DLD moa

Question 1

Statins/HMG CoA reductase inhibitors

moa

Answer 1

inhibit HMG CoA reductase which dec synthesis of cholesterol in the liver; inhibits rate limiting step (HMG CoA→ mevalonate)
Hepatic cholesterol is dec so LDL receptors are upregulated causing inc clearance of LDL from the blood

Question 2

myositis

Answer 2

inflammation of muscle

Question 3

statins pregnancy

Answer 3

x

Question 4

antilipid effects of statins

Answer 4

Mostly dec LDL

Also inc HDL and dec TG

Question 5

statins dose response?

Answer 5

NONLINEAR DOSE RESPONSE- doubling each dose only dec LDL by 6%; more meds not always = better

Question 6

which statins have a shorter half life

Answer 6

Simvastatin, Pravastatin, lovastatin, fluvastatin

take at night

Question 7

which statin uses CYP3A4?

Answer 7

simvastatin and lovastatin

Question 8

which statin uses no cyp?

Answer 8

pravastatin

Question 9

Over 1 quart of grapefruit juice a day is a problem with theses statins

Answer 9

atorvastatin, lovastatin, and simvastatin

Question 10

moa fibrates

Answer 10

Stimulates PPAR alpha in the liver which leads to inc TG removal
PPAR alpha is a transcription factor that upregulates LDL which breaks down FFA

Question 11

fibrates antilipid effects

Answer 11

Mostly TG dec

HDL inc and LDL dec

Question 12

moa zetia

Answer 12

MOA: binds to NPC1L1 (Niemann Pick C1 like 1) in brush border of jejunum which inhibits cholesterol absorption and enhances LDL clearance

Question 13

normally NPc1L1 does this

Answer 13

absorbes cholesterol in jejunum

Question 14

zetia antilipid effects

Answer 14

Mainly dec LDL

Also inc HDL and dec TG

Question 15

statins se

Answer 15

SE= liver effects, myopathy (myalgia, myositis, rhabdomyolysis), elevated glucose and A1C

Question 16

statins caution

Answer 16

Caution: inc blood glucose/A1C, caution with fibrates bc they have inc risk for myopathy too

Question 17

fibrates SE

Answer 17

SE: cholelithiasis, myopathy (inc risk when combined with statin)

Question 18

fibrates caution

Answer 18

Caution: risk of myopathy and rhabdo inc with statins

Question 19

zetia SE

Answer 19

SE: diarrhea, fatigue, nausea (overall very positive)

Question 20

Niacin/Nicotinic acid

moa

Answer 20

inhibits lipase from binding to adipose tissue

Reduction in TG synthesis dec LDL
Raises HDL as well

Question 21

Niacin/Nicotinic acid

effects on lipid profile

Answer 21

Affects all lipoproteins
DOSE INDEPENDENT
Best with at least 1.5 g daily
LINEAR dose response relationship for dec LDL

Question 22

Niacin/Nicotinic acid

se

Answer 22

SE: cutaneous flushing (take at bedtime, take ASA ½ hr before)

Question 23

moa omega 3 FA

Answer 23

inhibiting diglyceride acyltransferase which is involved in the biosynthesis of TG in the liver… so no TG are made

Question 24

Omega 3 fatty acids

lipid effects

Answer 24

Dec TG and inc LDL
Only omega 3 acid ethyl esters inc LDL bc it has DHA
Also inc HDL

Question 25

Omega 3 fatty acids | se

Answer 25

SE: burping, indigestion, fishy aftertaste

Question 26

Omega 3 fatty acids | caution

Answer 26

Caution: may inc LDL (can switch to Ethyl eicosapentaenoic acid)

Question 27

Bile acid sequestrants (BAS) | moa

Answer 27

MOA: bind bile acids in the SI; bind bile acid salts and prevent enterohepatic reutilization of bile salts. They also repair dietary cholesterol. Lower LDL

Question 28

Bile acid sequestrants (BAS) | antilipid effects

Answer 28

Dec LDL | Inc HDL

Question 29

Bile acid sequestrants (BAS) | se

Answer 29

none bc its not absorbed in the circulation; may have some GI complaints Safest drug to treat hypercholesterolemia

Question 30

Bile acid sequestrants (BAS) | drug interactions

Answer 30

Drug interactions: inhibit GI absorption of other drugs so take other drugs 1-2 hours before or 4-6 hrs after

Question 31

Safest drug to treat hypercholesterolemia

Answer 31

bas

Question 32

PCSK9 inhibitors | moa

Answer 32

Monoclonal Ab that binds to PCSK9 PCSK9 is a serine protease that binds to LDL receptors and destroys them. This causes dec LDL receptors and dec LDL clearance and inc plasma LDL levels PCSK9 inhibitors dec LDL receptors and improve LDL clearance

Question 33

PCSK9 inhibitors | lipid lowering effects

Answer 33

Dec LDL Dec risk of heart attack Dec risk of stroke Add a statin to get optimal effects

Question 34

Nexletol prodrug

Answer 34

Bempedoic acid

Question 35

Nexletol moa

Answer 35

MOA: inhibits ATP citrate lyase which is involved in livers biosynthesis of cholesterol upstream of HMG CoA reductase

Question 36

Nexletol se

Answer 36

SE: hyperuricemia, muscle pain with simvastatin and pravastatin (he found muscle pain interesting)