to Vit. A, D, E, or K deficiencies. GI motility disorders (eg, dysphagia). Pregnancy (Cat.B). Nursing mothers. Interactions for WELCHOL Monitor drugs with a narrow therapeutic index, glyburide, levothyroxine, oral contraceptives containing ethinyl estradiol and norethindrone, phenytoin, warfarin; give at least 4 hours prior to colesevelam. Adverse Reactions for WELCHOL Constipation, dyspepsia, nausea. How is WELCHOL supplied? Tabs—180 Susp 1.875g—60 (single-dose pkt) 3.75g—30 (single-dose pkt) WelCholGeneric name: ColesevelamBrand names: WelChol Why is WelChol prescribed? WelChol is used to lower blood cholesterol levels when diet and exercise prove insufficient. It works by binding with cholesterol-based bile acids to take them out of circulation. This prompts the liver to produce a replacement supply of bile acids, drawing the extra cholesterol it needs out of the bloodstream. Most important fact about WelChol WelChol is usually added to a treatment regimen only when other measures have failed to produce adequate results. Often, diet and exercise are enough to bring cholesterol levels under control. Likewise, it's sometimes sufficient to simply treat an underlying problem such as diabetes, underactive thyroid, kidney disease, a liver disorder, or alcoholism. Whatever your other treatment measures may be, it's important to remember that WelChol is intended to supplement them, rather than replace them outright. To get the full benefit of the medication, you need to stick to the diet, exercise program, and other treatments your doctor prescribes. All these efforts to keep your cholesterol levels normal are important because together they may lower your risk of heart disease. How should you take WelChol? WelChol should be taken at mealtime with a liquid. If you miss a dose...Take it as soon as you remember. If it is almost time for your next dose, skip the one you missed and go back to your regular schedule. Never take 2 doses at the same time. Storage instructions...Store at room temperature and protect from moisture. What side effects may occur? WelChol is not absorbed by the body, so it is relatively free of side effects. If any develop or change in intensity, inform your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking WelChol. Side effects may include:Constipation, indigestion, muscle aches, sore throat, weakness Why should WelChol not be prescribed? You should not take WelChol if you have a bowel obstruction or the product gives you an allergic reaction. Special warnings about WelChol If you have difficulty swallowing or suffer from severe digestive problems, use WelChol with caution; it hasn't been tested under these conditions. The drug has also not been studied in children. Possible food and drug interactions when taking WelChol If WelChol is taken with certain other drugs, the effects of either could be increased, decreased, or altered. Always check with your doctor before combining WelChol with other medication, especially verapamil. Special information if you are pregnant or breastfeeding There is no evidence that WelChol causes harm during pregnancy. Nevertheless, be sure to let the doctor know if you are pregnant, plan to become pregnant, or are breastfeeding. There is a possibility that WelChol could interfere with the absorption of needed vitamins. Recommended dosage for WelChol ADULTS The usual dosage is 6 tablets a day, taken as a single dose or divided into 2 doses. If you're taking WelChol with one of the cholesterol-lowering statin drugs, the maximum recommended daily dosage is 6 tablets. If you're taking WelChol alone, the maximum is 7. 附件： 2010112917273121.pdf --------------------------------------------------- 原产地英文商品名: WELCHOL TABLET 625mg/tab 180tabs/bottle 原产地英文药品名: COLESEVELAM HCL 原产地英文化合物名称: 1-Hexanaminium, N,N,N-trimethyl-6-(2-propenylamino)-, chloride, polymer with (chloromethyl)oxirane, 2-propen-1-amine and N-2-propenyl-1-decanamine, hydrochloride 中文参考商品译名: WELCHOL片剂 625毫克/片 180片/瓶 中文参考药品译名: 盐酸考来维仑 生产厂家中文参考译名: 第一三共 生产厂家英文名: DAIICHI SANKYO