Ezetimibe and PCSK-9 Inhibitors – Cholesterol Test Prep and Practice Pearls
Real Life Pharmacology - Pharmacology Education for Health Care Professionals
Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist
4.9 • 773 Ratings
🗓️ 12 February 2026
⏱️ 14 minutes
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Summary
In this pharmacology podcast episode, we focus on two key non-statin cholesterol-lowering therapies: ezetimibe and PCSK9 inhibitors (Click here to listen to the statin podcast episode). These agents play a role in lipid management, particularly for patients who are unable to reach LDL cholesterol goals with statins alone or who have statin intolerance.
Ezetimibe works by inhibiting the absorption of dietary and biliary cholesterol at the brush border of the small intestine. By reducing the amount of cholesterol delivered to the liver, ezetimibe lowers circulating LDL cholesterol by approximately 15 to 25 percent. It is taken orally once daily and is commonly used as add-on therapy to statins in patients with established atherosclerotic cardiovascular disease or high baseline LDL levels. Ezetimibe is generally well tolerated, with a favorable safety profile and minimal systemic exposure, making it an attractive option in older adults and patients with multiple comorbidities.
PCSK9 inhibitors, including alirocumab and evolocumab, offer a much more potent LDL-lowering effect. These monoclonal antibodies work by blocking PCSK9, a protein that promotes degradation of LDL receptors in the liver. By preserving LDL receptors, PCSK9 inhibitors enhance clearance of LDL cholesterol from the bloodstream, often reducing LDL levels by 50 to 60 percent. They are administered via subcutaneous injection every two to four weeks and are most commonly used in patients with familial hypercholesterolemia, established cardiovascular disease, or persistently elevated LDL despite maximally tolerated statin and ezetimibe therapy.
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Transcript
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| 0:00.0 | Hey all, welcome back to the Real Life Pharmacology podcast. Thank you so much for listening. |
| 0:05.1 | As always, go check out Real Life Pharmacology.com. Get your free 31-page PDF on the top 200 drugs. |
| 0:12.5 | Great study guide, great refresher. Definitely a great resource to have for any practicing healthcare professional |
| 0:19.7 | who enjoys learning about pharmacology or feels |
| 0:23.1 | like they need to brush up on their skills a little bit. So again, go check that out, |
| 0:27.7 | real-life pharmacology.com. All right. So the episode today that I wanted to cover were two |
| 0:36.9 | types of medications. |
| 0:38.8 | So we've got one Zetamib and the other PCSK9 inhibitors. |
| 0:43.3 | These two medications are, I wouldn't say crazy common in practice, |
| 0:48.6 | but you do see them periodically for sure. |
| 0:51.4 | And they lower LDL. |
| 0:53.4 | And specifically, they are going to be used after and or in |
| 1:00.0 | conjunction with statin therapy. So statin therapy, Torvastatin, or suvastatin, those are really the go-to |
| 1:06.3 | agents. Covered that podcast already. Go back, listen to that. |
| 1:16.1 | Now, once we need more medication, LDL is not low enough, |
| 1:17.3 | whatever the case may be, |
| 1:22.7 | these two medications are going to be what's typically used next. |
| 1:27.2 | So we're going to break down those two classes of medications. |
| 1:31.8 | And first, I'm going to start with azetamide. |
| 1:35.6 | This is the one that I see more often than the PCSK9 inhibitors. |
| 1:42.5 | Zetamib inhibits intestinal cholesterol absorption at the brush border, |
| 1:46.1 | ultimately reducing LDL cholesterol. |
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