FIBRATE DOSING

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• FENOFIBRIC ACID

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• GEMFIBROZIL

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• Kidney disease
• AHA recommendations
• The AHA 2013 cholesterol treatment guidelines state that serum creatinine should be checked before, within 3 months of initiation, and every 6 months thereafter in patients receiving fenofibrates
• If GFR is < 30 ml/min, fenofibrates should not be used. If GFR is 30 - 59 ml/min, the dose of fenofibrate should not exceed 54 mg/day [19]
• Antara®
• CrCl 30 - 89 ml/min - starting dose is 30 - 43 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Fenoglide®
• CrCl 30 - 89 ml/min - starting dose is 40 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Fibricor®
• CrCl 30 - 89 ml/min - starting dose is 35 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Lipofen®
• CrCl 30 - 89 ml/min - starting dose is 50 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Lofibra® capsule
• CrCl 30 - 89 ml/min - starting dose is 67 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Lofibra® tablet
• CrCl 30 - 89 ml/min - starting dose is 54 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Lopid®
• Use with caution
• Manufacturer makes no specific dosage recommendation
• Tricor®
• CrCl 30 - 89 ml/min - starting dose is 48 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE
• Triglide®
• CrCl ≤ 89 ml/min - DO NOT USE
• Trilipix®
• CrCl 30 - 89 ml/min - starting dose is 45 mg/day; increase if tolerated
• CrCl < 30 ml/min - DO NOT USE

• Liver disease
• Fibrates have not been studied extensively in liver disease
• Manufacturers make no specific dosage recommendations
• Fibrates are contraindicated in patients with significant liver disease

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• DRUG INTERACTIONS

• NOTE: Drug interactions presented here are NOT all-inclusive. Other interactions may exist. The interactions presented here are meant to encompass commonly prescribed medications and/or interactions that are well-documented. Always consult your physician or pharmacist before taking medications concurrently. CLICK HERE for more information on drug interactions.


• All fibrates
• Bile Acid Sequestrants (Questran®, Welchol®) - Bile acid Sequestrants may interfere with the absorption of fibrates. Fibrates should be taken 1 hour before or 4 hours after bile acid sequestrants. [5,6,7]
• Colchicine (Colcrys®) - Muscle toxicity including rhabdomyolysis has been reported in patients taking fenofibrates with colchicine. Use caution when prescribing together.
• Ezetimibe (Zetia®) - Both ezetimibe and fibrates may increase cholesterol excretion into the bile. This may increase the risk of gallstones in susceptible patients. Gemfibrozil and fenofibrate both increase blood levels of ezetimibe. The significance of this interaction is unknown.
• Immunosuppressants - immunosuppressants such as cyclosporine and tacrolimus can be nephrotoxic and this may reduce the elimination of fibrates. Use caution when combining fibrates with these medications.
• Warfarin (Coumadin®) - Fibrates may interfere with warfarin therapy. Monitor INR levels when adding fibrates to warfarin. [5,6,7]


• Gemfibrozil (Lopid®)
• CYP2C8 substrates - Gemfibrozil is a CYP2C8 strong inhibitor. It may increase blood levels of CYP2C8 substrates.
• Dasabuvir (Viekira Pak™) - Gemfibrozil can increase dasabuvir blood levels, and they should not be taken together
• Enzalutamide (Xtandi®) - Gemfibrozil may increase blood levels of enzalutamide and increase the risk of seizures. Enzalutamide doses should be reduced when given with gemfibrozil.
• Glitazones (pioglitazone, rosiglitazone, Actos®, Avandia®) - Gemfibrozil may increase blood levels of pioglitazone and rosiglitazone. Doses of pioglitazone should not exceed 15 mg when taken with gemfibrozil.
• OATP1B1 substrates - Gemfibrozil is a OATP1B1 inhibitor. It may increase blood levels of OATP1B1 substrates.
• Repaglinide (Prandin®) - Gemfibrozil can block the metabolism of repaglinide, and they should not be taken together
• Selexipag (Uptravi®) - Gemfibrozil has been shown to double selexipag levels and increase exposure to its active metabolite 11-fold. Concomitant administration is not recommended.
• Statins (Lipitor®, Zocor®, Crestor®, etc)
• Gemfibrozil should not be taken with simvastatin
• Gemfibrozil should not be taken with rosuvastatin. If concomitant use cannot be avoided, the starting dose of rosuvastatin should be 5 mg once daily, and doses should not exceed 10 mg/day.
• When gemfibrozil is prescribed with other statins, the risk of muscle toxicity (rhabdomyolysis) is increased [5,6]
• Fenofibrates do not appear to increase the risk of muscle toxicity, and they have been safely used with statins in a number of trials [6,11,12]

• Metabolism and clearance
• Gemfibrozil (Lopid®)
• CYP2C8 - strong inhibitor
• CYP2C9 - inhibitor
• CYP2C19 - inhibitor
• CYP1A2 - inhibitor
• OATP1B1 - inhibitor
• UGT1A1 and 1A3 - inhibitor


• Fenofibrate (Antara®, Fenoglide®, Lipofen®, Lofibra®, Tricor®, Triglide®)
• CYP2C9 - mild-moderate inhibitor
• CYP2C8 - weak inhibitor
• CYP2C19 - weak inhibitor
• CYP2A6 - weak inhibitor


• Fenofibric acid (Trilipix®, Fibricor®)
• CYP2C9 - mild-moderate inhibitor
• CYP2C8 - weak inhibitor
• CYP2C19 - weak inhibitor
• CYP2A6 - weak inhibitor

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• PRICE ($) INFO

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• BIBLIOGRAPHY

• Manufacturer's Package insert