Page 149 - pharma 1 theoretical updated MNU_Neat

Clinical pharmacy 2024/2025 Level 3 Pharm D Pharmacology 1 (PO 502)

 Non-statins for treatment for hypercholesterolemia

1- Bile acid resins (BAR)

 These are anion-exchange resins that bind negatively charged
bile acids and bile salts in the small intestine.

 The resin/bile acid complex is excreted in the feces, thus
lowering the bile acid concentration.
Mechanism of  This causes hepatocytes to increase conversion of cholesterol
action to bile acids, which are essential components of the bile.

 Consequently, intracellular cholesterol concentrations
decrease, which activates an increased hepatic uptake of

cholesterol-containing LDL particles, leading to a fall in
plasma LDL-C.

 Reduce LDL by 15%–26% & Raise HDL by 3%–6%.
Efficacy of BAR   TG concentrations & reduce major coronary events.

 Reduce CHD mortality.

Ex: cholestyramine, colestipol, colesevelam

 Starting dose 4g daily, increased to 12-24 g daily over 3-4
Dose
weeks

Used mainly in combination with statins

Adverse effects bloating, flatulence, constipation (fluid intake should be increased)

dyslipoproteinemia, elevated TGs>400 mg/dL
Contraindications (increases VLDL synthesis): total cholesterol and triglyceride

levels, HDL

 ↓ absorption of warfarin, beta blockers, thiazides, digoxin,
Drug interaction fat soluble vitamins

(so administer BAR one hour before or 4 hours after)

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