| In Vitro | In vitro activity: Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, triacylglycerols, free fatty acids (FFA) and glycerol, as well as the total and unesterified cholesterol concentrations, in liver microsomes of rats. Etofibrate increases the activity of liver cytosolic glycerol-3-P dehydrogenase in the rats, whereas it decreases the activity of both microsomal HMG-CoA reductase and cholesterol 7 alpha-hydroxylase and does not affect acyl-CoA: cholesterol acyltransferase (ACAT). Etofibrate decreases the availability of lipolytic products in the liver by acting on their release from adipose tissue and on their intrinsic hepatic metabolism. Etofibrate stimulates the rate of fatty acid re-esterification when incubations are done under basal conditions in epididymal fat pad pieces from fed rats. |
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| Formulation & Dosage | Male Sprague Dawley rats weighing 200 to 220 g, fed ad libitum a standard laboratory diet and subjected to a 12 hr on-off light cycle and 22 to 24°C are used. Food is removed from the cages at the onset of the light cycle (7.00 a.m.) and 3 hr later, Etofibrate is administered by stomach tube without anesthesia at a dose of 300 mg/kg body weight/day to one group of animals whereas another, control, group is treated with the medium. After treatments, rats are again allowed free access to food. On the 10th day, the animals are treated as above, but 2 hr after receiving the Etofibrate or the medium the rats are anesthetized with an intraperitoneal injection (0.30 mL/100 g body weight). Animals are maintained at 37°C in a thermostatically controlled cabinet |
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