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PHARMACOLOGY 2
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LIPIDS DISORDER
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VIDEO LEC 2 - LIPID LOWERING DRUGS
level: VIDEO LEC 2 - LIPID LOWERING DRUGS
Questions and Answers List
level questions: VIDEO LEC 2 - LIPID LOWERING DRUGS
Question
Answer
commonly known as Statins inhibit HMG-CoA REDUCTASE so they reduce concentration of cholesterol within the liver cell. S/E: increase risk of liver toxicity, myopathy, and in rare cases rhabdomyolysis
HMG-CoA Reductase Inhibitors
commonly known as Niacin Unlike statins, nicotinic acid works in adipose tissue where it inhibits an enzyme called HORMONE-SENSITIVE LIPASE effectively decreases hepatic VLDL synthesis increases HDL levels S/E: Flushing (cutaneous vasodilation), increase risk of hyperuricemia and gout (COMPETE WITH URIC ACID) LARGE DOSE: liver toxicity
Nicotinic Acid
work primarily by activating a nuclear transcription receptor called PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR ALPHA OR PPAR-ALPHA. increases the removal of triglycerides from circulation and their breakdown to fatty acids. decrease expression of a protein Apo-Clll (inhibits lipoprotein lipase activity). also increases expression of proteins Apo-AI and Apo-AII (major component of HDL, thus leading to increase in its concentrations). S/E: GI disturbances, Myopathy and rhabdomyolysis, increase risk of gallstone formation.
Fibrates
serves as an ion exchange resins that bind negatively charged bile acids and salts in the small intestine. decreased levels of circulating LDL
Bile Acid Sequestrants
necessary for normal digestion and absorption of fats and fat soluble vitamins in the small intestine; produced in the liver, stored in the gallbladder and excreted into the gut where they facilitate digestion and absorption of lipids. S/E: Limited to the GI tract, May decrease absorption of fat soluble vitamins, Have potential to form insoluble complexes with other drugs thus interfering with their absorption.
Bile Acids
free cholesterol that comes from bile or dietary sources first binds to protein abbreviated NPC1L1 This binding then triggers endocytosis which utilizes a protein complex called clathrin AP2 S/E: Few and mild; good choice for patients intolerant or unresponsive to statins.
Cholesterol Absorption Inhibitors
abbreviated name of enzyme circulating in the blood that binds to LDL receptors on the surface of liver cells and promotes their degradation. Its activity reduces the removal of LDL from the circulation. They are monoclonal antibodies that bind to and inactivate PCSK9 S/E: - Injection site reactions - Flu-like symptoms - Neurocognitive problems
PCSK9 Inhibitors
Used primarily for their triglyceride lowering effects thought to be caused by inhibition of VLDL and triglyceride synthesis in the liver. S/E: GI disturbances, Fishy aftertaste LARGE DOSE: RISK OF BLEEDING
Omega-3 Fatty Acids
1 Components of Omega-3 Fatty Acids: 2 Omega-3 derivative:
1) 1 Docosahexaenoic acid (DHA) 2 Eicosapentaenoic acid (EPA) 2 Icosapentethyl