Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Cardio - Elam > Drugs used in Dyslipidemia > Flashcards

Drugs used in Dyslipidemia Flashcards

1
Q

Fibric Acid Derivatives
• MOA
• Name them

A

MOA:
• Act as Ligands to for PPARa nuclear receptor
• PPARa turns on processes that help to get rid of TGs

(increased FA use in muscle, inc. apoA1/2, dec. apo CIII, inc. LDL-R)

Drugs:
• Gemfibrozil
• Fenofibrate
• Fenofibric Acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

**Statins
• MOA
• Name them

A

Blockage of Cholesterol Synthesis
• Competitive inhibitor of HMG-CoA Reductase

Increased LDL receptors
• causes SREBP to go from ER to Golgi and Finally to act as a transcription factor to up regulate LDLR synthesis

Drugs = Lo-SPAR:
• Lovastatin
• Simvastatin
• Pravastatin
• Atrovastatin
• Rosuvastatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

**Bile Acid Resins
• MOA
• Name them

A

MOA:
• Anionic ion exchange resins (they are Positively charged)
• Bind up bile acids and prevent recycling
• Cholesterol must then be pulled out of the blood to make new bile acids

Drugs:
• Colestipol
• Cholestyramine
• Coleevelam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

**Ezetimibe
• MOA
• Method of administration

A

MOA:
• Prevents uptake of CHOLESTEROL itself in SMALL INTESTINE and leaves the bile alone
• Decreased Cholesterol uptake cause liver to UPREGULATE LDL Receptors

*Given as a pill

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

**Niacin
• MOA
• Name them

A

MOA:
• Reduces Hepatic Triglyceride Synthesis
• Reduces Hepatic ApoB synthesis
• Enhances Macrophage transfer of Cholesterol to HDL
• Promotes VLDL conversion to LDL

Name:
• Niacor - IR
•Niaspan - ER

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How much can statins lower LDL compared to other drugs such as Bile acid resins, ezetimibe, or niacin?

A

Statins lower LDL by 25-60% while other drugs lower it by ~20%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Which statins are acted on by CYP3A4?
• Note any important differences

A

• Lovastatin

• Simvastatin

• Atorvastatin

**Atorvastatin is also metabolized by ß-oxidation so CYP3A4 interactions typically aren’t an issue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Which statins are the most effective at lowering cholesterol?

  • How effective are they?
  • What type of patients would you typically give these to?
A

• Atorvastatin
• Rosuvastastin

*Can give AT LEAST a 50% reduction in cholesterol **Typically given to patients who have lots of risk factors such as those with diabetes or heart disease**

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What statin would you consider giving to a patient with renal dysfunction?
• if this drug were not available, what backup would you use?
• Metabolism of these drugs?

A

Atorvastatin (only 2% renal excretion)
• ß-oxidation and CYP3A4 metabolized

Fluvastatin (only 5% renal excretion)
• CYP2C9, hydoxylation, and ß-oxidation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What statins are acted on by CYP2C9?

A

Rosuvastatin
• CYP2C9, Fecal excretion

Fluvastatin
• CYP2C9, Hydroxylation, ß-oxidation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Of the statins which are most susceptible to drug-drug interactions and why?

A

Simvastatin and Lovastatin
• Both are metabolized primarily by CYP3A4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are some drugs that inhibit CYP3A4?

A

• Macrolides
• Azole Antifungals
• Calcium Channel Blockers
• Grapefruit
• HIV protease Inhibitors
• Immunosuppressants

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the risk of Rhabdomyolysis other than severe muscle pain?
• indicators that this is happening

A

Indicators:
• Very High Levels of CPK
• Tea colored Urine

Risk:
• Myoglobin released from damaged muscle is nephrotoxic and can damage Kidneys

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are some drugs that inhibit p-glycoprotein mediated intestinal reabsorption?

A

• Cyclosporin
• Grapefruit Juice

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What drug should you not use with any of the statins and why?

A

Gemfibrozil - contraindicated
• Inhibits glucuronyltranserase-1 and glucuronidation used as one of the methods of elimination for almost all of the statins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How does myositis differ from Rhabdomyolysis?

