Bile-acid Sequestrants

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Bile-acid Sequestrants
2011-11-29 20:59:48
Anti Hyperlipidemic Drugs

Bile-acid Sequestrants
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  1. Bile-acid Sequestrant Drugs
    • Cholestyramine (Questran)
    • Colestipol (Colestid)
    • Colesevelam (Welchol)
  2. Indication & Role
    • Lowering LDLs 12%-25%
    • HDLs increase 4%-5%
    • Reduction in cardiovascular events with the use of cholestyramine.
  3. 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.
  4. RoA
    • Cholestyramine as powder
    • Colestipol as powder or tablets (sluree)
    • Colesevelam as solid tablet
    • (Poor compliance due to consistency & bloating SEs)
  5. Absorption & Elimination
    • No absorption
    • Entirely eliminated in feces
  6. 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
  7. Clinical Use
    • Pts that don't tolerate Statins
    • Usage limited due to unpleasant GI SEs