LIPOFEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIPOFEN (LIPOFEN).
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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIPOFEN (LIPOFEN).
| Breastfeeding | Fenofibrate is excreted in breast milk in rats; no human data. M/P ratio unknown. Due to potential for adverse effects in nursing infants, avoid use during breastfeeding or discontinue nursing. |
| 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. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Severe renal impairment (eGFR < 30 mL/min/1.73 m²)","Active liver disease including primary biliary cirrhosis and unexplained persistent liver function abnormalities","Pre-existing gallbladder disease","Known hypersensitivity to fenofibrate or any formulation components","Nursing mothers"]
| 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."] |
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| 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. |