30:718:409 Lecture 26: Drugs to treat dyslipidemia-Lecture 2-ClassNotes
10 Jan 2019
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Identified by random screening of a series of aryloxyisobutyric acid. Clofibrate was the first fibrate to be marketed. No conclusive clinical study evidence exists that fibrates can reduce cv morbidity or mortality. In clinical studies, the initial drug in this class, clofibrate, did not reduce cv mortality but increased morbidity and mortality from causes other than chd: newer fibrates gemfibrozil and fenofibrate are deemed safer compared to clofibrate. Mechanism of action and therapeutic effects of fibrates. Activates ppar (peroxisome proliferator-activated receptor- ) inhibits transcription of apoprotein c-iii (an inhibitor of lipoprotein lipase) stimulates lipoprotein lipase lipolysis (carried out by lipoprotein lipase) of chylomicrons and vldl. The pharmacological effect is stimulation of lipolysis: indicated for treating hypertriglyceridemia and familial combined hyperlipidemia (high cholesterol and high triglyceride), therapeutic effects: Triglyceride effect: reduce tg significantly: promote triglyceride degradation by stimulating the activity of lipoprotein lipase. Inhibit triglyceride synthesis (by ppar mediated stimulation of fatty acid metabolism)
