Gemfibrozil and other fibrates decrease triglyceride (TAG) levels by interacting with a specific receptor subtype, known as peroxisome proliferator-activated receptor alpha (PPAR alpha), present in the liver and brown adipose tissue. Activation of PRAR alpha results in increased production of lipoprotein lipase (LPL) and reduced production of apolipoprotein C-III (an inhibitor of LPL). These actions speed up the clearance of VLDLs leading to reduced levels of triglycerides.
Fibrates increase production of apoA-I and apoA-II in the liver. This leads to an increase of plasma HDL concentrations and a more efficient reverse cholesterol transport.
Treatment with these medications forms LDL which has a higher affinity for its receptor and are consequentially broken down more rapidly.
This drug is indicated for treating hyperlipidemia, which refers to abnormally high levels of lipids or lipoproteins in the blood. Fibrates are also used for other dyslipidemias, such as hypertriglyceremia.
Treatment with these drugs may lead to hepatotoxicity and increased liver function test (LFTs) values. Other side effects include myopathy, increased CPK, and renal failure.
As these drugs increase the cholesterol content of bile, there is an increased risk of cholesterol gallstones. Patients with pre-existing gallbladder disease should not take this drug.
Gemfibrozil, along with other fibrates, can cause myopathy. Patients should be educated to report any signs of muscle injury, such as weakness, abnormal muscle pain, and tenderness.
Gemfibrozil should not be combined with statins, or used with great caution, as the combination of a statin with gemfibrozil increases the risk of statin-induced myopathy.
Gemfibrozil increases the effects of warfarin, thereby increasing anticoagulant effects and increasing the risk of toxicity. To assess coagulation status, prothrombin time should be measured frequently, and warfarin dosage may need to be adjusted.
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