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Colesevelam hydrochloride: a novel bile acid-binding resin
1School of Pharmacy and Health Sciences, University of the Pacific, Stockton, CA, USA.
The Annals of Pharmacotherapy
|August 4, 2001
Summary
Colesevelam hydrochloride is an effective bile acid-binding resin for lowering LDL cholesterol. It offers a palatable tablet formulation with minimal adverse effects, alone or with statins.
Area of Science:
- Pharmacology
- Clinical Therapeutics
- Cardiovascular Medicine
Background:
- Bile acid-binding resins are used to manage hyperlipidemia.
- Older resins like cholestyramine and colestipol have limitations in palatability and adverse effects.
Purpose of the Study:
- To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of colesevelam hydrochloride.
- To compare colesevelam with existing bile acid-binding resins.
Main Methods:
- Literature search of MEDLINE (1966-June 2000) and manufacturer data.
- Inclusion of all relevant articles, prioritizing randomized, double-blind, placebo-controlled studies.
Main Results:
- Colesevelam HCl, a nonabsorbed hydrogel, significantly reduces total and LDL cholesterol.
- Monotherapy (1.5-4.5 g/day) yields up to 20% LDL reduction; HDL may increase up to 9%.
- Combination therapy with HMG-CoA reductase inhibitors provides greater LDL reduction; adverse effects are minimal compared to older resins.
Conclusions:
- Colesevelam is effective alone or with HMG-CoA reductase inhibitors for cholesterol reduction.
- The tablet formulation eliminates palatability issues associated with older powdered resins.
- Colesevelam presents a more palatable and potentially cost-effective option for bile acid-binding therapy.