Colesevelam hydrochloride: A novel bile acid-binding resin
Colesevelam hydrochloride: A novel bile acid-binding resin
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DOI：
10.1345/aph.10263
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发表时间：
2001-07-01
影响因子：
2.9
通讯作者：
Ito, MK
中科院分区：
文献类型：
--
作者：
Aldridge, MA;Ito, MK
目的：综述盐酸考来维仑（一种胆汁酸结合树脂）的药理学、药代动力学、功效和不良反应。方法：采用 MEDLINE 检索（1966 年至 2000 年 6 月）和制造商处方文献来查找有关考来维仑的文章。从审查文献的参考书目中确定了其他研究和摘要。研究选择和数据提取：对从数据源中确定的所有文章进行了评估，并且所有被认为相关的信息都包含在本次审查中。优先考虑随机、双盲、安慰剂对照研究。研究结果：盐酸考来维仑是一种不吸收的水凝胶，具有胆汁酸螯合剂特性。使用考来维仑单一疗法，每日一次或每日分两次服用 1.5-4.5 g 剂量，可显着降低总胆固醇和低密度脂蛋白 (LDL) 胆固醇。当患者每天服用 3.75-4.5 克时，平均 LDL 胆固醇会降低至 20%。在一些研究中，观察到高密度脂蛋白 (HDL) 胆固醇增加（高达 9%），而甘油三酯 (TG) 显着增加至 25%。在未发表的研究中，与单独使用他汀类药物或考来维仑相比，联合使用考来维仑和羟甲基戊二酰辅酶 A (HMG-CoA) 还原酶抑制剂可更大程度地降低 LDL 胆固醇。尽管考来维仑单药治疗在降低 LDL 胆固醇方面的功效略低于或类似于考来烯胺或考来替泊，但按克计算，考来维仑更有效。在已发表的研究中，考来维仑的不良反应很小；这表明比考来烯胺或考来替泊治疗有优势。考来维仑似乎比旧胆汁酸树脂品牌配方的包装剂型更具成本效益。在考虑不良反应和适口性问题时，应谨慎选择合适的药物。结论：考来维仑单独使用或与 HMG-CoA 还原酶抑制剂联合使用可有效降低总胆固醇和 LDL 胆固醇。由于考来维仑被配制为片剂，因此可消除诸如胆汁酸结合树脂粉末制剂的适口性问题。
OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of colesevelam hydrochloride, a bile acid-binding resin.METHODS: MEDLINE searches (1966-June 2000) and manufacturer prescribing literature were employed to find articles on colesevelam. Additional studies and abstracts were identified from the bibliographies of reviewed literature.STUDY SELECTION AND DATA EXTRACTION: All articles identified from data sources were evaluated, and all information deemed relevant was included in this review. Priority was given to randomized, double-blind, placebo-controlled studies.FINDINGS: Colesevelam HCl is a nonabsorbed hydrogel with bile acid sequestrant properties. Monotherapy using colesevelam in once-daily or two divided daily doses of 1.5-4.5 g has produced significant reductions in total cholesterol and low-density lipoprotein (LDL) cholesterol. Mean LDL cholesterol decreases to 20% have been noted when the patient is on 3.75-4.5 g/d. Increases in high-density lipoprotein (HDL) cholesterol have been observed (up to 9%), whereas triglycerides (TG) have increased significantly to 25% in some studies. In unpublished studies, combined use of colesevelam plus hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor have produced greater reductions in LDL cholesterol than either the statin or colesevelam administered alone. The efficacy of colesevelam monotherapy is slightly less than or similar to cholestyramine or colestipol in decreasing LDL cholesterol, although colesevelam is more potent on a gram-to-gram basis. Adverse effects have been minimal with colesevelam in published studies; this suggests an advantage over cholestyramine or colestipol therapy. Colesevelam appears to be more cost-effective than the packet dosage form of the brand formulation of the older bile acid resins. Care in selection of an appropriate agent should be exercised when considering the issues of adverse effects and palatability.CONCLUSIONS: Colesevelam alone or combined with an HMG-CoA reductase inhibitor is effective in the reduction of total and LDL cholesterol. Since colesevelam is formulated as a tablet, problems with palatability such as with the powder formulation of the bile acid-binding resins are likely to be eliminated.