Lipid Drugs Flashcards

1
Q

Why do people with familial hypercholesterolemia have such high LDL

A

They dont have (many) LDL receptors

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2
Q

What is the MOA of statins

A

Inhibiting HMG-CoA to increase LDL receptors = lower LDL

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3
Q

What is the most effective drug for lowering LDL

A

Statins

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4
Q

What are some of the other beneficial effects of statins?

A

Decrease CRP (anti-inflammation!)

Increase production of NO= vasodilation

Stabilize plaques

Decrease lipoprotein oxidation

Decreased platelet aggregation

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5
Q

Which two statins are considered Pro drugs and need to be hydrolyzed to be active

A

Lovastatin

Simvastatin

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6
Q

What time of day do statins need to be taken

A

Evening (due to the diurnal pattern of cholesterol synthesis)

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7
Q

What are the adverse effects of statin

A

Increased liver enzymes ***

Myopathy/muscle pain***

Increased CK with exercise***

Rhabdomyolysis***

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8
Q

Who can NOT have statins

A

Pregnant women*** cat X

Active liver disease*******

Use caution in alcoholics or hx of liver dz

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9
Q

What drugs/things inhibit p450 and will INCREASE the plasma concentrations (MORE TOXICITY) of statins?

A

Grapefruit juice***

Prob all you need to know but here are more:

Macrolides

Cyclosporine

Ketoconazole

Verapamil

Ritonavir

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10
Q

What drug will inhibit the metabolism of statins and cause increased toxicity?

A

Gemfibrozil (a fibrate!)

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11
Q

What happens if you wash your simvastatin down with a glass of grapefruit juice

A

Liver damage and rhabdomolysos

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12
Q

Name 3 resins

A

Cholestyramine (Questran)

Colestipol (Colestid)

Colesevelam (WelChol)

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13
Q

Why do patients hate taking bile acid-binding resins?

A

It has a sandy/gritty texture

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14
Q

What is the MOA of bile acid-binding resins

A

Binds bile acids and prevents their reabsorption

= liver makes more LDL receptors to increase uptake of LDL to make more bile

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15
Q

Who will not have any benefit from taking bile-acid resins?

A

Homozygous familial hypercholesterolemia -they don’t have functional LDL receptors

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16
Q

Will bile acid binding resins help lower triglycerides?

17
Q

When are bile acid binding resins effective?

A

When LDL is elevated

No effect on Triglycerides

18
Q

Are Bile Acid Bindinf resins safe in preganncy?

19
Q

What is the most common side effect of bile acid binding resins?

A

Constipation and bloating!

Bacteria get to feast on the lipids your bile should have been breaking down

20
Q

What effect will bile acid resins have on patients taking warfarin

A

Hypoprothrombinemia due to vitamin K malabsorption (increased bleeding)

Although it just fucks with your absorption of everything so warfarin effects could also be decreased

21
Q

What drugs will not be absorbed well if you take bile acid resins

A

Digitalis

Thiazides

Statins

Tetracycline

Thyroxine

Aspirin

22
Q

What si the MOA of niacin (Nicotinic acid/B3)

A

Inhibits VLDL secretion (VLDL is the source of LDL)

23
Q

What drug is the most effective at increasing HDL

24
Q

What are the main side effects of niacin

A

FLUSHING

Impairs glucose tolerance

25
How could you prevent the flushing from niacin?
Take aspirin before - flushing is dependent on prostaglandins
26
Name 3 fibrates
Gemfibrozil (Lopid) Fenofibrate (TriCor) Fenofibrate acid (Fibricor)
27
What lipid panel value will be lowered with fibrates
Triglycerides **** NOT LDL!!!! Might even RAISE LDL!
28
What is the MOA of fibrates
Increase LPL activity = VLDL broken down = Lower Triglycerides
29
What is the main side effect of fibrates
Gallstones!!**
30
30 yo woman with 2kids had high Triglycerides at her last checkup. She got a drug form the doctor and now complains that she has R-sided back pain especially after a fatty meal. What drug did she get
A fibrate (gave her gallstones)
31
What is the MOA of ezetimibe (Zetia)
Blocks intestinal absorption of cholesterol
32
What do you need to give Ezetemibe (Zetia) with for it to really do anything?
A statin Synergistic!
33
What are the 2 PCSK9 inhibitors
Alirocumab (Praluent) Evolocumab (Repatha)
34
Whaat is the MOA of PCSK9 inhibitors
Increases # of LDL receptors on the liver so LDL in blood drops
35
How are PCSK9 inhibitors given?
Monthly subcutaneous injections
36
What’s the big deal if you have high cholsterol
High= cardiovascular problems SUPER high= pancreatitis
37
Best drug to lower LDL
Statins
38
Best drug to decrease triglycerides
Fibrates