MEDizzy - A 57-year-old obese woman had low-density lipoprotein (LDL)

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Antihyperlipidemic Drugs

A 57-year-old obese woman had low-density lipoprotein (LDL) cholesterol of 350 mg/dL (normal < 130 mg/dL) despite 3 months of therapy with lovastatin. The physician decided to add to the patient’s regimen a drug that acts by increasing the elimination of bile acids. Which of the following drugs was most likely prescribed?

ExplanationCholestyramine is a bile acid−binding resin. Drugs of this class are highly positively charged (cholestyramine is a quaternary amine) and bind negatively charged bile acids in exchange with Cl−. Because of their large size, resins are not absorbed, and the bound bile acids are excreted in the stool. In this way, enterohepatic circulation of bile acids is prevented (normally, more than 95% of bile acids are reabsorbed; their excretion is increased up to 10-fold when the resins are given).