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Bile-acid Sequestrant Drugs
- Cholestyramine (Questran)
- Colestipol (Colestid)
- Colesevelam (Welchol)
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Indication & Role
- Lowering LDLs 12%-25%
- HDLs increase 4%-5%
- Reduction in cardiovascular events with the use of cholestyramine.
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MoA
- Highly positively charged and bind the negatively charged bile acids & their excretion in the stool.
- Decrease in pool of bile acids leads to hepatic bile acid synthesis and hepatic cholesterol content declines.
- This causes an increase in hepatic LDL receptors, which lowers LDL levels.
- This is partially offset with up-regulation of HMG-CoA reductase.
- There is also an increase in hepatic triglyceride synthesis.
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RoA
- Cholestyramine as powder
- Colestipol as powder or tablets (sluree)
- Colesevelam as solid tablet
- (Poor compliance due to consistency & bloating SEs)
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Absorption & Elimination
- No absorption
- Entirely eliminated in feces
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Common SEs
- Bloating
- Dyspepsia
- Constipation (rarely)
- Contraindicated in pre-existing hypertriglyceridemia
- Interfere w/ absorption of thiazides, furosemide, propanolol, L-thyroxine, digoxin, warfarin, and some statins
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Clinical Use
- Pts that don't tolerate Statins
- Usage limited due to unpleasant GI SEs
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