|Systematic (IUPAC) name|
|Bioavailability||Close to 100%|
|Biological half-life||1.5 hours|
|CAS Registry Number|
|Molecular mass||250.333 g/mol|
|(what is this?)|
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.
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.
- Is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), a nuclear 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.
- 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.
- Reduce triglyceride levels 
- Reduce very low density lipoprotein (VLDL) levels
- Modest reduction of low density lipoprotein (LDL) levels
- Moderate increase in high density lipoprotein (HDL) levels
Nontherapeutic effects and toxicities
- GI distress
- Musculoskeletal pain
- Increased incidence of gallstone
- Hypokalemia (low blood potassium)
- Increased risk of cancer
- Hyperlipidemia (Type III): Gemfibrozil is the drug of choice for therapy.
- Hypertriglyceridemia (Type IV): Gemfibrozil, though not as effective as niacin, is better tolerated.
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
- 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.
Gemfibrozil has been detected in biosolids (the solids remaining after wastewater treatment) at concentrations up to 2650 ng/g wet weight. This indicates that it survives the wastewater treatment process.
- 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.
- 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.
- "Gemfibrozil." WebMD.com Accessed 14 June 2014. http://www.webmd.com/drugs/drug-11423-gemfibrozil+oral.aspx
- DrugBank Gemfibrozil
- NIH Gemfibrozil Drug Info
- Lopid International Study
- Author (2004). "Safety of Statins". Circulation 109: III–50–III–57.