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Pharm II > Exam 2 - Hyperlipidemia > Flashcards

Exam 2 - Hyperlipidemia Flashcards

1
Q

What is the cause of Familial Hypercholesterolemia and what abnormality will you see in levels?

A

Cause: LDL receptor deficiency

Increased LDL

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2
Q

Lovastatin, Simvastatin, and Atorvastatin belong to what drug group?

A

HMG-CoA Reductase Inhibitors (Statins)

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3
Q

What is the MOA for HMG-CoA Reductase Inhibitors (Statins)?

A

Inhibits HMG-CoA reductase, reducing the livers ability to synthesize new cholesterol. The only way it will be able to make new cholesterol then is by increasing its LDL receptors to bring in LDL from the blood and using it, therefore reducing its levels.

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4
Q

What is the DOC in reducing LDL levels?

A

HMG-CoA Reductase Inhibitors (Statins)

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5
Q

What are uses for Statins?

A
  • Reduce LDL (DOC)
  • Reduce triglycerides
  • Increase HDL
  • Increase plaque stability
  • Decrease platelet aggregation
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6
Q

What is significant about Atorvastatin when compared to the other Statins?

A

Can be given in high dose which is used in high-risk ASCVD patients

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7
Q

Which two Statins are inactive and must be hydrolyzed into their active form?

A

Lovastatin and Simvastatin

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8
Q

What enzymes metabolize Statins?

A

P450s, CYP3A4

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9
Q

Which two Statins should be taken in the evening and why?

A

Lovastatin and Simvastatin should be taken in the evening as peak cholesterol synthesis occurs in the early morning hours and we want to block it

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10
Q

What are some adverse effects of Statins?

A
  • Increases levels of serum aminotransferase (enzyme to measure LFTs)
  • This increase in aminotransferase can lead to liver damage in alcoholics and those with liver disease
  • Myopathy and/or muscle pain due to muscle damage
  • Increases serum creatine kinase activity (hallmark)
  • Rhadomyolysis - myoglobinuria
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11
Q

What is a hallmark adverse effect of Statins?

A

Increased serum creatine kinase activity due to muscle damage

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12
Q

What are contraindications/precautions of Statins?

A
  • Pregnancy
  • Active hepatic disease
  • P450 inhibitors (grapefruit juice, macrolides, verapamil, ketoconazole, ritonavir will increase plasma concentrations)
  • P450 activators (phenytoin, griseofulvin, barbiturates, rifampin will decrease the plasma concentrations)
  • Gemfibrozil will inhibit metabolism
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13
Q

What drug class does Cholestyramine belong to?

A

Bile Acid-Binding Resins

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14
Q

What is the MOA for Cholestyramine?

A

Binds bile acids and prevents their intestinal reabsorption, leading to decreased serum LDL levels as the liver will have to take up serum LDL to make more bile acids

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15
Q

What are uses of Cholestyramine?

A

Decrease LDL levels

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16
Q

What is Cholestyramine not effective for?

A
  • No effect in homozygous familial hypercholesterolemia due to no functional LDL receptors
  • Not effective in hypertriglyceridemia
17
Q

What is important to remember when taking Cholestyramine in regards to its pharmacokinetics?

A

Should be taken with meals as bile production is needed for effect

18
Q

Why is Cholestyramine safe in pregnancy?

A

It is not absorbed

19
Q

What is the most common side effect and is a hallmark of Cholestyramine?

A

Constipation and bloating

20
Q

What is a rare side effect of Cholestyramine?

A
  • Gallstones in obese patients

- May cause hypoprothrombinemia due to vitamin K malabsorption

21
Q

What can Cholestyramine impair the absorption of?

A

Acid or fat-soluble drugs like digitalis, thiazides, statins, tetracycline, thyroxine, or aspirin

22
Q

What is the MOA for Niacin?

A

Inhibits VLDL secretion, leading to reduce levels of plasma VLDL and LDL

23
Q

What is the most effective agent for increasing levels of HDL? What type of patient is this used for?

A

Niacin - used in patients who cannot exercise

24
Q

What are uses of Niacin?

A
  • Decrease VLDL/LDL

- Increase HDL

25
Q

What are some adverse effects of Niacin?

A
  • Cutaneous vasodilation (flushing, warm sensation, pruritis) (hallmark)
  • Nausea/abdominal discomfort
  • Impairs glucose tolerance (hallmark)
  • Hyperuricemia
  • Rarely causes severe hepatotoxicity
26
Q

What are two hallmark side effects associated with Niacin?

A
  • Cutaneous vasodilation

- Impairs glucose tolerance

27
Q

Which patients should not be given Niacin and why?

A

Diabetics as it impairs glucose tolerance

28
Q

Gemfibrozil belongs to what class of drugs?

A

Fibric Acid Derivatives (Fibrates)

29
Q

What is the MOA for Gemfibrozil (Fibrates)?

A

PPAR-a ligand (nuclear receptor) which turns on genes in muscle/adipose to up-regulate LDL activity leading to increased catabolism of VLDL and decreased triglycerides

30
Q

What is Gemfibrozil/Fibrates used for?

A

Hypertriglyceridemia

31
Q

What are some adverse effects of Gemfibrozil/Fibrates?

A
  • Increased incidence of cholelithiasis/gallstones (hallmark)
  • Increased aminotransferases and alkaline phosatase
  • Skin rashes, GI, arrhythmias
  • Increase anticoagulant action of warfarin
  • Inhibits metabolism of statins
  • May increase LDL in some patients with combined hyperlipidemias
32
Q

What is a hallmark side effect associated with Gemfibrozil/Fibrates?

A

Increased incidence of cholelithiasis/gallstones (hallmark)

33
Q

What is the MOA for Ezetimibe?

A

Selectively blocks the intestinal absorption of cholesterol and related phytosterols

34
Q

What is Ezetimibe used for?

A

Moderate decrease in LDL

35
Q

What other medication is Ezetimibe always used with for synergistic effect?

A

Used in combination with statins

36
Q

What is the MOA for Alirocumab and Evolocumab?

A

They are antibodies that inhibit PCSK9 from binding to LDL receptors, leading to a decrease in LDL receptor degradation and more receptors being available to bring LDL into the liver, decreasing LDL serum levels

37
Q

What are the pharmacokinetics of Alirocumab and Evolocumab?

A

Monthly subcutaneous injections

38
Q

What is the DOC for Hypertriglyceridemia?

A

Gemfibrozil (Fibrates)

Pharm II (10 decks)

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