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PHRM 844: Therapeutics II > Lipid Junk > Flashcards

Lipid Junk Flashcards

1
Q

Which class of Lipoprotein has the most Triglycerides?

A

Chylomicins; VLDL is a close second

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2
Q

What class of Lipoproteins has the highest amount of Cholesterol?

A

LDL

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3
Q

Which class of Lipoproteins has the highest amounts of Proteins?

A

HDL

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4
Q

What enzyme helps breakdown chylomicins and VLDL within the capillaries?

A

Lipoprotein Lipase

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5
Q

What is the Apoprotein found on HDL?

A

Apo-A

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6
Q

Where are Apo-B found?

A

Apo-B 100: VLDL, LDL, IDL; Apo-B 48: Chylomicins

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7
Q

What are the ranges of Total Cholesterol?

A

Desirable: <200; Elevated: 200-249; High: >250

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8
Q

What are the ranges for LDL?

A

Desirable: <130; Elevated: 130-159; High: >160

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9
Q

What are the ranges for HDL?

A

[All are good] Desirable: Men - <40 & Female - <50 High: <60

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10
Q

What are the ranges for TGs?

A

Desirable: <150; Elevated: 150-199; High: >200

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11
Q

What medications are the Statins?

A

Lovastatin, Atrovastatin, Fluvastatin, Rosuvastatin, Simvastatin, Pravastatin, Pitavastatin

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12
Q

What is the MOA for the Statins?

A

HMG-COA Reductase Inhibitors; Basically they completely inhibit the HMG-COA enzyme which causes the DECREASE in cholesterol synthesis. This DECREASE will either; INCREASE the expression of LDL-R, causing an INCREASE of the re-uptake of LDL from the blood OR it will DECREASE the release of VLDL = DECREASING LDL. [Both will decrease LDL levels].

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13
Q

Which Statins are Prodrugs?

A

Lovastatin and Simvastatin

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14
Q

CYP interactions with Statins?

A

3A4: Simvastatin, Lovastatin, Atorvastatin
- Avoid: Grapefruit, Ketoconazole
2C9: Rosuvastatin, Fluvastatin
- Avoid: Metronidazole, cimetidine, amioridone
N/A: Pravastatin, Pitvastatin

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15
Q

Time sensitivities with Statins?

A

Short Half-Life: Lovastatin, Simvastatin, Fluvastatin
- Taken at night or Bedtime
Slow Release: Atorvastatin, Pravastatin, Rosuvastatin
-Taken at any time

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16
Q

How does food affect absorption within Statins?

A

Lovastatin, Simvastatin: Take with food to INCREASE absorption
Pravastatin, Pitavastatin: Take with food will DECREASE absorption

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17
Q

Which Statins are Lipophilic and which are Hydrophilic?

A

Hydrophilic: Rosuvastatin, Pravastatin
Lipophilic: Simvastatin, Atorvastatin, Lovastatin, Fluvastatin, Pitavastatin

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18
Q

What are the adverse effects of Statins? Contraindications?

A

Possibly Muscle weakness or Fatigue
- Rhadomylysis: the breakdown of muscle
Hepatotoxicities
- Low incidence, would have to check LTF, Dark-brown Urine.
*CONTRAINDICATED: pregnancy, acute liver disease

19
Q

What are the High Intensity Statins?

A

Atorvastatin 40mg & 80mg
Rosuvastatin 20mg & 40mg

20
Q

What is the MOA of Bempedoic Acid?

A

ASCVL-1 Inhibitor: [Same as Statins] Basically going to inhibit ASCVL-1, the first step in cholesterol biosynthesis, causing a DECREASE in cholesterol - affecting LDL-R and LDL levels = DECREASING LDL [NO affect on TGs] NO INCREASE in HDL

21
Q

What is the enzyme that actives Bempedoic Acid into Bempedoyl-CoA?

A

SLC272a

22
Q

Does this MOA work within the Muscle?

A

No, there are no ASCVL-1 found within the muscle. That is way there is no muscle issues compared to the Statins.

