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35 Cards in this Set
- Front
- Back
what are the two sources of cholesterol?
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dietary intake
endogenous synthesis |
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what organ is the major source of de novo synthesis of cholesterol?
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the liver
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how much cholesterol is reabsorbed from the cholesterol that is secreted into bile?
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50%
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which form of HMG-CoA reductase is more active, the unphosphorylated or phosphorylated form?
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unphosphorylated
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what effect does insulin have on HMG-CoA reductase?
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it dephosphorylates it, making it more active
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what is the function of Apo CII? where is Apo CII present?
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Apo CII is an activator of capillary lipoprotein lipase. it is located on the coat of chylomicrons.
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IDL (intermediate density lipoprotein) mostly bind to hepatic receptors and are repackaged as VLDL. what is the name of this hepatic receptor?
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Apo-E
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What are the two different possible fates of IDL?
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LDL or going back to the liver to be repackaged as VLDL.
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What is the name of the receptor on the liver and peripheral tissue that interacts with LDL?
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Apo B-100
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what is the potential effect of administering a statin with grapefruit juice?
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decrease metabolism of statin via inhibition of cyp3a4 by grapefruit juice --> increased serum levels of statin --> increased toxicity.
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what type of biotransformation reaction does ezetimibe have to go through before it becomes active? where does this occur?
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glucuronidation in the intestine
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what are the side effects associated with nicotinic acid?
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1. abnormal hepatic function
2. intense flushing and pruritis 3. decreased glucose tolerance 4. cardiac arrhythmias and palpitations |
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what are two contraindications for nicotinic acid?
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1. previous liver disease
2. pregnancy |
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which two fibric acid derivatives are considered pro drugs? what biotransformation reaction must they undergo before becoming active?
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clofibrates and fenofibrate - undergo ester hydrolysis
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what is the equation for total cholesterol?
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HDL + LDL + TG/5
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when is calculating LDL using the HDL +LDL + TG/5 equation not appropriate/accurate?
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when TG levels are above 400 mg/dL
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what does the 30 per 30 rule refer to?
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with every 30 mg/dL reduction in LDL you get a 30% reduction in heart disease risk.
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what is considered normal TG levels?
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less than 150 mg/dL
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what drugs can cause elevated TG?
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bile acid-binding resins
oral estrogens oral retinoids protease inhibitors non-ISA beta-blockers (not clinically significant) |
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why do we need to monitor TSH and vitamin D in patients receiving statin therapy?
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hypothyroidism and vitamin D deficiency can increase risk of statin-induced myopathy
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what are two ways to manage patients with myalgia (but not myopathy) while on statin therapy?
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concurrent use of CoQ-10 or alternating day dosing of long helflife statins (atorvastatin and rosuvastatin).
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what is the criteria for myopathy?
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myalgia + elevations in serum CK greater than 10xULN
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what is the criteria for rhabdomyolysis?
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CK greater than 1000o IU/L or
CK greater than 10xULN and elevation in SCr or medical intervention with IV hydration therapy (coca cola urine) |
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how often is fasting lipid panel monitored in statin therapy?
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baseline, 6 weeks after starting or changing dose, once or twice a year when on stable dose.
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if statin therapy is used in combination with these two drugs, CK measurements should be taken when combination therapy begins. what are these two drugs?
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fibrate or niacin
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which two statins are metabolized by CYP3A4?
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simvastatin and lovastatin.
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what are two contradictions for statin therapy?
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pregnancy and active liver disease
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what is the max dose of simvastatin when co-administerd with gemfibrozil?
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10mg/day
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double the dose of a statin has what general effect on LDL?
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6% additional LDL reduction from baseline a.k.a an additional 10 point reduction in LDL.
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what is the max starting dose of atorvastatin?
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40
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which three statins need to be dosed in the evening to maximize effect?
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lovastatin, simvastatin and fluvastatin
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which statin requires adminsitration with food to assure sufficient absorption?
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immediate-release lovastatin
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are bile acid sequestrants considered safe in pregnancy?
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yes
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what are common side effects for colestipol, cholestyramine and colesevelam?
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constipation and GI upset
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which of the three bile acid sequestrants has less binding interactions?
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colesevelam
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