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Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Ezetimibe Pharmacology

Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist

Education, Health & Fitness, Medicine

5716 Ratings

🗓️ 2 May 2019

⏱️ 11 minutes

🧾️ Download transcript

Summary

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.

Transcript

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0:00.0

Hey all, Eric Christensen here, pharmacist. Welcome back to the real-life pharmacology podcast.

0:05.9

On this episode, I am going to cover the drug isetamide, which is primarily used for cholesterol

0:14.0

lowering effects. The brand name of this medication is Zedia. It is dosed 10 milligrams once a day and there really isn't much variation on the dosing there

0:27.6

in the majority of patients.

0:29.6

It's pretty standard.

0:30.6

It's a starting dose as well as the treatment or therapeutic dose.

0:34.6

Now the mechanism of action of this drug, how it ultimately lowers cholesterol,

0:40.5

is the simplified version is it inhibits the intestinal absorption of cholesterol. So if you block it

0:47.8

from getting into the bloodstream, ultimately that's going to lower total cholesterol throughout

0:52.9

the body and the blood, obviously.

0:55.4

Now, the exact mechanism, it blocks the Neiman Pick C1, like one sterile transporter.

1:04.7

Okay, so that's a mouthful to remember.

1:08.3

But ultimately, this transporter allows cholesterol or facilitates the movement

1:15.0

of cholesterol across the intestinal wall and into the bloodstream.

1:19.4

So by blocking that transporter, we lower cholesterol.

1:24.7

So the primary use, talking about lowering cholesterol, getting into that a little bit further,

1:31.0

we're targeting LDL cholesterol is typically what we're going to do with this medication.

1:40.3

Now, the major, major first-line medication that everyone uses in lowering cholesterol or L-DL,

1:48.2

or targeting that LDL-Colesterol, reducing the risk of heart attack, stroke, ASCVD, and things like that,

1:56.1

that's going to be statins. That's the first-line go-to medication.

2:00.8

Now, if you've got patients that

2:02.7

do not tolerate statins, do not get enough efficacy from statins, here's where Zetamide may be added in.

...

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