Colesevelam hydrochloride in clinical practice: a new approach in the treatment of hypercholesterolaemia.
OBJECTIVE
Hypercholesterolaemia is a major risk factor for atherosclerosis and coronary heart disease. Treatment with lipid lowering agents reduces the risk of vascular events. Colesevelam is a novel bile acid sequestrant (BAS) indicated for the treatment of hypercholesterolaemia, either as monotherapy or in combination with statins.


METHODS
This article reviews the efficacy, tolerability and safety of colesevelam in clinical practice. The literature search was based on a PubMed search up to January 2008.


RESULTS
Colesevelam, used alone or in combination with other hypolipidaemic agents (statins, ezetimibe and fenofibrate), has an overall favourable effect on lipid profile. Specifically, colesevelam reduces total and low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B levels and increases high-density lipoprotein cholesterol and apolipoprotein AI. However, colesevelam may slightly raise triglyceride levels. Colesevelam can improve glycaemic control in diabetic patients. Moreover, it may have anti-inflammatory properties, as it can reduce high sensitivity C-reactive protein concentration. Colesevelam almost lacks the intense side effects of previously used BASs, thus resulting in better patient compliance. However, the dose regimen consisting of up to 7 tablets/day and high cost may limit its use.


CONCLUSIONS
Colesevelam is a safe alternative for those intolerant to other lipid lowering medication. This BAS also provides an option for patients who do not reach their LDL-C goal despite treatment with a statin.
Florentin
M
M
Department of Internal Medicine, Medical School, University of Ioannina, Ioannina, Greece.
Liberopoulos
E N
EN
Mikhailidis
D P
DP
Elisaf
M S
MS
D000499:Allylamine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D000924:Anticholesteremic Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D001055:Apolipoproteins B / Q000378:metabolism; D001384:Azetidines / Q000627:therapeutic use; D001647:Bile Acids and Salts / Q000378:metabolism*; D008078:Cholesterol, LDL / Q000187:drug effects; D000069472:Colesevelam Hydrochloride; D004359:Drug Therapy, Combination; D000069438:Ezetimibe; D011345:Fenofibrate / Q000627:therapeutic use; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000627:therapeutic use; D012307:Risk Factors
D000924:Anticholesteremic Agents; D001055:Apolipoproteins B; D001384:Azetidines; D001647:Bile Acids and Salts; D008078:Cholesterol, LDL; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000499:Allylamine; D000069438:Ezetimibe; D000069472:Colesevelam Hydrochloride; D011345:Fenofibrate