Article: Gemfibrozil

Gemfibrozil
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Identifiers
CAS number	25812-30-0
ATC code	C10AB04
PubChem	3463
DrugBank	APRD00293
Chemical data
Formula	C15H22O3
Mol. weight	250.333 g/mol
Pharmacokinetic data
Bioavailability	Close to 100%
Protein binding	95%
Metabolism	Hepatic (CYP3A4)
Half life	1.5 hours
Excretion	Renal 94% Feces 6%
Therapeutic considerations
Pregnancy cat.	Category C
Legal status	By Prescription
Routes	Oral

Gemfibrozil is the generic name for an oral drug used to lower lipid levels. 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), a receptor which is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation.

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 gallstones
• Hypokalemia

Indications

• Hyperlipidemia (Type III): Gemfibrozil is the drug of choice for therapy.
• Hypertriglyceridemia (Type IV): Gemfibrozil, though not as effective as nicotinic acid, 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.
• Lovastatin. Risk of myopathy when gemfibrozil is given to patients receiving lovastatin.