Gemfibrozil

Trade name Lopid.

Close to 100% oral bioavailability.

Metabolism is hepatic with CYP3A4 enzymes.

Half-life is 1.5 hours, and has renal excretion of 94%.

Oral drug used to lower lipid levels.

Classified as a fibrate drug.

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.

Results in an increase in the synthesis of lipoprotein lipase increasing the clearance of triglycerides.

Inhibits production of proinflammatory cytokines.

Reduce triglyceride levels.

Reduce very low density lipoprotein (VLDL) levels.

Associated with modest reduction of low density lipoprotein (LDL) levels.

Associated with moderate increase in high density lipoprotein (HDL) levels.

Associated with gastrointestinal distress, increased risk of gallstones, musculoskeletal pain, and hyperkalemia.

Drug of choice for therapy for hyperlipidemia (Type III).

Utilized for hypertriglyceridemia Type IV, though not as effective as niacin.

Contraindicated in hepatic dysfunction.

Should be used with caution in these higher risk categories:

Biliary tract disease

Renal dysfunction

Pregnant women

Obese patients

Potentiates the action of warfarin and indanedione anticoagulants.

Concomitant administration of fibrates with statin drugs increases the risk of muscle cramping, myopathy, and rhabdomyolysis.

Most consistent plasma changes are increased HDL-C and decrease in triglycerides.

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