Fenofibrate information from DrugsUpdate
L - Contraindicated in lactation
FI - Food *
LI - Lab *
Fenofibrate is a drug of the fibrate class. Fenofibrate was discovered by Groupe Fournier SA, before it was acquired in 2005 by Solvay Pharmaceutical, a business unit owned by the Belgian corporation, Solvay S.A. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease. Like other fibrates, it reduces both low-density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels, as well as increasing high-density lipoprotein (HDL) levels and reducing tryglycerides level. It also appears to have a beneficial effect on the insulin resistance featured by the metabolic syndrome. It is used alone or in conjunction with statins in the treatment of hypercholesterolemia and hypertriglyceridemia. Fenofibrate is sold under the brand name Tricor and Trilipix by Abbott Labs, Lipofen by Kowa Pharmaceuticals America Inc, Lofibra by Teva, Lipanthyl and Lipidil by Solvay Pharmaceutical, Fenocor-67 by Ordain Health Care Pvt Ltd and Fenogal by SMB Laboratories
A variety of clinical studies have demonstrated that elevated levels of total cholesterol (total-C), low density lipoprotein cholesterol (LDL-C), and apolipoprotein B (apo B), an LDL membrane complex, are risk factors for human atherosclerosis. Similarly, decreased levels of high density lipoprotein cholesterol (HDL-C) and its transport complex, apolipoprotein A (apo AI and apo AII) are risk factors for the development of atherosclerosis. Epidemiologic investigations have established that cardiovascular morbidity and mortality vary directly with the level of total-C, LDL-C, and triglycerides, and inversely with the level of HDL-C. The independent effect of raising HDL-C or lowering triglycerides (TG) on the risk of cardiovascular morbidity and mortality has not been determined. Fenofibric acid, the active metabolite of Fenofibrate, produces reductions in total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides, and triglyceride-rich lipoprotein (VLDL) in treated patients. In addition, treatment with Fenofibrate results in increases in high density lipoprotein (HDL) and apoproteins apo AI and apo AII.
Absorption Well absorbed. Absolute bioavailability is approximately 81%. T max within 4 to 5 h.
Distribution Protein binding is approximately 99%. Steady state is achieved within 8 days.
Metabolism Primarily conjugated with glucuronic acid. Small amount is reduced to a benzhydrol metabolite.
Elimination Primarily excreted in the urine (60%) in the form of fenofibric acid and fenofibric acid glucuronide. Approximately 25% is excreted in the feces. Elimination half-life is approximately 20 h.
CNS Delayed-release Headache (13%); dizziness (4%); insomnia (3%); fatigue (2%). Immediate-Release Headache (3%). Postmarketing Asthenia. EENT Delayed-release Nasopharyngitis (4%). Immediate-release Rhinitis (2%). GI Delayed-release Diarrhea, dyspepsia, nausea (4%); constipation (3%). Immediate-release Abdominal pain (5%); constipation, nausea (2%). Postmarketing Abdominal pain, pancreatitis. Genitourinary Postmarketing Acute renal failure, renal failure. Hepatic Postmarketing Cirrhosis, hepatitis. Hematologic-Lymphatic Postmarketing Anemia. Lab Tests Delayed-release Increased ALT (1%). Immediate-release Increased ALT, AST, and CPK (3%). Musculoskeletal Delayed-release Back pain (6%); pain in extremities (5%); arthralgia (4%); myalgia (3%). Immediate-release Back pain (3%). Postmarketing Muscle spasms, rhabdomyolysis. Respiratory Delayed-release Upper respiratory tract infection (5%); sinusitis (3%). Miscellaneous Delayed-release Pain (4%).
Monitor Perform regular periodic monitoring of liver function for duration of therapy. Evaluate serum lipids periodically (eg, 4 to 8 wk) during initial therapy to determine lowest effective dose; withdraw therapy if an adequate response is not achieved after 2 mo of treatment with the max dose. Perform periodic blood cell counts during first 12 mo of therapy.
Renal or Hepatic impairment. Monitor LFTs & blood count regularly. Increased risk of cholelithiasis, pancreatic, skeletal muscle effects. Withdraw treatment if no adequate response after two months of treatment at max recommended dose.
Coumarin Anticoagulants Caution should be exercised when coumarin anticoagulants are given in conjunction with Fenoglide. The dosage of the anticoagulants should be reduced to maintain the prothrombin time/INR at the desired level to prevent bleeding complications. Frequent prothrombin time/INR determinations are advisable until it has been definitely determined that the prothrombin time/INR has stabilized. Cyclosporine Because cyclosporine can produce nephrotoxicity with decreases in creatinine clearance and rises in serum creatinine, and because renal excretion is the primary elimination route of fibrate drugs including Fenoglide, there is a risk that an interaction will lead to deterioration of renal function. The benefits and risks of using Fenoglide with immunosuppressants and other potentially nephrotoxic agents should be carefully considered, and the lowest effective dose employed. HMG-CoA Reductase Inhibitors The combined use of fenofibric acid derivatives, particularly gemfibrozil, and HMG-CoA reductase inhibitors results in an increased risk of rhabdomyolysis and myoglobinuria leading in a high proportion of cases to acute renal failure. [See Concomitant HMG-CoA Reductase Inhibitors (5.11)] The combined use of Fenoglide and HMG-CoA reductase inhibitors should be avoided unless the benefit of further alterations in lipid levels is likely to outweigh the increased risk of this drug combination. In a single-dose drug interaction study in 23 healthy adults the concomitant administration of Fenofibrate and pravastatin resulted in no clinically important difference in the pharmacokinetics of fenofibric acid, pravastatin, or its active metabolite 3α-hydroxy iso-pravastatin when compared to either drug given alone. Bile-Acid Resins Since bile acid sequestrants may bind other drugs given concurrently, patients should take Fenoglide at least 1 hour before or 4-6 hours after a bile acid binding resin to avoid impeding its absorption.
40 mg: White to off-white oval tablets. Debossed "FLO". 120 mg: White to off-white oval tablets. Debossed "FHI".
List of Contraindications
Contraindicated in pregnancy Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindicated in lactation
Safety and efficacy not established.
Use with caution because decreased renal function is more likely in this age group.
Fenofibrate is contra-indicated in children, during pregnancy or lactation, in patients with liver insufficiency, presence of gallstones, renal insufficiency, in patients hypersensitive to fenofibrate and/or excipients, known photoallergy or phototoxic reaction during treatment with fibrates or ketoprofen.
Antara , Fenoglide , Lipofen , Tricor , Trilipix , Triglide Store at 59 °) to 86 °) F. Protect from light and moisture. Fenofibrate tablets, Lofibra tablets and capsules Store at 68 °) to 77 °) F. Protect from moisture.