Term
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Definition
| Statins, Bile Acid Sequestrants, Fibric Acid Derivatives, Niacin, Ezetimibe |
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Term
| Lipid disorders are important |
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Definition
Risk for vascular disease
High triglycerides increase risk for pancreatitis, metabolic syndrome |
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Term
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Definition
Transporting lipids in blood is a problem since blood is aqueous and lipids are hydrophobic
Most lipid transport in blood is via carriers called lipoproteins. These are particles of several million MW comprised of amphipathic proteins and lipids
Outer surface is largely a monolayer of triglycerides mixed with an apolipoprotein.
Inner layers are mixtures of lipids including cholesteryl esters (nonpolar) |
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Term
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Definition
| Remarkably effective. Cause up to 60% reductions in LDL cholesterol, 10% increase HDL, slight declines in triglycerides. Also reduce C-reactive protein. |
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Term
| Drug Therapies Bile acid sequestrants |
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Definition
| 20% decrease in LDL cholesterol |
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Term
| Drug Therapies Fibric Acids |
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Definition
| 20% reductions in LDL, 20% increase in HDL, 50% reduction in triglycerides/VLDL (additive with statins; no additional clnical benefit; ACCORD trial 2010). |
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Term
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Definition
| 40% decline in VLDL (and triglycerides), 25% decline in LDL, 30% increase HDL (additive with Stains; no additional clnical benefit; AIM-HIGH trial 2011) |
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Term
| Drug Therapies Cholesterol absorption inhibitor |
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Definition
| Ezetimibe. 20% reductions LDL and total cholesterol. No effects on triglycerides or HDL. Additive with statins (but no additional protection from heart disease). |
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Term
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Definition
Block HMG-coA reductase, the rate limiting enzyme in cholesterol synthesis in liver.
The decrease in liver intracellular cholesterol leads to increased LDL-R expression and uptake of LDL cholesterol from the circulation
Pleiotropic Effects- May require highest doses
Increases eNOS, benefiting vessels?
Reduces inflammation and C-Reactive Protein (independent risk factor)
Reduces platelet aggregation and oxidation |
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Term
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Definition
| Cholestyramine, colestipol, colesevelam |
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Term
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Definition
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Term
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Definition
| Block cholesterol synthesis in liver. Compensatory increase in LDL-R reduces circulating LDL |
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Term
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Definition
| Activate PPAR-alpha leading to increased lipoprotein lipase and reduced circulating triglycerides |
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Term
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Definition
| Binds bile acids in gut increasing excretion. Leads liver to increase LDL-R to obtain more cholesterol for synthesizing increased amounts of bile acids |
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Term
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Definition
| Reduces VLDL production by liver and Apo-B100 thereby reducing LDL in circulation |
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Term
| Absorption inhibitors Summary |
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Definition
| (ezetimibe). Block uptake from GI tract to liver. Increase liver LDL receptors. Reduces circulating LDL |
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