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26 Cards in this Set
- Front
- Back
Why do we use lipid lowering drugs?
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Increased Serum lipid plays a role in the pathogenesis of atherosclerosis.
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What are the 4 common types of Lipid lowering drugs?
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HMG CoA reductase inhibitors (statins); bile acid binding agents; niacin; fibrates
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What is the mechanism of the most effective type of lipid lowering drug, i.e. statins?
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Competitive inhibition of HMG CoA reductase in the liver, which rate limits cholesterol synthesis
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Name the 3 mechanism by which serum LDL falls in response to statins.
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1. increased LDLR expression;
2. increased clearance of LDL precursors (e.g. VLDL) via LDLR; 3. VLDL production falls due to decreased cholesterol(therefore less will form LDL) |
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Describe Statins effect on HDL, LDL, & TG.
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HDL increase; LDL & TG decrease
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True/False - LDL reduction promotes plaque stability and therefore decreases risk of thrombus formation.
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True
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True/False - Statins improve plaque stability by inhibiting monocyte penetration and increasing macrophage metalloproteinase secrection.
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False - Statins improve plaque stability by inhibiting monocyte penetration and decreasing macrophage metalloproteinase secrection.
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Statins are often used to treat CAD. What are the side effects for these drugs?
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Side effects: GI upset, Sleep disturbance, rare hepatoxicity & myotoxicity;
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What are the contraindications for statins?
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Drugs that inhibit isoform 3A4 Cytochrome P450.
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Describe the mechanism of Lipid Reduction in Bile Acid Binding Agents.
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These drugs bind/make polar bile acids thereby preventing reabsorption. This excretion causes the body to use cholesterol to make more Bile Acids.
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True/False - Unlike Statins, Bile Acid Binding Agents MAY increase serum TG levels.
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True - Bile Acid Binding Agents may increase cholesterol synthesis leading to increased VLDL.
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Give examples of Bile Acid Binding Agents.
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resins - cholestyramine, colestipol; hydrophilic polymer - colesevelam
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As a second line drug, Bile Acid Binding Agents have what side effects?
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bloating, constipation, nausea
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Bile Acid Binding Agents are contraindicated in what circumstances?
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interferes with certain drug absorptions (e.g. TH, propanolol, digoxin, warfarin)
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Describe Bile Acid binding Agents effect on HDL, LDL, & TG.
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HDL increase; LDL decrease; MAY increase TG
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Describe Niacin's effect on HDL, LDL, & TG.
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HDL increase; LDL & TG decrease
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Which of the lipid lowering drugs reduce lipoprotein a levels and is most effective at increasing HDL?
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Niacins
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What are the 4 mechanisms by which niacins work?
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1. inhibits FA release from fat which is necessary for TG synthesis ;
2. enhanced lipoprotein lipase action on circulating VLDL leads to TG clearance; (1/2 low TG = low VLDL = low LDL); 3. reduces proportion of small, dense LDL for larger forms; 4. increased HDL via reduced uptake of its Apoprotein A1 |
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What are the side effects of Niacin?
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Transient cutaneous flushing, GI upset, hepatoxicity, myotoxicity?
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In what 3 groups of people should Niacins be used cautiously?
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reactivation of gout; excaberation of peptic ulcer disease; induced insulin resistance in diabetics
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Give examples of fibrates, which are lipid lowering drugs most effective at lowering Tg's.
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Gemfibrozil, Fenofibrate
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Describe the effects of Fibrates on LDL, HDL, and Tg.
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LDL variable!; Increase HDL; lower TG
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Describe the mechanism of action of Fibrates.
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THOUGHT to activate PPAR-alpha which:
a. lowers TG via FA oxidation and increased Lipoprotein lipase activity; b. increase HDL via increased AI and AII |
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True/False - Fibrates are absolutely contraindicated in liver or kidney dysfunction.
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False - Fibrates are glucornoidated and excreted via the kidneys but can be used cautiously.
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Name the common side effects of Fibrates.
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Dyspepsia, gallstones, myalgias
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Name the 3 drug interactions that must be considered before concomitantly prescribing a Fibrates.
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1. risk of increased rhabdomyolysis with statins;
2. increased anticoagulation with warfarin; 3. increased potency of oral hypoglycemics drugs |