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Cardio - Antilipemic Drugs
Anti lipemics - statins, etc...
44
Pharmacology
Graduate
11/01/2010

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Term
Friedwald equation
Definition
LDL = Tc - (HDL + VLDL) where VLDL = TG/5
Term
Name 3 basic strategies to improve lipid profile
Definition
1. Lower LDL
2. Lower plasma TG
3. Increased synth of ApoA-1 and ApoA-1 increases HDL conc
Term
4 methods of lowering plasma LDL concentrations
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.
Term
2 strategies to lower plasma TG conc
Definition
1. decrease the synth of ApoB100 decr prod for hep VLDL
2. activate peroxisom proliferator actvated Receptor alpha
Term
What does PPAR alpha activation do?
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
Term
Name the statins which are met by CYP3A4
Definition
Fluvastatin
Atorvastatin
Lovastatin
Simvastatin
Term
Name the statins with few D-D interactions
Definition
Pravastatin
Rosuvastatin have good PR
Term
Basic MOA of statins
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
Term
overiding caveot of statins
Definition
Both LDL-R and HMG-CoA production are induced by low cholesterol levels. thus the effects of statins are blunted
Term
do statins work without LDL-receptors
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.
Term
Statin effect on VLDL metabolism
Definition
Term
Statins that will decrease LDL 30 to 35%
Definition
Lovastatin
Atorvastatin
Rosuvastatin
Simvastatin
Term
Other cardio protective effects of the statins
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
Term
Toxicity of Statins
Definition
Hepatic - so make a baseline AST ALT meas
Myopathy - incr in plasma creatine phosphokinase with or w/o myalgia
Term
Toxicity of Statins
Definition
Hepatic - so make a baseline AST ALT meas
Myopathy - incr in plasma creatine phosphokinase with or w/o myalgia
Term
inhibitors of CYP3A4
Definition
clarithro, fluconazole, fluoxetine, fluvoxamine, metronidazole, nefazodone, sertraline, zafirlukast, verapamil, and amiodarone
Term
Increased Myopathy with what drug combo?
Definition
statin + gemfibrozil or niacin
Term
Inh of CYP3A4 by other drugs increases the probability that which statin drugs will produce myalgia?
Definition
Atovastatin
Lovastatin
Simvastatin
Term
Inh of CYP2C9 will increase myalgia with
Definition
fluvastatin
Term
Inh of CYP2C9
Definition
warfarin cimetidine, phenytoin, omeprazole, and amiodarone
Term
Fatal rhabdomyolysis
Definition
release of massive myoglobin, occludes PT lumen - leads to ARF
Term
Elmination of Ezetimibe
Definition
FECES 80%
Term
MOA fo Ezetimibe
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
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
Term
Toxicity of Ezetimibe
Definition
Liver toxicity
does NOT increase risk of myopathy
NO effect of CYPs so no D-D interactions
Preg Cat C = Bad
Term
Ion exchange resins
Definition
cholestyramine
colestipol
colesevelan
Term
resin MOA
Definition
swap Cl- for neg charged bile acids which decreases chol abs which decreases sterol pool which upregulates LDL-R and HMG-CoA
Term
DO Resins work w/o LDL -R
Definition
NO - abs must have LDL-R
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
Term
If you have to take a resin which one do you take
Definition
Colesevelan - Preg cat B and
does not affect bioavail of digoxin, lovastatin, atorvastatin, simvastatin, and warfarin
Term
Niacin MOA
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
Term
Used to treat patients with low HDL and high TG?
Definition
Niacin
Term
Tox of Nicacin
Definition
Preg C
flusing at first
GI nausea and vom
Gout
Term
Big contraindication for Niacin
Definition
Dm type 2
Term
safer form of Niacin
Definition
Inositol Hexanicotinate
Term
Name the fibrate drugs
Definition
gemfibrozil
fenofibrate
Term
Fibrate MOA
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
Term
Drugs which significantly increase HDL synth
Definition
Fibrates
Niacin
Term
Drugs safe for Diabetics
Definition
Fibrates
Term
Drugs not safe for diabetics
Definition
Niacin
Term
only drugs somewhat safe for preg
Definition
resin colesvelan
Term
only drugs somewhat safe for preg
Definition
resin colesvelan
Term
Do you get myopathy with fibrates?
Definition
Yes, but use fenofibrate as opposed to gem for a lower risk of myopathy
Term
Omega 3 FA MOA
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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