Gemfibrozil

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Gemfibrozil
Gemfibrozil.svg
Clinical data
Trade names Lopid
AHFS/Drugs.com Monograph
MedlinePlus a686002
Pregnancy
category
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability Close to 100%
Protein binding 95%
Metabolism Hepatic (CYP3A4)
Elimination half-life 1.5 hours
Excretion Renal 94%
Feces 6%
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.042.968 Edit this at Wikidata
Chemical and physical data
Formula C15H22O3
Molar mass 250.333 g/mol
3D model (JSmol)
Melting point 61 to 63 °C (142 to 145 °F)
  (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]

The exact mechanism of action of gemfibrozil is unknown; however, several theories exist regarding the very low density lipoprotein (VLDL) effect; it can inhibit lipolysis and decrease subsequent hepatic fatty acid uptake as well as inhibit hepatic secretion of VLDL; together these actions decrease serum VLDL levels and increase HDL-cholesterol; the mechanism behind HDL elevation is currently unknown.

Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activating peroxisome proliferator-activated receptor alpha (PPARα) 'transcription factor ligand', a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Gemfibrozil also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL.[2]

Therapeutic effects[edit]

Side 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]

Environmental data[edit]

Gemfibrozil has been detected in biosolids (the solids remaining after sewage treatment) at concentrations up to 2650 ng/g wet weight.[4] This indicates that it survives the wastewater treatment process. It is also detected as environmental persistent micropollutant in aquifers and in groundwaters in karstic areas.[5]

References[edit]

  1. ^ Rodney, G; et al. (1976). "The Hypolipidemic Effect of Gemfibrozil (CI-719) in Laboratory Animals". Proc. R. Soc. Med. 69 (Supplement 2): 6–9. PMC 1864017Freely accessible. PMID 828263. 
  2. ^ https://pubchem.ncbi.nlm.nih.gov/compound/gemfibrozil#section=Mechanism-of-Action
  3. ^ "Gemfibrozil." WebMD.com Accessed 14 June 2014. http://www.webmd.com/drugs/drug-11423-gemfibrozil+oral.aspx
  4. ^ http://water.epa.gov/scitech/wastetech/biosolids/tnsss-overview.cfm
  5. ^ Doummar, Joanna; Aoun, Michel (2018-08-01). "Assessment of the origin and transport of four selected emerging micropollutants sucralose, Acesulfame-K, gemfibrozil, and iohexol in a karst spring during a multi-event spring response". Journal of Contaminant Hydrology. 215: 11–20. doi:10.1016/j.jconhyd.2018.06.003. ISSN 0169-7722. 

External links[edit]