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57 Cards in this Set
- Front
- Back
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What is metabolic syndrome classified as?
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3 of the following 5 risk factors.
Hypertension, Low HDL, Obesity, Hyperglycemia, High TGs. |
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What should be excluded before innitiating a patient on drug therapy for hyperlipidemia?
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Secondary causes of hyperlipidemia. Type 2 diabetes, hypothyroidism, obstructive liver disease, chronic renal failure and drugs.
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Dietary fat is taken up in the intestine and transported from the intestine into the bloodstream by what carrier?
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Chylomicrons
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What is the unique apolipoprotien found on chylomicrons?
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B-48
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What enzyme mobilizes FFAs and from chylomicrons and VLDL and where is it found?
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Lipoprotein lipase. It is found on endothelial cells.
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What is the unique apolipoprotein found on VLDL?
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B-100
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What is the mechanism of feedback regulation for lipid in the body?
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Increase or decrease in LDL receptor synthesis by the liver.
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What are the three bile acid sequestrants?
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Cholestyramine, Colestipol, Colesevelam.
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Which bile acid sequestrant is a polymeric hyrdophilic gel.
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Colesevelam.
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Why do bile acid sequestrants increase lipid plasma triglycerides?
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Decreased reabsorption of bile acids from the intestine leads to an increase in liver cholesterol and lipid synthesis. Leads to increased release of VLDL by the liver.
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By what mechanism do bile acid sequestrants decrease LDL?
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They cause the liver to increase LDL receptors which increases LDL uptake.
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What is the main effect of bile acid sequestrants?
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Decrease in LDL.
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What are the side affects associated with bile acid sequestrants?
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Bloating, Gas, Constipation.
(less severe with colesevelam) |
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What are the major drug interactions associated with bile acid sequestrants?
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They decrease the absorption of warfarin and digoxin. They can also decrease the absorption of fat soluble vitamins.
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How can the adverse drug-drug effects of bile acid sequestrants be prevented?
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By taking the other medications 2-4 hrs before bile acid sequestrants to minimize the decreased absorption.
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In which patients are bile acid sequestrants contraindicated?
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Patients with TGs above 400mg/dL
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What is the mechanism of action of the statin drugs?
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They inhibit HMG-CoA reductase leading to an increase in liver production of LDL receptors.
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Which statin drugs are the most efficacious?
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Rosuvastatin, Atorvastatin
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What statin drug is the least efficacious?
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Fluvastatin
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What is the effect of doubling a dose of any given statin?
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Modest increases in effect. Maximum decrease in LDL occurs at starting dose. Each doubling only produces 5-7% reduction in LDL.
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What are the effects of statins on LDL, HDL, and TGs?
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Decreased, Increased, Decreased.
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What is the outcome data results for statin drugs?
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They have been shown to decrease the risk of coronary heart disease and atherosclerosis.
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What are the adverse reactions associated with statin drugs use?
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They can cause myopathy, myalgia,myositis and rhabdomyolysis.
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Which stain drugs have are the most likely to be involved in a drug-drug interaction and why?
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Lovastatin and simvastatin. They are metabolized by CYP3A4 which can be inhibited or induced by other drugs.
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Which statin drugs are least likely to be involved in a drug-drug interaction/
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Pravastatin and Rosuvastatin.
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In which patients are statin drugs contraindicated?
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Patients with liver disease, preagnancy or breast feeding.
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What is the most efficacious drug class for lowering LDL?
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The statins
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What monitoring lab test should be run on patients taking statins?
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Liver enzyme tests and serum CK to measure the liver function and muscle breakdown.
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Which cholesterol drug affects the exogenous pathway?
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Cholesterol Absorption Blockers. Ezetimibe
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What is the mechanism of Ezetimibe
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Acts on the brush border of the small intestine to inhibit the absorption of cholesterol.
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What is the function of the Neimann-Pick C1 protein?
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It is a sterol influx transporter located at the apical membrane of enterocytes which facilitates the uptake of cholesterol. It is blocked by ezetimibe.
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What are the effects of ezetimibe on LDL HDL and TG's?
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Decreases, Increases, Decreases. Can be used with a statin to increase effectiveness.
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What is Vytorin.
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Combination drug of ezetimibe and simvastatin.
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What are the potential side effects of adding ezetimibe with a statin?
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Ezetimibe can increase the risk of developing myalgia or decreased liver function.
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What drugs interact with ezetimibe?
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Fibrates increase the bioavailability and cholestyramine can decrease absorption.
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What is the mechanism of action of Nicotinic Acid?
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It acts on GPR109A on adipocytes which inhibits cAMP. This decreases lypolysis and the release of FFA's
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What are the effects of nicotinic acid on LDL, HDL, TG, and LP?
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Moderate decrease, Significant increase, Significant decrease, Significant decrease.
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Simcor?
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Combination drug of simvastatin and niacin
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Advicor?
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Combination of lovastatin and niacin.
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What is the major side effect caused by nicotinic acid?
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Flushing. Nicotinic acid stimulates Langerhans cells in the skin to release arachidonic acid. This produces PG's which results in vasodilation.
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What are the secondary side effects of nicotinic acid.
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Increased insulin resistance leading to hyperglycemia
Hyperuricemia (gout) Hepatotoxicity (especially in sustained release preparation). |
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What are the three fibrates mentioned in class?
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Fenofibrate #1
Gemfibrozil Clofibrate (old) |
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What is the brand new fibrate that will potentially replace fenofibrate?
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Fenofibric acid
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What is the mechanism of action of the fibrates?
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They activate PPARa which forms a heterodimer with another nuclear receptor to regulate genes involved in lipid metabolism
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What is the effect of fibrates on liver and muscle tissue.
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It increases fatty oxidation in these tissues.
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What is the major effect of using fibrates?
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It increases HDL and lowers TG's. Fibrates are more efficacious than statins in these functions.
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What are the side effects of using fibrates?
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Myalgia -especially when combined with statins
Elevated liver enzymes Gallstones-mostly clofibrate |
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What are the drug-drug interactions associated with fibrates?
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They inhibit the glucuronidation of stains and antidiabetics.
They can increase the INR of warfarin. |
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In which patients are fibrates contraindicated?
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Patients with renal or heptaic dysfunction.
Preexisting gall bladder disease. Nursing mothers |
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What is the mechanism of action of PUFAs?
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Increased mitochondrial and peroxisomal B-oxidation in the liver.
Decreased lipogenesis in the liver Inhibition of acyl CoA 1,2 diacylglycerol acyltransferase. |
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What are PUFAs used to treat/
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Hypertriglyceridemia.
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What are the effects of PUFAs on LDL, HDL and TGs?
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Increased, Increased, Decreased
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What are the adverse effects of PUFAs?
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Generally well tolerated.
Dyspepsia, taste perversion, worsening of glycemic control in diabetics. |
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What is the mechanism of action of Orlistat?
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It inhibits gastric and pancreatic lipase. Results in decreased hydrolyzation of TGs and a reduction in FFAs.
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What is the primary use of Orlistat?
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Used as a weight loss drug.
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What are the major side effects of orlistat?
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GI. Fatty stools, increased defecation, flatulence.
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What are the drug-drug interactions associated with Orlistat?
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Decreased plasma levels of cyclosporin.
Decreased fat soluble vitamin absorption = increased bleeding in patients taking warfarin. |