23
Q

What other enzyme does Bempedoic Acid affect?

A

OAT2: inhibiting this will cause in INCREASE in Uric Acid = Gout.

24
Q

What Medications should you avoid when taking bempidoic acid?

A

Simvastatin, Pravastatin

25
Q

What are the adverse affects of Bempedoic Acid?

A

Gout, Tendon Rupture, UTI.

26
Q

What is the MOA for Ezetimibe?

A

Cholesterol Absorption Inhibitor: Binds to the surface of the receptor, blocking any absorption of cholesterol back into the endothelial. This will allow it to be excreted within the bile.

27
Q

What are the adverse effects of Ezetimibe? Contraindications?

A

Generally well tolerated BUT can cause GI upset, diarrhea, fatigue
*CONTRAINDICATIONS: pregnancy and breastfeeding when combined with a statin.

28
Q

What is the MOA for the Bile Acid Recombinants?

A

They just create an insoluble fatty, greasy hydrophobic molecule that will end up being pulled into the feces, removing bile acid. This will then cause the liver to resynthesizes bile acid from the cholesterol = DECREASING LDL

29
Q

What are the adverse effects of Bile Acids Recombinants?

A

Bloating, Cramping, increase in TGs

30
Q

Drug Interactions for Bile Acid Recombinants?

A

Acetaminophen, TZDs, Contraceptives, Corticosteroids, Ezetimibe, Fibrates, Thiazides, Warfarin, Digoxin.

31
Q

What is the MOA for the fibrates?

A

They bind PPARa which will activate PPRE causing an increased expression of Lipoproteins and Apo-A1 & A2. This will cause a HUGE DECREASE in TGs, a slight decrease in LDL and an increase in HDL.

32
Q

Which of the following is a prodrug? Gemfibrozil or Fenofibrate?

A

Fenofibrate

33
Q

Side effects of Fibrates?

A

Gallstones, GI Upset, muscle problems (especially when used with statins)

34
Q

What is the MOA for Omega-3?

A

It inhibits the synthesis of triglycerides in the liver by inhibiting DGAT, which is the final step. Decreasing TGs will decrease VLDL = decrease LDL

35
Q

What are the adverse effects for omega-3?

A

Taken alone will INCREASE LDL while taken with statins will DECREASE LDL

36
Q

What are the two most common Omega-3 Fatty Acid OTC products?

A

Lovaza or Vascepa

37
Q

What is the MOA for Niacin?

A

Niacin will use HSL, causing the conversion of TGs to FFA to not having. This will cause an DECREASE in LDL and an INCREASE of HDL. It will also stop FFA from going into the liver, causing a DECREASE in VLDL & LDL.

38
Q

What are the adverse effects of Niacin?

A

Itching, Flushing, Headache, Tingling [All are prostaglandin problems]
- Can be counteracted with NSAIDS

39
Q

What is the MOA of PCSK9 Inhibitors?

A

They will bind to the PSCK9 causing it to not bind to the LDL-R [this will decrease LDL-R] allowing an INCREASE in LDL-R = HUGE DECREASE in LDL

40
Q

What kind of medication is PCSK9 Inhibitors?

A

Monoclonal antibodies: Alirocumab & Evolocumab

41
Q

What are the adverse effects of PCSK9 Inhibitors?

A

GI upset, increase LFTs. Injection site reactions, Flu?

42
Q

What to do when the patient has LDL >190 mg/dl

A

Give them a High Intensity Statin

43
Q

What to do when the patient has DM and is between the Age of 40-75 years old?

A

Give them a Moderate Intensity Statin

44
Q

What to do when the patient does not have DM, had an LDL between 70-190 mg/dl & is between 40 -75 years old?

A

Have to look at there ASCVD Risk:
- >20% Risk: can give Low, Moderate, or High Statin
- 7.5 - 20% Risk: can give Moderate Statin
- <5% Risk: do lifestyle changes

PHRM 844: Therapeutics II (11 decks)

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