antilipemic agents - Sheet1 Flashcards

1
Q

What is the primary organ targeted by antilipemic agents?

A

The liver.

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2
Q

Where do some lipid-lowering drugs work besides the liver?

A

The intestines.

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3
Q

What is the desired total cholesterol level?

A

Less than 160 mg/dL.

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4
Q

What is the desired HDL cholesterol level?

A

Greater than 40 mg/dL.

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5
Q

Why is HDL cholesterol considered “good”?

A

It carries LDL cholesterol away from the liver to be excreted.

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6
Q

What is the desired LDL cholesterol level?

A

Less than 100 mg/dL.

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7
Q

Why is LDL cholesterol considered “bad”?

A

It contributes to fatty buildup in arteries.

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8
Q

What is the desired triglyceride (TG) level?

A

Less than 150 mg/dL.

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9
Q

What is the most common type of fat stored in the body?

A

Triglycerides (TGs).

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10
Q

What is the most effective drug class for lowering LDL cholesterol?

A

HMG-CoA reductase inhibitors (statins).

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11
Q

Besides lowering LDL, what other benefits do statins provide?

A

Increase HDL, lower triglycerides in some, stabilize plaques, reduce cardiovascular (CV) events, and increase bone formation.

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12
Q

Why is plaque stability important?

A

If unstable plaque breaks off, it can lead to strokes or myocardial infarctions (MIs).

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13
Q

What is the first-line treatment to lower cholesterol?

A

Statins.

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14
Q

How do statins work?

A

They inhibit cholesterol production in the liver, prompting the liver to produce more LDL receptors to remove cholesterol from the blood.

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15
Q

What organ function should be monitored when taking statins?

A

Liver function.

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16
Q

What conditions are statins used for?

A

Hypercholesterolemia, primary & secondary CV event prevention, post-MI therapy, and diabetes (protection against MI & stroke).

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17
Q

What are the common adverse effects (AEs) of statins?

A

Headache, rash, and GI upset (usually improve over time).

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18
Q

What are the rare but serious AEs of statins?

A

Myopathy/rhabdomyolysis, hepatotoxicity, cataracts.

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19
Q

What symptom should prompt lowering the statin dose?

A

Muscle aches (risk of myopathy/rhabdomyolysis).

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20
Q

What drugs interact with statins?

A

Other lipid-lowering drugs (fibrates, ezetimibe), CYP3A4 inhibitors (e.g., grapefruit juice).

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21
Q

Why should grapefruit juice be avoided with statins?

A

It inhibits CYP3A4, affecting statin metabolism.

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22
Q

What is the pregnancy category for statins?

A

Category X – contraindicated in pregnancy due to fetal harm.

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23
Q

What lab values should be monitored with statin use?

A

Lipid levels, liver function tests (LFTs), creatine kinase (CK).

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24
Q

Why is CK monitored in statin users?

A

To detect muscle breakdown (rhabdomyolysis).

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25
Q

What symptoms indicate possible rhabdomyolysis?

A

Muscle tenderness, pain, numbness, tingling.

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26
Q

When should statins be taken?

A

In the evening, preferably with an evening meal, because cholesterol is produced at night.

27
Q

What are some common statins?

A

Simvastatin, Simvastatin + Ezetimibe, Lovastatin, Pravastatin, Rosuvastatin, Fluvastatin, Pitavastatin.

28
Q

What is an example of a cholesterol absorption inhibitor?

A

Ezetimibe.

29
Q

How is ezetimibe typically used?

A

As an add-on with a statin, unless statins cannot be used.

30
Q

Where does ezetimibe work?

A

In the intestine.

31
Q

What does ezetimibe do?

A

Blocks cholesterol absorption, lowering total cholesterol, LDL, and apolipoprotein B.

32
Q

What are the adverse effects (AEs) of ezetimibe?

A

Myopathy/rhabdomyolysis, hepatitis, pancreatitis, thrombocytopenia.

33
Q

What should be monitored with ezetimibe use?

A

Lipids, liver function tests (LFTs), creatine kinase (CK).

34
Q

What drugs interact with ezetimibe?

A

Bile acid sequestrants (BAS), statins, fibrates.

35
Q

What are examples of bile acid sequestrants (BAS)?

A

Colesevelam, Cholestyramine, Colestipol.

36
Q

How do BAS lower cholesterol?

A

They are nonabsorbable resins that bind bile acids in the GI tract, causing the liver to pull cholesterol from the blood to make more bile acids.

37
Q

Can BAS be used alone?

A

Yes, but they are often combined with a statin.

38
Q

What is a common side effect of BAS?

A

Constipation (due to staying in the GI tract).

39
Q

How can constipation from BAS be managed?

A

Increase water, fiber, and food intake.

40
Q

What other GI side effects can BAS cause?

A

Bloating and nausea.

41
Q

Why do BAS have many drug interactions?

A

They can bind to other drugs in the GI tract and block their absorption.

42
Q

What medications can BAS interfere with?

A

Thiazide diuretics, digoxin, warfarin, fat-soluble vitamins, levothyroxine, oral contraceptives.

43
Q

What is the best way to take BAS with other medications?

A

Take other medications 1 hour before or 4 hours after BAS to avoid absorption issues.

44
Q

How should BAS be taken?

A

As a tablet or powder with at least 4–8 oz of fluid.

45
Q

Are BAS safe during pregnancy?

A

Yes, because they are not absorbed by the body and do not reach the fetus.

46
Q

What are examples of fibrates (fibric acid derivatives)?

A

Gemfibrozil, fenofibrate, fenofibric acid.

47
Q

What do fibrates primarily do?

A

Lower triglyceride (TG) levels (VLDLs), may raise HDL.

48
Q

When are fibrates used?

A

As 3rd-line drugs, only if LDL reduction is strongly needed.

49
Q

What are the adverse effects (AEs) of fibrates?

A

GI upset, gallstones, myopathy, hepatotoxicity.

50
Q

What risk increases when fibrates are combined with statins?

A

Rhabdomyolysis (muscle breakdown).

51
Q

What risk increases when fibrates are combined with warfarin?

A

Increased risk of bleeding.

52
Q

What lab values should be monitored with fibrate use?

A

CK, LFTs, PT/INR (if on warfarin).

53
Q

When should fibrates be taken?

A

30 minutes before breakfast or dinner.

54
Q

What is another name for niacin (nicotinic acid)?

A

Vitamin B6.

55
Q

What does niacin do to cholesterol levels?

A

Reduces LDL and TG, raises HDL (best at raising HDL).

56
Q

Does niacin significantly improve cardiovascular (CV) outcomes?

A

No, it has little impact on CV events.

57
Q

Why is niacin not preferred over statins?

A

It has more adverse effects than statins.

58
Q

What are the adverse effects (AEs) of niacin?

A

Intense flushing, GI upset, liver injury, muscle cramps, headache, rash, photosensitivity.

59
Q

How can flushing from niacin be reduced?

A

Take one adult-strength aspirin (325 mg) 30 minutes before the niacin dose.

60
Q

Should niacin be taken with or without food?

A

With food.

61
Q

What are examples of monoclonal antibodies for cholesterol?

A

Alirocumab, evolocumab.

62
Q

What is the primary effect of monoclonal antibodies on cholesterol?

A

They lower LDL.

63
Q

What are the adverse effects (AEs) of monoclonal antibodies?

A

Hypersensitivity reactions, injection site reactions.