TRICOR (MICRONIZED)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRICOR (MICRONIZED) (TRICOR (MICRONIZED)).
Tricor (micronized fenofibrate) is a peroxisome proliferator-activated receptor alpha (PPARα) agonist that increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apolipoprotein C-III.
| Metabolism | Fenofibrate is a prodrug that is rapidly hydrolyzed by esterases to the active metabolite, fenofibric acid. Fenofibric acid is further metabolized by glucuronidation and excreted in urine. Major metabolic pathways involve hepatic glucuronidation via UGT1A1 and UGT1A3, with minor CYP-mediated metabolism (CYP3A4, CYP2C9). |
| Excretion | Primarily renal excretion of glucuronide conjugate, accounting for approximately 60-70% of elimination; fecal excretion accounts for about 25%. Minimal unchanged drug in urine. |
| Half-life | Terminal elimination half-life is approximately 20 hours (range 15-25 hours) in patients with normal renal function. Half-life is prolonged in renal impairment, requiring dose adjustment when eGFR < 30 mL/min/1.73 m². |
| Protein binding | Highly protein-bound (>99%), primarily to albumin. |
| Volume of Distribution | Apparent volume of distribution is approximately 0.5 L/kg (range 0.2-0.9 L/kg). This moderate Vd indicates limited extravascular distribution, primarily intravascular and interstitial fluid spaces. |
| Bioavailability | Oral bioavailability is approximately 66% (range 50-90%) after administration of micronized fenofibrate capsules taken with food. Absorption is enhanced by food; bioavailability is reduced when taken on an empty stomach. |
| Onset of Action | Onset of lipid-lowering effect is within 2-5 days; maximal effect on triglycerides and VLDL is observed after 3-4 weeks of oral dosing. |
| Duration of Action | Duration of lipid-lowering effect persists for several days after discontinuation; clinical effect wanes gradually over 1-2 weeks. In hypertriglyceridemia, sustained use is required to maintain effect. |
| Molecular Weight | 360.83 |
Initial 48 mg (1 tablet) orally once daily with meals. May increase to 96 mg (2 tablets) once daily with meals. Maximum dose 96 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m²). For mild to moderate impairment (eGFR 30-80 mL/min/1.73 m²), reduce dose to 48 mg once daily. Not to exceed 48 mg/day. |
| Liver impairment | Contraindicated in active liver disease or unexplained persistent liver function abnormalities. For Child-Pugh class A or B, avoid use due to potential risk; no specific dose adjustment recommendations, but cautious use only if benefit outweighs risk. Contraindicated in Child-Pugh class C. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established; use not recommended in children. |
| Geriatric use | Select dose cautiously starting at the lower end of dosing range (48 mg once daily) due to possible decreased renal function and increased risk of adverse effects. Monitor renal function and adjust accordingly. |
| 1st trimester | Fetal risk cannot be ruled out. Animal studies have shown embryotoxicity and teratogenicity at doses similar to human therapeutic doses. No adequate human studies in first trimester. |
| 2nd trimester | Use only if clearly needed and benefit outweighs risk. May cause adverse effects on fetal development based on animal data. |
| 3rd trimester | Avoid use in third trimester due to risk of preterm delivery, fetal harm, and possible neonatal complications. Discontinue prior to delivery. |
Clinical note
Comprehensive clinical and safety monograph for TRICOR (MICRONIZED) (TRICOR (MICRONIZED)).
| Placental transfer | Crosses placenta in animals; human data limited but expected to cross due to molecular weight <500 Da. |
| Breastfeeding | Excreted into breast milk in animal studies; human data lacking. Potential for serious adverse reactions in nursing infants. Decision to discontinue nursing or drug based on importance of drug to mother. |
■ FDA Black Box Warning
There is no FDA black box warning for Tricor (micronized fenofibrate).
| Serious Effects |
Severe renal impairment (eGFR <30 mL/min/1.73 m²)Active liver disease including primary biliary cirrhosisPre-existing gallbladder diseaseNursing mothers (due to potential for serious adverse reactions)Hypersensitivity to fenofibrate or any component of the formulation
| Precautions | Hepatotoxicity: elevations of serum transaminases; monitor liver function tests, Cholelithiasis: fenofibrate may increase cholesterol excretion into bile, leading to gallstones, Pancreatitis: risk may be increased, especially in patients with severe hypertriglyceridemia, Myopathy/rhabdomyolysis: risk increased when used with HMG-CoA reductase inhibitors (statins) or other fibrates, Renal impairment: dose adjustment required; contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m²) |
| Food/Dietary | Take with food to enhance absorption. Avoid grapefruit juice. Limit alcohol intake. Maintain a low-fat diet as part of triglyceride management. |
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| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: No adequate human studies; animal studies show fetal skeletal variations at high doses. Second and third trimesters: Avoid due to potential fetal harm and insufficient data. Use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor liver function tests, renal function, and creatine kinase periodically. Assess triglycerides and lipid profile. Fetal ultrasound if exposure late in pregnancy. |
| Fertility Effects | No human data on fertility impairment. Animal studies at high doses showed reduced fertility in males. Clinical significance unknown. |
| Clinical Pearls | Monitor renal function before and during therapy; reduce dose in eGFR 30-59 mL/min; contraindicated in severe renal impairment (eGFR <30 mL/min). May increase serum creatinine and transaminases. Avoid in active liver disease or unexplained persistent transaminase elevation. Risk of myopathy increases when coadministered with statins, especially in renal impairment. Can be used in combination with statins but monitor for muscle symptoms. Dose adjustment not required in mild to moderate hepatic impairment but use with caution. |
| Patient Advice | Take with food to improve absorption and reduce GI side effects. · Swallow capsules whole; do not crush, chew, or open. · Avoid consuming grapefruit juice as it may increase drug levels. · Report unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise. · May cause gallstones; report right upper abdominal pain, nausea, or vomiting. · Avoid alcohol as it may increase triglyceride levels and liver effects. · This medication is not a substitute for a healthy diet and exercise; continue lifestyle modifications. · Inform your doctor if you have kidney or liver disease, diabetes, or if you are pregnant or breastfeeding. |