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Therapeutics P2 > Exam 2 lecture 2 > Flashcards

Exam 2 lecture 2 Flashcards

1
Q

HMG-COA reductase inhibitors also called

A

statins

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2
Q

What is mevalonic acid? used for?

A

The product of HMG-COA reductase. Important building block in synthesis of cholesterol in liver.

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3
Q

What are two prodrug statins? how are they activated

A

lovastatin and simvastatin.
Activated by bile acid

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4
Q

Which statins are not major substrates for CYP 450

A

Pravastatin and pitavastatin

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5
Q

How do statins work

A

bind to HMG coa reductase and inhibit it. Preventing conversion of HMG COA reductase to mevalonic acid. decreasing cholesterol in liver.

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6
Q

What happens when statins reduce cholesterol levels in liver

A

ldl receptors are increased on liver, Allowing it to take up more LDL cholesterol from Plasma.

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7
Q

Recognize chemical structures of statins

A

check brightspace

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8
Q

Direct vs indirect use of statin

A

direct- inhibit enzymatic activity of HMG-COA reductase
indirect- upregulation of LDL receptors and increased hepatic uptake of LDL

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9
Q

When are statins used? 2 uses

A

Hypercholesterolemia and immediately after MI

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10
Q

how do statins change LDL, HDL and TG

A

20-60% lowering of LDL
10-33% lowering of TG
5-10% increase in HDL

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11
Q

Which statins are substartes for CYP3A4

A

Simvastatin
Atorvastatin
Lovastatin,

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12
Q

Which drugs are substrates for CYP2C9

A

Fluvastatin
Rosuvastatin

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13
Q

How are pravastatin and Pitavastatin excreted

A

Pravastatin- excreted unchanged and undergoes sulfation
Pitavastatin- Excreted in bile unchanged, undergoes hepatic circulation

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14
Q

Adverse effects of HMG COA reductases

A

SKELETAL MUSCLE
1. Rhabdomylosis (myopathy) with renal dysfuction

  1. Hepatotoxicity

may increase incidence of T2 diabetes

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15
Q

What are two drugs that can be used in conjunction with statins

A

ATP citrate Lyase inhibitor (ACL)
PCSK9 inhibitors

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16
Q

Name a ACL drug

A

Bempedoic acid (nexletol)

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17
Q

What is ATP citrate lyase? Use of its inhibitor?

A

-an enzyme upstream of HMG COA in cholesterol synthesis pathway.
-used adjunct to statins to lower LDL levels

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18
Q

Who can use ACL

A

patients with HeFH and ASCVD

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19
Q

side effects of ACL? Route? Excretion?

A

May cause gout
orally taken
Excreted in kidney

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20
Q

PCSK9 inhibitor use

A

a protease that promotes LDL receptor in liver

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21
Q

Name PCSK9 drugs

A

Alirocumab(pralvent)
Evolocumab (Repatha)

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22
Q

dosing of alirocumab and evolocumab

A

Alirocumab- inject SQ every 2 weeks 75 or 150mg
Evolocuab- inj sq every 2 weeks 140 mg or once per month 420 mg

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23
Q

What are PCSK9 drugs used fro

A

Adjunct to statins in ASCVD and HeFH and ASCVD

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24
Q

adverse drug rxn of PCSK9 inhibitors

A

Arthralgia (inj site rxn)

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25
Q

Drugs used in homozygous familial hypercholesterolemia

A

Juxtapid (Lomitapide)
Mipomersen (Kynamro)
Evinakumab (evkeeza)di

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26
Q

difference between the drugs used to treat homozygous hypercholesterolemia

A

Juxtapid and mipomersen inhibit APO B

Evinakumab inhibit angiopoietin like protein 3

27
Q

Juxtapid MOA

A

(SiRNA) inhibitor of MTTP that inhibits the assembly of APO B containing lipoproteins in liver and intestine

28
Q

What does APO B do? What does its inhibition do?

A

APO B in liver makes VLDLs
In intestine makes chylomicrons

APO B interferes with VLDL and chylomicrons

29
Q

adverse effect of juxtapid

A

High risk for liver damage

30
Q

Mipomersen MOA. Which AOB is it more selective for?

