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Pharmacology II Exam 2 (Lauren) > Lipid Drugs > Flashcards

Flashcards in Lipid Drugs Deck (38)
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1
Q

Why do people with familial hypercholesterolemia have such high LDL

A

They dont have (many) LDL receptors

2
Q

What is the MOA of statins

A

Inhibiting HMG-CoA to increase LDL receptors = lower LDL

3
Q

What is the most effective drug for lowering LDL

A

Statins

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

5
Q

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

A

Lovastatin

Simvastatin

6
Q

What time of day do statins need to be taken

A

Evening (due to the diurnal pattern of cholesterol synthesis)

7
Q

What are the adverse effects of statin

A

Increased liver enzymes ***

Myopathy/muscle pain***

Increased CK with exercise***

Rhabdomyolysis***

8
Q

Who can NOT have statins

A

Pregnant women*** cat X

Active liver disease*******

Use caution in alcoholics or hx of liver dz

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

10
Q

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

A

Gemfibrozil (a fibrate!)

11
Q

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

A

Liver damage and rhabdomolysos

12
Q

Name 3 resins

A

Cholestyramine (Questran)

Colestipol (Colestid)

Colesevelam (WelChol)

13
Q

Why do patients hate taking bile acid-binding resins?

A

It has a sandy/gritty texture

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

15
Q

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

A

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

16
Q

Will bile acid binding resins help lower triglycerides?

A

NO

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?

A

Yes

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

A

Niacin

24
Q

What are the main side effects of niacin

A

FLUSHING

Impairs glucose tolerance

25
Q

How could you prevent the flushing from niacin?

A

Take aspirin before - flushing is dependent on prostaglandins

26
Q

Name 3 fibrates

A

Gemfibrozil (Lopid)

Fenofibrate (TriCor)

Fenofibrate acid (Fibricor)

27
Q

What lipid panel value will be lowered with fibrates

A

Triglycerides **

NOT LDL!!!! Might even RAISE LDL!

28
Q

What is the MOA of fibrates

A

Increase LPL activity = VLDL broken down = Lower Triglycerides

29
Q

What is the main side effect of fibrates

A

Gallstones!!**

30
Q

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

A fibrate (gave her gallstones)

31
Q

What is the MOA of ezetimibe (Zetia)

A

Blocks intestinal absorption of cholesterol

32
Q

What do you need to give Ezetemibe (Zetia) with for it to really do anything?

A

A statin

Synergistic!

33
Q

What are the 2 PCSK9 inhibitors

A

Alirocumab (Praluent)

Evolocumab (Repatha)

34
Q

Whaat is the MOA of PCSK9 inhibitors

A

Increases # of LDL receptors on the liver so LDL in blood drops

35
Q

How are PCSK9 inhibitors given?

A

Monthly subcutaneous injections

36
Q

What’s the big deal if you have high cholsterol

A

High= cardiovascular problems

SUPER high= pancreatitis

37
Q

Best drug to lower LDL

A

Statins

38
Q

Best drug to decrease triglycerides

A

Fibrates