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Fenofibrate - A Comprehensive Review on Its Uses, Dosage, Side Effects, and Precautions

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Fenofibrate helps lower high cholesterol along with a low-fat diet. Read the article below for more details on Fenofibrate.

Medically reviewed by

Dr. Arpit Varshney

Published At February 3, 2023
Reviewed AtJuly 6, 2023

Overview:

Fenofibrate helps lower triglycerides and cholesterol levels in the blood. The drug lowers the low-density lipoprotein or LDL and increases the amount of high-density lipoprotein or HDL cholesterol in the blood in adults. Fenofibrate is Food and Drug Administration (FDA) approved as an adjunct treatment to a low-fat diet in managing hypertriglyceridemia or dyslipidemia (abnormally elevated fats in the blood).

How Does Fenofibrate Work?

Fenofibrate is a fabric acid by-product and activates peroxisome proliferator-activated receptor alpha (PPAR), a nuclear receptor that alters lipid and amino acid homeostasis. This activates gene transcription and translation, generating peroxisomes filled with hydrogen peroxide, reactive oxygen species, and hydroxyl radicals and participating in lipolysis.

Fenofibrate enhances fatty acid oxidation and reduces triglyceride synthesis, resulting in an overall reduction of plasma triglycerides. The drug also facilitates an increase in uric acid excretion and fibrinogen that may help people with gout and thrombosis (which occurs when clots form inside the blood vessels).

Uses of Fenofibrate:

Fenofibrate is indicated for use in the following conditions.

  • The drug is used for the management and treatment of hypertriglyceridemia (too much fat in the blood), primary hypercholesterolemia (high levels of cholesterol in the blood), and mixed dyslipidemia (abnormal levels of cholesterol or fats in the blood).

  • Fenofibrate is combined with a low-fat diet and lifestyle modification to reduce low-density lipoprotein cholesterol in adults.

  • It is an adjunct therapy for treating increased uric acid levels in patients with gout.

Limitations:

Fenofibrate is less effective at lowering low-density lipoprotein cholesterol levels than statins. The drug is not shown to reduce coronary heart disease morbidity and mortality.

  • Patients are advised to follow a diet low in saturated fats and calories before starting the Fenofibrate therapy.

Dosage Restrictions:

Route of Administration - Oral.

Dosage Strengths-

  • Tablets - 40 mg, 48 mg, 54 mg, 120 mg, and 145 mg, and 160 mg tablets.

  • Capsules - 30 mg, 43 mg, 50 mg, 67 mg, 90 mg, 130 mg, 134 mg, 150 mg, and 200 mg.

  • Delayed-release capsule - 45 mg and 135 mg.

Dosage Forms -

  • Yellow, white, orange, and blue color tablets are imprinted with the letter “ FI.”

  • Yellow, orange, white, and blue color tablets imprinted with the” a” logo.

The recommended dose of Fenofibrate capsules is 150 mg once a day.

Special Considerations:

  • Pregnancy - Fenofibrate use has been associated with teratogenicity and is not indicated during pregnancy. There is limited data to determine the risk of major congenital disabilities and adverse effects on the fetus.

  • Lactation - Fenofibrate may disrupt infant lipid metabolism and is best avoided during breastfeeding.

  • Pediatric Patients - The safety and effectiveness of Fenofibrate are not established in pediatric patients.

  • Geriatric Patients - Elderly have a higher incidence of renal impairment and may require dose modifications. They should be regularly monitored for renal function.

  • Renal Impairment - Fenofibrate is excreted by the kidney and increases the risk of adverse reactions in patients with impaired renal function. The drug should be avoided in patients with severe impairment, while dose adjustments are recommended in patients with mild to moderate renal dysfunction.

  • Hepatic Impairment - Chronic treatment with Fenofibrate may be associated with hepatotoxicity and liver injury.

Warnings and Contraindications:

Therapy with Fenofibrate is contraindicated in the following cases:

  • Hypersensitivity - Fenofibrate can cause severe allergic reactions, such as anaphylaxis and angioedema, which may be life-threatening.

  • Biliary Cirrhosis - Therapy with Fenofibrate is contraindicated in patients with primary biliary cirrhosis (where the bile ducts are destroyed) as the drug may further exacerbate the cholesterol levels.

