Term
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Definition
| LDL = Tc - (HDL + VLDL) where VLDL = TG/5 |
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Term
| Name 3 basic strategies to improve lipid profile |
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Definition
1. Lower LDL
2. Lower plasma TG
3. Increased synth of ApoA-1 and ApoA-1 increases HDL conc |
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Term
| 4 methods of lowering plasma LDL concentrations |
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Definition
1. Increase hepatice LDL Receptors
2. Decrease the synthesis of ApoB100 to decrease the hep prod of VLDL
3. Increase the rate of clearance of VLDL and IDL cholesterol
4. decr plasma TG results in the production of larger less easily oxidized LDL particles. |
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Term
| 2 strategies to lower plasma TG conc |
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Definition
1. decrease the synth of ApoB100 decr prod for hep VLDL
2. activate peroxisom proliferator actvated Receptor alpha |
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Term
| What does PPAR alpha activation do? |
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Definition
1. Increase the oxidation of fatty acids thus reduces the availabiltiy of substrate needed for synthesis of TGs
2. increases the synth of lipoprotein lipase an enzyme which increases the clearance fo TG rich lipoproteins
3. reduces the expr. of the hep gene coding for ApoC-3 b/c ApoC-3 inhibits the receptor mediated and lipolytic clearance of VLDL |
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Term
| Name the statins which are met by CYP3A4 |
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Definition
Fluvastatin
Atorvastatin
Lovastatin
Simvastatin |
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Term
| Name the statins with few D-D interactions |
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Definition
Pravastatin
Rosuvastatin have good PR |
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Term
|
Definition
inhibit HMG-CoA reductase which inh the prod of cholesterol
depleted sterol pool leads to increased synthesis of hepatic LDL receptors which increases clearance of LDL and IDL from plasma |
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Term
| overiding caveot of statins |
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Definition
| Both LDL-R and HMG-CoA production are induced by low cholesterol levels. thus the effects of statins are blunted |
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Term
| do statins work without LDL-receptors |
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Definition
| NO - only a 7-10 % fall is seen, you need the plasma reuptake of LDL- receptors to get the full effect. Just blocking chol synth with HMG-CoA inhib isn't enough. |
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Term
| Statin effect on VLDL metabolism |
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Definition
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Term
| Statins that will decrease LDL 30 to 35% |
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Definition
Lovastatin
Atorvastatin
Rosuvastatin
Simvastatin |
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Term
| Other cardio protective effects of the statins |
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Definition
1. Increased stability of cholesterol plaques
2. Reversal of endothelial dysfxn with improved ability to synthesize NO
3. decreased oxidation of LDL cholesterol
4. an antiinflammatory effects which produces a fall in the plasma concentration of CRP |
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Term
|
Definition
Hepatic - so make a baseline AST ALT meas
Myopathy - incr in plasma creatine phosphokinase with or w/o myalgia |
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Term
|
Definition
Hepatic - so make a baseline AST ALT meas
Myopathy - incr in plasma creatine phosphokinase with or w/o myalgia |
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Term
|
Definition
| clarithro, fluconazole, fluoxetine, fluvoxamine, metronidazole, nefazodone, sertraline, zafirlukast, verapamil, and amiodarone |
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Term
| Increased Myopathy with what drug combo? |
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Definition
| statin + gemfibrozil or niacin |
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Term
| Inh of CYP3A4 by other drugs increases the probability that which statin drugs will produce myalgia? |
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Definition
Atovastatin
Lovastatin
Simvastatin |
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Term
| Inh of CYP2C9 will increase myalgia with |
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Definition
|
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Term
|
Definition
| warfarin cimetidine, phenytoin, omeprazole, and amiodarone |
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Term
|
Definition
| release of massive myoglobin, occludes PT lumen - leads to ARF |
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Term
|
Definition
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Term
|
Definition
| blocks the protein mediated transporter which absorbs dietary cholesterol from GI tract - leads to increased LDL-R and induction of HMG-CoA by sterol stat |
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Term
| Therapeutic uses of Ezetimibe |
|
Definition
used with a statin
allows a large decrease in the daily statin dose without losing the beneficial effect of a statin |
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Term
|
Definition
Liver toxicity
does NOT increase risk of myopathy
NO effect of CYPs so no D-D interactions
Preg Cat C = Bad |
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Term
|
Definition
cholestyramine
colestipol
colesevelan |
|
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Term
|
Definition
| swap Cl- for neg charged bile acids which decreases chol abs which decreases sterol pool which upregulates LDL-R and HMG-CoA |
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Term
| DO Resins work w/o LDL -R |
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Definition
|
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Term
| Ion exchange resin toxicities |
|
Definition
GI - Const, bloating and pain
Bind other drugs and prev abs - warfarin, propranolol, tetracyclines, furosemides, hydrochlorothiazides, pravastatin, fluvastatin, and thyroxine |
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Term
| If you have to take a resin which one do you take |
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Definition
Colesevelan - Preg cat B and
does not affect bioavail of digoxin, lovastatin, atorvastatin, simvastatin, and warfarin |
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Term
|
Definition
It inhibits lipolysis in adipocytes which leads to decreased plasma FFA's and decreased plasma FFA's decreases hep synth of TG's -> decreased synth of hep TG reduces the synth of VLDL
activation of lipoprotein lipase increases the clearance of VLDL
BIG - decr in rate of catab of apoA-1 increases plasma HDL |
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Term
| Used to treat patients with low HDL and high TG? |
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Definition
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Term
|
Definition
Preg C
flusing at first
GI nausea and vom
Gout |
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Term
| Big contraindication for Niacin |
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Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
bind to PPAR alpha in liver, brown adipose, sk m., heart and kidnery to cause a decrease plasma TG via increased clearance of VLDL
gives increased peroxisomes, lipoprotein lipase, and reduces expression of ApoC-3 which inh clearance of VLDL
stimulates Apoa-1 and apoa-3 leading to incr HDL
incr hep rel of SREBP which increases LDL-R and HMG-CoA Red |
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Term
| Drugs which significantly increase HDL synth |
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Definition
|
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Term
|
Definition
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Term
| Drugs not safe for diabetics |
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Definition
|
|
Term
| only drugs somewhat safe for preg |
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Definition
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|
Term
| only drugs somewhat safe for preg |
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Definition
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Term
| Do you get myopathy with fibrates? |
|
Definition
| Yes, but use fenofibrate as opposed to gem for a lower risk of myopathy |
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Term
|
Definition
activates PPAR alpha to enhance FA oxid in liver and sk muscle which reduces the substrate available for VLDL
Direct activation of lipoprotein lipase enhances the clearance of TG rich VLDL
incr degr of apoB100
incr hep glycogen synth |
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