Ezetimibe
A cholesterol absorption inhibitor that blocks NPC1L1 in the gut, used with a statin or alone to lower LDL cholesterol.
Drug card
- How it works
- Blocking the gut cholesterol transporter NPC1L1, so less cholesterol is absorbed
- Used for
- High LDL cholesterol, with a statin or alone
- Sitosterolemia (raised plant sterols)
- Known for
- Diarrhea
- Raised liver enzymes, more often with a statin
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does ezetimibe work?
An azetidinone that settles at the small-intestinal brush border and blocks NPC1L1, cutting uptake of cholesterol and plant sterols. It is conjugated in the gut and liver to an active glucuronide, recirculates through the bile and has a half-life of about 22 hours; most of a dose leaves in the feces.
Uses
What is ezetimibe used for?
- High LDL cholesterol, with a statin or alone
- Sitosterolemia (raised plant sterols)
Side effects
Side effects of ezetimibe
- DiarrheaKnown for
- Raised liver enzymes, more often with a statinKnown for
- Myopathy and rhabdomyolysisSerious
- Muscle aches (with a statin)
- Joint pain
- Tiredness
- Back pain (with a statin)
- Gallstones and cholecystitis
- PancreatitisSerious
- Low platelet count
- Allergic reactions, including angioedema and anaphylaxisSerious
- Abdominal pain
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- When given with a statin or fenofibrate, that drug's contraindications and warnings also apply.
- With fenofibrate, both raise cholesterol in bile; if gallstones are suspected, the gallbladder is checked. Other fibrates are not advised.
- Cyclosporine and ezetimibe raise each other's levels, so cyclosporine levels are monitored.
- Take it apart from bile acid sequestrants, which reduce its absorption.
Good to know: Works in the gut rather than on the liver's cholesterol synthesis, so it adds to a statin's effect; it is used alone when a statin is not possible.
Remember it
A way to remember it
Statins shut the factory; ezetimibe shuts the gate.
Statins cut the cholesterol the liver makes, while ezetimibe blocks NPC1L1 so less cholesterol is absorbed from the gut. The two routes add together, which is why they are often given as a pair.
Written for biofideX
Its class
Cholesterol absorption inhibitors
They act on the lining (brush border) of the small intestine, where they block the sterol transporter NPC1L1, so less cholesterol and fewer plant sterols are taken up from the gut. Less cholesterol reaches the liver; its stores fall, it adds LDL receptors and clears more LDL from the blood. Because this route differs from a statin's, the two are often combined.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Blood clots and cholesterol
Ezetimibe is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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