Samiksha Jaiswal (Editor)

Gemfibrozil

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Trade names
  
Lopid

MedlinePlus
  
a686002

Routes ofadministration
  
Oral

CAS ID
  
25812-30-0

Protein binding
  
95%

AHFS/Drugs.com
  
Monograph

Pregnancycategory
  
Category C

ATC code
  
C10AB04 (WHO)

Molar mass
  
250.333 g/mol

Classification
  
Valeric acid

Gemfibrozil

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

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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.

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  • Is an activator of peroxisome proliferator-activated receptor-alpha (PPARĪ±), 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.

    • Therapeutic effects

  • 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

    • Indications

  • 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

    • 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.
  • Gemfibrozil inhibits the activation of the liver's Cytochrome P450 system, reducing hepatic metabolism of many drugs, and prolonging their half lives and duration of action.
  • Drugs metabolized by the Cytochrome P450 system include:
  • Many antidepressants
  • Many antipsychotics
  • Many antiepileptics
  • Theophylline and other methylxanthine drugs
  • Several anesthetic agents
  • Oral contraceptive pills
  • Statins
  • Warfarin

    • Environmental data

    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.

    References

    Gemfibrozil Wikipedia
    (Text) CC BY-SA


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