Pharmacology of Dislipidemia

Question 1

What are the five classes of drugs for Dislipidemia?

Answer 1

1. Statins
2. Fibrates
3. Niacin
4. Bile Acid Resins/Sequestrants
5. Sterol/Cholesterol Absorption inhibitor

Question 2

What are the statins?

Answer 2

Simvastatin

Atorvastatin

Question 3

What is the MOA for statins?

Answer 3

Inhibit HMG-CoA reductase

Question 4

What do statins do to LDL, HDL and TG levels?

Answer 4

DEC. (3 arrows) LDL
Inc. HDL
Dec. TG

Question 5

What are the Fibrates?

Answer 5

Gemfibrozil
Clofibrate
Benzafibrate
Fenofibrate

Question 6

What is the MOA for fibrates?

Answer 6

Peroxisome proliferator-activated receptor-a (PPAR-a) agonists

• Inc. TG clearance
• Fxn as ligands for nuclear transcription receptor (the PPAR-a)
• Transcriptionally up regulate LPL (lipoprotein lipase), apo A-I and apo-AII, down regulate apo C-III, an inhibitor of lipolysis

Question 7

What do fibrates do to LDL, HDL and TG levels?

Answer 7

Dec. LDL
Inc. HDL
DEC. (3 arrows) TG

Question 8

What is niacin?

Answer 8

Nicotinic Acid

Question 9

What is the MOA for niacin?

Answer 9

Blocks peripheral adipolysis (dec. catabolism of apo AI) & Dec. hepatic VLDL synthesis and secretion

Question 10

What does niacin do to LDL, HDL and TG levels?

Answer 10

DEC. (2 arrows) LDL
INC. (2 arrows) HDL
Dec. TG

Question 11

What are the bile acid resins/sequestrants?

Answer 11

Colestipol
Cholestyramine
Colesevelam

Question 12

What is the MOA for bile acid resins/sequestrants?

Answer 12

Binds bile acids in intestine and Dec. absorption.
-Binds bile acids in intestine and forms a non absorbable complex that is excreted in feces. Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver. This causes inc. demand for cholesterol in liver cells, resulting in inc. in hepatic uptake and clearance of circulating LDL.

Question 13

What do bile acid resins/sequestrants do to LDL, HDL and TG levels?

Answer 13

DEC. (2 arrows) LDL
Slightly Inc. HDL
Slightly Inc. TG

Question 14

What is the Sterol/Cholesterol Absorption inhibitor?

Answer 14

Ezetimibe

Question 15

What is the MOA of Sterol/Cholestrol Absorption inhibitors?

Answer 15

Sterol transporter NPCILI blocker in intestinal brush border.
-Blocks sterol transporter NPC1L1 in intestinal brush boarder. Localizes at brush boarder of small intestine and inhibits absorption of cholesterol, resulting in decreased delivery of intestinal cholesterol to liver.

Question 16

What does Ezetimibe do to LDL, HDL and TG levels?

Answer 16

DEC. (2 arrows) LDL