LIPOFEN
Clinical safety rating
cautionComprehensive clinical and safety monograph for LIPOFEN (LIPOFEN).
Comprehensive clinical and safety monograph for LIPOFEN (LIPOFEN).
Adjunct to diet for treatment of hypertriglyceridemia (Fredrickson types IV and V hyperlipidemia)Adjunct to diet for treatment of primary hypercholesterolemia or mixed dyslipidemia (Fredrickson types IIa and IIb) when statins are contraindicated or not tolerated
Lipofen (fenofibrate) is a peroxisome proliferator-activated receptor alpha (PPARα) agonist. It activates PPARα, which increases lipolysis and elimination of triglyceride-rich particles from plasma by stimulating lipoprotein lipase activity and reducing apolipoprotein C-III production. This leads to decreased triglyceride levels and increased HDL cholesterol.
| Metabolism | Primarily metabolized by glucuronidation via UDP-glucuronosyltransferases (UGT1A1, UGT1A3, UGT2B7) to fenofibric acid, the active metabolite. Minor CYP450 involvement (CYP3A4, CYP2C8, CYP2C19). Renal elimination of conjugates and unchanged drug. |
| Excretion | Primarily renal (90% as unchanged drug), with <5% fecal. |
| Half-life | 5-7 hours (prolonged in renal impairment; may exceed 24 hours in severe CKD). |
| Protein binding | >99% bound to albumin. |
| Volume of Distribution | Approximately 0.5 L/kg (low, indicating minimal tissue distribution). |
| Bioavailability | Oral: 30% (first-pass effect; absorption increased with food). |
| Onset of Action | Oral: 2-4 weeks for significant lipid reduction. |
| Duration of Action | Lipid effects persist for several weeks after discontinuation; optimal effect at 6-8 weeks. |
| Molecular Weight | 408.57 |
For hypertriglyceridemia: 67-134 mg (as fenofibric acid) orally three times daily with meals. Maximum dose 200 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 50% (e.g., 67 mg once daily). GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh Class A: no dose adjustment. Child-Pugh Class B or C: contraindicated due to risk of hepatotoxicity. |
| Pediatric use | Not recommended in children <18 years; safety and efficacy not established. |
| Geriatric use | Start at lower end of dosing range; monitor renal function and adjust accordingly. |
| 1st trimester | Contraindicated. Risk of fetal harm; animal studies show embryotoxicity and teratogenicity. |
| 2nd trimester | Contraindicated. Potential for impaired fetal liver development and lipid metabolism. |
| 3rd trimester | Contraindicated. May interfere with fetal lung maturity and essential fatty acid supply. |
Clinical note
Comprehensive clinical and safety monograph for LIPOFEN (LIPOFEN).
| Placental transfer | Extensive placental transfer demonstrated in animal studies; human data limited but expected to cross. |
| Breastfeeding | Excreted in human milk; potential for serious adverse effects in nursing infants. Decision to discontinue nursing or drug based on importance of drug to mother. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | LIPOFEN (fenofibrate) is classified as FDA Pregnancy Category C. Animal studies have shown embryotoxicity and teratogenicity at high doses, but no adequate human studies exist. First trimester: potential risk of congenital anomalies cannot be ruled out. Second and third trimesters: may cause fetal skeletal abnormalities and growth retardation; risk of neonatal complications if used near term. Contraindicated in pregnancy unless clearly needed. |
| Fetal Monitoring | Monitor liver function tests (ALT, AST) and renal function (serum creatinine) at baseline and periodically. Check lipid profile. In pregnant women, monitor fetal growth and development via ultrasound. Observe for signs of myopathy or rhabdomyolysis. |
| Fertility Effects | Fenofibrate has not been studied for effects on human fertility. Animal studies show no impairment of fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
PregnancySevere hepatic impairmentGallbladder diseaseNursing mothersHypersensitivity to fenofibrate
| Precautions | Hepatotoxicity: Elevations of serum transaminases; monitor liver function. Discontinue if ALT > 3x ULN., Cholelithiasis: Increases cholesterol excretion into bile, risk of gallstones., Pancreatitis: Has been reported, especially during initiation or dose escalation., Myopathy/Rhabdomyolysis: Risk increased when co-administered with statins., Renal impairment: Dose adjustment required. Use with caution in patients with serum creatinine > 2.0 mg/dL., Venothromboembolic disease: Increased risk of pulmonary embolism and deep vein thrombosis in some trials. |
| Food/Dietary | Take with food to enhance bioavailability. Avoid high-fat meals immediately before dosing as they may delay absorption. Grapefruit juice has no significant interaction. Alcohol should be limited or avoided due to potential for increased triglyceride levels and hepatotoxicity. No specific restriction on caffeine. Ensure adequate hydration to prevent renal complications. |
| Clinical Pearls | LIPOFEN (fenofibrate) is a PPAR-alpha agonist that reduces triglycerides and increases HDL-C. Monitor renal function before initiation and periodically; dose adjustment required if eGFR <60 mL/min/1.73m2. Avoid use in severe renal impairment (eGFR <30). May increase serum creatinine transiently. Increases risk of cholelithiasis due to cholesterol supersaturation. Concomitant statin therapy increases risk of myopathy; monitor for muscle symptoms. Use with caution in patients with hepatic impairment; contraindicated in active liver disease. May potentiate effect of oral anticoagulants; monitor INR. |
| Patient Advice | Take with meals to improve absorption. Do not break, crush, or chew capsules. · Avoid alcohol consumption as it can increase triglyceride levels and risk of liver damage. · Report unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise. · Notify your doctor if you develop abdominal pain, nausea, or jaundice (yellowing of skin/eyes). · Maintain a low-fat diet and exercise regularly to maximize lipid-lowering benefits. · Do not take supplements containing red yeast rice or niacin without consulting your physician. |
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