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Cardio 1 > Pharm - Cholesterol > Flashcards

Pharm - Cholesterol Flashcards

1
Q

Drugs that are primarily used to lower cholesterol

A 
Statins
Ezetimibe 
Resins
PCSK9 inhibitors
ApoB antisense
MTP inhibitor
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2
Q

Drugs that are primarily used to lower triglycerides

A

Fibrates

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3
Q

Drugs that are primarily used to lower both cholesterol and triglycerides

A

Niacin

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4
Q

Drugs to lower LDL cholesterol:
Statins
MOA

A
  • Inhibit biosynthesis
  • Induce LDL receptors to increase removal of LDL
  • binds to HMG CoA reductase
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5
Q

1st line drugs for both primary and secondary prevention of ASCVD

A

Statins

-monotherapy or combined with resins or ezetimibe

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6
Q

What is the most potent statin?

A

Rosuvastatin

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7
Q

Adverse effects of statins

A 
Mild GI disturbances
Reversible memory loss
Headache
Rash
Diabetes
***Myopathy (common)
Rhabdomyolysis (rare)
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8
Q

Contraindications for statins

A

Pregnant and lactating women

Serious illness, trauma, major surgery, or liver disease

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9
Q

Drug-drug interactions of statins

A

Any drug that affects
CYP3A4 (lovastatin, simvastatin, atorvastatin) or
CYP2C9 (fluvastatin, rosuvastatin)

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10
Q

Ezetimibe

MOA

A
  • Inhibits intestinal sterol absorption (NPC1L1)

- inhibits expression of hepatic LDL receptors

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11
Q

For patients who can’t tolerate statins

For primary and secondary preventions of ASCVD

A

Ezetimibe

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12
Q

Resins

MOA

A

Increase bile acid excretion
induce up regulation of LDL receptors

*not absorbed orally

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13
Q

Resins:

Examples

A

Colestipol
Cholestyramine
Colesevelam

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14
Q

Primary and secondary prevention of ASCVD
antitoxic agents for cardiac glycosides
Bile malabsorption caused diarrhea

A

Resins

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15
Q

___ can be used to treat hyperlipidemia in pregnant women

A

Resins

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16
Q

Side effects of resins

A

Relatively safe
Constipation and bloating
Increase VLDL

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17
Q

Side effects of ezetimibe

A

Few

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18
Q

Contraindications for resins

A

Diverticulitis

Elevated VLDL

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19
Q

Drug-drug interactions for resins

A

Absorption of some oral drugs may be reduced

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20
Q

PCSK9 inhibitors

Examples

A

“Proprotein convertase subtilisin hexin 9”

  • alirocumab
  • evilocumab
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21
Q

Used as an adjunct to diet and maximally tolerated statin in patients with HeFH when require additional lowering of LDL cholesterol

A

PCSK9 inhibitors

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22
Q

Side effects of PCSK9 inhibitors

A

Injection site reaction

Myalgia

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23
Q

Standard treatment for HoFH (homozygous familial hypercholesterolemia)

A
  • low fat diet, high dose statin
  • ezetimibe
  • bile acid sequestrants
  • niacin
  • LDL apheresis
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24
Q

2 orphan drugs for HoFH

A

Mipomerson

Lomitapide

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25
Q

Adverse effects of Mipomerson and Lomitapide

A
  • both: Liver toxicity (transaminase elevations and hepatic steatosis)
  • lomitapide: GI side effects
  • mipomerson: injection site rxns
26
Q

MOA

  1. Mipomerson
  2. Lomitapide
A
  1. Binds to apoB to decrease expression
  2. Binds to MTP to inhibit it
    * both inhibit synthesis
27
Q

Drug-drug interactions for lomitapide

A

CYP3A4 inhibitors

P-glycoprotein substrates

28
Q

Major contraindications for lomitapide and mipomerson

A

Hepatic diseases

*lomitapide: pregnant and lactating women

29
Q

Fibrates

MOA

A

Bind to PPAR alpha

  • increase LDL expression, increases lipolysis of triglycerides, lowers VLDL
  • oxidizes FFA, lowers VLDL synthesis
  • increases apoA1 expression, increases HDL
30
Q

