Gemfibrozil API

Gemfibrozil is the generic name for a drug used for lowering lipid levels. Belonging to the class of drugs known as fibrates it is administered to effectively treat hyperlipidemia (Type III) and hypertriglyceridemia (type IV). It is marketed under the brand name Lopid, with other names being Jezil and Gen-Fibro. It has the chemical formula C24H34N4O5S.

Therapeutic Effects

Gemfibrozil is an activator or Peroxisome proliferator-activated receptor-alpha or PPARα, a nuclear receptor involved in the metabolism of carbohydrates and fat. It is also involved in adipose tissue differentiation.

The resulting effect is a reduction of triglyceride levels, reduction of very low density lipoprotein (VLDL) levels and a minor reduction of LDL levels. It also results in a small increase in high density lipoprotein (HDL) levels. The recommended dosage of gemfibrozil is 600 mg half-an-hour before breakfast and dinner.

Precautions and Toxicities

Gemfibrozil should not be given to those suffering from hepatic or renal dysfunction. It should also be used with caution in individuals with biliary tract disease, obese patients, native Americans and pregnant women.

Gemfibrozil increases levels of repaglinide in people with diabetes therefore increasing the chances of developing hypoglycaemia. In this way this combination should be avoided.

Use of gemfibrozil can also cause GI distress, musculoskeletal pain, increased incidence of gallstones, hypokalemia as well as an increased risk of cancer.

Drug Interactions

When used together with statins such such as simvastatin or pravastatin, this increases the chances of developing a condition known as rhabdomyloysis or muscle injury. This can lead to severe kidney damage and even death.

Patients on warfarin may require their doses to be reduced as gemfibrozil can increase warfarin’s effects on the body leading to bleeding.

Colestipol is also known to reduce the absportion of gemfibrozil and thereby reduce its effectiveness. In this way, gemfibrozil should be given one hour before, or 4-6 hours after administering colestipol or cholestyramine.

 

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