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Fibrate

Fenofibrate

A fibrate prodrug, turned into fenofibric acid, used mainly to lower very high triglycerides.

Drug card

Class
Fibrate
How it works
Activating PPAR-alpha, so triglyceride-rich particles are cleared faster
Used for
  • Severe high triglycerides
  • High LDL cholesterol when usual LDL drugs cannot be used
Known for
  • Myopathy and rhabdomyolysis, more with a statin
  • Gallstones
Its name
-fibrate means a fibrate (PPAR-alpha agonist)

Study it as a flashcard, and it comes back before you forget it.

Mechanism of action

How does fenofibrate work?

A phenoxy-isobutyric acid ester that is hydrolyzed to its active form, fenofibric acid, which activates PPAR-alpha. Lipoprotein lipase activity rises and apolipoprotein C-III falls, so VLDL and triglycerides are cleared faster, HDL and apoA-I rise, and LDL particles become larger and are removed more quickly.

Uses

What is fenofibrate used for?

  • Severe high triglycerides
  • High LDL cholesterol when usual LDL drugs cannot be used

Side effects

Side effects of fenofibrate

  • Myopathy and rhabdomyolysis, more with a statinKnown forSerious
  • GallstonesKnown for
  • Abnormal liver tests; rarely serious liver injurySerious
  • Raised serum creatinine
  • PancreatitisSerious
  • Deep vein thrombosis and pulmonary embolismSerious
  • Mild falls in hemoglobin and white cells
  • Anaphylaxis and angioedemaSerious
  • Severe skin reactionsSerious
  • Paradoxical fall in HDL cholesterol
  • Abdominal pain
  • Constipation

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Contraindicated in severe kidney impairment or dialysis, active liver disease and existing gallbladder disease.
  • With a statin, weigh the extra risk of myopathy and watch for muscle symptoms; colchicine adds to the risk.
  • Boosts warfarin and other coumarins: lower the anticoagulant dose and check the INR often.
  • Monitor ALT, AST and bilirubin at the start and during treatment.

Good to know: It lowers triglycerides well, but it did not reduce heart attacks or deaths in two large trials of people with type 2 diabetes.

Remember it

A way to remember it

Fibrates fix fat in the blood: PPAR-alpha switches on lipoprotein lipase, which empties triglyceride-rich particles.

Triglycerides fall the most. The two classic harms are gallstones, because more cholesterol is sent into bile, and muscle damage, which is likelier when a statin is added.

Written for biofideX

Its name

  • -fibrate means fibrate (PPAR-alpha agonist)

    Fenofibrate, bezafibrate and ciprofibrate are clofibrate relatives that activate PPAR-alpha and lower triglycerides.

  • Every drug name stem

Its class

Fibrates

Fibrates (fenofibrate works as fenofibric acid) bind and activate the receptor PPAR-alpha. Lipoprotein lipase becomes more active and apolipoprotein C-III, which inhibits it, falls, so triglyceride-rich VLDL is broken down and cleared faster. Triglycerides fall most; HDL and apoA-I rise, and small dense LDL particles become larger.

Easily mixed up with statins and thiazolidinediones.

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.

Practice it

Blood clots and cholesterol

Fenofibrate 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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