Colesevelam HCl: a non-systemic lipid-altering drug

Expert Opin Pharmacother. 2003 May;4(5):779-90. doi: 10.1517/14656566.4.5.779.


Colesevelam HCl (WelChol, Sankyo Pharmaceuticals Inc.) is a bile acid sequestrant polymer, which has been shown to significantly lower low density lipoprotein cholesterol and favourably affect high-density lipoprotein cholesterol blood levels in monotherapy and in combination with statins (HMG-CoA reductase inhibitors). Although it is similar to other bile acid sequestrants in that it binds bile acids and is non-systemic, colesevelam HCl differs in that it has a unique polymer structure that allows for greater tolerability with less potential drug interactions than with resins. Currently, statins are the most commonly prescribed lipid-altering drugs. However, it is not uncommon that patients demonstrate true or perceived intolerances to statin therapy, that are often dose-related and may include elevations in liver or muscle enzyme blood levels, or myalgias or muscle weakness without muscle enzyme elevation. In rare circumstances, myopathy and even rhabdomyolysis can occur with statins. In addition, many statins also have important potential drug interactions. Finally, statin monotherapy is often not sufficient in achieving lipid treatment goals in many severely dyslipidaemic patients and the availability of colesevelam HCl provides a lipid-altering treatment addition to other lipid-altering drugs. From a clinical perspective, such combination therapy is often required to achieve treatment goals [1] in patients with more complicated or severe dyslipidaemia. Colesevelam HCl may also be an alternative in monotherapy for many patients with mild-to-moderate hypercholesterolaemia, as well as in some patients at potential risk from systemic exposure to alternative lipid-altering drugs (such as young children and fertile women).

Publication types

  • Review

MeSH terms

  • Allylamine* / analogs & derivatives*
  • Allylamine* / metabolism
  • Allylamine* / pharmacokinetics
  • Allylamine* / therapeutic use
  • Animals
  • Child
  • Clinical Trials as Topic
  • Colesevelam Hydrochloride
  • Drug Interactions
  • Female
  • Half-Life
  • Humans
  • Hypercholesterolemia / drug therapy*
  • Hypolipidemic Agents* / metabolism
  • Hypolipidemic Agents* / pharmacokinetics


  • Hypolipidemic Agents
  • Allylamine
  • Colesevelam Hydrochloride