Cholesterol Drugs

Question 1

Statins that are prodrugs

Answer 1

Lovastatin, Simvastatin (they’re metabolized SL-owly)

Question 2

Statins metabolized by CYP3A4

Answer 2

Lovastatin, Simvastatin, Atorvastatin (also oxidized)

Question 3

Statins metabolized by CYP2C9

Answer 3

Fluvastatin, Rosuvastatin

Question 4

Statin metabolized solely by Sulfonation

Answer 4

Pravastatin

Question 5

Statin mechanism of action?

Answer 5

Inhibit HMG-CoA Reductase, the rate limiting step in cholesterol biosynthesis. Also cause indirect up-regulation of hepatic LDL receptors

Question 6

Statins with highest potency/efficacy?

Answer 6

Atorvastatin, Rosuvastatin (longest half lives)

Question 7

Statins with moderate potency/efficacy?

Answer 7

Lovastatin, Simvastatin

Question 8

Statin with lowest potency/efficacy?

Answer 8

Pravastatin

Question 9

Niacin mechanism of action?

Answer 9

Inhibits VLDL secretion, thereby decreasing LDL

Question 10

Niacin’s most useful clinical aspects?

Answer 10

Best way to increase HDL, only agent that lowers Lp(a)

Question 11

Adverse effects seen with Statin therapy?

Answer 11

Sleep disturbance/memory loss (most common) Elevations in serum aminotransferases, myositis. Severe CK activity increase can cause rhabdomyolysis

Question 12

Niacin adverse effects?

Answer 12

The 3 H’s

1. Harmless cutaneous vasodilation (flushing, sense of warmth)
2. Hepatotoxicity (rare)
3. Hyperuricemia that can exacerbate gout

Question 13

When should statins be administered?

Answer 13

At night, most cholesterol biosynthesis occurs at night. Should be given with food to increase absorption

Question 14

Mechanism of action of Fibrates?

Answer 14

Ligands for PPAR-a. Transcriptionally up-regulate LPL, apo A-1, apo A-II, and down-regulate apo C-III. Also increase fatty acid oxidation in liver/striated muscle

Question 15

What statin should be given to someone with Renal dysfunction?

Answer 15

Atorvastatin

Question 16

Names of the Fibrates?

Answer 16

Gemfibrozil, Fenofibrate

Question 17

Mechanism of action of Bile acid sequestrants?

Answer 17

Positively charged drugs that inhibit the enterohepatic recycling of bile acids–> cause the liver to use cholesterol to make more bile

Question 18

Most common adverse effects seen with Bile acid sequestrants

Answer 18

GI side effects (bloating and constipation)

Question 19

Drug-drug intercations seen with Bile acid sequestrants?

Answer 19

Inhibit the absorption of drugs like warfarin, digoxin, beta-blockers, and thyroxine

Question 20

Bile acid sequestrants

Answer 20

Colestipol, Cholestyramine, Colesevelam

Question 21

Unique form of bile acid sequestrant administration?

Answer 21

They come in powder form

Question 22

Mechanism of action of Ezetimibe?

Answer 22

Inhibits the cholesterol uptake transporters NPC1L1

Question 23

How does Niacin cause hyperuricemia?

Answer 23

It competes with uric acid for excretion in the Renal tubules

Question 24

Dietary substance that has significant hypotriglyceridemic effect?

Answer 24

Omega-3 fatty acids, found in cold water fish. Also has anti-platelet, anti-arrhythmic, and blood pressure lowering effects