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ANTIHYPERLIPIDEMICS: BILE ACID SEQUESTRANTS AND CHOLESTEROL ABSORPTION INHIBITORS | ||
DRUG NAME | cholestyramine (Questran, Prevalite), colestipol (Colestid), colesevelam (Welchol) | ezetimibe (Zetia) |
CLASS | Bile acid sequestrants | Cholesterol absorption inhibitors |
MECHANISM of ACTION | Bind with bile acids in the intestine → decrease reabsorption of bile acids → decrease cholesterol levels in blood | Blocks cholesterol transporter in the small intestine → decreases cholesterol absorption and levels in the blood |
INDICATIONS | Hypercholesterolemia | |
ROUTE(S) of ADMINISTRATION | PO | |
SIDE EFFECTS |
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CONTRAINDICATIONS and CAUTIONS |
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NURSING CONSIDERATIONS | Assessment and monitoring Assessment
Monitoring
Client education
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Antihyperlipidemics are medications used to treat increased levels of lipids in the blood, like cholesterol, particularly low density lipoprotein, or LDL cholesterol; as well as triglycerides. Therefore, they’re also indicated in coronary artery disease therapy. Antihyperlipidemics include different classes of medications, among which are bile acid sequestrants, like cholestyramine, colesevelam and colestipol, as well as cholesterol absorption inhibitors like ezetimibe. All of them are administered orally.
Once administered, bile acid sequestrants, which are positively charged molecules, bind to the negatively charged bile acid in the intestine, preventing it from being reabsorbed. In turn, the liver compensates by increasing the production of bile salts, which uses up a lot of cholesterol. To get more cholesterol from the rest of the body, the liver increases uptake of LDLs, lowering its levels in the blood. The downside is that this also increases endogenous cholesterol and triglyceride synthesis.
And then cholesterol absorption inhibitors work by blocking a transport protein that mediates cholesterol absorption in the small intestine. This medication is mainly used to treat high levels of LDL and is typically used in combination with other lipid lowering agents like statins.
Common side effects of bile acid sequestrants include gastrointestinal disturbances, mostly constipation, abdominal pain, bloating, and nausea; and they can decrease absorption of fat soluble vitamins such as A,D,E and K; and with decreased vitamin K absorption, increased bleeding risk can ensue. Similarly, all bile acid sequestrants can decrease the absorption and effect of fat-soluble medications like digoxin, oral contraceptives and warfarin. Side effects of ezetimibe include headache, arthralgias, and myalgias; and rarely, rhabdomyolysis.
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