Non-statins Flashcards

Dr. Hess

1
Q

MOA and dose of Ezetimbie (Zetia)

A

-10 mg tablet daily
-with or without food (so it doesn’t rely on timing with cholesterol production like statins), can be taken together with statins
-long half-life (it doesn’t matter when it is taken)
-decreases cholesterol absorption in the GI

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2
Q

Effectiveness of Ezetimibe

A

20-25%
-if taken with statins - LDL reduction is added on top

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3
Q

Combination products of Ezetimibe

A

EZETIMIBE + Rosuvastatin (Roszet)
EZETIMIBE + Simvastatin (Vytorin)
EZETIMIBE + Bempedoic Acid (Nexletol)

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4
Q

Ezetimibe has been shown to reduce cardiac events
True or False?

A

False
Only in combination with statins

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5
Q

Adverse effects of Ezetimibe

A

-Muscle injury
-Liver toxicity -> run a LFT
-diarrhea, steatorrhea

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6
Q

Which labs to run for Ezetimibe?

A

-CPK for muscle damage
-LFT for liver function

Contraindication: active liver disease 3x ULN
Q: Would you run a LFT anyway or just in case of symptoms

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7
Q

Administration of PCSK-9 inhibitor

A

SubQ
-every 2 weeks or 1x a month due to long-halflife

-Alirocumab (Praluent) and Evolocumab (Repatha)

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8
Q

MOA of PCSK-9

A

PCSK-9 breaks down LDL receptors
the drug blocks PCSK-9 -> more LDL receptors taking up LDL from the blood -> lowering LDL plasma level

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9
Q

Effectiveness of PCSK-9 inhibitor

A

> 50%
Role: 2nd line (2b) ->
EZETIMIBE (2a) -> cheaper, oral

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10
Q

PCSK-9 inhibitors reduce ASCVD events

A

True
Alone and together with statins
-also used in HoFH and HeFH

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11
Q

Side effects

A

Well tolerated
injection reaction

Contraindication: Hypersensitivity

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12
Q

PCSK-9 dose

A

Alirocumab (Praluent):
75 mg SQ every 2 weeks or 150 mg q 2 weeks
300 mg SQ 1x a month

Evolocumab (Repatha):
140 mg SQ q 2 weeks
420 mg 1x a month

if they miss the dose for less than a week, take it and reverse to the original schedule

if more than a week, take it and start a new schedule on the same day OR wait until the next administration day of the old schedule

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13
Q

MOA of Bempedoic Acid

A

-ATP Citrate Lyase Inhibitor
-Blocks synthesis of cholesterol (1st step block Acetyl-CoA synthesis)

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14
Q

Administration of Bempedoic Acid

A

Dose: 180 mg daily
with or without food

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15
Q

Effectiveness Bempedoic Acid

A

20-25%
-3rd line
-has been shown to reduce ASCVD in statin-intolerant!!!

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16
Q

Side Effects of Bempedoic Acid

A

-Uric acid (gout)
-Tendon rupture
-not much muscle pain (it is a prodrug activated in the liver)
-Drug-Drug Interaction:
Simvastatin 20mg
Pravastatin 40 mg

OATP1B1/B3 (transporters that move statins from blood to the liver -> so higher concentration of statins -> side effects)

17
Q

MOA Inclisiran (Leqvio)

A

siRNA -> preventing the gene expression of PCSK-9 (doesnt get produced -> no LDL-receptor removal -> more LDL receptors to clear the blood)

18
Q

Administration of Inclisiran (Leqvio)

A

-284 mg SQ

-Day 1 -> day 90 (3 months after day 1) -> day 270 (every 6 months after dose 2)
-if a dose is missed within 3 months take it and stick to the schedule

19
Q

Effectiveness of Inclisiran (Leqvio)

A

-40-50%
-4th line
-not known if it reduces ASCVD

20
Q

Side effects of Inclisiran (Leqvio)

A

injection site reactions
No contraindications

21
Q

Bile Acid Sequestrants Administration

A

-tables, granules/powder (has to be mixed)

22
Q

Effectiveness of Bile Acid Sequestrants

A

-20%
-Role: not used -> rather used for diarrhea due to constipating effect
-no evidence in reducing ASCVD

23
Q

Side effect of Bile Acid Sequestrants

A

Constipation, bloating, GI upset

24
Q

Contraindications and DDI of Bile Acid Sequestrants

A

Contraindications: patients with Pancreatitis (bc it increases TG >400)
obstructive bowel disease (these drugs work by binding bile acids in the intestine)

Drug-Drug-interactions:
reduce drug absorption of warfarin, levothyroxine
-> space 1h before or 4h after

25
Q

Dose of Bile Acid Sequestrants

A

Colesevelam (Welchol)
-3.75 g/day - 6 tabs a day (or 3 tabs BID)

Cholestyramine (Questran)
4-24 g/day - 2 doses

Colestipol (Colestid)
2-16g/day once or divided doses