Antihyperlipidemic Drugs

Question 1

Causes of hyperlipidemia:
Primary:
Secondary:
1-
2-
3-
4-

Answer 1

Familiar history
1-diabetes
2-liver disease
3-alcoholism
4-hypothyrodism

Question 2

Statins or ———:
Natural:1——-(from—–)
Semi-synthetic:1—–2—-
Sunthetic:1——2—–3——

Answer 2

HMG coA reductase inhibitors
Natural: lovastatin (from fungus)
Semi:1-simva 2-prava
Synthe: 1-fluva 2-atorva 3-rosuva

Question 3

Mechanism of action of statins:
1-
2-

Answer 3

Inhibut hmgcoa leading to dec of choles
2- low cholesterol stimulate LDL receptors —–uptake of LDL from blood
3- low cholesterol decrease secretion of VLDL

Question 4

Effects of statins:
1-
2-
3-
4-
5-

Answer 4

Decrease LDL TG
Increase HDL
Improve indothelial function
Decrease CRP levels (anti-inflammatory)
Inhibit platelet thrombus formation

Question 5

Pharmacokinetics of statins
Oral absorption
Plasma protein binding
——,——– and —— are primarily metabolized by CYP3A4
——– and —– are insignificantly metabolized
Half life of : atorva and rosuvastatin
Others?

Answer 5

Oral absorption is variable
High plasma proteins binding
Ator,lova,simvastatins
Prava and rosuva
Atorva(14 hr) rosuva ( 20hr )
Others 1-4 hr

Question 6

Side effects of statins:
1-
2-
3-
4-

Answer 6

1- GI discomfort
2-hepatotoxicity and elevation of trans
3-myopathy and rhabdomyolysis
4-grapefruit juice incr the side effects

Question 7

Cyp3A4 inhibitors
1-
2-
3-
4-
5-
6-

Answer 7

Anti retrovirals
Ketoconazole
Cimetidine
Grapefruit
Fibrates
Erythromycin
Macrolides

Question 8

Bile acid binding resins:
1-
2-

Answer 8

Cholestyramine
Colestipol
(Oldest and safest)

Question 9

T or F
Bile acid binding resins are first line of therapy

Answer 9

False second

Question 10

T or F
Cholestyramine reduces LDL by 40%

Answer 10

False
20%

Question 11

BAS are—– charged they bind to —– charges bile acids
Because of their large size the resin is not absorbed and the bile acide are ——-
Then hepatic bile-acid synthetis will—- then there is —— of cholesterol

Answer 11

Positive
Negative
Via stool
Increase
Depletion
Bseru mtl l statins mn hun

Question 12

Pharmacokinetics of BAS:
Oral?
Metabolized by intestine?

Answer 12

Yes orall because its not soluble in water and very large
Not metabolized by any directly excreted by feces

Question 13

Adverse effects of BAS

Answer 13

GI: constipation,nausea,flatulence

Question 14

Drug-drug: (BAS)

Answer 14

They bind and decrease absorption of many drugs:
1-some thiazides
2-digoxin
3-warfarin
4-some statins (prava and fluva)
These drugs should be taken 1-2 hr before or 4-6 after

Question 15

Niacin:
Form:
Role:
Mode of adm:
Converted to:

Answer 15

Water soluble vitamin B3
Precursor of NADH and NADPH
DNA repair/production of steroid hormones in the adrenal gland
Orally
Nicotinamide

Question 16

Mode of action:

Answer 16

Inhibit lipolysis in adipose
Decr TG decr VLDL dec LDL
Decr in cholesterol(LDL,VLDL) TG(VLDL)
Increase HDL
Boost tissue plasminogen(reverse thrombose and atherosclerose)

Question 17

Therapeutic uses of niacin:
1-
2-

Answer 17

1-tx of familial hypercholesterolimia
2-pootent antihypelipidemic agent for raisinggggg HDL

Question 18

Side effects of niacin:
1-
2-
3-
4-
5-

Answer 18

1-Flushing affects compliance
2- dyspepsia
3- diarrhea
4- severe hepatotoxicity
5- inc uric acid (they inhibit tubular secretion of uric acid)

Question 19

Fibrates:
Mode of action:
Names:
1-
2-

Answer 19

Activates PPAR (peroxisome proliferation receptors)
Activation of PPAR causes transpcription of number of genes that ficulitate lipid metabolism
After activation of PPAR: incr LPL lipoprotein lipase (incr hydrolysis of chylomicrons and VLDL),express apoA-I and apoAII so they increase HDL
Stimulate synthesis of acyl coA dehydrogenase then decrease TG liver synthesis yaane decrease VLDL
1-fenofibrate
2-gemfibrozil

Question 20

Adverse effects of fibrates:
1-
2-
3-

Answer 20

GI
Myalgia
Gallstones

Question 21

Drug drug interaction:
1
2-

Answer 21

Potentiate oral anticoagulant and some hypoglycemic drugs displacing them from plasma proteins
Cause myopathy when co-administered with statins

Question 22

T or F
Fibrates can be used in pregnant or lactating women

Answer 22

False
Not used

Question 23

Ezetimibe inhibits——
This will lead to refuction of —–

Answer 23

Intestinal absorption of dietary and billiary cholesterol in small intestine
Reduction of hepatic cholesterol stores and an increase clearance of cholesterol

Question 24

Ezetimibe lowers LDL by 17% TG by 20% and increase HdL by 1.3%

Answer 24

False
TG by 6%

Question 25

Metabolism of ezetimibe:

Answer 25

Small intestine and liver via glucuronude conjugation(phase II) with renal and biliary excretion