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37 Cards in this Set
- Front
- Back
First line treatment for hyperlipidemia |
Diet and Lifestyle modification |
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Second-line treatment for hyperlipidemia |
Pharmacologic intervention |
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Drugs that increase LDL Cholesterol |
1. Progestins 2. Steroids 3. Corticosteroids 4. Cyclosporine 5. Thiazide diuretics |
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Drugs that increase Triglycerides |
1. Estrogen 2. Protease inhibitors 3. Corticosteroids 4. Isotretinoin 5. Atypical psychotics 6. Thiazide diuretics 7. Beta blockers |
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Drugs that decrease HDL cholesterol |
1. Progestins 2. Protease inhibitors 3. Steroids 4. Isotretinoin 5. Atypical psychotics 6. Beta blockers |
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Diet therapy for Hyperlipidemia |
1. Cholesterol lowering diets (decrease HDL and LDL) 2. Mediterranean diet 3. Vegetables and fruits 4. Foods that reduce LDL (Oats, garlic, soy protein, vitamin C) |
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Lifestyle changes to treat hyperlipidemia |
1) Weight reduction 2) Increased physical activity 3) No alcohol or smoking |
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Names of Fibrates |
1) Clofibrate 2) Gemfibrozil 3) Fenofibrate |
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Fibrates - Mechanism of Action |
1) Activate PPAR alpha, which increases transcription of lipoprotein lipase, apo A-I and apo A-II, and decreased levels of apo C-III 2) Increased catabolism of VLDL and IDL due to increased lipoprotein lipase levels 3) Increase plasma HDL levels via induction of apo A-I and apo A-II 4) Inhibits lipolysis via reduction in apo C-III 5) Decreases plasma VLDL and triglycerides |
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Clinical use of fibrates |
Treatment of patients with type IV and V hyperlipidemia who are at greater risk for pancreatitis and who have not undergone dietary intervention |
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Adverse effects of Fibrates |
1) Mild GI disturbances and distress 2) Cholelithiasis 3) Malignancy (primarily with clofibrate) 4) Myositis 5) Hypoglycemia 6) May increase LDL in patients with hypertriglycemia |
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Drug interactions associated with Fibrates |
Potentiates warfarin and sulfonyurea |
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Fibrates - Contraindications |
1) Patients with liver or severe renal disease 2) Primary biliary cirrhosis 3) Preexisting gall bladder disease |
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Bile Acid Resins - Mechanism of Action |
1) Bind bile acids in the intestine to form complex that is excreted in feces 2) Increases conversion of plasma cholesterol to bile acids and increase expression of LDL receptors 3) Feedback inhibition of 7 alpha hydroxylase |
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Clinical use of Bile Acid Resins |
1) Treat patients with elevated LDL (used with other drugs) 2) To treat heterozygous familial hypercholesterolemia 3) To reduce itching in cholestasis 4) To bind toxicological agents like digoxin 5) As adjunctive treatment for pseudomembranous colitis |
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Adverse Effects of Bile Acid Resins |
1) GI disturbances (constipation, nausea, bloating, abdominal pain) 2) Reduction of fat soluble vitamins 3) Malabsorption of vitamin K, vitamin C and folic acid 4) Interferes with absorption of other drugs (like tetracycline, phenobarbital, and digoxin) |
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Bile acids - Contraindications |
1) Pregnant or lactating women 2) Patients with severe hepatic and renal dysfunction 3) Pre-existing gall bladder disease 4) Patients with elevated triglycerides |
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Ezetimibe |
1) Prevents intestinal absorption of cholesterol 2) Decreases LDL (but not HDL) 3) Often used in combination with statins |
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Ezetimibe - Side effects |
1) GI distress 2) Headache 3) Increased risk of hepatic toxicity |
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Colesvelam |
1) Synthetic soluble fiber that reduces LDL cholesterol 2) Does not bind digoxin, warfarin or statins 3) Required to take 6 tablets a day |
