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Gemfibrozil (Lopid), mechanism Of Action, Therapeutic Uses, Side Effects

Gemfibrozil (Lopid)
Mechanism Of Action:
Gemfibrozil (Lopid) stimulates the activity of peroxisome proliferating activating receptors (PPAR alpha), a class of nuclear receptor. Activation of these receptors alters the transcription of a number of genes involved in triglyceride metabolism including lipoprotein lipase and apolipoprotein CIII. This increases the peripheral catabolism (breakdown) of VLDL and chylomicrons, resulting in a reduction in the plasma concentration of VLDL, most notably in triglycerides, moreover, Gemfibrozil (Lopid) also reduce the synthesis of cholesterol, which further reduces plasma triglycerides.

Clinical and therapeutic uses:
a) Gemfibrozil (Lopid) can be used to treat hyperlipidemia of several etiologies, especially hypertriglyceridemia due to dysbetalipoproteinemia, a defect in apolipoprotein E that impairs clearance of chylomicron remnants and VLDL.
b) it is ineffective in primary chylomicronemia (caused by a deficiency in lipoprotein lipase).
c) it has antidiuretic action in individuals with mild to moderate diabetes insipidus
d) it is more effective than fenofibrate in some cases

Adverse effects:
1. cholelithiases
2. Cholecystitis
3. GI intolerance
4. Nausea
5. Diarrhoea
6. Myalgia
7. displace other albumin bound drugs esp. sulfonylureas and warfarin
8. should be used cautiously in hepatic and renal impairment.

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