Term
| What are the 3 classes of drugs that lower LDL Cholesterol? |
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Definition
Bile Acid Sequestrants
HMG-CoA Reductase Inhibitors (Statins)
Cholesterol Absorption Inhibitors |
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Term
| What is the Bile Acid Sequestrants? |
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Definition
Cholestyramine
Non-systemic
Safe
OK for patients with liver disease and kids
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Term
| What is the mechanism of the Bile Acid Sequestrants? |
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Definition
(Cholestyramine)
Anionic (+ charge) resins that bind bile acids (- charge) and interrupt cholesterol recycling --> liver excretes more cholesterol |
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Term
| What effects do the Bile Acid Sequestrants have on each type of cholesterol? |
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Definition
(Cholestyramine)
LDL - lowers up to 25%
HDL - modest effect
TG - no decrease |
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Term
| What form is the Bile Acid Sequestrants in to take? |
|
Definition
|
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Term
| What are the side effects of Bile Acid Sequestrants? |
|
Definition
(Cholestyramine)
Gritty texture
Fecal impaction (take with water)
Hypertriglyceridemia |
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Term
| What effects do Bile Acid Sequestrants have with other drugs? |
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Definition
(Cholestyramine)
Prevents absorption of:
Digoxin
B-blockers
Thyroxine
Coumadin
(Take 1 hour prior or 3 hours after BAS)
|
|
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Term
| What is the mechanism of the Statins? |
|
Definition
Inhibit HMG-CoA Reductase
This upregulates LDL receptors via SREBP-2 |
|
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Term
| What is one of the main benefits of lowering LDL? |
|
Definition
| Decreases risk of coronary events |
|
|
Term
| What are some side effects of Statins? |
|
Definition
(Generally well tolerated)
Teratogenic
Myalgia
Myositis
Rhabdomyolysis
A million drug interactions (CYP3A4) |
|
|
Term
| What class of drugs may cause Rhabdomyolysis? |
|
Definition
Statins
Skeletal Muscle Breakdown
CPK elevation
Dark colored urine
Acute renal failure
|
|
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Term
| Which statin does not require reduced dosage with renal disease? |
|
Definition
Atorvastatin
(low renal clearance)
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|
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Term
| Which Statin is contraindicated with CYP3A4 Inhibitors, Cyclosporine, and Gemfibrozil? |
|
Definition
|
|
Term
| What drug inhibits cholesterol absorption? |
|
Definition
Ezetimibe
Inhibits absorption in the small intestine up to 50%
(The reduced cholesterol upregulates LDL receptors which increases LDL clearance from plasma) |
|
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Term
| In what special populations is Ezetimbe not recommended? |
|
Definition
Below age 10
Hepatic Insufficiency
Lactation |
|
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Term
| How does Ezetimibe interact with Bile Acid Sequestrants? Cyclosporine? Fibrates? |
|
Definition
Bile Acid Sequestrants decrease absorption up to 80%
Cyclosporine increases levels up to 4x
Fibrates increase levels up to 2x
(increase gallstones) |
|
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Term
| What classes of drugs may increase biliary cholesterol excretion and increase the risk of gallstones? |
|
Definition
Fibrates
(Fenofibrate)
Cholesterol Absorption Inhibitors
(Ezetimibe)
|
|
|
Term
| Plasma levels of Ezetimibe increase in what patient populations? |
|
Definition
Elderly
Women
Hepatic Insufficiency (CI)
Renal Insufficiency |
|
|
Term
| What is the mechanism of Ezetimibe? |
|
Definition
Cholesterol Absorption Inhibitor
Blocks internalization of NPC1L1 by blocking the Clathrin/AP2 complex (inhibits the cholesterol transporter) |
|
|
Term
| What effect does Ezetimibe have on each type of cholesterol? |
|
Definition
LDL - decrease
HDL - increase
TG - decrease
|
|
|
Term
| What 2 classes of drugs primarily lower Triglyceride and raise HDL levels? |
|
Definition
Fibric Acid Derivatives (Fibrates)
Nicotinic Acid (Niacin) |
|
|
Term
| What is the Fibrate? Mechanism? |
|
Definition
Fenofibrate
Activate PPARα (Peroxisome Proliferator-Activated Receptor) --> fatty acid oxidation
|
|
|
Term
| What are the effects of the Fibrates? |
|
Definition
(Fenofibrate)
Increase lipoprotein lipase activity
Increase ApoA1
Increase HDL
Decrease TG
Increase biliary excretion |
|
|
Term
| What are the effects of the Fibrates on each type of cholesterol? |
|
Definition
(Fenofibrate)
VLDL - decreased
LDL - unchanged/decreased
HDL - increased
TG - decreased
|
|
|
Term
| What drug can cause Azotemia? |
|
Definition
Fenofibrate
Azotemia - increase in nitrogen compounds such as urea and creatinine due to decreased GFR
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|
|
Term
| Which classes of Anti-lipid drugs are teratogenic? |
|
Definition
|
|
Term
| Vitamin B3 is also known as what? |
|
Definition
|
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Term
| What are the effects of Niacin on each type of cholesterol? |
|
Definition
VLDL - reduced synthesis and converted to LDL
HDL - increased
TG - decreased
|
|
|
Term
| What drug when combined with Niacin has been known to benefit coronary disease? |
|
Definition
| Niacin + Simvastatin = Simcor |
|
|
Term
| What are some side effects of Nictonic Acid? |
|
Definition
(increased with immediate release formula)
Flushing
Hepatotoxicity
Hyperuricemia / Gout
Conjunctivitis / Retinal detachment
Insulin resistance (acanthosis nigricans) |
|
|
Term
| What class of LDL lowering drugs are OK for use in kids and those with liver disease? |
|
Definition
Bile Acid Sequestrants
(Cholestyramine)
|
|
|
Term
| What class of drugs are anionic resins? |
|
Definition
Bile Acid Sequestrants
(Cholestyramine) |
|
|
Term
| What class of drugs interupt bile recycling? |
|
Definition
Bile Acid Sequestrants
(Cholestyramine) |
|
|
Term
| Which class of drugs need to be taken with water to avoid fecal impaction? |
|
Definition
Bile Acid Sequestrants
(Cholestyramine) |
|
|
Term
| What class of drugs upregulate LDL receptors via SREBP-2? |
|
Definition
|
|
Term
| What drug blocks the Clathrin/AP2 complex that acts as a cholesterol symporter? |
|
Definition
|
|
Term
| What class of drugs activate PPARα (Peroxisome Proliferator-Activated Receptor) which leads to fatty acid oxidation? |
|
Definition
|
|
Term
| What class of drugs should not be taken with grapefruit juice? |
|
Definition
|
|
Term
| What drug has a side effect of increased insulin resistance? |
|
Definition
|
|
Term
| What drug has a side effect of flushing? |
|
Definition
|
|
Term
| What drug has a side effect of gout? |
|
Definition
|
|
Term
| What drug has a side effect of eye problems? |
|
Definition
Niacin
(conjunctivitis, retinal detachment, macular edema)
|
|
|
Term
| What class of drugs have a side effect of Hypertryglyceridemia? |
|
Definition
Bile Acid Sequestrants
(Cholestyramine) |
|
|
Term
| What Fibrate has an active metabolite? |
|
Definition
|
|
Term
| Which Fibrate should be given if a patient is already taking a Statin? |
|
Definition
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