Tulane University School of Medicine, Section of Endocrinology, New Orleans, LA 70112, USA.
Expert Opin Drug Saf. 2011 Mar;10(2):305-10. doi: 10.1517/14740338.2011.548320. Epub 2011 Jan 19.
Patients with hypercholesterolemia and type 2 diabetes mellitus often require multiple medications to attain their LDL-C and A1C goals. Colesevelam, a bile acid sequestrant (BAS), which was FDA approved 10 years ago for the reduction of LDL-C in patients with dyslipidemia is also the only BAS that is approved for glycemic control in adults with type 2 diabetes to date. From both the physician and patient standpoint, safety and tolerability are the most important factors when considering initiating pharmacological therapy. Several randomized controlled studies have examined the safety, tolerability and efficacy of colesevelam over the last decade.
This manuscript focuses on the safety and tolerability based on the evaluation of data obtained from several human randomized controlled studies. In addition, the pharmacology, pharmacodynamics and key clinical efficacy data are reviewed using research articles accessed through MEDLINE/PubMed (2000 - 2010).
Current data suggest that colesevelam is safe, well tolerated and offers the potential for improved adherence. Colesevelam is a valid option for long-term therapy for patients with hypercholesterolemia and type 2 diabetes. It can be used in combination with HMG-CoA reductase inhibitors for hypercholesterolemia, not controlled at their cholesterol goals with HMG-CoA reductase inhibitors, and should be considered in patients with type 2 diabetes mellitus with concomitant hypercholesterolemia to improve both risk factors.
患有高胆固醇血症和 2 型糖尿病的患者通常需要多种药物来达到他们的 LDL-C 和 A1C 目标。考来烯胺（一种胆酸螯合剂（BAS））于 10 年前被 FDA 批准用于降低血脂异常患者的 LDL-C，也是迄今为止唯一被批准用于 2 型糖尿病成人血糖控制的 BAS。从医生和患者的角度来看，安全性和耐受性是考虑开始药物治疗时最重要的因素。过去十年中，已有几项随机对照研究检查了考来烯胺的安全性、耐受性和疗效。
本文稿重点介绍了安全性和耐受性，评估数据来自几项人类随机对照研究。此外，还通过 MEDLINE/PubMed（2000-2010 年）检索的研究文章，回顾了药理学、药效学和关键临床疗效数据。
目前的数据表明，考来烯胺安全、耐受性良好，并有改善依从性的潜力。考来烯胺是高胆固醇血症和 2 型糖尿病患者长期治疗的有效选择。它可与 HMG-CoA 还原酶抑制剂联合用于高胆固醇血症，对于 HMG-CoA 还原酶抑制剂不能控制胆固醇目标的患者，以及伴有高胆固醇血症的 2 型糖尿病患者，应考虑使用该药来改善两种危险因素。
