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Hypolipidemics
lecture 14 sternweis
| Question | Answer |
|---|---|
| LDL-C | long-lived reservoir of chol and the major way chol is carried in the blood; conc'n of this is thus most closely correlated with atheromatous dz |
| triglycerides are transported as | chylomicrons, the levels of which are very responsive to and correlate well with meals |
| VLDL | released from the liver after it has taken up chylomicron remnants, composed of triglycerides and chol esters; levels are especially high after eating a carb heavy meal |
| familial hypercholesterolemia | specific elevation of LDL due to a genetic defect in the LDL-R in extrahepatic tissues (cells can't signal to LDL that they need it to release chol for their uptake, so it stays in the blood) |
| chol metabolism and the liver | liver makes 1g of chol de novo per day, along with what's eaten it's converted to bile acids, secreted into intestine or converted to esters for storage in liver or made into VLDL |
| enzyme that liver uses to make chol | HMG-coA reductase, transcription and activity of this enzyme are suppressed when levels of chol are high within cells (signaled by SREBPs) |
| VLDL accounts for the bulk of circulating _____ | triglycerides, as long as chylomicron metaboism is intact |
| avg value of total serum chol | 200 mg/dL (sum of VLDL-C, LDL-C & HDL-C); 240+ mg/dL is considered high |
| VLDL values in serum | chol:triglyceride levels should normally be 1:5 --> chol = 20-40 mg/dL and triglycerides 100-150 mg/dL |
| LDL values in serum | normal values are 120-130 mg/dL; however optimally it should be < 100 mg/dL. cutoff of high vs very high is 190 mg/dL |
| HDL values in serum | 45-55 mg/dL; < 40 is considered abnormal in males, <50 mg/dL abnl in females |
| lipid triad that promotes higher risk for developing CAD | elevated TG and LDL-C with lowered HDL-C |
| adverse effect of hypertriglyceridemia | pancreatitis, must treat high risk pts with levels above 200 mg/dL |
| the higher one's risk factors, the more aggressive the antihyperlipidemic tx and values that should be maintained (generally < 100 mg/dL) | those with CAD, DM or prev atherosclerotic event should keep LDL-C < 70 |
| therapeutic use of statins and why | lower total and LDL-C up to 50%, lower high trigylceride level by ~ 20%, modest increase in HDL |
| atorvastatin, simvastatin and lovastatin are all metabolized by which P450 | CYP3A4 thus warfarin, macrolides, cyclosporines, azoles, etc can inc amts of statins in body through competitive inhibition for metabolism |
| mechanism of statin action | inhibits HMG-CoA reductase, which forces liver to clear more LDL, its precursors and receptors in order to have sufficient amts of chol. may inhibit apoB100 and VLDL production? |
| major adverse effect of statins | inhibition of endogenous steroid production. DON'T GIVE TO PREG WOMEN |
| side effects of statins | decreased liver function (elevated liver enzymes), proximal muscle myopathy. both are dose-dependent and completely reversible |
| food that inc amt of statins in body when eaten | grapefruit; all drugs but prevastatin |
| drug class for tx of hypercohlesterolemia and sitosterolemia (plant sterol excess) | chol uptake inhibitors block absorption in the SI |
| physiologic results of chol uptake inhibitors | lowers total and LDL-C by up to 20% (not as much as statins), modest dec in triglycerides and inc in HDL; limited by upregulation of HMG-CoA reductase |
| example of chol uptake inhibitor | ezetimibe (now combination with statin is available = Vytorin aka ezetimibe/simvastatin that has more than double the efficacy of single drug therapy) |
| bile acid sequestrant mechanism of action | binds bile acid in the gut and prevents reabsorption so liver must make more de novo from chol that's in the blood |
| population that bile acid sequestrants works best for | those for whom you want to avoid systemic therpy: women of childbearing age, children with FH, pts with only modest inc LDL leels |
| example of bile acid sequestrant | cholestyramine |
| problems with bile acid sequestrants | they taste nasty, cause constipation, bind fat soluble vitamins (vit K) and other drugs like digitalis, warfarin and thyroxine |
| major effect of nicotinic acid (supraphysiologic level of niacin) | dec hepatic synthesis of triglycerides through unk mechanism; also somewhat limits lipolysis in adipose tissue) |
| therapeutic use of nicotinic acid | it can lower both total chol (LDL-C dec by up to 20%) and triglycerides (up to 70% reduction) |
| side effect of nicotinic acid | severe cutaneous flushing, nausea, abd pain, pruritis and dry skin. may exacerbate hyperglycemia, hyperuricemia, PUD and liver dz |
| gemfibrozil | fibrate: activates PPARs to dec apoCIII, triglyc. synthesis and inc activity of LPL. used for those with severe hypertriglyceridemia, well-tolerated generally in diabetics with mild risk for myopathy |
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sirprakes
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