Term
| Statins are the most effective at lowering |
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Definition
| LDL-C by inhibition of cholesterol synthesis (HMG-CoA reductase inhibitors) |
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Term
| Which statins have longer half lifes and can be administered anytime? |
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Definition
| atorvastatin, pravastatin, and rosuvastatin |
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Term
| side effects of statins and what do you monitor |
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Definition
| hepatotoxicity, rhabdomyolysis AL/AST/LFT, diabetes, minor reversible cognitive impairment |
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Term
| contraindications for statins |
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Definition
| pts with liver disease, pregnant, elevated liver function |
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Term
| what statin does not undergo hepatic clearance via cyp450 and is eliminated in the kidneys unchanged, can also be used with gemfibrozil |
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Definition
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Term
| verapamil requires a dose adjustment of which statin |
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Definition
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Term
| which two statins are administered as inactive lactone prodrug |
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Definition
| lovastatin (mevacor, altoprev) simvastatin (zocor) |
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Term
| first line agents for lowering plasma TG, may increase LDL-C levels when TG's are over 500mg/dL |
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Definition
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Term
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Definition
| bind to and activate PPAR-alpha receptors which behave as transcription factors and cause a change in gene expression for genes that code for proteins |
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Term
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Definition
| GI, muscle toxicity, elevated LFT, gallstone formation, elevated sCR |
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Term
| contraindications of fibrates |
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Definition
| pts with gallbladder disease, active liver disease, nursing, renal dysfunction |
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Term
| elimination and excretion of fibrates |
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Definition
| metabolized by glucuronidation via UGB2B7 and are renally excreted unchanged or glucuronide conjugated form |
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Term
| gemfibrozil is an inhibitor of... |
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Definition
| UGT1A1, UGT1A3, CYP2C8, 2C9 and 2C19 |
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Term
| fenofibrate is an inhibitor of.. |
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Definition
|
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Term
| 3 ways that gemfibrozil interactis with statins |
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Definition
| OATP2 (decreases statin clearance), inhibits statin phase 1 metabolism by CYP450 (2C9), inhibits statin phase II metabolism by UGT isoforms |
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Term
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Definition
| Fenofibrate, fenoglide, piofen, tricor, triglide, gemfibrozil (lopid) |
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Term
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Definition
| antara, fenofibrate, lofibra capsules |
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Term
| fenofibric acid formulations |
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Definition
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Term
| Bile-acid sequestrants lower ________ without _______. |
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Definition
| plasma cholesterol, a decrease in TG |
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Term
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Definition
consists of polymeric resin containing ammonium cations which function as ion exchange agents because Cl- ions combined with the BARs can be exchanged for bile acids;
decrease the bile acid concentration and decrease the feedback inhibition of bile acids on cholesterol metabolism -> increased conversion of cholesterol to bile acid |
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Term
|
Definition
| all are sustained release, do not crush or chew, titrate dose |
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Term
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Definition
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Term
| contraindications of BARs |
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Definition
| avoid in patients with elevated TG levels, in patients with history of bowel obstruction, TG induced pancreatitis |
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Term
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Definition
| Cholestyramine (Questran, prevalite), Colestipol (colestid) Colesevelam (Welchol) |
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Term
| Niacin lowers _____ and increases ________ |
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Definition
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Term
|
Definition
| must be titrated for all formulations |
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Term
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Definition
| inhibits the action of hormone sensitive lipase in adipose tissue; inhibiting lipolysis in adipose tissue. Also stimulates lipoprotein lipase which increases the breakdown of TG which decreases VLDL levels |
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Term
|
Definition
| flushing, pruritus, rash nausea, dyspepsia, abdominal pain, diarrhea, hepatotoxicity |
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Term
| precautions/contraindications for niacin |
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Definition
| diabetes (minor increase in glucose), raise uric acid so avoid in pts with gout, contraindicated in pts with active liver disease, active peptic ulcer, arterial bleeding |
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Term
| niacin eliminations (2 ways) |
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Definition
Pathway 1-hepatic metabolism by conjugation to form nicotinuric acid which is excreted in the urine along with uncharged niacin
*Pathway responsible for flushing
*Pathway 1 low affinity, high capacity system = niacin is metabolized by this pathway only after pathway 2 is saturated.
Pathway 2-involves number of re-dox RXNs that yield nicotinamide and ultimately pyridine metabolites.
*Pathway responsible for hepatoxicity
*Pathway 2 is high affinity, low capacity system which = niacin is metabolized initially via Path 2 until it becomes saturated (occurs rapidly) |
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Term
| combination of ______ with niacin enhances flushing |
|
Definition
| dihydropyridine calcium channel antagonists |
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Term
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Definition
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Term
| site and mechanism of action of ezetimibe |
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Definition
| cholesterol transporter on mucosal cells in brush border of small intestine, weak ACAT inhibitor, lowers cholesterol due to inhibition of cholesterol absorption via blocking transport protein in brush border of GI tract. Selective for cholesterol inhibition and onlyy slightly decreases TG levels |
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Term
| 2 types of omega-3's responsible for lowering levels |
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Definition
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Term
|
Definition
| competitive inhibition of TG uptake into lipoproteins such that chylomicron and VLDL-C formations are decreased |
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Definition
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Definition
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