Overview
11 DESCRIPTION Fenofibric acid delayed-release capsules are lipid regulating agent available as delayed release capsules for oral administration. Each delayed release capsule contains choline fenofibrate, equivalent to 45 mg or 135 mg of fenofibric acid. The chemical name for choline fenofibrate is ethanaminium, 2-hydroxy-N,N,N-trimethyl, 2-{4-(4-chlorobenzoyl)phenoxy] -2-methylpropanoate (1:1)...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The active moiety of fenofibric acid delayed-release capsules are fenofibric acid. The pharmacological effects of fenofibric acid in both animals and humans have been extensively studied through oral administration of fenofibrate. The lipid-modifying effects of fenofibric acid seen in clinical practice have been explained in vivo in transgenic mice and in vitro in human hepatocyte cultures by the activation of peroxisome proliferator activated receptor α (PPARα). Through this mechanism, fenofibric acid increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of Apo CIII (an inhibitor of lipoprotein lipase activity).
Indications
- 1 INDICATIONS AND USAGE Fenofibric acid delayed-release capsules are peroxisome proliferator-activated receptor (PPAR) alpha agonist indicated as adjunctive therapy to diet to: Reduce TG in patients with severe hypertriglyceridemia ( 1.1 ). Reduce elevated LDL-C, Total-C, TG and Apo B, and to increase HDL-C in patients with primary hypercholesterolemia or mixed dyslipidemia ( 1.2 ). Limitations of Use: Fenofibrate at a dose equivalent to 135 mg of fenofibric acid delayed-release capsules did not reduce coronary heart disease morbidity and mortality in patients with type 2 diabetes mellitus (...
Common Doses
- 45 mg
- 135 mg
Dosage
2 DOSAGE AND ADMINISTRATION Hypertriglyceridemia: 45 mg to 135 mg once daily ( 2.2 ). Primary hypercholesterolemia or mixed dyslipidemia: 135 mg once daily ( 2.3 ). Renally impaired patients: 45 mg once daily ( 2.4 ). Maximum dose: 135 mg once daily ( 2.1 ). May be taken without regard to food ( 2.1 ). 2.1 General Considerations Patients should be placed on an appropriate lipid-lowering diet before receiving fenofibric acid delayed-release capsules and should continue this diet during treatment. Fenofibric acid delayed-release capsules can be taken without regard to meals.
Contraindications
- 4 CONTRAINDICATIONS Fenofibric acid delayed-release capsules are contraindicated in: patients with severe renal impairment, including those receiving dialysis [see Clinical Pharmacology ( 12.3 )] . patients with active liver disease, including those with primary biliary cirrhosis and unexplained persistent liver function abnormalities [see Warnings and Precautions ( 5.2 )] . patients with preexisting gallbladder disease [see Warnings and Precautions ( 5.5 )] . nursing mothers [see Use in Specific Populations ( 8.2 )] .
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in the labeling: Mortality and coronary heart disease morbidity [see Warnings and Precautions ( 5.1 )] Hepatoxicity [see Warnings and Precautions ( 5.2 )] Pancreatitis [see Warnings and Precautions ( 5.7 )] Hypersensitivity reactions [see Warnings and Precautions ( 5.9 )] Venothromboembolic disease [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS Coumarin Anticoagulants: ( 7.1 ). Bile Acid Binding Resins: ( 7.2 ). Immunosuppressants: ( 7.3 ). 7.1 Coumarin Anticoagulants Potentiation of coumarin-type anticoagulant effect has been observed with prolongation of the PT/INR. Caution should be exercised when oral coumarin anticoagulants are given in conjunction with fenofibric acid. The dosage of the anticoagulant should be reduced to maintain the PT/INR at the desired level to prevent bleeding complications.