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80 Cards in this Set

  • Front
  • Back
What is hyperlipidemia?
Increase in plasma cholesterol, liproteins, triglycerides or a combination.
Hyperlipidemia puts you at a risk for what heart disease?
CAD
What are the 5 classes of anti-hyperlipidemics?
1. HMG-CoA Reductase Inhibitors (Statins)
2. Bile Acid Sequestrants
3. Cholesterol Absorption Inhibitors
4. PPAR-alpha Activators (Fibrates)
5. Miscellaneous
Name 7 HMG-CoA Reductase inhibitors
Pitavastatin, Rosuvastatin, Atorvastatin, Simvastatin, Lovastatin, Pravastatin, Fluvastatin

"Pit a Rose At Simva's Love -- Prada Flu"
Which 2 HMG-Coa Reductase inhibitors are prodrugs?
Lovastatin & Simvastatin

(Love Simva, the pro)
MOA of HMG-CoA reductase inhibitors?
competitively inhibit HMG-CoA reductase, which is the rate limiting step in making cholesterol. Up regulates LDL-C receptors & increases lipid metabolism
What are Statins' lipoprotein effects?
Most potent choleterol effector by reducing LDL & TG, and raising HDL.
What are the potency relationships between the Statin drugs?
Pitavastatin (2mg), Rosuvastatin (5mg), Atorvastatin (10mg), Simvastatin (20mg), Lovastatin/Pravastatin (40mg), Fluvastatin (80mg)

"Pit a Rose at Simva's Love -- Prada Flu"
Adverse effects of Statins?
Muscle & Liver!

AST/ALT elevations, myopathy
Drug-drug interactions of Statins
CYP3A4/2C9 inhibitors (Lova/Simva pro drugs)
Contraindications for STATINS?
Liver & Renal failure, Pregnancy
Name 3 Bile Acid sequestrants
Cholestyramine, Colestipol, Colesevelam

CholestyraMINE is powder like MINING power.

ColestipOl has O for Oral granules & tablets.

Colesevelam is a tablet.
MOA of bile acid sequestrants
non-absorbable anion-exchange resin/polymers, binds bile acids in intestinal lumen, upregulation of LDL-C receptors, and cholesterol 7-aplha hydroxtlase

Overall reduces LDL.
What state/form of drugs is especially susceptible to drug-drug interactions?
prodrugs
True or False. The higher the anti-hyperlipidemic drug the greater the effect.
False. Doesn't always correlate.
What is the rate-limiting step in formation of cholesterol?
HMG-CoA reductase
True or False. If I raise the dose of Fluvastatin from 40 mg to 80 mg I can expect a proportional drop in cholesterol.
FALSE... see slide titled "majority of LDL-C lowering occurs at the LOWEST-statin dose
What are the two major AE's of pretty much all anti-hyperlipedemics?
MUSCLE AND LIVER
You put a pt. on Lovastatin. 2 weeks later they come in and say "i feel like i have the flu!". What lab should you (have been) monitoring?
CK for myopathy! (An important AE is myopathy)
Before you get into a "statin cocktail" with a patient what baseline labs should you probably order?
AST/ALT, and CK
What is the MOA of cholestryamine?
non-absorbabale anion-exchange resins/polymers bind bile acids in intestinal lumen. this results in upregulation of LDL-C receptors and cholesterol 7-alpha hydroxlyase
Hypercholesterol pt. has a major problem w/ low HDL and high TG. What drug do you NEVER choose as monotherapy in this case?
Bile Acid sequestrants
You're taking a med history of a pt. you saw a couple months ago. They say, "well i've been taking my colestipol, antacid, and my other meds in the morning w/ breakfast." What are they doing wrong?
Don't take bile acid sequestrants or antacids w/ any other drugs!
If you realllly need to raise HDL in your pt., (their level for HDL is 21) what is the target drug to add to the statin?
Niacin (potent inc. in HDL)
Pt. is taking 1000 mg of Niacin. What is the biggest AE? How can you prevent it?
cutaneous flushing (cherry red); prevent by starting low (even though its ineffective at first) and take an ASA before taking niacin
Pt. has gout or diabetes. What anti-hyperlipidemic do you avoid?
niacin (elevates serum glucose and uric acid)
Pt. primarily has hypertriglyceridemia problem. What is your DOC?
Fibrates (PPAR-alpha activators)
What lipoproteins have high TG's?
chylomicrons and VLDL
What lipoprotein has the most protein content (opposed to lipid)
HDL
What does the LCAT do?
It esterifies the cholesterol in HDL so HDL becomes spherical
What is the apoprotein for chylomicrons?
apo B48
What is the apoprotein for VLDL?
apo B100
VLDL carries ?
LDL carries ?
VLDL- TG's; LDL- cholesterol esters
What is the MOA of lovastatin?
competitively inhibits HMG-Coa Reductase
LPL (lipoprotein lipase) is on the surface of the endothelium of capillaries in what parts of the body?
capillaries of adipose tissue, skeletal muscle, and smooth muscle
In what tissues is Km of LPL high? Low?
high in adipose tissue, low in cardiac and skeletal muscle
Where is the apo B100 made?
Liver
In the blood, what are FA's bound to (when not free)?
albumin
What is the common intermediate of triacylglycerol formation in adipose tissue and the liver?
phosphatidic acid
A critical functional protein, MTP, is missing in what disease? (the result is inability for form VLDL and chylomicrons)
Abetalipoproteinemia
Exogenous trigylcerides are carried by what? Endogenous?
Exo: chylomicrons; Endo: VLDL
What apoprotein activates LPL?
CII
What apoprotein helps chylomicron remnants get taken up by the liver?
apoE
What apoproteins are associated with HDL?
A (I & II) and carries CII and E to other lipoproteins
What is the function of CETP?
An enzyme found in HDL. It transfers cholesterol ester from HDL to VLDL and takes TG from VLDL converting it to LDL
What is defective in familial hypercholesterolemia?
LDL receptor
What is wrong in type II hyperlipidemia?
Lack of functional LDL receptors
What is wrong in cholesterol ester storage disease?
Decreased activity of lysosomal esterase (acid lipase)
What goes wrong in Wolman’s Disease
Absence of lysosomal esterase
Characteristics of Alpha-lipoprotein deficiency?
– Decreased HDL
– VLDL and LDL may be decreased
– Deposition of cholesterol esters in RES
– Defective ABC1
Characteristics of Lecithin-Cholesterol Acyltransferase Deficiency?
– Decreased esterification of cholesterol
– Decreased LDL and HDL
– Increased VLDL and chylomicrons
– Foam cells in bone marrow and kidneys
Big one. What are the characteristics of the types of hyperlipoproteinemias?
– Type I = Presence of chylomicrons (Increased
triglyceride)
– Type IIa = Increased LDL (Increased cholesterol)
– Type IIb = Increased LDL and VLDL (Increased
cholesterol and triglyceride)
– Type III = Increased IDL (Increased cholesterol and
triglyceride)
– Type IV = Increased VLDL (Increased triglyceride)
– Type V = Increased VLDL and presence of
chylomicrons (Increased triglyceride)
What is the primary means of clearance of HDL from the blood?
Uptake by the liver and other tissues via scavenger receptor SR-B1
What are the 2 types of local therapy for hypercholesterolemia?
Bile acid sequestrates & cholesterol absorption inhibitors
What are AE of bile acid sequestrants?
GI, liver enzyme elevation, pancreatitis, bledding/hypothrombinemia (messes up vit K absorption)
What vitamins should not be taken with bile acid sequestrants bc of drug durg interactions?
Fat soluble - vit A, D, E, K
When should pts take drugs that interact with their hyperlipidemia drugs?
1-2 hrs before or 2-4 hrs after
If a pregnant lady has to take a bile acid sequestrant, which one should it be?
Colesevelam (B)
MOA of Niacin (nicotinic acid)
reduces cellular/enzymatic hepatic synthesis of TG, VLDL-C and LDL-C, increases LDL-C receptor activity, and decreases HDL-C catabolism.

