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55 Cards in this Set
- Front
- Back
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What binds and transports Cholesterol and Triglycerides?
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Apoproteins
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Apoprotein + Lipid = ???
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Lipoprotein
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% of LDL and HDL that is cholesterol?
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LDL: 45
HDL: 20 |
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Two main roles of LDL?
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Provides CH for necessary body fxns
Promotes CH accumulation in arterial walls |
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Main Role of HDL?
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Helps to remove excess CH from blood
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Risk Factors for CHD?
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High LDL
Low HDL Smoking HTN Type 2 DM Advancing Age FH |
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Who are the high risk groups that need Lipid-Lowering Drugs?
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Existing Vascular Disease
FH of CV disease in first degree relative < 60yrs old Familial Hypercholesterolemia DM |
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Principles of Management
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1. Determine risk
2. Rx Diet and Lifestyle 3. Risk remains high...continue #2 and add drugs |
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Rx Goals?
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Cholesterol <230
Triglycerides < 150 LDL < 130 HDL > 45 |
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STATINS
Action? |
Inhibit HMG CoA Reductase
Induce increase in high-affinity LDL receptors |
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Role of HMG-CoA Reductase?
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Enzyme necessary for synthesis of Cholesterol.
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STATINS
Therapeutic Effects? |
1. Inhibits Hepatic CH synthesis-->increased expression of LDL receptors-->removal of LDL from blood
2. Increases fractional catabolism of LDL + liver extraction of LDL precursors--> Decreased LDL levels 3. Dec Triglycerides 4. Modest Inc in HDL |
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STATINS
% dec in LDL and triglycerides |
LDL: dec from 20-55%
Triglycerides: dec 35-45% |
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STATINS
When to administer? |
all of them at bedtime or after dinner b/c of 4 hour half life
EXCEPT Atorvastatin and Rosuvastatin have 1/2 lives of 20-30 hrs so give em during the day |
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STATINS
Potential Cardioprotective Effects other than LDL lowering? |
1. Increase endothelial production of NO
2. Breakdown of Plaques 3. Decrease Inflammation 4. Dec Coagulation 5. Dec Lipoprotein Oxidation |
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STATINS
What do they do to Plaques to break them down? |
Inhibit monocyte infiltration
Inhibit Macrophage production of metalloproteinases Inhibit SMC prolif All of which enhance apoptotic cell death |
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STATINS
how do they dec coagulation? |
inhibit aggregation
dec fibrinogen levels |
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STATINS
SE and contraindications? |
Hepatotoxic
Myopathy/Rhabdomyolysis Preggers Children under 8 |
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STATINS
Indications? |
Hypercholesterolemia
Combined hyperlipidemia Severe Hypercholesterolemia w/ DM or MI |
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STATINS
Drug Interactions |
Cyclosporine
Gemfibrozil Niacin (myopathy) Erythromycin |
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STATINS
good tag team partner? |
Resin
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STATINS
which ones are given as prodrugs? |
Lovastatin
Simvastatin |
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Wait so what are Resins?
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Bile Acid Sequestrants
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How do resins work?
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Bind Bile in intestine inhibiting their reabsorption and increasing their excretion
Also inc LDL receptors expression--> Inc Clearance |
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Two main Resins?
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Cholestyramine
Colestipol |
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Kinda not helpful effect of Resin?
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Weakly stimulate VLDL synthesis
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SE of Resins?
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GI disturbances
Constipation Bloating all lead to non-compliance |
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Indications for Resins?
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Kids can take it
Familial Hypercholesterolemia Combined Hyperlipidemia Slow growth of plaques |
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Contraindications of Resins?
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Hypertriglyceridemia
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Drug Interactions of Resins?
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Impairs the absorption of a lot of drugs
Reduces absorption of lipid-soluble drugs and vitamins So take it 1hr before or 3 after other drugs |
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Fibric Acid Derivatives
ACTION? |
-Increase lipoprotein lipase activity in fat tissue--> inc catabolism of VLDL
-Bind PPARa in liver --> dec triglycerides -Stimulate apoA-1 and apoA-3 to inc HDL |
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How do Fibrates decrease triglycerides?
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Inc FA oxidation
Inc LPL synthesis Reduce expression of apo-C-III |
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Therapeutic Effects of Fibrates?
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Dec Tri's by 35%
Dec VLDL Dec LDL by 11% Inc HDL by 11% |
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SE of Fibrates?
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GI distress
MS pain Inc incidence of gallstones Hepatic or Renal dysfxn |
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Indication of Fibrates?
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Type III Hyperlipidemia
Hypertriglyceridemia Hypertriglyceridemia + Chylomicronemia Syndrome |
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Drug Interactions of Fibrates?
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Anticoagulants
Statins except for fenofibrate (myopathy) |
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Contraindicated Pts for Fibrates?
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Preggers
Kids Pts w/ metabolic syndrome or DM (type 2) |
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when to take Fibrates?
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w/ meal
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NIACIN
Therapeutic Effects |
Inc HDL 30%
Dec TG 35-45% Dec LDL 20-30% |
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NIACIN
MOA? |
1. Inhibit cAMP-->decreased TG lysis into FA's --> dec hepatic TG synthesis
2. Dec VLDL synthesis 3. Dec LDL production 4. Inc LPL activity-->clearance of chylomicrons and VLDL TG's 5. Dec clearance of HDL |
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NIACIN
SE? |
Flushing
Skin disorders GI Distress May reactivate Gout Hepatotoxic |
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NIACIN
indications? |
HyperTG
Elevated VLDL or combined lipid levels Hyperlipidemia Low HDL |
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NIACIN
Contraindications? |
Severe Peptic Disease
Hepatotoxic Statin use-->myopathy Preggers Diabetes |
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NIACIN
good tag team partner? |
Resins
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What is CETP? and why would an inhibitor of it be a good drug?
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Cholesteryl Ester Transfer Protein
it carries Cholesteryl Esters from HDL to LDL |
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Actions of Ezetimide?
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Inhibits absorption of CH by enterocytes (54%)--> dec CH in chylomicrons, dec CH going to liver, inc in LDL receptors >>> inc LDL clearance (15-20%)
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Ezetimide indications?
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Hyperlipidemia
Compliment statins |
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Contraindications of Ezetimide?
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W/ Bile Acid Sequestrants
Possible Allergic Rxn |
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If you have a predominant Hypercholesterolemia, which drugs could you use?
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Resins
Statins Fibrates Niacin |
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If Combined Hyperlipidemia, what drugs?
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Fibrates
Statins Niacin |
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If predominant hyperTG, what drugs?
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Fibrates
Niacin |
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Who can lower LDL the most?
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Statins
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Who can raise HDL the most?
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Niacin
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Who can lower TG's teh most?
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Fibrates
Niacin Statins |
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Who causes myopathy w/ statins?
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Niacin
Fibrates |
