Gemfibrozil

Gemfibrozil

File:Gemfibrozil.svg
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Clinical data
Pregnancy category	Category C
Routes of administration	Oral
Legal status
Legal status	By Prescription
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 Number	25812-30-0
ATC code	C10AB04 (WHO)
PubChem	CID 3463
DrugBank	APRD00293
ChemSpider	3345
Chemical data
Formula	C15H22O3
Molar mass	250.333 g/mol[[]]
(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.

Actions

• Increases activity of 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.

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
• Increased risk of cancer[1]

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
  • Renal dysfunction

• Gemfibrozil should be used with caution in these higher risk categories:
  • Biliary Tract Disease
  • Pregnant women
  • Obese patients
  • Native Americans

Drug Interactions

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

External links

• DrugBank Gemfibrozil
• NIH Gemfibrozil Drug Info}
• Lopid International Study
• Safety of Statins - Circulation. 2004;109:III-50 – III-57

es:Gemfibrozil