Description

Simple

A medication used to lower cholesterol.

Clinical

A peroxisome proliferator receptor alpha activator used to lower LDL-C, total-C, triglycerides, and Apo B, while increasing HDL-C in hypercholesterolemia, dyslipidemia, and hypertriglyceridemia.

Overview

Fenofibrate is a fibric acid derivative like [clofibrate] and [gemfibrozil].[4] Fenofibrate is used to treat primary hypercholesterolemia, mixed dyslipidemia, severe hypertriglyceridemia.[11,12]

Fenofibrate was granted FDA approval on 31 December 1993.[10]

Pharmacology

Indication

Fenofibrate is indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C, Triglycerides, and Apo B, and to increase HDL-C adults with primary hypercholesterolemia or mixed dyslipidemia.[ Read more

Pharmacodynamic

Fenofibrate is a fibrate that activates peroxisome proliferator activated receptor alpha (PPARα) to alter lipid metabolism and treat primary hypercholesterolemia, mixed dyslipidemia, and severe hypertriglyceridemia.[ Read more

Mechanism of action

Fenofibrate activates peroxisome proliferator activated receptor alpha (PPARα), increasing lipolysis, activating lipoprotein lipase, and reducing apoprotein C-III.[ Read more

Absorption

A single 300mg oral dose of fenofibrate reaches a Cmax of 6-9.5mg/L with a Tmax of 4-6h in healthy, fasting volunteers.[ Read more

Protein binding

Fenofibrate is 99% protein bound in serum,[11,12] primarily to albumin.... Read more

Volume of distribution

The volume of distribution of fenofibrate is 0.89L/kg,[ Read more

Clearance

The oral clearance of fenofibrate is 1.1L/h in young adults and 1.2L/h in the elderly.[11, Read more

Half life

Fenofibric acid, the active metabolite of fenofibrate, has a half life of 23 hours.[11, Read more

Route of elimination

5-25% of a dose of fenofibrate is eliminated in the feces, while 60-88% is eliminated in the urine.[2, Read more

Toxicity

The oral LD50 in rats is >2g/kg and in mice is 1600mg/kg.[13] The oral TDLO in rats is 9mg/kg.[13... Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • true
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Active liver disease
      • Drugbank Id: DBCOND0107507
      • Modification Of:
        • Condition Status: active
        • Base:
          • Name: Liver Disease
          • Drugbank Id: DBCOND0028338
  • Regions: US
  • Patient Conditions:
      • Name: Renal Impairment
      • Drugbank Id: DBCOND0031781
  • Regions: US
  • Patient Conditions:
      • Name: Nursing mothers
      • Drugbank Id: DBCOND0107390
  • Regions: US
  • Patient Conditions:
      • Name: Gallbladder Disease
      • Drugbank Id: DBCOND0033389

Food Interactions

  • Take with food. Bioavailability is increased 2- to 3-fold when taken with food.

Interactions

Type in a drug name to check for interaction with Fenofibrate
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding can be increased when Fenofibrate is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding can be increased when Fenofibrate is combined with (S)-Warfarin.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Fenofibrate.
6-Deoxyerythronolide B
The metabolism of Fenofibrate can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Fenofibrate can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Fenofibrate.
Abacavir
Fenofibrate may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Fenofibrate can be increased when combined with Abatacept.
Acalabrutinib
The metabolism of Fenofibrate can be decreased when combined with Acalabrutinib.
Acarbose
Acarbose may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Fenofibrate.
Acetaminophen
The metabolism of Fenofibrate can be increased when combined with Acetaminophen.
Acetazolamide
The metabolism of Fenofibrate can be decreased when combined with Acetazolamide.
Acetohexamide
The risk or severity of hypoglycemia can be increased when Fenofibrate is combined with Acetohexamide.
Acetylsalicylic acid
The metabolism of Acetylsalicylic acid can be decreased when combined with Fenofibrate.
Acipimox
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Fenofibrate is combined with Acipimox.
Aclidinium
Fenofibrate may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Fenofibrate may decrease the excretion rate of Acrivastine which could result in a higher serum level.
13 References
  1. 1 . Wei X, Li P, Liu M, Du Y, Wang M, Zhang J, Wang J, Liu H, Liu X: Absolute oral bioavailability of fenofibric acid and choline fenofibrate in rats determined by ultra-performance liquid chromatography tandem mass spectrometry. Biomed Chromatogr. 2017 Apr;31(4). doi: 10.1002/bmc.3832. Epub 2016 Oct 10.PubMed: 27594083
  2. 2 . Chapman MJ: Pharmacology of fenofibrate. Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9.PubMed: 3318449
  3. 3 . Miller DB, Spence JD: Clinical pharmacokinetics of fibric acid derivatives (fibrates). Clin Pharmacokinet. 1998 Feb;34(2):155-62. doi: 10.2165/00003088-199834020-00003.PubMed: 9515185
  4. 4 . Balfour JA, McTavish D, Heel RC: Fenofibrate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in dyslipidaemia. Drugs. 1990 Aug;40(2):260-90. doi: 10.2165/00003495-199040020-00007.PubMed: 2226216
  5. 5 . Barbier O, Villeneuve L, Bocher V, Fontaine C, Torra IP, Duhem C, Kosykh V, Fruchart JC, Guillemette C, Staels B: The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83. Epub 2003 Feb 11.PubMed: 12582161
  6. 6 . Laizure SC, Herring V, Hu Z, Witbrodt K, Parker RB: The role of human carboxylesterases in drug metabolism: have we overlooked their importance? Pharmacotherapy. 2013 Feb;33(2):210-22. doi: 10.1002/phar.1194.PubMed: 23386599
  7. 7 . Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4.PubMed: 27599626
  8. 8 . Liu A, Patterson AD, Yang Z, Zhang X, Liu W, Qiu F, Sun H, Krausz KW, Idle JR, Gonzalez FJ, Dai R: Fenofibrate metabolism in the cynomolgus monkey using ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometry-based metabolomics. Drug Metab Dispos. 2009 Jun;37(6):1157-63. doi: 10.1124/dmd.108.025817. Epub 2009 Feb 27.PubMed: 19251819
  9. 9 . Qi C, Zhu Y, Reddy JK: Peroxisome proliferator-activated receptors, coactivators, and downstream targets. Cell Biochem Biophys. 2000;32 Spring:187-204.PubMed: 11330046
  10. 10 . FDA Approved Drug Products: Lipidil Fenofibrate Oral Capsules (Discontinued) Link
  11. 11 . FDA Approved Drug Products: Fenofibrate Oral Tablets Link
  12. 12 . FDA Approved Drug Products: Fenofibrate Oral Capsules Link
  13. 13 . Cayman Chemicals: Fenofibrate MSDS Link