Flashcards in Antihyperlipidemi Drugs: Ezetimibe and Omega Fatty Acids Deck (17)
The last category of lipid lower drugs is a cholesterol absorption inhibitor called Ezetimibe. What is the use?
Inhibits intestinal absorption of cholesterol and phytosterols
What is the MOA for Ezetimibe?
Selective Inhibitor of NPC1L1 in jejunal enterocytes which takes up cholesterol from the lumen
--reduces cholesterol absorption but however increases cholesterol synthesis (need to use a statin)
--reduced delivery of the cholesterol to the liver leads to upregulation of LDL receptors which enhances LDL clearance.
The actions of ezetimibe are complementary to those of statins. Therefore combined therapy does what?
Prevents enhanced cholesterol synthesis and the increase in cholesterol absorption.
--reduces LDL levels
Ezetimibe is effective even in the absence of dietary cholesterol, how?
Inhibits reabsorption of cholesterol excreted in bile
What are the uses of Ezetimibe?
Used in combo with a statin in patients unable to reach their LDL goal on statin monotherapy
What are the adverse effects and drug interactions of Ezetimibe?
Low incidence of reversible impaired hepatic function
Bile acid sequestrants inhibit absorption of ezetimibe. Therefore do not administer together
Next drugs are the Omega 3 fatty acids, Eicosapentaenoic Acid (EPA) and Docosahexaenoic Acid (DHA). What is their role in lipid lowering?
Reduce plasma TG
--reduce TG biosynthesis and increase fatty acid oxidation in the liver
--long term may increase HDL
What is the FDA approved omega 3 product ?
--indicated as an adjunct to diet to reduce triglyceride levels in adult patients with very high TG levels
In summary what is the best drug for LDL lowering?
Combination drug therapy is used in what situations?
1. Patients unable to reach their LDL goal in a single drug
2. Patients with combined hyperTAG and hypercholesterolemia that cannot be adequately controlled with a single drug
3. Patients with elevated LDL and low HDL levels
What are the suggested drug therapy for dyslipidemias?
Elevated LDL: Initial Drug = Statin and Additions = Niacin, Resin and Ezetimibe
Elevated LDL and TG: Initial Drug= Statin and Additions = Niacin and Fibrate
Isolated low HDL: Initial Drug= Statin and Additions= Niacin
Isolated Severe HyperTAGs: Initial Drug = Fibrate and Additions = Statin
Statins and Pregnancy?
Gemfibrozil and Fenofibrate and pregnancy?
Should be used in pregnancy only if the potential benefits justifies the potential risk to the fetus
Niacin and Pregnancy?
Safety is unknown
Cholestyramine and Colestipol and Pregnancy?
Interferes with absorption of important nutrients
Colesevlam and Pregnancy?
Can be used during pregnancy