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Statins - Mechanism of action |
1) Inhibit HMG-CoA reductase 2) Results in decreased liver and plasma cholesterol 3) Increases HDL and cell surface LDL receptors 4) Decreases hepatic production of VLDL and apoB |
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Clinical uses of Statins |
1) Primary prevention of cardiovascular disease 2) Secondary prevention of cardiovascular disease in patients with evidence of heart disease 3) Treatment of type IIa, IIb, III and IV hyperlipidemias 4) Treatment of primary dysbetalipoproteinemia 5) Treatment of homozygous and heterozygous familial hypercholesterolemia |
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Side Effects of Statins |
1) Liver toxicity --> increased aminotransferase activity 2) Muscle disintegration 3) Renal insufficiency--> increased creatine kinase 4) Systemic lupus erythrematosus (SLE)-like syndrome 5) Decreased ATP synthesis |
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Statins - Key Drug Interactions |
1) Enhanced toxicity with P450 inhibitors (especially those that compete with CYP3A4 and CYP2C9) 2) Increases coumadin (warfarin) levels 3) Interacts with the drugs amiodarone, amlodipine and ranolazine 4) Increased catabolism of statins by drugs that induce CYP3A4 |
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Statins - Contraindications |
1) Pregnancy and nursing mothers 2) Children and teenagers 3) Patients with liver disease |
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Niacin - Mechanism of Action |
1) Inhibits lipolysis in adipose tissue, resulting in decreased hepatic VLDL and LDL synthesis 2) Activates lipoprotein lipase, resulting in enhanced VLDL clearance 3) Decreases plasma VLDL, LDL and triglycerides 4) Increases plasma HDL levels 5) Increase tPA and decreases fibrinogen |
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Clinical Uses of Niacin |
1) Adjunctive treatment of dyslipidemias 2) Used in combination with other anti-dyslipidemic agents (such as bile acid resins and reductase inhibitors) 3) Treatment of hypertriglyceridemia in patients at risk for pancreatitis 4) Treatment of peripheral vascular disease and circulatory disorders 5) Treatment of pellagra
6) Also used as a dietary supplement |
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Adverse effects of Niacin |
1) Intense cutaneous flush and pruritus 2) Nausea and abdominal pain 3) Predisposes to hyperuricemia and gout
4) Hyperglycemia 5) Hepatotoxicity (RARE) 6) GI ulcer exacerbation |
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Niacin - Contraindications |
1) Patients with liver disease 2) Active peptic ulcer disease (PUD) 3) Arterial bleeding 4) Use with caution in patients with diabetes and gout 5) Interacts with statins; use niacin+statin combination with caution |
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Rimonabant |
1) Endocannabinoid receptor blocker that increases HDL and reduces triglycerides 2) Side effects include nausea, vomiting, diarrhea, headache, dizziness and anxiety 3) Contraindicated in patients with depression and those on antidepressant medication |
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Orlistat |
1) Inhibitor of pancreatic, gastric and carboxylester lipase enzymes 2) Reduce intestinal absorption of fat, LDL cholesterol and triglycerides 3) Increases HDL |
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Sibrutamine |
1) Monoamine uptake inhibitor 2) Increases HDL and reduces triglycerides (NO effect on LDL cholesterol!) |
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Omega-3-Fatty Acids |
1) Reduce VLDL particle synthesis 2) Used as treatment for hypertriglyceridemia or adjunct to diet in type IV hyperlipidemia 3) Used in combination with statins to treat type IIb hyperlipidemia |
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Plant Sterols |
1) Reduces LDL cholesterol by up to 15% 2) Used along with diet to treat patients with hypercholesterolemia |
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Surgery (Partial Ileal Bypass) |
1) Potential therapy for hypercholesterolemia 2) Side effects include diarrhea, renal calculi, gallstones and intestinal obstruction |
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Combination therapies used to reduce LDL |
1) Statins + ezetimibe 2) Statins + bile acid resin 3) Bile acid resin + ezetimibe |
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Combination therapies used to increase HDL and lower triglycerides |
1) Statins + niacin 2) Statins + fibrate |