Pharmacotherapy Newsletter

Volume 2, Issue 9, 03/02/2010

Question

Why is there no lipid lowering advantage in dosing the cholesterol absorption inhibitor, ezetimibe (Zetia), twice a day versus its recommended dosing of once daily?

Answer

Ezetimibe (Zetia) is the first cholesterol absorption inhibitor that can reduce low density lipoprotein cholesterol (LDL-C) either as monotherapy or in combination with HMG CoA reductase inhibitor (statin) therapy.(1-4)  It has been especially useful in helping some patients with significant hyperlipidemia to get to their individualized LDL-C goals when maximum doses of statins have been tried.(5)  In addition, ezetimibe can reduce the statin dose to tolerable levels in patients experiencing statin-related myopathy, while not losing LDL-C control.  Additional advantages include no significant drug interactions, overall good tolerability profile and being approved for once daily dosing. 

What is it about ezetimibe's pharmacokinetic profile that allows it to be dosed once daily and how does that impact its lipid lowering efficacy? 
After oral administration, ezetimibe passes into the small intestine where it enters into the enterocyte and predominately undergoes...

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