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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
Drugs used in homozygous familial hypercholesterolemia
Juxtapid (Lomitapide) Mipomersen (Kynamro) Evinakumab (evkeeza)di
26
difference between the drugs used to treat homozygous hypercholesterolemia
Juxtapid and mipomersen inhibit APO B Evinakumab inhibit angiopoietin like protein 3
27
Juxtapid MOA
(SiRNA) inhibitor of MTTP that inhibits the assembly of APO B containing lipoproteins in liver and intestine
28
What does APO B do? What does its inhibition do?
APO B in liver makes VLDLs In intestine makes chylomicrons APO B interferes with VLDL and chylomicrons
29
adverse effect of juxtapid
High risk for liver damage
30
Mipomersen MOA. Which AOB is it more selective for?
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
Adverse reaction of Mipomersen
Liver damage
32
adverse rxn of both mipomersen and juxtapid
liver damage
33
Evinacumab (Evkeeza) MOA
Monoclonal antibody against protein called Angiopoitein like protein 3 (ANGPTL 3)
34
What is ANGPL3
Plays regulatory role on activity of lipases called lipoprotein lipase (LPL) and endothelial lipase (EL)
35
What do ANGPTL3 inhibitors do?
By binding with ANGPTL3 with antibody, we interfere with its ability to inhibit the activity of LPL and EL, lowering LDL
36
Name drugs that lower triglycerides
Fibric acid derivatives Niacin Omega 3 fatty acids
37
Fibric acid derivative drugs
GEmfibrizol Fenofibrate
38
Which fibric axcid drug is a prodrug
Fenofibrate
39
Target of fibric acid derivative drugs
bind to PPAR alpha to reduce triglyceride levels
40
indication of fibric acid drugs
Hypertriglyceridemia
41
Adverse effects of fibric acid derivatives
rhabdomylosis if used with statin
42
drug interactions of fibric acid derivateves
Warfarin efffects potentiated. q
43
Use of Niacin? what is it also known as?
Used to lower triglyceride Vit B3 At dietary levels- no effect on lipid, 1-3 grams a day lowers lipids
44
MOA of niacin
Niacin blocks the mobilization of FFA from adipose tissue, Less fatty acid taken to liver leading to less triglyceride synthesis.
45
How does niacin affect LPL, VLDL, LDL, TG and HDL levels
increase LPL, increase VLDL clearence reduce, VLDL reduce LDL and TG increase HDL
46
2 main tissues targeted by niacin
Hepatocytes (liver) and adipose tissue
47
What does Niacin do in adipose tissue
inhibits TG lipolysis by hormone sensitive lipase (HSL), decreasing FA transport to liver.
48
what does Niacin do in liver
Niacin inhibits fatty acid synthesis and esterification, reducing TG export via VLDL
49
Indication of Niacin
Pts with high levels of TG Raise HDL levels
50
adverse effects of niacin
Vasodilation leading to itching, flushing, headache, tingling some hepatotoxicity
51
Name 2 omega 3 fatty acid compounds
Eicosapentanoic acid (EPA) Docosahexaenoic acid (DHA)
52
difference between EPA vs DHA omega 3 fatty acids structurally
EPA- 5 double bonds DHA- 6 double bonds
53
MOA of omega 3 fatty acids
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
indication of o-3 fatty acid
severe hypertriglyceridemia (>500)
55
adverse effects of omega 3 fatty acid
combo products can increase LDL, not vascepa (EPA only)
56
omega 3 fatty acid + ethyl ester drug name
Omtryg
57
Dyslipidemia sx
Mostly asymptomatic if severe- chest pain, palpitation, sweating
58
what symptom do we see hen triglycerides are over 400-500
pancreatitis
59
Fasting lipid panel we look at
Total cholesterol LDL TG HDL
60
Which equation estimates LDL from FLP
TC-HDL-TG/5 if asked for non-hdl, just dont include HDL in calculation
61
Lifestyle modification for dyslipidemia
DASH diet lower percentage of calories from transfats and saturated fats lower sodium intake 90-150 mins of exercise a week smoking cessation
62
do omega 3 fatty acids reduce LDL?
yes
63

Therapeutics P2 (41 decks)

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