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Pharmacology 3805 > Lipid Lowering Drugs > Flashcards

Lipid Lowering Drugs Flashcards

1
Q

Density: What lipoprotein sinks?

A

HDL, it is protein-rich

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2
Q

Density: What lipoprotein floats?

A

Chylomicrons and VLDL. Fat floats and these are triglyceride rich

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3
Q

Density: What lipoprotein floats?

A

Chylomicrons and VLDL. Fat floats and these are triglyceride-rich

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4
Q

Liver _____ drives reverse cholesterol transport in macrophages

A

SR-BI

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5
Q

Who discovered Mevastatin?

A

Dr.Akira Endo

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6
Q

Who discovered Lovastatin?

A

Dr. P.Roy Vagelos

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7
Q

Who created simvastatin?

A

Dr.P.Roy Vagelos

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8
Q

What is the MOA of statins?

A

-Overall: reduction of LDL
-Reduces HMG-CoA to mevalonate
-Affects blood cholesterol levels by inhibiting hepatic cholesterol synthesis, thus increasing expression of LDL receptor gene
-Reducing hepatic production of VLDL/LDL the precursors of LDL

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9
Q

What is the half-life of statins?

A

1-4 hours

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10
Q

When is most hepatic cholesterol synthesis done?

A

Between midnight to 2 am

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11
Q

When should you take a statin medication?

A

In the evening

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12
Q

What is the half-life of atorvastatin and rosuvastatin?

A

Approx 20 hours

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13
Q

What is the half-life of simvastatin?

A

5 hours

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14
Q

When is the peak plasma concentration of statins exhibited?

A

1-4 hours

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15
Q

What percentage of statins are eliminated in the feces?

A

> 70%

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16
Q

Therapeutic Effects of statins: When do they exhibit the maximal effect on plasma cholesterol? (answer is in days)

A

7-10 days

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17
Q

Are statins effective for hoFH patients?

A

NO

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18
Q

What are the adverse effects of statins?

A

Hepatotoxicity and Myopathy (muscle weakness)

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19
Q

What is the MOA of bile acid sequestrants?

A

-Depletion of bile acid, decreases re-absorption )via enterohepatic circulation)
-Increases hepatic synthesis of bile acids
-Increases LDL receptor number, decreases plasma LDL-C

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20
Q

Do bile acid sequestrants work the same no matter the dosage?

A

No, they are dose dependant

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21
Q

What formulations can you have for bile acid sequestrants?

A

-Powder mixed with juice/water
-tablets
-capsules

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22
Q

Adverse reactions to bile acid sequestrants:

A

-bloating, dyspepsia, constipation
-Reduction of plasma levels of lipid-soluble vitamins (A,E,D,K)

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23
Q

What is the MOA for Niacin in adipose tissue and in hepatic tissue?

A

In adipose tissue: inhibits the lipolysis of TG by inhibiting hormone-sensitive lipase (HSL) and decreasing free fatty acids
In hepatic tissue: it decreases esterification of TG, increasing ApoB-100 degradation, decreasing VLDL
It also enhances LPL activity by increasing clearance of both chylomicrons and VLDL

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24
Q

What effect does Niacin have on lipoprotein levels?

A
  • 2-6g/day reduces TG by about 35-50%, with maximal effect in 4-7 days
  • 4.5-6g/day reduces LDL-C level by about 25%, with maximal effect in 3-6 weeks
    -Increases HDL-C by about 30-40%
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25
Q

When is the peak plasma concentration of niacin seen?

A

30-60 mins

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26
Q

What is the half-life of niacin?

A

60 mins

27
Q

What is the therapeutic use of niacin?

A

It is indicated for hypertriglyceridemia and elevated LDL-C

28
Q

What forms of niacin are there?

A

-regular tablets
-ER tablets

29
Q

What are the adverse effects of niacin?

A

-Flushing
-Dyspepsia
-Hepatotoxicity: increased AST, ALT
-Hyperglycemia
-Reactive gout: increase uric acid

30
Q

What is the MOA of fibrate derivatives?

A

-Interaction with PPAR alpha affecting gene expression
-Increases lipo-protein lipase which breaks down free fatty acids, decreasing TG-rich VLDL in blood
-Increases HDL concentration by increasing Apo-A-I and A-II synthesis

31
Q

Should fibrates be taken with or without food?

A

With

32
Q

When is the peak plasma concentration of fibrates?

