Anti hyperlipidemic agents 1 | Medicinal Chemistry | III B Pharm V Semester - Unit 3 | III Pharm D
prema anandan・2 minutes read
Hyperlipidemia is categorized into six groups of lipid-lowering agents, including fibric acid derivatives that activate PPAR-alpha, reduce triglycerides, and increase HDL levels. These derivatives act as prodrugs, increasing half-life, reducing plasma concentrations, and exchanging chloride ions for bile acids to lower cholesterol levels.
Insights
- Fibric acid derivatives like clofibrate act as prodrugs due to their ester structure, leading to increased half-life and reduced plasma concentrations of triglycerides and cholesterol.
- Bile acid sequestrants such as cholestyramine resin bind bile acids in the GI tract, inhibiting lipid solubilization, blocking cholesterol absorption, and competing with cholesterol synthesis in the liver, ultimately reducing LDL cholesterol levels.
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Recent questions
What are fibric acid derivatives?
Fibric acid derivatives are lipid-lowering agents that decrease triglyceride levels, reduce LDL levels, and increase HDL levels by activating PPAR-alpha and lipoprotein lipase.
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Summary
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Lipid-lowering agents: mechanisms and classifications
- Hyperlipidemia is classified into six categories: HMG-CoA reductase inhibitors (e.g., lovastatin, simvastatin), fibric acid derivatives (e.g., clofibrate), bile acid sequestrants (e.g., cholestyramine), inhibition of LDL oxidation (e.g., probucol), pyridine derivatives (e.g., nicotinic acid), and miscellaneous agents (e.g., beta-sitosterol).
- Fibric acid derivatives are broad-spectrum lipid-lowering agents that decrease triglyceride levels, reduce LDL levels, and increase HDL levels by activating the peroxisome proliferator-activated receptor alpha (PPAR-alpha) and lipoprotein lipase.
- Fibric acid derivatives like clofibrate act as prodrugs due to their ester structure, leading to increased half-life and reduced plasma concentrations of triglycerides and cholesterol.
- Dextrothyroxine sodium stimulates the enzyme 7-alpha cholesterol hydroxylase, converting cholesterol into bile acids, making it a hypocholesterolemic agent recommended for patients without coronary artery disease.
- Bile acid sequestrants are resins that bind bile acids in the GI tract, inhibiting lipid solubilization, blocking cholesterol absorption, and competing with cholesterol synthesis in the liver, reducing LDL cholesterol levels.
- Cholestyramine resin, a styrene copolymer with divinylbenzene and quaternary ammonium functional group, exchanges chloride ions for bile acids, increasing fecal bile acid loss and reducing cholesterol levels without affecting triglycerides.
- Probucol, a phenol compound with tertiary butyl groups and sulfur, lowers serum cholesterol by increasing LDL catabolism, aiding in cholesterol elimination and acting as a potent antioxidant. Niacin, or nicotinic acid, with a pyridine nucleus and carboxylic acid, promotes lipolysis in adipose tissue and reduces peripheral fatty acid release, aiding in lipid management.
