Pharm - Prog2 - Lipids

Front 1

What are the 3 bile acid binding agents? Which is used and why?

Back 1

"coles"
Cholestyramine - poor palatability, Colestipol, COLESEVELAM - large, hard to swallow tablet, low AE

Front 2

What is the MOA of bile acid binding agents?

Back 2

Prevent reabsorption (recycling) of bile acids in GI, upregulate cholesterol 7-alpha hydroxylase for the synthesis of new bile acid
Upregulate LDL receptors

Front 3

What are the actions of bile acid binding agents on LDL, HDL, TG?

Back 3

Dec LDL modestly
Inc HDL barely
Inc TG (AE! esp if TG elevated)

Front 4

What are the side effects of bile acid binding agents?

Back 4

GI distress, constipation (bc poop them out)
Decreased absorption of other drugs, lipophilic drugs (statins)

Front 5

What is the CI for bile acid binding agents?

Back 5

Elevated TGs!

Front 6

When are bile acid binding agents used?

Back 6

Monotx not often bc not potent
Combo with statins, Atorvastatin (additive effect)

Front 7

What is the MOA of plant stanol esters and sterol esters?

Back 7

Preferentially form micelle instead of cholesterol bc substituted by sterols

Front 8

What is the MOA of ezetimibe?

Back 8

Selectively inhibits absorption of cholestrol at GI brush border

Front 9

What are the effects of cholesterol absorption inhibitors (plant stanol esters, sterol esters, ezetimibe) on LDL, TG, HDL?

Back 9

Dec LDL modestly
Dec TG somewhat
Inc HDL barely

Front 10

What are the uses of cholesterol absorption inhibitors (plant stanol esters, sterol esters, ezetimibe)?

Back 10

Monotx not often (not potent)
Combo with statin, Simvastatin (additive)

Front 11

What is the MOA for the nicotinic acid (Niacin)- B vitamin?

Back 11

DEC FFA mobilization, less TG synthesis!
DEC HDL uptake

Front 12

What are the effects of niacin on LDL, TG, and HDL?

Back 12

Dec LDL, modestly
Dec TG, significantly
Inc HDL, significantly

Front 13

What effect does niacin have on endothelium and how do you treat this?

Back 13

Causes release of PG's --> flushing, itching, hypotension, transient HA
Pretreat with PG-inhibitor, aspirin or give extended release form

Front 14

What 5 AE's does niacin cause? Where is it CI?

Back 14

Hyperglycemia, by dec glucose tolerance (Diabetes)
Upper GI distress (Peptic ulcers)
Hyperuricemia, can't excrete uric acid (Gout)
Hepatotoxicity, LFTs (Liver disease)
Myopathy (don't use with fibric acids or additive myopathy)

only use EXTENDED RELEASE form bc of liver toxicity

Front 15

What are the 2 fibric acids (fibrates)? Which is preferred?

Back 15

Gemfibrozil, FENOFIBRATE (less toxic, less doses)

Front 16

What is the MOA of the fibrates?

Back 16

INC Lipoprotein lipase activity, breaks down TG to LDL
Activate PPARalpha, inc apoA --> HDL

PPAR takes longer bc affecting gene transcription

Front 17

What effects do fibrates have on LDL, TG, HDL?

Back 17

Dec LDL modestly --BUT can transiently INC LDL bc lipoprotein lipase breaks down TG to LDL
Dec TG, significantly
Inc HDL, significantly

Front 18

What are the side effects of fibrates?

Back 18

Dyspepsia (assoc with peptic ulcer dz), MYOPATHY

Front 19

What are the side effects of gemfibrozil?

Back 19

Gallstones, drug interactions, anticoagulants (Warfarin), rhabdomyalysis

Front 20

Where are fibrates CI?

Back 20

Severe renal or hepatic dz

Front 21

What are the statins and what are their relative strengths?

Back 21

Rosuvastatin > Simvastatin > Pravastatin/Lovastatin > Fluvastatin (except in HDL increase, Atorvastatin dec increase with higher dose)
Really Awkward Sex Post-Lame Foreplay

Front 22

What is the MOA of statins?

Back 22

Inhibit HMG-CoA reductase, rate-limiting step of cholesterol synthesis from acetyl-CoA
Upregulates LDL receptors

Front 23

What are the effects of statins on LDL, TG, HDL?

Back 23

Dec LDL, significantly
Dec TG, significantly
Inc HDL, significantly (atorvastatin paradoxical)
RASPLF

Most POTENT cholesterol lowering drug

Front 24

What are the side effects of statins? Where are they CI?

Back 24

Myopathies!! (myalgia, myositis (elev CK), rhabdomyolysis (with renal damage)) -- rosuvastatin can't be dosed higher. Monitor CK levels

Liver Dz: CHECK LFTs

Pregnancy bc fetus needs cholesterol

Drug interactions, many: don't take with Fibrates (myopathies) and nicotinic acid and p450 inhibitors

Front 25

What is the rule of 6's?

Back 25

Each doubling of a dose of STATINS produces only a 6% reduction of LDL. Better to use combinations

Front 26

What are the benefits of statins?

Back 26

Dec coronary events
Dec CHF mortality
Dec coronary procedures
Dec stroke
Dec overall mortality

Front 27

What are the effects of combining simvastatin and ezetimibe?

Back 27

Greater dec in LDL and c-Reactive protein
NO improvement in carotid inter-media thickness (so not necessarily better outcomes)

Front 28

What are the effects of combining simvastatin and fibric acids?

Back 28

Huge dec in TG

Front 29

Which are the three lipophilic statins and what do they cause?

Back 29

ALS: Atorvastatin, Lovastatin, Simvastatin
Higher risk of myopathies

Front 30

How are the statins metabolized?

Back 30

Pravastatin - Kidney (no hepatotoxicity)
ALS: Atorvastatin, Lovastatin, Simvastatin - CYP3A4
Fluvastatin, Rosuvastatin - CYP3C9