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Pharmacology Test 2
Lipid Drugs
7
Pharmacology
Undergraduate 4
03/22/2011

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Cards

Term
4 Lipoproteins
Definition
Chylomicrons – transport dietary fat from intestine to tissues (almost all TG)
VLDL – transports fatty acids to muscle and adipose tissue (mostly TG)
LDL – atherogenic (mostly cholesterol)
HDL – transports cholesterol from peripheral tissue to liver (GOOD)
Term
5 Apoproteins
Definition
ApoB48 - marker to help guide chylomicrons

ApoCIII - found on VLDL and inhibits LPL

ApoB100 - found on LDL and binds to LDL-receptors found in other tissues causing problems

ApoAI/II - found on HDL (good)
ApoCII - found on HDL, activates LPL which breaks down TGs
Term
atorvastatin

(Lipitor)
Definition
class - HMG-CoA reductase inhibitor
MOA - lowers cholesterol synthesis in the liver by inhibiting the enzyme that produces mevalonate (cholesterol precursor) [rate-limiting step]
where: liver
Increases: LDL-receptors, SREBP2 (facilitates cholesterol synthesis)
Decreases: cholesterol
AE - muscle pain, elevated transaminases
Term
gemfibrozil

(Lopid)
Definition
class - fibrate/PPARα agonist
MOA - mimics FFA and activates PPARα which decreases ApoCII which increases LPL
where: liver, muscles, heart
Increases: LPL, fatty acid oxidation
Decreases: ApoCIII, TGs
AE - muscle pain, arrhythmias
Term
colesevelam

(Welchol)
Definition
class - bile acid sequestrant
MOA - huge cationic polymer that remains in the GI and binds bile salts (mostly cholesterol) and then is eleiminated. this facilitates the breakdown of cholesterol in the body in order to form new bile salts
where: GI
Increases: bile salt production
Decreases: cholesterol
TX - can be used in children since its not absorbed
AE - GI discomfort, acidosis, multiple food/drug interactions
Term
ezetimibe

(Zetia)
Definition
class - cholesterol absorption inhibitor
MOA - binds Neimann (NPC1L1) protein on GI cells and inhibits the absorption of cholesterols and phytosterols
where: GI
Increases: LDL-receptors
Decreases: cholesterol absorption, cholesterol incorporation into LDL
AE - muscle pain, elevated transaminases, diarrhea
Term
niacin

(Niaspan)
Definition
class - vitamin B3
MOA - binds to fat cells and inhibits the breakdown of TG into FFA which the liver normally uses to make LDL cholesterol
where: fat cells
Increases: HDL levels
Decreases: FFA, TG synthesis, LDL synthesis, ApoB100
AE - flushing (has a strong vasodilating effect) and itching
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