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pharmacology > DLD moa > Flashcards

DLD moa Flashcards

1
Q

Statins/HMG CoA reductase inhibitors

moa

A

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

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2
Q

myositis

A

inflammation of muscle

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3
Q

statins pregnancy

A

x

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4
Q

antilipid effects of statins

A

Mostly dec LDL

Also inc HDL and dec TG

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5
Q

statins dose response?

A

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

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6
Q

which statins have a shorter half life

A

Simvastatin, Pravastatin, lovastatin, fluvastatin

take at night

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7
Q

which statin uses CYP3A4?

A

simvastatin and lovastatin

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8
Q

which statin uses no cyp?

A

pravastatin

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9
Q

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

A

atorvastatin, lovastatin, and simvastatin

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10
Q

moa fibrates

A

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

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11
Q

fibrates antilipid effects

A

Mostly TG dec

HDL inc and LDL dec

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12
Q

moa zetia

A

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

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13
Q

normally NPc1L1 does this

A

absorbes cholesterol in jejunum

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14
Q

zetia antilipid effects

A

Mainly dec LDL

Also inc HDL and dec TG

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15
Q

statins se

A

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

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16
Q

statins caution

A

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

17
Q

fibrates SE

A

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

18
Q

fibrates caution

A

Caution: risk of myopathy and rhabdo inc with statins

19
Q

zetia SE

A

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

20
Q

Niacin/Nicotinic acid

moa

A

inhibits lipase from binding to adipose tissue

Reduction in TG synthesis dec LDL
Raises HDL as well

21
Q

Niacin/Nicotinic acid

effects on lipid profile

A

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

22
Q

Niacin/Nicotinic acid

se

A

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

23
Q

moa omega 3 FA

A

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

24
Q

Omega 3 fatty acids

lipid effects

A

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

25
Q

Omega 3 fatty acids

se

A

SE: burping, indigestion, fishy aftertaste

26
Q

Omega 3 fatty acids

caution

A

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

27
Q

Bile acid sequestrants (BAS)

moa

A

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

28
Q

Bile acid sequestrants (BAS)

antilipid effects

A

Dec LDL

Inc HDL

29
Q

Bile acid sequestrants (BAS)

se

A

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

30
Q

Bile acid sequestrants (BAS)

drug interactions

A

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

31
Q

Safest drug to treat hypercholesterolemia

A

bas

32
Q

PCSK9 inhibitors

moa

A

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

33
Q

PCSK9 inhibitors

lipid lowering effects

A

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

34
Q

Nexletol prodrug

A

Bempedoic acid

35
Q

Nexletol moa

A

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

36
Q

Nexletol se

A

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

pharmacology (16 decks)

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