盐酸考来维仑是三共公司开发的一个非吸收性聚合物类降脂药物，它可与肠道中的胆酸结合并显著减少后者的再吸收。由于胆酸的耗竭会提高胆固醇转化为胆酸的平衡，故能用来降低胆固醇浓度。盐酸考来维仑的这种作用机制与考来烯胺（cholestyramine／Questran等）和考来替泊（ colestipol/Colestid）等已有药物相似，但因其对胆酸的结合亲和力更强，所以可以更低剂量使用，胃肠道副反应减少，药物相互作用潜力亦更低。 盐酸考来维仑被批准用作饮食和运动疗法的辅助疗法，单用或再并用一种他汀类药物降低原发性高血胆固醇症患者的高水平低密度脂蛋白胆固醇（LDL－C）。在临床研究中，盐酸考来维仑显现可以降低LDL－C浓度15％～18％，提高高密度脂蛋白胆固醇（HDL－C）浓度3％。受试患者的甘油三酯浓度稍有上升，然与安慰剂治疗者相比没有统计学显著差异性。盐酸考来维仑尚未与考来烯胺和考来替泊进行对照研究，但其对脂质构成作用的类型和程度似仍和此两药相似。 胆酸螫合剂、包括盐酸考来维仑对脂质浓度的作用强度均不如他汀类药物，故单用此类药物治疗高血胆固醇症患者大多会逐渐转向单用他汀类药物或再并用一种他汀类药物。在并用阿伐他汀、洛伐他汀或辛伐他汀的临床研究中，盐酸考来维仑显现可使患者的LDL－C浓度较单用他汀类药物再额外最高降低16％。这些研究发现,阿伐他汀80mg／天剂量与阿伐他汀10mg／天加盐酸考来维仑3.8g／天两方案所致患者LDL－C浓度降低值在统计学显著范围内没有差异。研究还发现，阿伐他汀和辛伐他汀即使在它们剂量低至10mg／天时亦能显著降低甘油三酯。但若并用盐酸考来维仑，则阿伐他汀的这一作用几乎完全抵消，然辛伐他汀降低甘油三酯的效应却仅受到很小影响。盐酸考来维仑并用辛找他汀似更有益。 盐酸考来维仑的最常见副反应包括肠胃气胀（12％）、便秘（11％）、消化不良（8％）、感染（l％）和头痛（6％）等，其中胃肠道副应、尤是便秘发生率明显小于考来烯胺和考来替泊、上述三个胆酸鳌合剂的胃肠道副反应都大于他汀类药物，然因它们不被吸收，故系统副反应发生率却小于他汀类药物。盐酸考来维仑禁忌用于肠梗阻患者并应谨慎给药于吞咽困难、吞烟机能障碍、严重胃肠道功能障碍或已施行主要胃肠道手术者。 考来烯胺和考来替泊会减少脂溶性维生素A、D．E、K的吸收，但盐酸考来维仑却无此不良作用。考来烯胺和考来替泊因也能与其它药物结合，故它们通常宜于使用其它药物前1小时或4小时后给药。然盐酸考来维仑却在药物相互作用研究中显现，其并不明显影响地高辛、洛伐他汀、美托洛尔（meto-prolol／LOpressor）、奎尼T、丙戌酸（valproicacid／DePakene等）或华法林的生物利用度。盐酸考来维仑似亦不会降低缓释维拉帕米（veraPamil／Calan SR）的血药峰值和生物利用度，尽管后者的个体生物利用度变化很大。 盐酸考来维仑为片剂，每片含药625mg。盐酸考来维仑的推荐初始剂量每天2次、每次3片或每天1次6片。盐酸考来维仑的最大治疗效应约出现于开始给药的2周时，其最大治疗剂量推荐为每天7片。盐酸考来维仑与他汀类药物合用时可以同服，且其推荐剂量方案不变。 圣路易斯(MD Consult)——2009年10月7日，日本第一制药三共公司宣布，美国食品药物管理局(FDA)已批准增加降胆固醇药考来维仑(Welchol)的一个新适应证。这项新批准令使得考来维仑可作为10~17岁、患杂合子家族性高胆固醇血症(heFH)男孩及月经初潮后女孩饮食和运动疗法外的辅助治疗药，以降低其升高的低密度脂蛋白胆固醇(LDL-C)水平。可在这类患者对充分的饮食疗法试验无效后单独应用考来维仑，亦可联用一种他汀类药物。 FDA同时还批准了考来维仑口服混悬液，这使得现有片剂有了替代剂型。口服混悬液可作为成人2型糖尿病患者饮食和运动疗法外的辅助治疗药以改善血糖控制，还可作为成人原发性高脂血症患者饮食和运动疗法外的辅助治疗药以降低其升高的LDL-C水平，以上两种情况均可单独应用考来维仑口服混悬液或联用羟甲基戊二酰辅酶A还原酶抑制剂(他汀类药物)。口服混悬液亦适用于10~17岁、患heFH男孩及月经初潮后女孩饮食控制和运动疗法外的辅助治疗，以降低其升高的LDL-C水平，在认为其对饮食疗法无效后应用，既可单独用药，亦可与他汀类药物联合应用。考来维仑口服混悬液的推荐剂量为1日1包(规格：3.75 g/包)。 批准考来维仑用于治疗儿科heFH患者是基于一项历时8周、多中心、随机、安慰剂对照临床研究的数据。该研究旨在评价考来维仑单药(1.875 g/d 或3.75 g/d，片剂)或与他汀类药物联用的疗效。研究所纳入的男孩及月经初潮后女孩的年龄介于10~17岁，他们先前未接受过治疗或一直接受稳定剂量的他汀类药物治疗。 Brand names: WelChol™ Colesevelam Hydrochloride Oral tablet What is this medicine? COLESEVELAM (koh le SEV e lam) is used to lower cholesterol in patients who are at risk of heart disease or stroke. This medicine is only for patients whose cholesterol level is not controlled by diet. It is also used in combination with diet and exercise to help lower blood sugar in adults with type 2 diabetes.   