antilipemic agents - Sheet1 Flashcards
What is the primary organ targeted by antilipemic agents?
The liver.
Where do some lipid-lowering drugs work besides the liver?
The intestines.
What is the desired total cholesterol level?
Less than 160 mg/dL.
What is the desired HDL cholesterol level?
Greater than 40 mg/dL.
Why is HDL cholesterol considered “good”?
It carries LDL cholesterol away from the liver to be excreted.
What is the desired LDL cholesterol level?
Less than 100 mg/dL.
Why is LDL cholesterol considered “bad”?
It contributes to fatty buildup in arteries.
What is the desired triglyceride (TG) level?
Less than 150 mg/dL.
What is the most common type of fat stored in the body?
Triglycerides (TGs).
What is the most effective drug class for lowering LDL cholesterol?
HMG-CoA reductase inhibitors (statins).
Besides lowering LDL, what other benefits do statins provide?
Increase HDL, lower triglycerides in some, stabilize plaques, reduce cardiovascular (CV) events, and increase bone formation.
Why is plaque stability important?
If unstable plaque breaks off, it can lead to strokes or myocardial infarctions (MIs).
What is the first-line treatment to lower cholesterol?
Statins.
How do statins work?
They inhibit cholesterol production in the liver, prompting the liver to produce more LDL receptors to remove cholesterol from the blood.
What organ function should be monitored when taking statins?
Liver function.
What conditions are statins used for?
Hypercholesterolemia, primary & secondary CV event prevention, post-MI therapy, and diabetes (protection against MI & stroke).
What are the common adverse effects (AEs) of statins?
Headache, rash, and GI upset (usually improve over time).
What are the rare but serious AEs of statins?
Myopathy/rhabdomyolysis, hepatotoxicity, cataracts.
What symptom should prompt lowering the statin dose?
Muscle aches (risk of myopathy/rhabdomyolysis).
What drugs interact with statins?
Other lipid-lowering drugs (fibrates, ezetimibe), CYP3A4 inhibitors (e.g., grapefruit juice).
Why should grapefruit juice be avoided with statins?
It inhibits CYP3A4, affecting statin metabolism.
What is the pregnancy category for statins?
Category X – contraindicated in pregnancy due to fetal harm.
What lab values should be monitored with statin use?
Lipid levels, liver function tests (LFTs), creatine kinase (CK).
Why is CK monitored in statin users?
To detect muscle breakdown (rhabdomyolysis).
What symptoms indicate possible rhabdomyolysis?
Muscle tenderness, pain, numbness, tingling.
When should statins be taken?
In the evening, preferably with an evening meal, because cholesterol is produced at night.
What are some common statins?
Simvastatin, Simvastatin + Ezetimibe, Lovastatin, Pravastatin, Rosuvastatin, Fluvastatin, Pitavastatin.
What is an example of a cholesterol absorption inhibitor?
Ezetimibe.
How is ezetimibe typically used?
As an add-on with a statin, unless statins cannot be used.
Where does ezetimibe work?
In the intestine.
What does ezetimibe do?
Blocks cholesterol absorption, lowering total cholesterol, LDL, and apolipoprotein B.
What are the adverse effects (AEs) of ezetimibe?
Myopathy/rhabdomyolysis, hepatitis, pancreatitis, thrombocytopenia.
What should be monitored with ezetimibe use?
Lipids, liver function tests (LFTs), creatine kinase (CK).
What drugs interact with ezetimibe?
Bile acid sequestrants (BAS), statins, fibrates.
What are examples of bile acid sequestrants (BAS)?
Colesevelam, Cholestyramine, Colestipol.
How do BAS lower cholesterol?
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.
Can BAS be used alone?
Yes, but they are often combined with a statin.
What is a common side effect of BAS?
Constipation (due to staying in the GI tract).
How can constipation from BAS be managed?
Increase water, fiber, and food intake.
What other GI side effects can BAS cause?
Bloating and nausea.
Why do BAS have many drug interactions?
They can bind to other drugs in the GI tract and block their absorption.
What medications can BAS interfere with?
Thiazide diuretics, digoxin, warfarin, fat-soluble vitamins, levothyroxine, oral contraceptives.
What is the best way to take BAS with other medications?
Take other medications 1 hour before or 4 hours after BAS to avoid absorption issues.
How should BAS be taken?
As a tablet or powder with at least 4–8 oz of fluid.
Are BAS safe during pregnancy?
Yes, because they are not absorbed by the body and do not reach the fetus.
What are examples of fibrates (fibric acid derivatives)?
Gemfibrozil, fenofibrate, fenofibric acid.
What do fibrates primarily do?
Lower triglyceride (TG) levels (VLDLs), may raise HDL.
When are fibrates used?
As 3rd-line drugs, only if LDL reduction is strongly needed.
What are the adverse effects (AEs) of fibrates?
GI upset, gallstones, myopathy, hepatotoxicity.
What risk increases when fibrates are combined with statins?
Rhabdomyolysis (muscle breakdown).
What risk increases when fibrates are combined with warfarin?
Increased risk of bleeding.
What lab values should be monitored with fibrate use?
CK, LFTs, PT/INR (if on warfarin).
When should fibrates be taken?
30 minutes before breakfast or dinner.
What is another name for niacin (nicotinic acid)?
Vitamin B6.
What does niacin do to cholesterol levels?
Reduces LDL and TG, raises HDL (best at raising HDL).
Does niacin significantly improve cardiovascular (CV) outcomes?
No, it has little impact on CV events.
Why is niacin not preferred over statins?
It has more adverse effects than statins.
What are the adverse effects (AEs) of niacin?
Intense flushing, GI upset, liver injury, muscle cramps, headache, rash, photosensitivity.
How can flushing from niacin be reduced?
Take one adult-strength aspirin (325 mg) 30 minutes before the niacin dose.
Should niacin be taken with or without food?
With food.
What are examples of monoclonal antibodies for cholesterol?
Alirocumab, evolocumab.
What is the primary effect of monoclonal antibodies on cholesterol?
They lower LDL.
What are the adverse effects (AEs) of monoclonal antibodies?
Hypersensitivity reactions, injection site reactions.
