Description

Simple

A medication used to lower the amount of cholesterol in the blood and decrease the chance of having a heart attack or stroke.

Clinical

A lipid regulator that is used in the reduction of serum triglyceride levels in high-risk patients with hyperlipidemia.

Overview

Gemfibrozil is a fibric acid agent, similar to [clofibrate], used to treat Type IIb, IV, and V hyperlipidemias.[3,11] Gemfibrozil is not a first line treatment and is prescribed to patients who have not responded adequately to weight loss, diet, exercise, and other medications.[11]

Gemfibrozil was granted FDA approval on 21 December 1981.[11]

Pharmacology

Indication

Gemfibrozil is indicated to treat patients with Types IV and V hyperlipidemia who have elevated serum triglycerides (usually above 2000mg/dL), elevated VLDL cholesterol, fasting chylomicrons, are at risk of developing pancreatitis, and do not adequately respond to dietary restrictions.[ Read more

Pharmacodynamic

Gemfibrozil alters lipid metabolism to treat patients with hyperlipidemia.[11] The duration of action requires twice daily dosing as the mean residence time of gemfibrozil is up to 9.6h... Read more

Mechanism of action

Gemfibrozil activates peroxisome proliferator-activated receptor-α (PPARα), which alters lipid metabolism.[3] This activation leads to increased HDL, apo AI, apo AII, lipoprotein lipase (... Read more

Absorption

Gemfibrozil is absorbed from the gastrointestinal tract.[11]

In healthy volunteers, a 900mg oral dose of gemfibrozil has a Cmax of 46±16µg/mL with a Tmax of 2.2±... Read more

Protein binding

Gemfibrozil is 99% protein bound.[3, Read more

Volume of distribution

The volume of distribution of gemfibrozil is estimated to be 0.8L/kg.[ Read more

Clearance

The clearance of gemfibrozil is estimated to be 6.0L/h.[ Read more

Half life

Gemfibrozil has a plasma half-life of 1.5 hours.[11] In patients with renal failure the half life is 2.4h and in patients with liver disease the half life is 2.1h.[ Read more

Route of elimination

Approximately 70% of a dose of gemfibrozil is eliminated in the urine.[11] The majority of a dose is eliminated as a glucuronide conjugate and Read more

Toxicity

The oral TDLO of gemfibrozil in humans is 18gm/kg/3Y.[12] The oral LD50 in mice is 2218mg/kg and in rats is 1414mg/kg.[ Read more

Adverse Effects

Contraindications

  • Regions: US
  • With Drugs:
      • Name: Selexipag
      • Drugbank Id: DB11362
  • Regions: US
  • With Drugs:
      • Name: Dasabuvir
      • Drugbank Id: DB09183
  • Regions: US
  • With Drugs:
      • Name: Simvastatin
      • Drugbank Id: DB00641
  • Regions: US
  • With Drugs:
      • Name: Repaglinide
      • Drugbank Id: DB00912
  • Hypersensitivity:
    • true
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Primary Biliary Cirrhosis
      • Drugbank Id: DBCOND0035493
      • Modification Of:
        • Condition Status: primary
        • Base:
          • Name: Biliary cirrhosis
          • Drugbank Id: DBCOND0013178
  • Regions: US
  • Patient Conditions:
      • Name: Preexisting gallbladder disease
      • Drugbank Id: DBCOND0108302
  • Regions: US
  • Patient Conditions:
      • Name: Hepatic dysfunction
      • Drugbank Id: DBCOND0094733
  • Regions: US
  • Patient Conditions:
      • Name: Severe renal dysfunction
      • Drugbank Id: DBCOND0108301
      • Modification Of:
        • Base:
          • Name: Renal Dysfunction
          • Drugbank Id: DBCOND0034336
        • Severity:
          • Includes:
            • severe

Food Interactions

  • Take before a meal. Take 30 minutes before meals.

