TAILIEUCHUNG - Color Atlas of Pharmacology (Part 14): Drugs used in Hyperlipoproteinemias

Drugs li KT used in Hyperlipoproteinemias port vehicles in the aqueous media of lymph and blood. To this end, small amounts of lipid are coated with a layer of phospholipids, embedded in which are additional proteins—the apolipoproteins (A). According to the amount and the composition of stored lipids, as well as the type of apolipoprotein, one distinguishes 4 transport forms: Lipid-Lowering Agents Triglycerides and cholesterol are essential constituents of the organism. Among other things, triglycerides represent a form of energy store and cholesterol is a basic building block of biological membranes. . | 154 Drugs used in Hyperlipoproteinemias Lipid-Lowering Agents Triglycerides and cholesterol are essential constituents of the organism. Among other things triglycerides represent a form of energy store and cholesterol is a basic building block of biological membranes. Both lipids are water insoluble and require appropriate trans port vehicles in the aqueous media of lymph and blood. To this end small amounts of lipid are coated with a layer of phospholipids embedded in which are additional proteins the apolipoproteins A . According to the amount and the composition of stored lipids as well as the type of apolipoprotein one distinguishes 4 transport forms Origin Density Mean sojourn in blood plasma h Diameter nm Chylomicron Gut epithelium 500 VLDL particle liver 3 100-200 LDL particle blood 50 25 HDL particle liver - 5-10 Lipoprotein metabolism. Entero-cytes release absorbed lipids in the form of triglyceride-rich chylomicrons. Bypassing the liver these enter the circulation mainly via the lymph and are hydrolyzed by extrahepatic endothelial lipoprotein lipases to liberate fatty acids. The remnant particles move on into liver cells and supply these with cholesterol of dietary origin. The liver meets the larger part 60 of its requirement for cholesterol by de novo synthesis from acetylcoen-zyme-A. Synthesis rate is regulated at the step leading from hydroxymethylglutaryl CoA HMG CoA to mevalonic acid p. 157A with HMG CoA reductase as the rate-limiting enzyme. The liver requires cholesterol for synthesizing VLDL particles and bile acids. Triglyceride-rich VLDL particles are released into the blood and like the chylomicrons supply other tissues with fatty acids. Left behind are LDL particles that either return into the liver or supply extrahepatic tissues with cholesterol. LDL particles carry apolipoprotein B 100 by which they are bound to receptors that mediate uptake of LDL into the cells including the hepatocytes .

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