  • Liver Dysfunction - Fenofibrate must be avoided in patients with active liver dysfunction or disease, and the therapy should be discontinued if any signs or symptoms of liver injury develop. Liver function tests should be performed throughout the treatment.

  • Cholelithiasis - Fenofibrate therapy is contraindicated in patients with gallbladder disease. The increased cholesterol excretion into the bile is associated with the risk of developing cholelithiasis and cholecystitis.

  • Renal Impairment Dysfunction - Chronic therapy of Fenofibrate is contraindicated in patients with significantly impaired renal function. The decreased rate of clearance of the Fenofibrate can increase the accumulation of the drug and result in increased adverse effects, including rhabdomyolysis (breakdown of skeletal muscle fibers) and hyperkalemia.

  • Rhabdomyolysis - Treatment with Fenofibrate should be avoided in patients with preexisting myopathy as it may exacerbate the condition.

Precautions:

  • High-Density Lipoprotein Level - Therapy with Fenofibrate can cause a severe decrease in HDL cholesterol within two weeks after the initiation of treatment. Regular monitoring of HDL cholesterol is recommended within the first few months.

  • Anemia - Long-term administration of Fenofibrate is associated with decreased white blood cell count, resulting in thrombocytopenia and agranulocytosis.

  • Myopathy - Fenofibrate increases the risk of myopathy and rhabdomyolysis, or serious muscle toxicity, especially in the elderly and patients with diabetes, renal dysfunction, and hypothyroidism.

For Patients:

What Is Cholesterol?

Cholesterol is a waxy, fat-like material produced by the liver. It helps in the formation of cell membranes and is transported through the bloodstream by particles called lipoproteins. High-fat foods increase the low-density lipoprotein (known as LDL or bad cholesterol), which builds up in the arteries, causing serious health problems. The high-density lipoproteins (known as HDL or good cholesterol) help in the elimination of LDL.

Symptoms of High Cholesterol:

High cholesterol can lead to serious emergencies, such as heart attacks or strokes. It usually shows signs and symptoms but is a hidden risk factor for serious adverse events.

Why Is Fenofibrate Prescribed for High Cholesterol?

When taken with a low-fat diet, Fenofibrate helps to lower the cholesterol levels and fats such as LDL and triglycerides. This prevents the development of pancreatitis (inflammation or swelling in the pancreas) or other complications caused by increased triglyceride levels in the blood. The drug helps increase HDL fat, decreasing the risk of heart disease.

Facts One Should Know About Fenofibrate:

  • Fenofibrate is available in tablet and capsule form and is usually prescribed at 120 mg daily.

  • While Fenofibrate is usually prescribed for treating high cholesterol, the drug is used to treat mixed dyslipidemia and hypertriglyceridemia.

How Should a Person Take Fenofibrate?

  • Fenofibrate is available as tablets and capsules to be taken by mouth. It is usually taken once a day.

  • Fenofibrate can be taken with or without meals.

  • The drug needs to be taken around the same time every day.

  • The dosage should not be increased or decreased.

  • Fenofibrate is usually started on an average dose that may be increased or decreased depending on the results of laboratory tests.

  • The person should inform the doctor of any adverse effects. Do not stop taking the drug.

  • The tablets of Fenofibrate should be swallowed whole and not crushed or chewed.

Information to Be Given to the Doctor Before Starting Fenofibrate Therapy:

  • Allergies - Make it a point to check the ingredient list of Fenofibrate tablets and capsules and inform the physician if one is allergic to the drug or any of the other ingredients in the formulations. Fenofibrate can cause severe allergic reactions, including anaphylaxis and angioedema, which may be fatal.

  • Medical History - Inform the doctor of any concurrent illnesses one may be suffering from, especially heart disease or muscle pain, or have a history of gallbladder disease, kidney disease, or liver disease.

  • Drug History - Fenofibrate should not be combined with statins as this can inhibit its metabolism and increase myopathy risk. It is recommended to get the serum creatinine levels and renal function test done before using the two drugs.