Interactions

Type in a drug name to check for interaction with Gemfibrozil
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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 metabolism of (R)-warfarin can be decreased when combined with Gemfibrozil.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Gemfibrozil.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Gemfibrozil is combined with 4-hydroxycoumarin.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Gemfibrozil.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Gemfibrozil.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Gemfibrozil.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Gemfibrozil.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Gemfibrozil.
Abacavir
The metabolism of Abacavir can be decreased when combined with Gemfibrozil.
Acarbose
Acarbose may decrease the excretion rate of Gemfibrozil which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Gemfibrozil which could result in a higher serum level.
Acefylline
The metabolism of Acefylline can be decreased when combined with Gemfibrozil.
Acemetacin
Acemetacin may decrease the excretion rate of Gemfibrozil which could result in a higher serum level.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Gemfibrozil.
Acetaminophen
Acetaminophen may decrease the excretion rate of Gemfibrozil which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Gemfibrozil which could result in a lower serum level and potentially a reduction in efficacy.
Acetohexamide
The metabolism of Acetohexamide can be decreased when combined with Gemfibrozil.
Acetylsalicylic acid
The metabolism of Acetylsalicylic acid can be decreased when combined with Gemfibrozil.
Acipimox
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Gemfibrozil is combined with Acipimox.
Aclidinium
Gemfibrozil may decrease the excretion rate of Aclidinium which could result in a higher serum level.
12 References
  1. 1 . Saku K, Gartside PS, Hynd BA, Kashyap ML: Mechanism of action of gemfibrozil on lipoprotein metabolism. J Clin Invest. 1985 May;75(5):1702-12. doi: 10.1172/JCI111879.PubMed: 3923042
  2. 2 . Okerholm RA, Keeley FJ, Peterson FE, Glazko AJ: The metabolism of gemfibrozil. Proc R Soc Med. 1976;69 Suppl 2:11-4.PubMed: 828261
  3. 3 . Quintanilla Rodriguez BS, Correa R: Gemfibrozil .PubMed: 31424850
  4. 4 . Mano Y, Usui T, Kamimura H: The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4. doi: 10.1124/dmd.107.017269. Epub 2007 Aug 1.PubMed: 17670842
  5. 5 . Sallustio BC, Fairchild BA, Pannall PR: Interaction of human serum albumin with the electrophilic metabolite 1-O-gemfibrozil-beta-D-glucuronide. Drug Metab Dispos. 1997 Jan;25(1):55-60.PubMed: 9010630
  6. 6 . Hamberger C, Barre J, Zini R, Taiclet A, Houin G, Tillement JP: In vitro binding study of gemfibrozil to human serum proteins and erythrocytes: interactions with other drugs. Int J Clin Pharmacol Res. 1986;6(6):441-9.PubMed: 3468088
  7. 7 . Knauf H, Kolle EU, Mutschler E: Gemfibrozil absorption and elimination in kidney and liver disease. Klin Wochenschr. 1990 Jul 5;68(13):692-8. doi: 10.1007/bf01667018.PubMed: 2381138
  8. 8 . Fereshetian AG, Davidson M, Haber H, Black DM: Gemfibrozil treatment in patients with elevated lipoprotein a: a pilot study. Clin Drug Investig. 1998;16(1):1-7. doi: 10.2165/00044011-199816010-00001.PubMed: 18370512
  9. 9 . Takahiro M, Haruo I, Toshihiko, I: Identification of Gemfibrozil Metabolites, Produced as Positional Isomers in Human Liver Microsomes, by On-line Analyses Using Liquid Chromatography/Mass Spectrometry and Liquid Chromatography/Nuclear Magnetic Resonance Spectroscopy J. Mass Spectrom. Soc. Jpn.. 2004 Jun 6;52(5):277-283.PubMed:
  10. 10 . Varma MV, Lin J, Bi YA, Kimoto E, Rodrigues AD: Quantitative Rationalization of Gemfibrozil Drug Interactions: Consideration of Transporters-Enzyme Interplay and the Role of Circulating Metabolite Gemfibrozil 1-O-beta-Glucuronide. Drug Metab Dispos. 2015 Jul;43(7):1108-18. doi: 10.1124/dmd.115.064303. Epub 2015 May 4.PubMed: 25941268
  11. 11 . FDA Approved Drug Products: Gemfibrozil Oral Tablets Link
  12. 12 . Cayman Chemicals: Gemfibrozil MSDS Link