A

instead of si RNA, it is an anti sense oligonucleotide inhibitor of APO B

more selective for APO B 100 (APO B made in liver). No effect in intestine

31
Q

Adverse reaction of Mipomersen

A

Liver damage

32
Q

adverse rxn of both mipomersen and juxtapid

A

liver damage

33
Q

Evinacumab (Evkeeza) MOA

A

Monoclonal antibody against protein called Angiopoitein like protein 3 (ANGPTL 3)

34
Q

What is ANGPL3

A

Plays regulatory role on activity of lipases called lipoprotein lipase (LPL) and endothelial lipase (EL)

35
Q

What do ANGPTL3 inhibitors do?

A

By binding with ANGPTL3 with antibody, we interfere with its ability to inhibit the activity of LPL and EL, lowering LDL

36
Q

Name drugs that lower triglycerides

A

Fibric acid derivatives
Niacin
Omega 3 fatty acids

37
Q

Fibric acid derivative drugs

A

GEmfibrizol
Fenofibrate

38
Q

Which fibric axcid drug is a prodrug

A

Fenofibrate

39
Q

Target of fibric acid derivative drugs

A

bind to PPAR alpha to reduce triglyceride levels

40
Q

indication of fibric acid drugs

A

Hypertriglyceridemia

41
Q

Adverse effects of fibric acid derivatives

A

rhabdomylosis if used with statin

42
Q

drug interactions of fibric acid derivateves

A

Warfarin efffects potentiated. q

43
Q

Use of Niacin? what is it also known as?

A

Used to lower triglyceride
Vit B3
At dietary levels- no effect on lipid, 1-3 grams a day lowers lipids

44
Q

MOA of niacin

A

Niacin blocks the mobilization of FFA from adipose tissue, Less fatty acid taken to liver leading to less triglyceride synthesis.

45
Q

How does niacin affect LPL, VLDL, LDL, TG and HDL levels

A

increase LPL, increase VLDL clearence
reduce, VLDL
reduce LDL and TG
increase HDL

46
Q

2 main tissues targeted by niacin

A

Hepatocytes (liver) and adipose tissue

47
Q

What does Niacin do in adipose tissue

A

inhibits TG lipolysis by hormone sensitive lipase (HSL), decreasing FA transport to liver.

48
Q

what does Niacin do in liver

A

Niacin inhibits fatty acid synthesis and esterification, reducing TG export via VLDL

49
Q

Indication of Niacin

A

Pts with high levels of TG
Raise HDL levels

50
Q

adverse effects of niacin

A

Vasodilation
leading to itching, flushing, headache, tingling

some hepatotoxicity

51
Q

Name 2 omega 3 fatty acid compounds

A

Eicosapentanoic acid (EPA)
Docosahexaenoic acid (DHA)

52
Q

difference between EPA vs DHA omega 3 fatty acids structurally

A

EPA- 5 double bonds
DHA- 6 double bonds

53
Q

MOA of omega 3 fatty acids

A

reduce synthesis of TG in liver. Omega 3 fatty acids are poor substrates for enzyme responsible for TG synthesis. They also inhibit esterification of other fatty acids

54
Q

indication of o-3 fatty acid

A

severe hypertriglyceridemia (>500)

55
Q

adverse effects of omega 3 fatty acid

A

combo products can increase LDL, not vascepa (EPA only)

56
Q

omega 3 fatty acid + ethyl ester drug name

A

Omtryg

57
Q

Dyslipidemia sx

A

Mostly asymptomatic
if severe- chest pain, palpitation, sweating

58
Q

what symptom do we see hen triglycerides are over 400-500

A

pancreatitis

59
Q

Fasting lipid panel we look at

A

Total cholesterol
LDL
TG
HDL

60
Q

Which equation estimates LDL from FLP

A

TC-HDL-TG/5

if asked for non-hdl, just dont include HDL in calculation

61
Q

Lifestyle modification for dyslipidemia

A

DASH diet
lower percentage of calories from transfats and saturated fats
lower sodium intake
90-150 mins of exercise a week
smoking cessation

62
Q

do omega 3 fatty acids reduce LDL?

A

yes

63
Q
A

Therapeutics P2 (41 decks)

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