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This Concept Map, created with IHMC CmapTools, has information related to: Hyperlipidemia, Drugs for Hyperlipidemia Diet Fat Content ណ% caloric intake Saturated Fats < 10% caloric intake Good Foods: Soluble Fiber Psyllium Garlic Antioxidants - Vit E, C, beta-carotene, Se EtOH/Wine, Drugs for Hyperlipidemia Fibrates GEMFIBROZIL fenofibrate clofibrate-old, many ADRs MOA -Activate PPARalpha ->LPL->remove TGs from VLDL ->apoproteins A-I, A-II ->increase HDL Indications -hyper-TG-emia -hypercholesterolemia -HDL deficiency ADRs -blood cell deficiencies -hypersensitivity rxns -rhabdomyolysis (no statins!!), Drugs for Hyperlipidemia HDL DECREASE HDL Androgens Obesity Cigarette Smoking Fam HDL def DM-II Hyper-TG-emia, Drugs for Hyperlipidemia Fish Oils Omega-3 PUFAs (Omacor) -eicosapentanoic+docosahexaenoic MOA -dec. hep synth of TGs, VLDL -dec. plt aggregation ADRs -eructation, dyspepsia, dysgeusia -dec. LDL -hyperglycemia, Drugs for Hyperlipidemia NICOTINIC ACID = Vitamin B3 = Niacin MOA - inhibit FFA mobilization Lipid Effects - 500 mg/day -inhibit lipolysis in adipose ->reduce FFAs ->inhibit VLDL synth/secretion -SIGNIFICANTLY INCREASES HDL ->decrease totalC/HDL ->decrease LDL/HDL ->decrease ApoB/ApoAI Non-lipid Effects - 20mg/d -Precursor of NAD ->redox, ATP from ETC -Anti-inflam, antiox -Inhibit TNF, NFkb, PPARg ADRs -Release of PGD2 in skin -vasodilation, flushing, pruritus -preTx w/ aspirin -Hepatotoxicity, Gastric ulcers -Hyperuricemia -Impaired insulin sensitivity, MOA-block xport at sm int brush border -blocks dietary and biliary cholesterol -better tolerance than resins -no effect on liver/mm fcn Uses - can combine w/ statin ->same effect as highest statins -less toxicity Pharmacokinetics -conjugated (glucuronide) -T1/2 = 22 hrs ADRs - few -may predispose to GALL STONES -HA, myalgia + MOA - competitively inhibits HMG-CoA-R ->reduce hep cholesterol biosynthesis ->increase LDL receptors ->more LDL to liver, less VLDL made Effects -> 20-40% LDL decrease, 10% HDL inc. ->increase plaque stability Non-lipid Effects -anti-inflam: stroke, osteo, Pharmacokinetics-take in pm to prevent synth -Metabolized by CYP3A4 -[] inc'd by: erythromycin, antifungals, grapefruit juice, HIV anti-RVs, mafzolidone ADRs -generally well-tolerated -myalgia, myositis->rhabdomyolysis (watch for dark urine) -don't combine w/ fibrates COMBO - statin + resin OR ezetimibe, Drugs for Hyperlipidemia HDL INCREASE HDL Estrogens Exercise Leanness EtOH Fam. hyperalphaproteinemia Antihyperlipidemic Rx, MOA -bound Cl- exchanged for bile acid ->excreted in feces -more bile acid synth, hep LDL-Rs ->decrease serum LDL Indications -younger pts -pts who can't tolerate other Rx -take powder w/ before meals/bedtime ADRs - few -constipation, fecal impaction -take w/ full glass of water -can bind other Rx (statins, warf, digoxin) -take 2 hrs pre or post to prevent + MOA - competitively inhibits HMG-CoA-R ->reduce hep cholesterol biosynthesis ->increase LDL receptors ->more LDL to liver, less VLDL made Effects -> 20-40% LDL decrease, 10% HDL inc. ->increase plaque stability Non-lipid Effects -anti-inflam: stroke, osteo, Pharmacokinetics-take in pm to prevent synth -Metabolized by CYP3A4 -[] inc'd by: erythromycin, antifungals, grapefruit juice, HIV anti-RVs, mafzolidone ADRs -generally well-tolerated -myalgia, myositis->rhabdomyolysis (watch for dark urine) -don't combine w/ fibrates COMBO - statin + resin OR ezetimibe, Drugs for Hyperlipidemia Bile Acid Sequestrants (resins) CHOLESTYRAMINE-powder Colestipol-powder Colesevelam-tablet (OK w/ other Rx) MOA -bound Cl- exchanged for bile acid ->excreted in feces -more bile acid synth, hep LDL-Rs ->decrease serum LDL Indications -younger pts -pts who can't tolerate other Rx -take powder w/ before meals/bedtime ADRs - few -constipation, fecal impaction -take w/ full glass of water -can bind other Rx (statins, warf, digoxin) -take 2 hrs pre or post to prevent, Drugs for Hyperlipidemia Cholesterol Absorption Inhibitor EZETIMIBE MOA-block xport at sm int brush border -blocks dietary and biliary cholesterol -better tolerance than resins -no effect on liver/mm fcn Uses - can combine w/ statin ->same effect as highest statins -less toxicity Pharmacokinetics -conjugated (glucuronide) -T1/2 = 22 hrs ADRs - few -may predispose to GALL STONES -HA, myalgia, Drugs for Hyperlipidemia HMG CoA Reductase Inhibitors LOVASTATIN-cross BBB simvastatin-cross BBB (->ADRs) atorvastatin MOA - competitively inhibits HMG-CoA-R ->reduce hep cholesterol biosynthesis ->increase LDL receptors ->more LDL to liver, less VLDL made Effects -> 20-40% LDL decrease, 10% HDL inc. ->increase plaque stability Non-lipid Effects -anti-inflam: stroke, osteo, Pharmacokinetics-take in pm to prevent synth -Metabolized by CYP3A4 -[] inc'd by: erythromycin, antifungals, grapefruit juice, HIV anti-RVs, mafzolidone ADRs -generally well-tolerated -myalgia, myositis->rhabdomyolysis (watch for dark urine) -don't combine w/ fibrates COMBO - statin + resin OR ezetimibe