Viljoen Adie, Wierzbicki Anthony S
a Lister Hospital, Stevenage, Hertfordshire, SG1 4AB, UK.
b Guy's & St Thomas Hospitals, Lambeth Palace Road, London, SE1 7EH, UK.
Expert Rev Endocrinol Metab. 2010 Nov;5(6):825-834. doi: 10.1586/eem.10.53.
There is a well-established association between serum cholesterol and coronary heart disease. Statins are the first-line agents for the treatment of hypercholesterolemia, yet combination therapy is required to achieve the desired reduction in low-density lipoprotein cholesterol (LDL-C). Niacin and bile acid sequestrants were among the first lipid-lowering drugs developed to lower LDL-C and have been established to be effective both in monotherapy and in combination therapy. However, tolerability and compliance issues have limited their use. Colesevelam HCl is the newest bile acid sequestrant and reduces LDL-C by 16-22% in monotherapy and adds 12-14% in combination dual therapy with statins, fibrates and ezetimibe or in triple therapy with statin and ezetimibe. It reduces C-reactive protein levels by 16-19% in monotherapy or by 23% in combination with statins and other lipid-lowering therapies. In addition, it consistently reduces hemoglobin A by 0.5% in addition to other hypoglycemic drugs in studies of patients with diabetes. Compared with other bile acid sequestrants it has a higher bile acid-binding capacity, reduced adverse effects and, therefore, has better compliance. Colesevelam HCl is thus a useful addition to the lipid-lowering formulary as a second-line agent, particularly for patients with metabolic syndrome requiring extra reduction in LDL-C.
血清胆固醇与冠心病之间存在着已被充分证实的关联。他汀类药物是治疗高胆固醇血症的一线药物，但需要联合治疗才能实现低密度脂蛋白胆固醇（LDL-C）的预期降低。烟酸和胆汁酸螯合剂是最早开发用于降低LDL-C的降脂药物之一，已证实其在单药治疗和联合治疗中均有效。然而，耐受性和依从性问题限制了它们的使用。盐酸考来维仑是最新的胆汁酸螯合剂，单药治疗可使LDL-C降低16% - 22%，与他汀类药物、贝特类药物和依折麦布联合双药治疗或与他汀类药物和依折麦布联合三联治疗时可额外降低12% - 14%。单药治疗可使C反应蛋白水平降低16% - 19%，与他汀类药物及其他降脂疗法联合使用时可降低23%。此外，在糖尿病患者的研究中，除其他降糖药物外，它还能持续使糖化血红蛋白降低0.5%。与其他胆汁酸螯合剂相比，它具有更高的胆汁酸结合能力，不良反应减少，因此依从性更好。因此，盐酸考来维仑作为二线药物是降脂药物配方中的有益补充，尤其适用于需要进一步降低LDL-C的代谢综合征患者。