A

Both result in high CPK and muscle pain, but Rhabdomyolysis is so severe that it can cause increased risk of Renal failure and death

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Which of the statins has the lowest risk of drug-drug interactions and why?

A

Pravistatin

• Eliminated via Sulfation, Oxidation, and Gluroonidation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Lovastatin Simvastatin
• Metabolism
• Systemic Bioavailability

A

Metabolism
•CYP3A4
• Glucoronidation

Bioavailability:
• 5% (lowest)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Pravastatin
• Metabolism
• Systemic Bioavailability

A

Metabolism
• Sulfation
• Oxidation
• Glucoronidation

Bioavailability:
• 17%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Fluvastatin
• Metabolism

• Systemic Bioavailability

A

Metabolism
• CYP2C9
• Hydroxylation
• ß-oxidation

Bioavailability
• 24%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Atorvastatin
• Metabolism

• Systemic Bioavailability

A

Metabolism
• ß-oxidation
• CYP3A4
• Glucoronidation

Bioavailability
• 14%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Rosuvastatin
• Metabolism
• Systemic Bioavailability

A

Metabolism
• CYP2C9

• Fecal Excretion

Bioavailability
• 20%

23
Q

Besides muscle pain what are 4 other side effects of statins?

A
  • Pregnancy Category X
  • Sleep Disturbance, Memory Loss, Reduced daytime Vigilance
  • Increased Liver Enzymes (rarely Hepatitis)
  • Mild GI distress
24
Q

If a patient has liver disease or another disease where they can’t handle drugs in their system, what options are available to lower their cholesterol?

A

Bile Acid Sequesterants
• No systemic effect because they never even enter the circulation

25
Q

How will your lipid profile change after taking a bile acid sequestrant?

A

• ONLY LDL decreases - there is NO EFFECT ON TRIGLYCERIDES

26
Q

What are the 3 bile acid sequestering drugs?

• how are they administered?

A

Colestipol - Powder or Tablet

Cholestyramine - Powder

Colesvelam - Tablet

27
Q

What are some common adverse effects/down sides of the Bile Acid Sequestrants?

A
  • Gritty Texture
  • Constipation, Nausea, Flatulence

• Fecal Impaction

• HYPERtriglyceridemia

28
Q

What problems do the bile acid sequensterants pose when taking other drugs with them?
• how can this be avoided?

A

Problems:
• Prevents absorption of other drugs

*take other drugs 1 hour before or 3 to 4 hours after bile sequesterant

29
Q

What conditions are bile sequestrants contrainidicated with?

A

• Hypertriglyceridemia
• Complex Drug Regimens
• Hx of Constipation

30
Q

What is the most common use of Ezetimibe?

A

• Given along with Statins to achieve extremely low LDL levels required in patients with CV risk factors

31
Q

What drugs can be given the BOTH LOWER LDL and RAISE HDL?

A

• Fibric Acid Derivatives (fibrates)
• Nicotinic Acid (niacin)
• Omega-3 (fish oil)

32
Q

What is the relationship between triglycerides and HDL-C?

A

Inverse Relationship, if HDL falls then TGs go up and vise vesa

33
Q

T or F: adding drugs besides Ezetimibe to Statins has proven to be highly effective.

A

False, using Niacin, Fibrates, or Fish Oil has shown little effect

34
Q

What group of drugs activates PPARalpha and what is the effect?
• Name drugs

A

Fibrinates PPARa
• Decreased ApoCIII synthesis
• Increased Apo AI and AII synthesis
• Increased LPL synthesis

Drugs:
• Gemfibrozil

• Fenofibrate

• Fenofibric Acid

35
Q

How do the Fibrates effect Lipids?
• Adverse effects?

