On this episode, I discuss ezetimibe pharmacology. Ezetimibe works by inhibiting Niemann-Pick C1-Like1 (NPC1L1) transporter. This transporter aids in cholesterol absorption so by blocking it, we can reduce cholesterol levels (and LDL) in the bloodstream.



Ezetimibe is usually very well tolerated. Diarrhea, myopathy, and elevations in LFT's are adverse effects that have been reported but do not occur at high rates.



Ezetimibe is dosed at 10 mg once daily. This is a nice advantage because this is a starting dose and the usual treatment dose.



With the most recent cholesterol guideline updates, I do expect ezetimibe to be utilized a little more than it used to be. They place more emphasis on a target LDL and getting patients to goal.



Statins are going to be used first line for cholesterol and ezetimibe will be an add on therapy to consider. They don't, unfortunately, lower cholesterol as much as high-intensity statins do.