I. LIPOPROTEINS
4. Bile Acid Sequestrant Resins
a. Cholestyramine
This agent has been available since the early 1970s. It was rarely used by doctors and patients because of poor compliance. The gritty taste and gastrointestinal side effects with only an approximate 10% reduction in choles¬terol and elevation of triglycerides render this agent unsuitable for control of dyslipidemias.
b. Colesevalem
This agent is a new formulation of the bile acid binding resins introduced for use in 2002. The 4.5-mg dose has been shown to reduce LDL cholesterol by 18% and the combination of 2.3 g of the agent with 20 mg of simvastatin reduced LDL cholesterol by 42%, but it increased triglycerides approximately 10%. Thus the drug is not advisable in patients with mixed dyslipidemias. Colesevalem is better tolerated than cholestyramine, but in a study of 240 patients adverse events were similar between each of the groups. It may find a role in patients with pure hypercholesterolemia and LDL elevation. This drug does not have a significant interaction with digoxin, lovastatin, metoprolol, quinidine, or warfarin as is noted with cholestyramine.
5. New Agent
a. Torcetrapib
Torcetrapib increases HDL cholesterol 30 to 50%. Clinical trials are awaited. See chapter entitled Cholesterol.
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