A

Lipid Effects:
• Reduced TGs up to 50%

  • Reduced VLDL, Increased HDL
  • LDL relatively unaffected

Adverse Effects:
• GI upset
• Increased Creatinine or Liver enzyme
• Gallstones

36
Q

Gemfibrozil
• Drug Class
• Metabolism

A

Drug Class:
• Fibrinates

Metabolism:
• LIVER - (oxidation and glucuronidation by UGTA1) - do not give other drugs that are elminated by glucoronidation (most statins) with this drug

37
Q

Fenofibrate
• Drug Class
• Metabolism

A

Drug Class:
• Fibrinates

Metabolism:
• Hepatic to become Fenofibric acid then Renally Excreted

38
Q

Between the fibrinates which do you think would be safer to give to a patient in renal failure?
• Liver disease?

A

Best for renal failure:
Gemfibrozil - almost entirely hepatically metabolized

Best for Liver disease:
• Fenofibric acid because it doesn’t have to undergo activation in the liver like fenofibrate

39
Q

Fenofibric Acid
• Drug Class
• Metabolism

A

Drug Class:

• Fibrinates

Metabolism:

• Almost Exclusively Renally Excreted

40
Q

Which of the Fibric Acid derivatives is contraindicated with statins? why?

A

Gemfibrozil - both gemfibrozil and statins are extensively metabolized in the liver and can lead to inhibition of statin effect

41
Q

Do fibrinates show a benefit when added to statins?

A

NO, BUT due to discrepancies in studies it might be worth trying in your own patients to get them to safe cholesterol levels

42
Q

What are the 2 different preparations of niacin and how should they be administered?
• Dose?

A

Niacor - (IR) - immediate Release
• must incrementally increase dose over time to minimize flushing
• 6 grams/day

Niaspan - (ER) - Extended Release
• Less Flushing and usually given before bed to minimize flushing
• 1-2 grams/day

43
Q

What are some adverse side effects of Niacin?

A

• Cutaneous Flushing
• Elevated Hepatic Enzymes (also caused by statins)
• GI irritation
• Hyperuricemia/Gout
• Dry Skin
• Insulin Resistance

44
Q

taking niacin with statins does not significantly reduce the risk of a CHD event

A

taking niacin with statins does not significantly reduce the risk of a CHD event

45
Q

What are some food sources for Omega-3 and Omega-6 fatty acids?

A

Omega-3
• Walnuts, Flaxseed, Soybean
• Canola Oil
• Fatty fish

Omega-6
• Corn, Safflower, soybean, sunflower oils
• meat, poultry, and eggs

46
Q

What is the effect of Omega-3 fatty acids on lipid profile?

A
  • Reduced Plasma Triglycerides
  • Little to NO effect on HDL or LDL cholesterol *

*May also have antiplatelet, hypotensive, and hypolidemic effects

47
Q

Omega-3
• MOA

A

Increased Fatty acid oxidation via PPARa

PPARa
• Decreased ApoCIII synthesis
• Increased Apo AI and AII synthesis
• Increased LPL synthesis

48
Q

T or F: statins have a large effect on triglycerides

A

False

49
Q

What drugs have a significant effect on triglycerides?

A
  • Niacin
  • Fish Oils
  • Fibrinates
50
Q

If someone is under 75 and has known atherosclerotic CV disease what should you prescribe them?

• what is older than 75

A
  • Under 75 - HIGH intensity statins (if no safety concerns)
  • Over 75 or have safety concerns - Moderate intensity statin
51
Q

What is the protocol for treatment of someone with LDL-C level is greater than 190 mg/dl?

A
  • If over 21 = HIGH intensity statin
  • Consider adding an additional drug to lower cholesterol
52
Q

What treatment should you give someone with diabetes and no vascular disease age 40-75 with LDL 70-189 mg/dl?

A

• High intensity statin if at High (>7.5%) 10 yr risk of CV disease
• Moderate intensity statin if at Lower risk of CV disease

53
Q

What treatment should you give someone without diabetes or CV disease if they are 40-75 and have LDL 70-189?

A
  • Moderate or High Intensity statin for patients with (>7.5%) 10 yr risk of CV disease
  • Moderate intensity statin for patients with (5%-7.4% risk)
54
Q
A

Cardio - Elam (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions