Clinical Medicine Reviews in Vascular Health

Background: Statins are recommended as first line therapy for the prevention of cardiovascular disease. Some individuals are statin intolerant or may need additional cholesterol lowering to achieve their cholesterol targets.

Purpose: To review the pharmacology, clinical efficacy and safety of colesevelam mono- and combination therapy in patients with hypercholesterolemia.

Data source: English-language journals from PUBMED MEDLINE (without restriction of date) using key word colesevelam.

Results: Trials of colesevelam as monotherpy or in combination had baseline LDL-c levels of 130 to 202 mg/dl and triglycerides levels of 114 to 230 mg/dl. Colesevelam monotherapy reduced LDL-c by 9%–20% while increasing triglycerides 6%–25%. When added to low or moderate dose statin therapy, colesevelam decreased LDL-c an additional 6%–16%; when added to fenofibrate, colesevelam additionally decreased LDL-c by 17% and non-HDL-c by 7%; and when added to statin + niacin 2 gr additionally decreased LDL-c by 10%. The hypertriglyceridemia observed with colesevelam monotherapy was largely attenuated when colesevelam was coadministered with statins, fenofibrate, or niacin 2 gr. Coadministration of colesevelam with ezetimibe provided variable additional LDL-c reductions ranging from 0 to 20% over ezetimibe alone, and triglyceride responses were similarly variable. In diabetic individuals with modest hypertriglyceridemia, colesevelam reduced hemoglobin A1c by 0.5%. Colesevelam has fewer drug interactions than older bile acid sequestrants and is well-tolerated when used in combination with other lipid-lowering medications as well as with oral anti-diabetes medications or insulin.

Conclusion: Colesevelam is an option for patients who have not achieved their LDL-c and non-HDL-c goals with statin therapy, or who are statin intolerant. Colesevelam is also an option to lower both LDL-c and glucose levels in patients with inadequately controlled diabetes.