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Antihyperlipidemic Drugs

Terms in this set (8)

a Inhibit synthesis/Metabolism
i Statins (we need to remember Atorvastatin (Lipitor))
1 MOA - Inhibition of HMG-CoA reductase and prevents the rate limiting step of cholesterol synthesis → reduce cholesterol synthesis
2 can also increase expression of LDL receptors → decrease LDL in blood
3 ADR - Skeletal muscle weakness, myalgia, liver dysfunction, diarrhea, Brown urine, Rhabdomyolysis
ii Fibrates
1 MOA- Reduction in cholesterol synthesis increases expression of LDL receptors on liver cells, increase internalization of LDL by liver cells where LDL is degraded → reduction in LDL
(This is wrong...Increase in LPL synthesis>>increase clearance of triglycerides>>decrease in triglycerides)
2 Mainly for High Triglycerides
3 ADR - Gi disturbances, skin rashes, liver tumor
iii Niacin
1 MOA : decreases liver synthesis of VLDL and reduction of LDL in the plasma, increases synthesis of HDL
2 Vitamin B3 (water soluble)
3 one of the oldest drugs for lowering lipids
4 vasodilator so ADR: flushing
5 Reduce LDL and increase HDL
b Inhibit absorption
i Ezetimibe (Zetia)
1 MOA - inhibit absorption of cholesterol in the small intestine by acting on the sterol transporter -Niemann-Pick C1-Like 1 (NPC1L1), a protein located in jejunal enterocytes.
2 ADR - Diarrhea, fatigue, arthralgia, liver toxicity
ii Bile Acid Sequestrants
1 MOA: prevents reabsorption of bile acids from small intestine during entero-hepatic circulation>>bile acid excreted in the feces. Inhibition of reabsorption reduces liver bile acid>> increase cholesterol degradation >> reduce cholesterol levels in liver>> increase in the number of LDL receptors >> increased uptake of LDL >> decrease in LDL in the blood.
2 ADR - constipation, reduce absorption of lipid soluble vitamins, muscle weakness