This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions. What should I tell my health care provider before I take this medicine? They need to know if you have any of these conditions: •constipation or bowel obstruction •high triglyceride levels •history of pancreatitis caused by high triglyceride levels •an unusual or allergic reaction to colesevelam, other medicines, foods, dyes, or preservatives •pregnant or trying to get pregnant •breast-feeding How should I use this medicine? Take this medicine by mouth with at least 4 ounces (half a glass) of water. Follow the directions on the prescription label. Take with food. Take your medicine at regular intervals. Do not take it more often than directed. Do not stop taking except on your doctor's advice.   Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. Because of the tablet size, it is recommended that children use the oral suspension.   Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once. NOTE: This medicine is only for you. Do not share this medicine with others. What may interact with this medicine? •birth control pills •cyclosporine •insulin •medicines for diabetes like glimepiride, glipizide, and glyburide •medicines for seizures like carbamazepine, phenobarbital, phenytoin •thyroid hormones •verapamil •vitamins •warfarin   This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine. What should I watch for while using this medicine? Visit your doctor or health care professional for regular checks on your progress. Your blood sugar and other tests will be measured regularly. This medicine is only part of a total cholesterol or blood sugar-lowering program. Your health care professional or dietician can suggest a low-cholesterol and low-fat diet that will reduce your risk of getting heart and blood vessel disease. Avoid alcohol and smoking, and keep a proper exercise schedule. To reduce the chance of getting constipated, drink plenty of water and increase the amount of fiber in your diet. Ask your doctor or health care professional for advice if you are constipated. If you are taking this medicine for diabetes, wear a medical ID bracelet or chain, and carry a card that describes your disease and details of your medicine and dosage times. What side effects may I notice from receiving this medicine? Side effects that you should report to your doctor or health care professional as soon as possible: •allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue •bloody or black, tarry stools •breathing problems •muscle pain •nausea, vomiting •severe stomach pain Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome): •heartburn or indigestion •stomach upset This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. Where should I keep my medicine? Keep out of the reach of children. Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from moisture. Throw away any unused medicine after the expiration date. 【中文品名】盐酸考来维仑 【英文药名】Welchol (Colesevelam Tablets) 【药效类别】降血脂药 【通用药名】COLESEVELAM HYDROCHLORIDE 【别　　名】Welchol 【化学名称】 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 【用　　途】本品可单独或与他汀类药物联合使用，用作原发性高胆固醇血症病人饮食和运动的辅助治疗，以降低其升高的低密度脂蛋白胆固醇〔LDL—C)水平。