Gemfibrozil

Gemfibrozil

Gemfibrozil
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Clinical data
Trade names Lopid
AHFS/Drugs.com
MedlinePlus
Pregnancy
category
  • Category C
Legal status
  • By Prescription
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability Close to 100%
Protein binding 95%
Metabolism Hepatic (CYP3A4)
Biological half-life 1.5 hours
Excretion Renal 94%
Feces 6%
Identifiers
CAS Registry Number  Y
ATC code C10
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C15H22O3
Molecular mass 250.333 g/mol
Physical data
Melting point 61 to 63 °C (142 to 145 °F)
 Y   

Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro.

Contents

  • Development history 1
  • Actions 2
  • Therapeutic effects 3
  • Nontherapeutic effects and toxicities 4
  • Indications 5
  • Contraindications and precautions 6
  • Drug interactions 7
  • Environmental data 8
  • References 9
  • External links 10

Development history

Gemfibrozil was selected from a series of related compounds synthesized in the laboratories of the American company Parke Davis in the late 1970s. It came from research for compounds that lower plasma lipid levels in humans and in animals.[1]

Actions


Therapeutic effects

Nontherapeutic effects and toxicities

Indications

Contraindications and precautions

  • Gemfibrozil should not be given to these patients:
    • Hepatic dysfunction
  • Gemfibrozil should be used with caution in these higher risk categories:
    • Biliary tract disease
    • Renal dysfunction
    • Pregnant women
    • Obese patients

Drug interactions

  • Anticoagulants: Gemfibrozil potentiates the action of warfarin and indanedione anticoagulants.
  • Statin drugs: Concomitant administration of fibrates (including gemfibrozil) with statin drugs increases the risk of muscle cramping, myopathy, and rhabdomyolysis.

Environmental data

Gemfibrozil has been detected in biosolids (the solids remaining after wastewater treatment) at concentrations up to 2650 ng/g wet weight.[3] This indicates that it survives the wastewater treatment process.

References

  1. ^ Rodney, G; et al. (1976). "The Hypolipidemic Effect of Gemfibrozil (CI-719) in Laboratory Animals". Proc. roy. Soc. Med. 69 (Supplement 2): 6–9.  
  2. ^ "Gemfibrozil." WebMD.com Accessed 14 June 2014. http://www.webmd.com/drugs/drug-11423-gemfibrozil+oral.aspx
  3. ^ http://water.epa.gov/scitech/wastetech/biosolids/tnsss-overview.cfm

External links

  • DrugBank Gemfibrozil
  • NIH Gemfibrozil Drug Info
  • Lopid International Study
  • Author (2004). "Safety of Statins". Circulation 109: III–50–III–57. 
  • http://www.ihs.gov/nptc/documents/NPTC%20Lipid%20Review.pdf