  • Pregnancy - Limited data is available on using Fenofibrate to determine the risk or adverse reactions to the developing fetus. However, the user may be associated with teratogenicity and should be avoided.

  • Lactation - Let the doctor know if one is breastfeeding. There may be a possibility of Fenofibrate passing into the breastmilk and disrupting the lipid metabolism in infants.

  • Geriatrics - Older adults are more likely to have age-related kidney and other medical problems and should discuss them with the doctor before starting the treatment.

  • Children - Fenofibrate should not be used in people younger than 18.

Safety With Fenofibrate:

Fenofibrate is a safe medication. The drug should not be taken with statins (also used to lower cholesterol and protect against heart attack and stroke) as it can inhibit the metabolism of statins, resulting in an increased risk of myopathy (muscle pain and tenderness). The drug is used for long-term treatment and should not be stopped abruptly as it may cause uncontrollable cholesterol levels and lead to the risk of heart problems, such as heart disease or heart attack.

Effectiveness of Fenofibrate:

  • Fenofibrate is quite effective regarding long-term benefits, especially when used with a proper diet and lifestyle change.

  • Fenofibrate may take up to a week to stabilize the cholesterol levels and may be taken up to four months to make apparent changes in the laboratory tests.

  • The drug effectively lowers total cholesterol levels by 9 to 13 %, very low-density lipoprotein by 44 %, and increases HDL by 22 %.

Side Effects Expected With Fenofibrate:

The common side effects that occur with the use of Fenofibrate are as follows:

  • Nausea.

  • Vomiting.

  • Runny nose.

  • Sneezing.

  • Headache.

  • Indigestion.

  • Stuffy nose.

  • Stomach pain.

Serious side effects may include:

  • Stomach pain spread to the back and shoulder.

  • Loss of appetite.

  • Fever.

  • Chills.

  • Weakness.

  • Sore throat.

  • Chest pain.

  • Swelling in the arms and legs.

  • Jaundice.

  • Mouth sores.

  • Unusual bleeding.

  • Trouble breathing.

  • Rash.

  • Trouble swallowing.

Can a Person Stop Taking Fenofibrate Without Doctors Approval?

  • Always take Fenofibrate with approval from the doctor. Consult a physician or visit the emergency room if one experiences any side effects that require immediate attention.

  • Remember that a person must continue taking Fenofibrate, regardless of how well one responds to it unless the doctor explicitly mentions otherwise. The drug is meant for long-term use and should not be stopped even if the person responds well. It can lead to uncontrolled cholesterol levels, causing an increased risk of heart problems.

Dietary Restrictions to be Considered While Taking Fenofibrate:

Fenofibrate is best absorbed when taken with food.

  • Avoid eating high-cholesterol foods such as fried food and red meat and increase consumption of low-fat diets, such as low-fat milk, vegetables, egg whites, and polyunsaturated oils (corn, soybean, sunflower).

  • Intake of grapefruit juice with Fenofibrate can increase the drug concentration in the blood and causes unwanted side effects.

  • Avoid drinking alcohol while taking Fenofibrate treatment as it may aggravate the side effects.

Storage of Fenofibrate:

  • Store Fenofibrate at room temperature between 59 to 70 degrees Fahrenheit. It is stored away from moisture in a cool, dry place.

  • The medication should be stored in the original packaging or container with a tightly closed lid.

  • Keep this drug far from the reach of children and pets.

Disposal of Fenofibrate:

  • Only used tablets and capsules of Fenofibrate should be disposed of by flushing or throwing them out with regular garbage.

  • The medicines should be disposed of through the local medicine take-back program, which one can access or learn more about through the local pharmacist.

  • If the person does not have a medicine take-back program accessible, ask the local pharmacist about other drug disposal options.

Overdose of Fenofibrate:

  • If a person overdoses on Fenofibrate, contact a doctor immediately and do not take another tablet until the doctor tells.

  • Severe side effects like seizures or breathing difficulty may happen; bystanders or family members should take the person to the emergency room or contact local poison control services.

For Doctors:

Indications:

Fenofibrate is indicated for the following purposes:

  • Fenofibrate is FDA-approved to treat patients with hypertriglyceridemia, primary hypercholesterolemia, or mixed dyslipidemia.

