Usage
- Choline fenofibrate is prescribed to lower high levels of cholesterol and triglycerides (a type of fat) in the blood. It is specifically used for primary hypercholesterolemia or mixed dyslipidemia (high cholesterol and triglycerides) and severe hypertriglyceridemia. It may also be used in combination with statins when other treatments have not effectively controlled cholesterol and triglyceride levels.
- Pharmacological classification: Antihyperlipidemic agent, specifically a fibrate.
- Mechanism of action: Choline fenofibrate activates peroxisome proliferator-activated receptor alpha (PPARα). This action leads to several beneficial effects on lipid metabolism, including increased lipoprotein lipase activity (breaks down triglycerides), reduced triglyceride production, and increased HDL (“good”) cholesterol levels.
Alternate Names
- Trilipix (brand name)
- Fibricor (brand name)
How It Works
- Pharmacodynamics: Choline fenofibrate primarily affects lipid metabolism by activating PPARα. This results in decreased triglyceride levels, increased HDL cholesterol, and modest reductions in LDL (“bad”) cholesterol. It can also reduce levels of apolipoprotein C-III, which plays a role in triglyceride metabolism.
- Pharmacokinetics: Choline fenofibrate is readily absorbed orally, with peak plasma concentrations achieved within 2 to 4 hours. It is hydrolyzed to its active metabolite, fenofibric acid, which is highly protein-bound. Fenofibric acid undergoes conjugation with glucuronic acid and is eliminated mainly through the kidneys, with a half-life of approximately 20 hours. Dose adjustment is needed in renal impairment.
- Mode of action: Choline fenofibrate’s mechanism involves binding to and activating PPARα, a nuclear receptor involved in gene regulation of various metabolic processes, including lipid metabolism. PPARα activation leads to increased lipoprotein lipase activity, decreased triglyceride production in the liver, and enhanced clearance of triglyceride-rich particles from the blood.
- Elimination pathways: Primarily renal excretion, with some fecal elimination.
Dosage
Standard Dosage
Adults:
- Mixed Dyslipidemia: 135 mg orally once daily.
- Severe Hypertriglyceridemia: 45-135 mg orally once daily, titrated based on lipid levels and response. Maximum dose is 135mg.
- Primary Hyperlipidemia: 135 mg once daily.
Children:
- Not established. Use is generally not recommended for patients under 18 years.
Special Cases:
- Elderly Patients: Initial dose of 45 mg once daily is recommended in elderly patients. Dose adjustments should be made based on renal function.
- Patients with Renal Impairment: Mild to moderate renal impairment (creatinine clearance 30-80 mL/min): Starting dose of 45 mg once daily, titrated cautiously based on response. Severe renal impairment (creatinine clearance <30 mL/min): Avoid use.
- Patients with Hepatic Dysfunction: Not studied; use with caution.
- Patients with Comorbid Conditions: Diabetes: Monitor closely for potential drug interactions and adverse effects. Monitor glycemic control. Hypothyroidism: Increased risk of myopathy.
Clinical Use Cases
- Choline fenofibrate is not typically indicated for use in acute clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its role is in chronic lipid management.
Dosage Adjustments
- Renal impairment requires dosage adjustments based on creatinine clearance.
- Hepatic dysfunction: use with caution and consider lower doses.
Side Effects
Common Side Effects
- Gastrointestinal issues (diarrhea, stomach pain, nausea, flatulence)
- Headache, back pain
- Respiratory tract infections
Rare but Serious Side Effects
- Myopathy (muscle pain, tenderness, weakness), potentially progressing to rhabdomyolysis (muscle breakdown)
- Liver enzyme elevations (monitor liver function tests)
- Gallstones
Long-Term Effects
- Cholelithiasis with long term use
- Potential for liver or muscle issues with prolonged use.
