Fenofibrate: Formula, Presentation, Indications, Mechanism of Action, Dosage, Side Effects and Interactions

It is used to treat high levels of cholesterol and triglycerides in the blood.

In conjunction with this treatment, patients must undergo an adequate diet of lipid reduction .

Fenofibrate tablets should be administered with meals, thus optimizing the bioavailability of the medication.

The initial treatment for dyslipidemia is a specific dietary therapy for this type of lipoprotein disorder.

Estrogen therapy, thiazide diuretics and beta-blockers are sometimes associated with massive increases in plasma triglycerides, especially in those with genetic hypertriglyceridemia .

In such cases, the interruption of the specific causative agent may obviate the need for pharmacological treatment for hypertriglyceridemia.

Lipid levels should be monitored periodically and a dose reduction of fenofibrate should be considered if lipid levels fall significantly below the target range.

Chemical formula

  • C20H21O4C1.

Presentation

The administration of fenofibrate capsules should be for oral use.

Fenofibrate capsules are available as hard gelatin capsules of 54 or 160 mg.

Indications

Fenofibrate is indicated as a therapy that includes a diet, to reduce the high levels of low density of cholesterol lipoproteins, total cholesterol, triglycerides and apolipoprotein B.

It is also used to increase high-density lipoprotein cholesterol in patients with primary hypercholesterolemia or mixed dyslipidemia .

Mechanism of action

The modification of lipids by fenofibrate is carried out by the activation of peroxisome proliferators that control the expression of genes in the synthesis and oxidation of fatty acids, and are involved in the storage of fatty acids in different tissues.

Dose

Severe hypertriglyceridemia:

The initial dose in these cases is 54 to 160 mg per day.

The dose should be individualized according to the patient’s response, and should be adjusted if necessary after repeating lipid determinations in a range of 4 to 8 weeks.

The maximum dose is 160 mg once a day.

Renal insufficiency:

Treatment with fenofibrate should be initiated at a dose of 54 mg per day in patients with mild to moderate renal impairment, and should only increase after evaluation of effects on renal function and lipid levels at this dose.

Geriatric patients:

The selection of the dose for patients of this age group should be made on the basis of the patient’s renal function.

Side effects

The following adverse reactions have been identified during administration of fenofibrate as:

Myalgia , muscle spasm, severe pain in the upper part of the stomach that extends into the back, chest pains, joint pain, swelling, warmth or redness in the legs, headaches.

Bruising easily, unusual bleeding from the nose, mouth, vagina or rectum, spots in the form of purple or red spots on the skin, anemia, decreased levels of hemoglobin , decreased hematocrit.

Decreased white blood cells, nausea and vomiting, pancreatitis , hepatitis, cirrhosis , asthenia , sudden cough, wheezing, fever, nasal congestion, rapid breathing and rapid heartbeat.

Because these reactions are voluntarily reported from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship with exposure to the drug.

In rare cases, fenofibrate can cause a condition that causes the breakdown of skeletal muscle tissue or rhabdomyolysis and lead to kidney failure.

Allergic reactions can also occur with the following symptoms:

Skin lesions, edema on the face, lips, tongue, throat and difficulty breathing.

Warnings and contraindications

Fenofibrate should not be used in patients with known hypersensitivity to fenofibrate or fenofibric acid.

If you have liver disease, gallbladder disease, severe kidney disease, or if you are on dialysis therapy, diabetes, heart disease, a thyroid disorder or a history of pancreatitis, great care should be taken as they have been treated. reported the following risks:

Skeletal muscle:

Fibrates increase the risk of myopathy and have been associated with rhabdomyolysis, especially in those patients who are elderly, suffer from diabetes, kidney failure or hypothyroidism , the risks of severe muscle toxicity seem to increase.

Liver function:

Fenofibrate in doses equivalent to 107 mg to 160 mg per day have been associated with increases in serum transaminases.

Serum creatinine:

Elevations of serum creatinine have been reported in patients treated with fenofibrate.

