Cholesterol Drugs Flashcards Preview

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Flashcards in Cholesterol Drugs Deck (24)
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1
Q

Statins that are prodrugs

A

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

2
Q

Statins metabolized by CYP3A4

A

Lovastatin, Simvastatin, Atorvastatin (also oxidized)

3
Q

Statins metabolized by CYP2C9

A

Fluvastatin, Rosuvastatin

4
Q

Statin metabolized solely by Sulfonation

A

Pravastatin

5
Q

Statin mechanism of action?

A

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

6
Q

Statins with highest potency/efficacy?

A

Atorvastatin, Rosuvastatin (longest half lives)

7
Q

Statins with moderate potency/efficacy?

A

Lovastatin, Simvastatin

8
Q

Statin with lowest potency/efficacy?

A

Pravastatin

9
Q

Niacin mechanism of action?

A

Inhibits VLDL secretion, thereby decreasing LDL

10
Q

Niacin’s most useful clinical aspects?

A

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

11
Q

Adverse effects seen with Statin therapy?

A

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

12
Q

Niacin adverse effects?

A

The 3 H’s

  1. Harmless cutaneous vasodilation (flushing, sense of warmth)
  2. Hepatotoxicity (rare)
  3. Hyperuricemia that can exacerbate gout
13
Q

When should statins be administered?

A

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

14
Q

Mechanism of action of Fibrates?

A

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

15
Q

What statin should be given to someone with Renal dysfunction?

A

Atorvastatin

16
Q

Names of the Fibrates?

A

Gemfibrozil, Fenofibrate

17
Q

Mechanism of action of Bile acid sequestrants?

A

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

18
Q

Most common adverse effects seen with Bile acid sequestrants

A

GI side effects (bloating and constipation)

19
Q

Drug-drug intercations seen with Bile acid sequestrants?

A

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

20
Q

Bile acid sequestrants

A

Colestipol, Cholestyramine, Colesevelam

21
Q

Unique form of bile acid sequestrant administration?

A

They come in powder form

22
Q

Mechanism of action of Ezetimibe?

A

Inhibits the cholesterol uptake transporters NPC1L1

23
Q

How does Niacin cause hyperuricemia?

A

It competes with uric acid for excretion in the Renal tubules

24
Q

Dietary substance that has significant hypotriglyceridemic effect?

A

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