A

1-4 hours

33
Q

What is the half-life of gemfibrozil and fenofibrate?

A

Gemfibrozil- 1.1 hours
Fenofibrate- 20 hours

34
Q

Where are fibrates concentrated to in the body?

A

Liver, kidney, intestine

35
Q

What is the dosing of gemfibrozil?

A

600mg BID, 30 mins before meals

36
Q

Fibrates are the drug of choice for treating hyperlipidemia individuals with type __ hyperlipoproteinemia

A

3

37
Q

What adverse effects do fibrates have?

A

GI upset, rash, urticaria, hair loss, muscle pain, fatigue, headache

38
Q

What drugs do fibrates interact with?

A

Statins

39
Q

What is an example of a cholesterol absorption inhibitor?

A

Ezetimibe

40
Q

What is the MOA of cholesterol absorption inhibitors

A

Inhibit NPC1L1 protein on the GI tract epithelial cells as well as hepatocytes.
This blocks formation of clathrin AP2 cargo complex involved in trafficking cholesterol
Lowering circulating cholesterol to the liver
Increases LDL-R to remove circulating LDL

41
Q

Are cholesterol absorption inhibitors first, second, or third line agents to lower LDL?

A

Second line together with statins

42
Q

What does PCSK9 protease do?

A

PCSK9 binds to LDL receptor on the surface of the hepatocytes and enhances lysosomal degradation of the LDL receptor,

43
Q

Do PCSK9 inhibitors decrease LDL, HDL, VLDL, or chylomicrons?

A

LDL

44
Q

Who can use PCSK9 inhibitors?

A

They can be used alongside diet and maximum statin therapy in adult patients with hoFH and heFH or established ASCVD requiring additional LDL lowering

45
Q

What is a drawback to PCSK9 inhibitors?

A

They are very expensive

46
Q

What are the two PCSK9 inhibitors?

A

Evolocumab and Alirocumab

47
Q

What is the dosing of Evolocumab?

A

140mg Injection biweekly or 420mg once monthly

48
Q

What is the half life of Evolocumab?

A

11-20 days

49
Q

What is the Evolocumab and Alirocumab dosing for a patient with hoFH?

A

Evolocumab: 420mg monthly or biweekly
Alirocumab: (75mg or 150mg) once every 2 weeks

50
Q

Adverse effects of PCSK9 inhibitors:

A

Risk of infections such as nasopharyngitis, UTI, or upper respiratory infection is increased

51
Q

Inclisiran is a ____

A

New PCSK9 inhibitor

52
Q

How many doses a year are required for Inclisiran?

A

2

53
Q

What is the MOA of Omega-3 fatty acids?

A

Reduces the production of TG in the liver and enhances clearance of TG from circulating VLDL

54
Q

Whats the half-life of Omega-3 fatty acids?

A

50-80 hours

55
Q

Adverse effects of Omega-3 fatty acids:

A

arthralgia
nausea
fishy burps
dyspepsia
increased LDL
prolonged bleeding time

56
Q

What is the MOA of inhibitors of MTP (microsomal triglyceride transfer protein)

A

Inhibit TG rich lipoprotein
Decrease TG and chlymicrons

57
Q

Should inhibitors of MTP be administered with food?

A

No, but they should be administered with water

58
Q

What are inhibitors of MTP metabolized by?

A

CYP 450 enzymes

59
Q

What are the adverse effects of MTP inhibitors?

A

Diarrhea
Vomiting
Abdominal pain
Hepatotoxicity and liver steatosis

60
Q

What is the MOA of ApoB-100 synthesis inhibitors?

A

They bind to the mRNA of apo B-100 which breaks down the mRNA and reduces expression of the ApoB-100 protein
Therefore, decreasing VLDL

61
Q

What is the recommended dose of ApoB-100 synthesis inhibitors?

A

1mL of 100mg/ml solution, injected subcut. once weekly

62
Q

What is the half-life of ApoB-100 synthesis inhibitors?

A

1 to 2 months

63
Q

What are adverse effects of ApoB-100 synthesis inhibitors?

A

Injection site reactions, including erythema, pain, itching and hematoma
Flue like symptoms such as fatigue and headache

64
Q

What is the MOA of LDL apheresis?

A

Pumps patient blood into. a column using affinity chromatography with an antibody to recognize ApoB-100, LDL is decreased, and blood returned to patient’s body

Pharmacology 3805 (5 decks)

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