  • The drug is used to lower the total cholesterol, LDL- cholesterol, triglycerides, and apolipoprotein B and increase HDL cholesterol in adults.

  • Fenofibrate is safe and effective for the elderly and may be used in pregnancy only if the benefits outweigh the risks to the fetus.

  • Fenofibrate may be prescribed as an adjunct therapy to treat elevated uric acid levels in patients with gout.

What Is the Pharmacology of Fenofibrate?

Description -

  • Fenofibrate is a lipid-regulating agent. The chemical name for Fenofibrate is 2-4[4-(-chlorobenzene)phenoxy].-2-methyl1-propanoic acid, 1-methyl ethyl ester.

Components-

Active Ingredients-

  • Fenofibric acid.

Inactive Ingredients-

  • Hypromellose 2910.

  • Docusate sodium.

  • Sucrose.

  • Sodium lauryl sulfate.

  • Lactose monohydrate.

  • Silicified microcrystalline cellulose.

  • Crospovidone.

  • Magnesium stearate.

Clinical Pharmacology:

Mechanism of Action:

Fenofibrate activates peroxisome proliferator-activated receptor alpha (PPAR). The PPAR is a nuclear receptor that alters lipid, glucose, and amino acid homeostasis. This increases the activity of lipolysis and activates lipoprotein lipase while reducing apoprotein. The activation of PPAR activates the gene transcription, generates peroxisomes, and participates in lipolysis.

Pharmacodynamics:

  • Fenofibrate stimulates cellular fatty acid uptake and promotes conversion to acyl-CoA derivative.

  • The drug also stimulates catabolism by the oxidation pathway, which combines with fatty acid reduction, resulting in a decrease in VLDL production.

Pharmacokinetics:

  • Mean Cmax- The mean Cmax occurs within four to five hours after oral administration.

  • Median Tmax- The absorption of Fenofibrate is increased when taken with food.

[Cmax- Maximum concentration of a drug achieved in the blood, cerebrospinal fluid (CSF), or target organ after administration of a single dose].

[Tmax- Average time taken for a drug to reach maximum concentration in the body after taking a dose].

Pharmacokinetic Changes - Continuous treatment and a single dose of Fenofibrate do not allow the accumulation of the drug.

Distribution -

  • Steady-state Plasma Levels - The plasma concentration is stable and approximately double when given in continuous treatment.

  • Time to Approach Steady-State Levels- Within nine hours.

  • Binding to Plasma Proteins- 99 %.

Metabolism -

  • Metabolic Processes - Esterases rapidly hydrolyze the drug to the active metabolite, fenofibric acid.

  • Fenofibrate is primarily conjugated with glucuronic acid and then excreted in the urine. A small amount of Fenofibrate is reduced at the carbonyl moiety to a benzhydryl metabolite which conjures with glucuronic acid.

Excretion - The drug is mainly excreted in the urine through metabolites, fenofibric acid, and fenofibric acid glucuronide.

  • Recovery of Fenofibrate - Approximately 60 % of the administered dose appears in the urine and 25 % in the feces.

Elimination-

  • 100 % carried out by hepatic metabolism.
  • Mean Elimination Half-Life - 20 hours.

Special Considerations:

  • Renal Impairment - Fenofibrate should be avoided in patients with severe renal impairment as there may be more than a two-fold increase in the accumulation of the drug in the body when used for the long term. A reduction in the dosage of Fenofibrate may be required in patients with mild to moderate renal impairment.

  • Hepatic Impairment- No studies have been conducted on patients with hepatic impairment.

  • Age - Elderly with normal renal function may be given a similar dosage regimen. The drug’s pharmacokinetics (activity of the drug in the body) is not studied in children.

Drug Interactions:

  • Coumarin Anticoagulants - Combining Fenofibrate with Coumarin anticoagulants can prolong the prothrombin time (PT) and INR (international normalized ratio). The dosage should be reduced to maintain PT/INR to prevent bleeding complications.

  • Immunosuppressants - Immunosuppressants such as Cyclosporine and Tacrolimus can decrease creatinine clearance and cause a rise in serum creatinine, producing nephrotoxicity. Low doses of Fenofibrate must be given with immunosuppressants, and regular monitoring of renal function tests must be done.