Adverse Drug Reactions (ADR)
- Rhabdomyolysis
- Severe allergic reactions (rare)
Contraindications
- Hypersensitivity to fenofibrate or its components
- Severe renal impairment
- Active liver disease (including primary biliary cirrhosis and unexplained persistent liver abnormalities)
- Preexisting gallbladder disease
- Nursing mothers
Drug Interactions
- Statins (increased risk of myopathy)
- Anticoagulants (e.g., warfarin - enhanced blood-thinning effects)
- Bile acid sequestrants (reduced absorption of choline fenofibrate)
- Immunosuppressants (e.g., cyclosporine - altered efficacy)
- Alcohol (increased risk of muscle problems)
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C. Avoid use during pregnancy unless the potential benefits outweigh the risks.
- Not recommended during breastfeeding due to potential risk to infant. Discontinue breastfeeding or avoid choline fenofibrate.
Drug Profile Summary
- Mechanism of Action: PPARα agonist, leading to decreased triglycerides, increased HDL, and modest LDL reduction.
- Side Effects: Diarrhea, stomach pain, back pain, headache, respiratory infections. Rarely: Myopathy, liver enzyme elevations, gallstones.
- Contraindications: Hypersensitivity, severe renal impairment, active liver disease, gallbladder disease, breastfeeding.
- Drug Interactions: Statins, anticoagulants, bile acid sequestrants, immunosuppressants.
- Pregnancy & Breastfeeding: Avoid use.
- Dosage: Adults: 135 mg once daily for mixed dyslipidemia. 45-135 mg once daily for hypertriglyceridemia. Adjust for renal impairment.
- Monitoring Parameters: Lipid panel, liver function tests, renal function (especially if impaired), creatine kinase (if muscle symptoms occur).
Popular Combinations
- Atorvastatin + Choline Fenofibrate: Combination used for the treatment of mixed dyslipidemia when statin therapy alone doesn’t adequately control lipid levels.
Precautions
- General Precautions: Monitor liver and kidney function. Evaluate for preexisting gallbladder disease. Screen for myopathy.
- Specific Populations:
- Pregnant Women: Avoid use.
- Breastfeeding Mothers: Contraindicated.
- Children & Elderly: Not recommended for children. Elderly: Start with lower doses.
- Lifestyle Considerations: Low-fat diet and regular exercise are important adjuncts to therapy. Limit alcohol intake.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Choline fenofibrate?
A: 135 mg orally once daily for mixed dyslipidemia or primary hyperlipidemia. For severe hypertriglyceridemia 45–135 mg once daily. Lower doses may be needed for elderly or renally impaired patients.
Q2: How does Choline fenofibrate differ from other fibrates?
A: It is a prodrug of fenofibric acid, providing similar lipid-lowering effects. It is available in specific delayed-release formulations which can affect the dosing compared to other fibrates.
Q3: What are the most serious side effects to watch out for?
A: Myopathy (muscle pain/weakness) and rhabdomyolysis (muscle breakdown) are rare but serious. Elevated liver enzymes and gallstones can also occur.
Q4: Can Choline fenofibrate be used with statins?
A: It can be, but with caution. The combination increases the risk of myopathy. Close monitoring of muscle symptoms and creatine kinase levels is necessary.
Q5: Is Choline fenofibrate safe in pregnancy?
A: It is generally avoided during pregnancy unless the benefits clearly outweigh the risks.
Q6: What should patients know about taking Choline fenofibrate?
A: Take as directed, usually once daily with or without food. Report muscle pain or weakness to your doctor immediately. Maintain a healthy lifestyle with diet and exercise.
Q7: How long does it take for Choline fenofibrate to work?
A: Effects on lipid levels can usually be seen within a few weeks, but optimal benefits may take several months.
Q8: Does Choline fenofibrate interact with alcohol?
A: Yes, alcohol can increase the risk of muscle-related side effects. It is best to limit alcohol consumption while taking this medication.
Q9: What should be monitored in patients on Choline fenofibrate?
A: Lipid profile, liver function tests, renal function tests (especially in patients with renal impairment), and creatine kinase levels (if muscle symptoms occur) should be monitored.
Q10: Can it be used in patients with liver disease?
A: It should be used with caution in patients with mild to moderate liver disease. Avoid use in patients with severe liver disease. Close monitoring is recommended.
