Antihyperlipidemics

Question 1

Chylomicrons mainly consist of (2)

Ratio?

Answer 1

Dietary triglycerides
Cholesteryl esters

10:1

Question 2

VLDL primarily consists of (2)

Ratio?

Answer 2

Endogenous triglycerides
Cholesteryl esters

5:1

Question 3

IDL primarily consists of (2)

Ratio?

Answer 3

Endogenous triglycerides
Cholesteryl esters

1:1

Question 4

LDL primarily consists of (1)

Answer 4

Cholesteryl esters

Question 5

HDL primarily consists of (2)

Answer 5

cholesteryl esters

phospholipids

Question 6

Major Apolipoproteins of CHYLOMICRONS (4)

Answer 6

B-48, C, E, and A

Question 7

Major apolipoproteins of VLDL (3)

Answer 7

C, B-100, and E

Question 8

Major apolipoproteins of LDL (1)

Answer 8

B-100

Question 9

Major Apolipoproteins of HDL (5)

Answer 9

A-I, A-II, C, E, and D

Question 10

What is the important transporter for cholesterol in intestines?

Answer 10

NPC1-L1

Question 11

Chylomicron Synthesis Steps

Answer 11

Formed in small intestine - Apo-B48 attached

Enter circulation - Apo-CII and Apo-E attached

LPL breaks down triglycerides through activation by Apo-CII

Chylomicron remnants lose Apo-CII to HDL

Reuptaken by liver through Apo-E protein

Question 12

VLDL Synthesis Steps

Answer 12

Formed in Liver

Apo-B100 attached

Received Apo-E and Apo-CII in circulation

LPL removes TG’s

IDL forms and loses Apo-CII and Apo-E

LDL finally forms - Apo-B100 allows uptake into liver and extrahepatic tissue

Question 13

Where is the only place to get rid of excess cholesterol?

Answer 13

Liver

Question 14

Reverse cholesterol transport is performed by what molecule?

What apolipoprotein is important in the process?

Answer 14

HDL

Apo-AI

Question 15

Apo-AI on HDL increases activity of what?

Also binds to what in the liver?

Answer 15

LCAT

SR-B1 - to allow exchange of cholesterol

Question 16

Primary chylomicronemia associated with?

Manifests as?

Answer 16

decreased LPL activity

Increased chylomicrons/VLDL

Question 17

Familial Hypertriglyceridemia associated with?

Manifests as

Answer 17

impaired VLDL/chylomicron removal

Increased VLDL (moderate)

Question 18

Familial Combined Hyperlipoproteinemia associated with?

Manifests as?

Answer 18

Increased VLDL production

high conversion of VLDL to LDL

Increased VLDL and LDL

Question 19

Familial Hypercholesterolemia associated with?

Manifests as?

Answer 19

LDLR impairments

Increased LDL

Question 20

Familial Ligand-defective Apo-B associated with?

Manifests as?

Answer 20

mutated apo-B100

results in impaired endocytosis of LDL

Increased LDL

Question 21

Familial Dysbetalipoproteinemia associated with?

Manifests as?

Answer 21

decreased clearance of VLDL, IDL, and chylomicrons due to DEFECT OF APO E

Increased IDL, Chylomicrons

Question 22

HMG-CoA reductase inhibitors end in?

Answer 22

statin

Question 23

Fibrates MOA

Answer 23

activate PPAR

increases Apo-AI and A-II

Decreases Apo-CIII

Increases LPL expression

ultimately leads to increased plasma HDL and decreased Plasma triglycerides

Question 24

Fibrates (2)

Answer 24

gemfibrozil

fenofibrate

Question 25

Bile acid-binding resins (3)

Answer 25

cholestyramine colesevelam colestipol

Question 26

Bile-acid binding resins MOA

Answer 26

bind up bile acids and lead to excretion causes liver to increase bile synthesis which uses more cholesterol leads to decreased LDL

Question 27

Bile-acid binding resins shouldn't be used in

Answer 27

Hypertriglyceridemia patients can cause increase in TG's

Question 28

Niacin MOA

Answer 28

decreases LPL activity in fat tissue increases HDL production decreases free fatty acids in plasma which decreases VLDL synthesis by liver

Question 29

Niacin useful in?

Answer 29

all hypertriglyceridemias and hypercholesterolemias

Question 30

Bile-acid binding resins useful in?

Answer 30

Moderately effective drugs in hypercholesterolemia treatment Treatment of hypercholesterolemia in patients for whom statins do not provide sufficient LDL reduction familial hypercholesterolemia

Question 31

Niacin adverse effects

Answer 31

cutaneous flushing/itching hyperuricemia hepatotoxicity increased risk of statin-induced myopathy

Question 32

Ezetimibe MOA

Answer 32

inhibits NPC-L1 cholesterol transporter in intestines leads to decreased Chylomicron size, decreased LDL, and Increased VLDL

Question 33

Ezetimibe useful in

Answer 33

treatment of all types hypercholesterolemia

Question 34

Statins MOA

Answer 34

inhibit HMG-CoA reductase prevents formation cholesterol leads to increased LDL receptor expression leading to decreased LDL

Question 35

Most potent statins? least?

Answer 35

atorvastatin and rosuvastatin Fluvastatin

Question 36

Adverse effects of Statins Contraindicated in?

Answer 36

Myopathy/myositis Rhabdomyolysis Liver toxicity PREGNANCY