Better than Statins at giving an HDL boost.
What are the AE of Niacin (nicotinic acid)?
1. Cutaneous FLUSHING (prevent by taking ASA 30-40 min before, start with low dose & titrate up)
2. GI stress
3. elevated serum glucose - don't give to Diabetics
4. elevation of serum uric acid - Gout
5. myopathy
6. AST/ALT elevation 3x
Contraindications for Niacin?
chronic liver/gallbrallder disease, sever gout, peptic ulcer disease, diabetes, bleeding disorders (on Warfarin), pregnancy (C)
Name 2 PPAR-alpha- activators "fibrates"
Fenofibrate (prodrug) and Gemfibrozil

"Fibrates are Fine Gems"
MOA of fibrates?
Activate PPARs which transcribe genes involved in lipoprotein metabolism.

Best at reducing TG
AE o"Ef fibrates?
AST/ALT elevation, myopathy, predisposition to gallstones
Contraindications of fibrates?
severe renal/hepatic disease, biliary cirrhosis,/cholelithiasis, pregnancy (C)
Name 1 cholesterol absorption inhibitor
Ezetimibe

"Ezet is Timid and inhibits cholesterol absorption"
MOA of Ezetimibe
selectively inhibits at the brush border of the small intestine the absorption of cholesterol & phytosterols

Never use as 1st DOC
AE of Ezetimibe
GI - diarrhea, abdominal pain/fatigue/back pain, increased AST/ALT, myopathy
Contraindications of Ezetimibe
Severe hepatic disease, pregnancy (C)
Name 1 miscellaneous agent against hypercholesterolemia
Fish Oil (omega-3 FA, EPA, DHA & ALA)
Name an FDA approved miscellaneous agent
Lovaza - ethyl esters formulation
What is TLC and how does it relate to drug theraphy?
Therapeutic Lifestyle Changes. Drug theraphy is always ADDED to TLC; it NEVER replaces it!
What class of agents has the greatest potential to have the greatest TG lowering effect?
Firbrates - Fenofibrate or Gemfibrozil
What 1 negative lipid effect is possible with the class of fibrates?
Can potentially increase LDL-C by 5-20% in some pts
What class of agents has the greatest potential to have the greatest HDL-C raising effect?
Niacin (nicotinic acid)
What patients should not get niacin?
Those with chronic liver/gallbadder disease, gout, peptic ulcer disease, diabetes, bleeding disorders, and preganancy
What type of patients should not get the cholesterol absoprtion inhibitor, Ezetimibe?
those with severe hepatic disease or pregnant women
What 3 lipid lowering drugs are prodrugs?
Lovastatin, Simvastatin, and FenoFibrate

"Love a Fine Simva"
What patients should not get a bile acid sequestrant?
people with hypertriglyceridemia (high TGs), dysbetalipoproteinemia, ileus/GI obstruction, dysphagia, advanced renal disease bc of Cl balance, and pregnant women
If you have a hypercholesterolemic pt or a young female who is hypercholererolemic who desires to have a child, what drug class is the best choice (carries the least risk)?
Give local theraphy with a bile acid sequestrant - Colesevelam and possible Fish Oil