  • Bile Acid Binding Resins - Patients should be advised to take Fenofibrate at least one hour before or four to six hours after a bile-binding resin. This will help to avoid delayed absorption.

  • Colchicine - Co-administration of Fenofibrate with Colchicine can increase myopathy and should be prescribed with caution.

What Have Clinical Trials Shown Concerning Fenofibrate?

Trial 1.

Objective - Effects of Long-Term Fenofibrate Therapy on Cardiovascular Events in People With Type-2 Diabetes Mellitus.

A randomized controlled trial with 9795 participants aged 50 to 75 with type-2 diabetes mellitus (not taking statin therapy). Patients with previous cardiovascular disease 2131 and 7664 without and with a total cholesterol concentration of 3.0 to 6.5 mmol/L and micronized Fenofibrate 200 mg daily.

Duration - Five years.

Primary Endpoint - Significant 24 % reduction in non-fatal myocardial infarction and a non-significant increase in coronary heart disease mortality. Cardiovascular disease events were markedly reduced from 13.9 % with decreased retinopathy. The finding included a 21 % fall in coronary revascularization.

Secondary Endpoint - Fenofibrate was associated with less albuminuria progression. An increase in pancreatitis and pulmonary embolism was 12.5 % but with no other significant adverse effects.

Result - Fenofibrate does not markedly lower the risk of the primary outcome of coronary events. The drug reduced cardiovascular events due to fewer non-fatal myocardial infarctions and revascularizations. The higher rate of initial statin treatment in patients given a placebo might mask the treatment benefit.

Trial 2.

Objective - Effect of Fenofibrate in 1113 Patients at Low-Density Lipoprotein Cholesterol Goal but High Triglyceride Levels.

A study population of patients with triglyceride levels >150 mg/dL and low-density lipoprotein cholesterol, lower than the target levels, and one or more cardiovascular risk factors, undergoing treatment with Fenofibrate160 mg. The patient’s median age was 61, and 71 % were men. Patients who had changed the lipid-modifying regimen within three to nine months were excluded.

Duration - Three to six months.

Primary Endpoint - Lipid profile performed post-treatment; the median changes in total cholesterol are - 6.5 mg. The percentage reduction of triglyceride was greater in women with atherogenic dyslipidemia or without statin use.

Secondary Endpoint - Diabetes mellitus was associated with a lower than median percentage reduction of triglycerides. Patients with diabetes exhibit a pattern of high triglycerides and low HDL-C.

Result - The usual dose of Fenofibrate reduced triglyceride to <150 mg/dL in only half of the patients at LDL-C goal but with hypertriglyceridemia. Several clinical variables, including females, non-diabetic status, and history of coronary artery disease, were identified to be independently associated with reducing triglyceride levels. These results confirm that more attention is needed to subgroups, such as males or with diabetes when treating this population with Fenofibrate.

Patient Counseling Information:

Administration Instructions-

  • Take Fenofibrate only as prescribed by the doctor.

  • This drug may be taken with or without food. However, it is best to be taken with food.

  • Swallow these tablets and capsules whole and do not crush, split, or chew them.

Complications or Side Effects:

  • Pregnancy - Patients should be warned of the possible ill effects on the fetus if they take Fenofibrate during pregnancy. Limited data are available to determine the risk of major congenital disabilities in the fetus.

  • Breastfeeding - As it is unknown whether the drug will pass into breast milk, patients should be advised to stop or terminate it. Depending on individual needs and other relevant factors, this decision will rest on the doctor and the patient.

  • Hypersensitivity - Patients should be warned of the potential for severe allergic reactions, including swelling of the face, throat, tongue, and lips swelling and difficulty breathing or swallowing. They must immediately contact their physician if they experience such reactions.

  • Cholelithiasis - The drug increases cholesterol excretion into the bile leading to cholelithiasis.

  • Hematologic Changes - Long-term treatment with Fenofibrate can decrease white blood cells. Thrombocytopenia and agranulocytosis are also seen with the treatment of Fenofibrate.

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Dr. Arpit Varshney
Dr. Arpit Varshney

General Medicine

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