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Pharm 2 Final - LLD
Lipid Lowering Drugs
68
Health Care
Graduate
03/29/2009

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Cards

Term
Lipid Lowering Therapy is aimed at reducing _____ and _____.
Definition

reducing LDL and total cholesterol

 

 

specific targets levels are chosen based on the existance (or not) of coexisting conditions

Term
VLDL is produced by ___________ and have a ________ core composed primarily of __________.
Definition

the liver

 

lipid

 

trigs

Term
> 500 trigs assc. with increased risk of ______________ and should be treated with which drugs?
Definition

pancreatitis

 

VLDL lowering drugs (ie nicotinic acid)

Term
If the total cholesterol in someone >45 years old is >200, it increases the risk of ______ significantly.
Definition
CAD
Term
Lowering LDL by 25% may reduce CAD risk by ______.
Definition
50%
Term
What are the desirable cholesterol levels?
Definition

TC <200

LDL <130

HDL >60

Trigs <150

Term
What are the moderate cholesterol levels?
Definition

TC 200-239

LDL 130-159

HDL 35-60

Trigs 150-199

Term
High Cholesterol Levels
Definition

TC >240

LDL >160

HDL <35

Trigs >200

Term
List the HMG-CoA Reductase Inhibitors.
Definition

Atorvastatin

Lovastatin

Pravastatin

Fluvastatin

Simvastatin

Rosuvastatin

Cerivastatin

Term
What do statins inhibit?
Definition
inhibit HMG-CoA reductase, the rate limiting enzyme in chol. biosynthesis
Term
How do statins effect cholesterol levels?
Definition

decs TC, LDL-C, VLDL-C and total trigs

 

HDL-C remains the same or increases

Term
Which statins have the best oral absorption?
Definition
Pravastatin and Fluvastatin
Term
statins are metabolized by...
Definition
CYP 450
Term
Which statins have the most drug interactions?
Definition

Atorvastatin

Lovastatin

Simvastatin

Term
Statins are excreted via ___________ and ___________.
Definition
bile and feces
Term
How are statins administered?
Definition

PO once daily

usually at night

Term
List the AEs of statins.
Definition

Liver problems

Mm problems: myalgia and rhabdo

renal problems

Term
What should you monitor while using statins?
Definition

LFTs

CK

 

Term
Renal problems are more likely to occur with statin use if the patient also...
Definition

has renal dz

 

(or is taking erythromycin, niacin, gemifibrozil, itraconazole or cyclosporin)

Term
Who should not use statins?
Definition

pregnant women

nursing moms

kids

Term
What should you make sure your patients report to you if they are on statins?
Definition

unusual, diffuse or persistant mm pain, tenderness or weakness

 

esp if accompanied by fever or malaise

Term
What would make you D/C statins?
Definition

myopathy is diagnosed or

CPK increases

Term
(DI) statins + fibrates =
Definition
increased risk of mm damage
Term
Itraconazole, erythromycin and cyclosporin can ________  ________ of statins. (DI)
Definition
increase levels
Term
Statins may increase the levels of what drug? (DI)
Definition
warfarin
Term
List the bile acid binding resins.
Definition

cholestyramine

colestipol

colesevelam

Term
Which drugs are good to give to someone who can't tolerate a statin?
Definition
bile acid binding resins
Term
Bile Acid Binding Resins form an_____________ complex with bile acids present in the intestines; This complex prevents the ____________ of bile acids and is then excreted. (MOA)
Definition

insoluble

 

reabsorption

 

 

(the increased excretion of bile acids creates a demand for inc bile acid synthesis...

bile acids are made from cholesterol provided by LDL)

Term
How do Bile Acid Binding Resins effect Cholesterol levels?
Definition

lowers LDL

 

sometimes raises HDL levels, but response is not uniform

Term

PK of bile acid binding resins

 

 

Definition

PO

insoluble

not absorbed

not metabolized

 

total fecal excretion

Term
Which drugs are DOC for phenotypes of IIa and IIIb hyperlipidemia?
Definition

 

cholestyramine

colestipol

colesevelam

Term
__________________ is used to relieve pruritis caused by accumulation of bile in patients with biliary obstruction.
Definition
Cholestyramine
Term
List the AEs of Bile Acid Binding Resins.
Definition

- nothing systemic bc its not absorbed

- safest of all lipoprotein lowering drugs

 

GI: constipation, bloating, indigestion, N, flatulence

decreases if taken with full glass of water

 

rarely: dec fat absorption, def of fat soluble vits, folic acid and ascorbic acid

