Gemfibrozil

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Gemfibrozil
Gemfibrozil.svg
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Clinical data
Trade names Lopid
AHFS/Drugs.com monograph
MedlinePlus a686002
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 25812-30-0 YesY
ATC code C10AB04
PubChem CID: 3463
IUPHAR/BPS 3439
DrugBank DB01241 YesY
ChemSpider 3345 YesY
UNII Q8X02027X3 YesY
KEGG D00334 YesY
ChEBI CHEBI:5296 YesY
ChEMBL CHEMBL457 YesY
Chemical data
Formula C15H22O3
Molecular mass 250.333 g/mol
 YesY (what is this?)  (verify)

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.[citation needed]

Development history[edit]

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[edit]

  • Preliminary data has shown that gemfibrozil inhibits production of proinflammatory cytokines in addition to its clinically useful lipid-lowering activity, increased survival in BALB/c mice that were already ill from infection by influenza virus A/Japan/305/57 (H2N2). Gemfibrozil was administered intraperitoneally once daily from days 4 to 10 after intranasal exposure to the virus. Survival increased from 26% in vehicle-treated mice (n = 50) to 52% in mice given gemfibrozil at 60 mg/kg/day (n = 46) (P = 0.0026). If this principle translates to patients, a drug already approved for human use, albeit by a different route for another purpose, might be adapted relatively fast for use against influenza, conceivably including human infection with a derivative of the avian H5N1 strain.[2]

Therapeutic effects[edit]

Nontherapeutic effects and toxicities[edit]

Indications[edit]

Contraindications and precautions[edit]

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

Drug Interactions[edit]

References[edit]

  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. PMC 1864017. PMID 828263. Retrieved 18 April 2015. 
  2. ^ Budd, A; Alleva, L; Alsharifi, M et al. (Aug 2007). "Increased Survival after Gemfibrozil Treatment of Severe Mouse Influenza". Antimicrob Agents Chemother 51 (8): 2965–8. doi:10.1128/AAC.00219-07. PMC 1932503. PMID 17562808. 
  3. ^ "Gemfibrozil." WebMD.com Accessed 14 June 2014. http://www.webmd.com/drugs/drug-11423-gemfibrozil+oral.aspx

External links[edit]