Cardio - Pharm (Part 2: Lipid-lowering agents)

Question 1

What is the common suffix for HMG-CoA reductase inhibitors? What are 5 examples of such drugs?

Answer 1

STATINS (-vastatin) = (1) Lovastatin, (2) pravastatin, (3) simvastatin, (4) atorvastatin, (5) rosuvastatin

Question 2

What kind of cholesterol is LDL considered to be? What kind of cholesterol is HDL considered to be?

Answer 2

“Bad cholesterol”; “Good cholesterol”

Question 3

What is the mechanism of action of HMG-CoA reductase inhibitors?

Answer 3

Inhibit conversion of HMG-CoA to mevalonate, a cholesterol precursor

Question 4

What is the effect of HMG-CoA reductase inhibitors on the following: (1) LDL (2) HDL (3) Triglycerides?

Answer 4

(1) Very significant decrease (3 down arrows); (2) Increase (1 arrow up); (3) Decrease (1 arrow down)

Question 5

What are 2 side effects/problems associated with HMG-CoA reductase inhibitors? What is important to associate with each of these side effects/problems?

Answer 5

(1) Hepatotoxicity (Increased LFTs) (2) Rhabdomyolysis (especially when used with fibrates and niacin)

Question 6

What is another name for niacin? What is this drug’s mechanism of action?

Answer 6

Vitamin B3 (water soluble vitamin); (1) Inhibits lipolysis in adipose tissue, (2) Reduces hepatic VLDL synthesis

Question 7

What is the effect of Niacin (vitamin B3) on the following: (1) LDL (2) HDL (3) Triglycerides?

Answer 7

(1) Significant decrease (2 arrows down) (2) Significant increase (2 arrows up) (3) Decrease (1 arrow down)

Question 8

What are 3 side effects/problems associated with niacin (vitamin B3)? What is important to remember about each of these side effects/problems?

Answer 8

(1) Red, flushed face (decreased by aspirin) (2) Hyperglycemia (causes acanthosis nigricans) (3) Hyperuricemia (exacerbates gout)

Question 9

What are 3 examples of bile acid resins?

Answer 9

Cholestyramine, colestipol, colesevelam

Question 10

What is the mechanism of action of bile acid resins?

Answer 10

Prevent intestinal reabsorption of bile acid = Liver must use cholesterol to make more

Question 11

What are general kinds/groups of lipid-lowering agents? Give examples belonging to each class, where applicable.

Answer 11

(1) HMG-CoA reductase inhibitors - lovastatin, pravastatin, simvastatin, atorvastatin, rosuvastatin (2) Niacin (vitamin B3) (3) Bile acid resins - cholestyramine, colestipol, colesevelam (4) Cholesterol absorption blockers - ezetimibe (5) Fibrates - gemfibrozil, clofibrate, benzofibrate, fenofibrate

Question 12

What is the effect of Bile acid resins on the following: (1) LDL (2) HDL (3) Triglycerides?

Answer 12

(1) Significant decrease (2 down arrows) (2) Slightly increase (3) Slightly increase

Question 13

What are 2 common side effects/problems associated with bile acid resins?

Answer 13

(1) Patients hate it - tastes bad and causes GI discomfort (2) Decreased absorption of fat-soluble vitamins

Question 14

What is the prime example of cholesterol absorption blockers?

Answer 14

Ezetimibe

Question 15

What is the mechanism of action of cholesterol absorption blockers (ezetimibe)?

Answer 15

Prevent cholesterol absorption at small intestine brush border

Question 16

What is the effect of Cholesterol absorption blockers (ezetimibe) on the following: (1) LDL (2) HDL (3) Triglycerides?

Answer 16

(1) Significant decrease (2 down arrows) (2) No effect (3) No effect

Question 17

What are 2 side effects/problems associated with cholesterol absorption blockers (ezetimibe)?

Answer 17

(1) Rare increased LFTs (2) Diarrhea

Question 18

What are 4 examples of Fibrates?

Answer 18

Gemfibrozil, clofibrate, bezafibrate, fenofibrate

Question 19

What is the mechanism of action of fibrates?

Answer 19

Upregulate LPL –> Increased TG clearance; Activates PPAR-alpha to induce HDL synthesis

Question 20

What is the effect of Fibrates on the following: (1) LDL (2) HDL (3) Triglycerides?

Answer 20

(1) Decreased (1 down arrow) (2) Increased (1 up arrow) (3) Very significant decrease (3 down arrows)

Question 21

What are 3 side effects/problems associated with fibrates? What is important to remember about each of these side effects/problems?

Answer 21

(1) Myositis (increased risk with concurrent statins) (2) Hepatotoxicity (increased LFTs) (3) Cholesterol gallstones (esp. with concurrent bile acid resins)

Question 22

Draw a diagram depicting the mechanisms of action of the different kinds of lipid-lowering agents.

Answer 22

See diagram on p. 281 in First Aid (bottom of page)