Fibrates examples

A

Gemfibrozil

Fenofibrate

31
Q

Drug of choice for hypertriglyceridemia

A

Fibrates

32
Q

Adverse effects of fibrates

A

Rare
Rashes
GI effects
*risk of myopathy and rhabdomyolysis increases when used with statins

33
Q

Contraindications for fibrates

A

Hepatic dysfunction

Renal dysfunction

34
Q

Drug-drug interactions for fibrates

A
  • gemfibrozil: myopathy with statins
  • fenofibrate: nephrotoxic drugs
  • both can potentiate the anticoagulation effects of warfarin and the antihyperglyceremic effects of pioglitazone
35
Q

Drugs used to lower LDL and VLDL
Nicotinic acid
MOA

A
  • niacin, vitamin B3
  • reduces Lp(a)
  • increases HDL and tPA
36
Q

Uses of nicotinic acids

A

Hypercholesterolemia by combining with resins and statins

Hypertriglyceridemia

37
Q

Adverse effects of nicotinic acids

A

Flush (PGE2 and PGD2) and dyspepsia

-high dose=GI distress, liver dysfunction, insulin resistance, hypotension, hyperuricemia

38
Q

Contraindications of nicotinic acids

A

Hepatic dysfunction and active peptic ulcer

39
Q

True or false: if one statin is not working well enough we should add another statin

A

False

Never!

40
Q

Which statins are prodrugs?

A

Lovastatin

Simvastatin

41
Q

Statins are analogues of ___and inhibit ___

A

HMG-CoA
HMG-CoA Reductase
*rate limiting step of synthesis

42
Q

Medications that inhibit CYP3A4 or CYP2C9 can ____ statins concentrations, while medications that induce them ____ statins concentrations

A

Increase

Decrease

43
Q

____ is the first drug that inhibits intestinal absorption of cholesterol.
It is absorbed and conjugated in the intestine to an active glucuronide

A

Ezetimibe

44
Q

Ezetimibe’s duration of action is ___

A

Long

22 hour half life

45
Q

____ binds to NPC1L1 on GI epithelial cells to reduce absorption. What else does this drug do?

A

Ezetimibe

Increases expression of hepatic LDL receptors thus promoting uptake

46
Q

Examples of resins:

A

Colestipol
Cholestyramine
Colesevelam

47
Q

Resins enhance the conversion of cholesterol to ____

They also do what?

A

Bile acids in the liver by 7 alpha hydroxylation and increasing excretion from feces
*also induce up regulation of LDL receptors

48
Q

___ can be used for pregnant women with hyperlipidemia

What else can they be used for?

A

Resins

Digitalis toxicity

49
Q

PCSK9 inhibitors are human monoclonal antibodies that prevent PCSK9 from binding to ___

A

LDL receptors and degradation of LDL receptors thus increasing hepatic uptake and metabolism of LDL-C

50
Q

___ are given subcutaneously once every two weeks or every month

A

PCSK9 inhibitors

51
Q

Apo B-100 synthesis inhibitors are used to treat ___

A

Homozygous familial hypercholesterolemia

52
Q

___ binds to and cleaves apoB mRNA in the nucleus of hepatocytes, which inhibits apoB protein leading to reduced production of VLDL and LDL

A

Mipomersen

53
Q

Administration route of mipomersen

A

Subcutaneous injections once a week

54
Q

Administration route of Lomitapide

Metabolism

A

Orally once a day

CYP3A4

55
Q

True or false:

Mipomersen has no interactions with simvastatin from, ezetimibe, or warfarin

A

True

56
Q

Fibrates decrease VLDL by ___

A
  1. Increase LPL expression
  2. Reducing synthesis of VLDL
  3. Increasing HDL
57
Q

True or false: fibrates do not pass the placenta

A

False. They easily pass it

58
Q

___ is the most effect be agent for increasing HDL and is the only agent for reducing Lp(a)

A

Niacin

59
Q

These drugs lower LDL

A 
Statins 
Resins
Ezetimibe
PCSK9 inhibitors 
ApoB antisense
MTP inhibitor 
Nicotinic acid
60
Q

These drugs lower VLDL

A

Fibrates
Omega 3 PUFAs
Nicotinic acid

61
Q

___ acts as a PPAR alpha agonist to lower trigs

A

Gemfibrozil

Cardio 1 (14 decks)

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