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50 Cards in this Set
- Front
- Back
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Free fatty acids in the liver are converted first to ________ and then packaged as ________ and sent to the ___________.
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Triglycerides, VLDLs, blood stream.
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Cholesterol in the liver comes from 3 places. What are they?
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1) Dietary cholesterol 2) Cholesterol biosynthesis from acetyl CoA and bile salts 3) LDLs that leave the blood stream and enter the liver via LDL receptor.
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Can the heart use fatty acids as energy?
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Yes.
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Which drug class blocks the rate-limiting step in cholesterol biosynthesis?
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HMG-CoA reductase inhibitors
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What is the mechanism of ezetimibe?
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It inhibits the absorption of dietary and biliary cholesterol from the intestines.
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What is the mechanism of Niacin?
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Niacin inhibits packaged VLDLs from exiting the liver.
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What is the mechanism of fibrates?
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They stimulate the secretion of lipoprotein lipase to increase the breakdown of VLDL triglycerides. This allows fatty acids to be delivered to adipose and other tissues.
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What does Niacin do to HDL levels?
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Increases HDL levels (MOST EFFECTIVE AGENT)
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What disease is niacin really good at treating, especially when you combine niacin with bile acid-binding resin?
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Heterozygous familial hypercholesterolemia.
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Tell me how niacin is administered and how it is excreted.
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Oral absorption. Renal excretion.
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T/F: Niacin may have the side effect of impairing glucose tolerance.
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True
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T/F: Niacin my cause severe hepatotoxicity.
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True
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How does gemfibrozil lower triglycerides?
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by lowering VLDL concentration.
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T/F: gemfibrozil is effective in treating chylomicronemia and familial hypercholesterolemia.
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False
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What diseases might you treat using fibrates?
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Familial dysbetalipoproteinemia and hypertriglyceridemia.
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Why is clofibrate seldom used?
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It increases risks for GI and hepatobiliary neoplasms.
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T/F: Gemfibrozil may cause increased incidence of cholelithiasis.
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True
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What drug class might fibrates interfere with?
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Statins (inhibits metabolism of statins).
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What electrical charge do bile acid-binding resins have?
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Positive (+)
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How do BAB resins reduce plasma cholesterol?
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Reduction in bile acids >>>> Increased LDL receptors >>>>> increase LDL uptake >>>>> reduced plasma cholesterol
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How are BAB resins absorbed?
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They are not absorbed.
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How should BAB resins be administered.
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Orally with meals.
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Are BAB resins effective in treating hypertriglyceridemia?
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Nope
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What diseases can be treated using BAB resins?
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Any disease in which LDL is elevated (heterozygous familial hypercholesterolemia and combined hyperlipoproteinemia)
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Compared to other lipid-lowering drugs, BAB resins are the ________ (safest, most dangerous). Why?
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Safest. They are not absorbed.
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What are the most common side effects of BAB resins?
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Constipation and bloating.
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BAB resins may inhibit absorption of a number of drugs. Name some of them please.
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digitalis, thiazides, tetracycline, thyroxine, aspirin
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What drug class might colestipol, cholestyramine, and colesevelam belong to?
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Bile acid-binding resins
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Which of the statin drugs are prodrugs?
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lovastatin and simvastatin.
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What do HMG-CoA reductase inhibitors do in regards to high affinity LDL receptors?
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increase the number of receptors.
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Do HMG-CoA reductase inhibitors have any effect on triglycerides?
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Yes. triglycerides are lowered.
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In addition to being effective at controlling lipid levels, HMG-CoA reductase inhibitors also have a number of other beneficial effects. Name some of those effects please.
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1) decrease c-reactive protein in CHD patients
2) enhance NO production by endothelial cells 3) increase plaque stability 4) reduce lipoprotein oxidation 5) decrease platelet aggregation |
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How should statins be administered?
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Orally in the evening.
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Where are HMG-CoA reductase inhibitors metabolized? How are they excreted?
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In the liver (High first pass effect), GI excretion
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What diseases might you treat with HMG-CoA reductase inhibitors?
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Most effective when LDLs are high (eg. heterozygous familial hypercholesterolemia and hyperlipoproteinemia).
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When are HMG-CoA reductase inhibitors contraindicated?
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Contraindicated in pregnancy. Also may produce liver damage in alcoholics or patients with preexisting liver problems.
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What drugs might increase the plasma concentration of statins?
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macrolides, cyclosporine, ketoconazole, verapamil, ritonavir
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What drugs might decrease the plasma concentration of statins?
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phenytoin, barbiturates, rifampin, griseofulvin
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What lipid lowering drug inhibits the metabolism of statins?
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gemfibrozil
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What juice enhances the bioavailability of statins?
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grapefruit juice
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Which drug reduces LDL-cholesterol more? Statins or ezetimibe?
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Statins.
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If you give your patient both ezetimibe and a statin, what happens?
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synergistic cholesterol-lowering effects
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T/F: ezetimibe is enterohepatically recirculated.
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True
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Why might you prescibe orlistat?
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For weight loss.
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How does orlistat do it's job?
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inhibits pancreatic lipase
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What are the side effects of orlistat?
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Oily stools, diarrhea
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If your patient has elevated cholesterol with other lipid values being normal, what drugs might you choose to use?
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BAB resins, ezetimibe
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If your patient has elevated triglycerides only, what drug might you choose to use?
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Fibrates (Gemfibrozil)
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If your patient has elevated cholesterol and hypertriglyceridemia, what drug(s) might you choose to use?
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Statins and niacins, ezetimibe
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T/F: It is always best to just treat with drugs and ignore lifestyle changes and side effect profiles.
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False
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