Glossary of Chapter 17 Lipid-Regulating Drugs

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

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