Term
Which group of drugs is the safest of all lipoprotein lowering drugs?
Definition

bile acid binding resins

 

cholestyramine

colestipol

colesevelam

Term
What are the doses for bile acid binding resins?
Definition

cholestyramine 4-12 grams bid (powdered or wafer)

 

colestipol 10-20 grams/day (granular)

 

colesevelam 625 mg tablets, 3 bid

Term
Bile acid binding resins may form complexes with:
Definition

thiazides

digoxin

warfarin

some Abx

tetracyclines

aspirin

phenobarbital

statins

Term
Nicotinic acid's effect on cholesterol is ...
Definition

lowers LDL and VLDL

 

modest increase in HDL

Term
Nicotinic Acid reduces hepatic LDL an VLDL _____________ and _______________. (MOA)
Definition

synthesis and secretion

 

 

(inhibition of tissue lipolysis reduces the supply of circulating free fatty acids that the liver uses to synthesize trigs for incorporation into VLDL)

Term
Nicotinic acid is converted into ________ in the body.
Definition

nicotinamide

 

 

Term
How is nicotinic acid administered?
Definition
PO
Term
What are the indications for nicotinic acid?
Definition

patients who have elevations in LDL and VLDL,

type IIa and IV hyperlipidemia

 

other severe hypercholesterolemias

Term
What drug increases plasma HDL levels the best?
Definition
nicotinic acid
Term
Which drug is the least expensive but also least well tolerated of all the lipid lowering drugs?
Definition
nicotinic acid
Term
What is the main AE for nicotinic acid?
Definition
Intense cutaneous flush
Term
List the AEs for nicotinic acid.
Definition

intense cutaneous flush

GI upset, NVD

Liver injury

Glucose Intolerance

Hyperuricemia

Metabolic syndrome

Term
Nicotinic acid is contraindicated in people with:
Definition

hepatic dysfunction

PUD

Hyperuricemia

DM

Term
How can you diminish the effects of the intense cutaneous flush caused by nicotinic acid?
Definition

begin with low doses

take with a meal

take ASA before dose

time released prep

Term
List the Fibric acid derivatives.
Definition

gemifibrozil

fenofibrate

clofibrate

Term
Fibric acid derivative  active _______________, thus promoting delivery of triglycerides to adipose tissue and interfere with the formation of ________ in the liver. (MOA)
Definition

lipoprotein lipase

 

VLDL

 

 

 

(HDL is likely increased)

Term
List the AEs of Gemfibrozil, Fenofibrate, Clofiberate.
Definition

GI disturbances

Cholelithiasis

myositis (more common if pt is also taking a statin)

ED

malignancy

Term
Which drugs can interact with Fibric acid derivatives
Definition

warfarin

 

sulfa drugs

Term
How is gemfibrozil administered?
Definition
PO
Term
How is Fenofibrate metabolized and excreted?
Definition

metabolized by liver

 

excreted in urine

Term
What should you monitor when using fibric acid derivatives?
Definition

LFTs

lipids

investigate mm complaints

CK

CBCs during first year

Term
Fibric acid derivative contraindications:
Definition

patients w/ gallbladder disease,

severe hepatic/renal disease, and

preg. or lactating women

Term
Fibric acid derivative are indicated for:
Definition
hypertriglyceridemia assc. with low levels of HDL
Term
DOC for hypertriglyceridemia assc with low levels of HDL:
Definition
fibric acid derivatives
Term
What is Ezetimibe?
Definition
a cholesterol absorption inhibitor
Term
List the SEs of ezetimibe.
Definition

tiredness

stomach pain

 

Term
Ezetimibe inhibits ___________ absorption in the intestines from the ________.
Definition

cholesterol

 

diet

Term
Ezetimibe works better if it is combined with what?
Definition
a statin
Term

How is Ezetimibe administered, metabolized and excreted?

 

Definition

PO

 

metabolized by glucuronide conjugation

 

renally excreted

Term
Ezetimibe is indicated for...
Definition
primary hypercholesterolemia
Term
What is Advicor?
Definition

a combination of niacin ER + lovastatin

 

500/20; 750/20; 1000/20

Term
What is Pravigard PAC?
Definition

a combination of Aspirin + Pravastatin

 

81/20; 81/40; 81/80

325/20; 325/40; 325/80

Term
What is Vytorin?
Definition

a combination of ezetimibe + simvastatin

 

10/10; 10/20; 10/40; 10/80

Term
What is Caduet?
Definition

a combination of Amlodipine + Atorvastatin

 

5/10 to 10/80

Term
HMG-CoA Reductase Inhibitors end in...
Definition
- statin
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