LIPIDIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for LIPIDIL (LIPIDIL).
Comprehensive clinical and safety monograph for LIPIDIL (LIPIDIL).
Primary hypercholesterolemia or mixed dyslipidemia (as adjunct to diet)Severe hypertriglyceridemiaPrevention of pancreatitis in patients with hypertriglyceridemia
Nausea Muscle pain Increased transaminase level in blood Upper respiratory tract infection
LIPIDIL (fenofibrate) is a fibric acid derivative that activates peroxisome proliferator-activated receptor-alpha (PPAR-alpha), leading to increased lipolysis and clearance of triglyceride-rich particles, and increased synthesis of apolipoproteins A-I and A-II.
| Metabolism | Fenofibrate is metabolized primarily by glucuronidation; fenofibric acid is further metabolized via reduction to benzhydrol metabolite. Minor involvement of CYP450 enzymes, predominantly CYP3A4. |
| Excretion | Primarily renal excretion of glucuronide conjugates; approximately 70% of a single oral dose is recovered in urine (mostly as fenofibric acid glucuronide), and about 6% is excreted in feces. |
| Half-life | Terminal elimination half-life of fenofibric acid is approximately 20 hours (range 15-25 hours). This supports once-daily dosing; steady-state is achieved after ~5 days. |
| Protein binding | Fenofibric acid is highly bound to plasma proteins, primarily albumin, with >99% binding. |
| Volume of Distribution | Apparent volume of distribution (Vd/F) is approximately 0.9 L/kg, indicating distribution into total body water. |
| Bioavailability | Absolute bioavailability of fenofibrate (prodrug) is not determined; fenofibrate is rapidly converted to fenofibric acid with a relative bioavailability of approximately 81-96% compared to the micronized formulation when taken with food. Absorption is enhanced when taken with meals. |
| Onset of Action | Significant reductions in triglycerides and LDL-C are observed within 2 weeks of oral therapy; maximal effect typically by 4-8 weeks. |
| Duration of Action | With once-daily dosing, lipid-lowering effects persist over the 24-hour dosing interval. Upon discontinuation, lipid levels return to baseline within several weeks. |
| Molecular Weight | 361.59 |
130 mg orally once daily.
| Dosage form | CAPSULE |
| Renal impairment | GFR 30-89 mL/min: 130 mg once daily; GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh class A: 130 mg once daily; Child-Pugh class B or C: contraindicated. |
| Pediatric use | Not recommended for use in pediatric patients. |
| Geriatric use | No dose adjustment required, but monitor renal function due to age-related decline. |
| 1st trimester | Contraindicated due to risk of fetal harm (animal studies show embryotoxicity). |
| 2nd trimester | Contraindicated; no adequate human studies, animal studies show fetal risk. |
| 3rd trimester | Contraindicated; may interfere with fetal lipid metabolism and cause neonatal complications. |
Clinical note
Comprehensive clinical and safety monograph for LIPIDIL (LIPIDIL).
| Placental transfer | Crosses placenta in humans; levels in fetal circulation are approximately 10-20% of maternal serum levels. |
| Breastfeeding | Excreted in human milk; potential for serious adverse reactions in nursing infants, including interference with lipid metabolism. Decision to discontinue nursing or drug based on importance of drug to mother. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | Lipidil (fenofibrate) is contraindicated in pregnancy. Animal studies show fetal toxicity at high doses. Human data are insufficient, but risk cannot be excluded. First trimester: possible embryotoxicity; second and third trimesters: potential for fetal harm due to interference with lipid metabolism. |
| Fetal Monitoring | Monitor hepatic function, renal function, and lipid profiles periodically. Avoid use during pregnancy; if unintentional exposure occurs, assess fetal well-being via ultrasound for growth parameters and organogenesis. |
| Fertility Effects | Animal studies have shown effects on spermatogenesis and fertility at high doses. Human data are lacking; potential for reversible impairment of fertility in males and females should be considered. |
■ FDA Black Box Warning
There is no FDA black box warning for LIPIDIL.
| Common Effects | Nausea Muscle pain Increased transaminase level in blood Upper respiratory tract infection |
| Serious Effects |
Severe hepatic impairmentPregnancyBreastfeedingGallbladder diseaseHypersensitivity to fenofibrate or any excipient
| Precautions | Hepatotoxicity: elevated liver enzymes reported; monitor liver function, Myopathy/rhabdomyolysis: increased risk when combined with statins or in renal impairment, Renal impairment: dose adjustment required; avoid in severe renal impairment, Cholelithiasis: increased bile cholesterol saturation may lead to gallstones, Pancreatitis: despite triglyceride reduction, pancreatitis can occur |
| Food/Dietary | Take with food to enhance absorption. Avoid high-fat meals that may exacerbate hypertriglyceridemia. Grapefruit juice has minimal interaction but caution is advised with statin combinations. Alcohol should be limited or avoided due to potential for elevated triglycerides and hepatotoxicity. |
| Clinical Pearls | Lipidil (fenofibrate) is a PPARα agonist used primarily for severe hypertriglyceridemia and mixed dyslipidemia. Monitor renal function at baseline and periodically; reduce dose in CKD (eGFR <60 mL/min). Avoid in severe hepatic impairment or gallbladder disease. Combines with statins but increases risk of myopathy; monitor for muscle symptoms. May raise serum creatinine and homocysteine levels. Tablet should be swallowed whole; do not crush or chew. |
| Patient Advice | Take with food to improve absorption and reduce stomach upset. · Avoid alcohol as it can worsen triglyceride levels and liver effects. · Report unexplained muscle pain, tenderness, or weakness immediately. · Inform your doctor if you have kidney or liver disease, or gallbladder problems. · This medication may increase the effects of blood thinners (warfarin); monitor INR closely. · Do not take if you are pregnant or breastfeeding without consulting your doctor. |
Loading safety data…