These elevations tend to return to the baseline after discontinuation of fenofibrate treatment.

Colelitiasis:

Fenofibrate can increase the secretion of cholesterol in the bile, which causes cholelithiasis.

In those patients in whom cholelithiasis is suspected, studies of the gallbladder should be indicated.

Fenofibrate therapy should be discontinued if gallstones are found.

Pancreatitis:

Pancreatitis has been reported in patients taking fenofibrate.

This occurrence may represent a failure of efficacy in patients with severe hypertriglyceridemia , a direct effect of the drug or a secondary phenomenon mediated by the formation of gallstones or sludge with obstruction of the common bile duct.

Hematological changes:

Mild to moderate decreases in hemoglobin, hematocrit, and white blood cells have been reported in patients after fenofibrate therapy has been initiated.

However, these levels usually stabilize during their long-term administration.

Agranulocytosis and thrombocytopenia have been reported in individuals treated with fenofibrate.

Periodic monitoring of red and white blood cell counts during the first 12 months of fenofibrate administration is recommended.

Use in specific populations

Pregnant women:

Safety in pregnant women has not been established.

When the risk of the drug during pregnancy has been reviewed, it has been placed in category C, since there are no controlled studies of the effects on the fetus.

Therefore its use is not recommended in case of pregnant women.

Nursing mothers:

Fenofibrate should not be used in nursing mothers, as this medicine can pass into breast milk and cause harm to the baby.

A decision must be made about whether to stop breastfeeding or stop the medication, taking into account the importance of the medication to the mother.

Pediatric use:

Safety and efficacy have not been established in patients of this age group.

Geriatric use:

It is known that fenofibric acid is substantially excreted by the kidney, and the risk of adverse reactions to this drug may be higher in patients with renal insufficiency.

Exposure to fenofibric acid is not influenced by age. Elderly patients have a higher incidence of renal failure, the selection of the dose for the elderly should be made on the basis of renal function.

Interactions

Alcohol should not be consumed while being treated with fenofibrate, as triglyceride levels may rise and liver damage may also occur.

It should be taken into account that the use of the following medications can cause effects if used in conjunction with fenofibrate:

Coumarin anticoagulants:

An enhancement of the anticoagulant effects of the coumarin type with prolongation of the protombine time has been observed. Caution should be exercised when administering coumarin anticoagulants together with fenofibrate.

The dose of anticoagulants should be reduced to keep the clotting time at the desired values ​​to prevent bleeding complications.

Frequent determinations of protombine time are advisable until it has been definitively determined that they have stabilized.

Immunosuppressants:

Immunosuppressants such as cyclosporine and tacrolimus can produce nephrotoxicity with decreases in creatinine clearance and increases in serum creatinine.

Since renal excretion is the main route of elimination of drugs such as fenofibrate, there is a risk that the interaction impairs renal function.

Bile acid binding resins:

Because resins that bind to bile acids can bind to other medications administered simultaneously, patients should take fenofibrate at least one hour before or 4 to 6 hours after a bile acid binding resin to avoid hampering its absorption.

Colchicina:

Cases of myopathy, including rhabdomyolysis , have been reported with fenofibrates coadministered with colchicine.

Caution should be exercised when prescribing fenofibrate concomitantly with colchicine.

Special caution should be used in cases of concomitant administration of fenofibrate with:

  • Medications to treat an intestinal disorder.
  • Medications to prevent rejection of organ transplantation.
  • Antiviral drugs.
  • Chemotherapy
  • Medications for pain or arthritis (including aspirin, Tylenol, Advil and Aleve).
  • Any type of antibiotic injected.

All instructions on the prescription of the medication must be followed.

The medication should not be given in larger or smaller amounts or for longer than recommended.

Fenofibrate is only part of a treatment program that may also include diet, exercise and weight control.

While using fenofibrate, it is necessary to perform frequent blood tests to monitor certain values ​​associated with the administration of the drug.