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58 Cards in this Set
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complexes of cholesterol, TGs, and protein used to transport cholesterol from the liver to peripheral cells and back.
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lipoproteins
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transports fatty acids and cholesterol derived from the diet or synthesized in the intestine from the gut to the liver
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chylomicrons
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- formed mainly in the liver
- transports endogenous TGs and cholesterol - contains 15-20% of the total blood cholesterol and most of the TGs measured in the fasting pt |
VLDLs
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the cholesterol in VLDL is about ___ of total TG conc
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1/5
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- formed by VLDL catabolism
- transports (60-70%) of cholesterol to the cells - greatest contribution to the development of artherosclerosis - main target of cholesterol lowering drugs |
LDLs
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- formed in the liver and intestine
- transports cholesterol from peripheral cells to the liver |
HDLs
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a ___ hr fast is req'd to measure cholesterol
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12
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TG level must be < ___ to measure cholesterol
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400 mg/dL
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total cholesterol - (HDL + VLDL) = ___
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LDL
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what is not directly measured with a cholesterol measurement
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VLDL (TG/5) and LDL (cholesterol - HDL and VLDL)
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Type I hyperlipoproteinemia
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elevated chylomicrons
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Type IIa hyperlipoproteinemia
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elevated LDL
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Type IIb hyperlipoproteinemia
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elevated LDL and VLDL
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Type III hyperlipoproteinemia
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elevated IDL
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Type IV hyperlipoproteinemia
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elevated VLDL
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Type V hyperlipoproteinemia
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elevated VLDL and chylomicrons
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MC lipid abnormality
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polygenic hypercholesterolemia
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caused by a combination of environmental and genetic factors
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according to ATP III classification, what are goals for LDL, HDL, TG, and total cholesterol levels?
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LDL < 100 mg/dL
HDL 40-60 mg/dL TG < 150 mg/dL Total cholesterol <200 |
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three categories of risk that modify LDL goals
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(1) CHD and Diabetes < 100 mg/dL
(2) 2+ risk factors < 130 mg/dL (3) <2 risk factors < 160 mg/dL |
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major risk factors
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- cigarettes
- HTN (>140/90 mmHg) - low HDLs (<40 mg/dL) - FamHx of premature CHD - men >45 y/o women >55 y/o |
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LDL level for considering drug therapy for (1) CHD (2) 2+ risk factors (3) <2 risk factors
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(1) >130 mg/dL
(2) >130 mg/dL if 10 yr risk @ 10-20%; >160 mg/dL if 10 yr risk @ <10% (3) >190 mg/dL |
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HMG CoA Reductase Inhibitors
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"-statins"
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contraindications for statins
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absolute: liver dz
relative: drugs that inhibit P450 3A4 (macrolides, CCBs, and azole antifungals) |
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BCF statin
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Simvastatin
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most efficacious statins (2)
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atorvastatin and rosuvastatin
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statins that can be dosed anytime
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atorvastatin and rosuvastatin
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statins that can be used w/ renal insufficiency
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atorvastatin and fluvastatin
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statins that are not affected by C P450 drug interactions
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pravastatin and fluvastatin
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statin not highly protein bound
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pravastatin
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statin assoc w/ rhabdomyolysis or myopathy when combined w/ fibric acid
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lovastatin
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what must be monitored when administering statins?
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CPK (myopathy and rhabdomyolysis)
LFTs (obtain baseline and repeat q 6 mos) |
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how long in between dosing changes w/ statins?
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6 wks
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which antihyperlipid drug class if liver dysfunction is present?
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bile acid sequestrants (BAS)
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what are SEs of BAS agents?
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- GI distress/constipation
- decreased absorption of other drugs |
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MOA of BAS agents
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more cholesterol gets converted into bile acids
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how long between BAS agents and fat-soluble vits, folic and ascorbic acid?
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6 hrs
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colestipol (colestid) BCF
cholestyramine (questran) colesevelam (welchol) |
bile acid sequestrants
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which antihyperlipid class is last line due to GI side effects?
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BAS
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which BAS agent reqs the smallest dose (best for pt compliance)?
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colesevelam
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which antihyperlipid class is DoC for pregnancy?
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BAS
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demonstrated therapeutic benefits of BAS incl:
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- reduce major coronary events
- reduce CHD mortality - only approved agent in pregnancy |
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MOA of nicotinic acid (niacin)
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reduces VLDLs resulting in reduced LDLs
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what is best antihyperlipid agent for increasing HDLs?
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nicotinic acid (niacin)
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what are SEs of Niacin?
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- flushing and itching
- hyperglycemia - hyperuricemia - upper GI stress - hepatotoxicity |
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how can flushing and itching assoc w/ niacin be minimized?
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- ASA 30 min prior
- take w/ meals - titrate up slowly - use controlled release products |
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CIs for Niacin use:
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- liver dz
- PUD - hypersensitivity - caution w/ statins (myopathy and rhabdomyolysis) |
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MOA of Fibric acids
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stimulates lipoprotein lipase which removes chyolmicrons and VLDLs from plasma
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what is best agents for decreasing TGs?
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fibric acids
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what happens to VLDLs when they are catabolized by lipases?
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broken down into IDLs and LDLs
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SEs of fibric acids:
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- GI distress
- gallstones (Lithiasis) - myopathy and muscle inflammation |
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CIs of Fibric Acids
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- severe renal dz
- severe liver dz - caution w/ statins (myopathy and rhabdomyolysis) |
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therapeutic benefits of fibric acids
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- reduce progression of coronary lesions
- reduce major coronary events |
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Ezetimibe (Zetia)
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Selective Cholesterol Absorption Inhibitor
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lower doses of statins may be possible during combined therapy with:
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Ezetimibe (Zetia)
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antihyperlipidemic approved for children 10-18 y/o
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Ezetimibe (Zetia)
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tx for hypertriglyceridemia
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niacin, fibrates, and atorvastatin
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in txing hyper-TGs, avoid ___ in diabetics and ___ in high LDL pts
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niacin; fibrates
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stop HMG-CoA reductase inhibitor medication if LFT levels go to ___x the normal upper limit
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3x
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