Antiplatelets Flashcards

1
Q

What are antiplatelet drug uses

A
  • since arterial clots are primarily made up of a platelet core, antiplatelet agents are primarily used to prevent arterial clots
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2
Q

Which of the antiplatelet drugs have similar function

A

1) aspirin (cox inhibitor), P2Y12 inhibitors, and other miscellaneous antiplatelets drugs affect only one pathway in platelet activation
2) GP IIb/IIIa inhibitors block the final common step in platelet activation and thus are much more potent antiplatelets

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3
Q

Aspirin indications

A

1) ischemic stroke
2) . TIA
3) chronic stable angina
4) unstable agnina
5) coronary stenting
6) acute myocardial infarction

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4
Q

aspirin moa

A
  • irreversible inhibition of COX

- decreases thromboxane a2 production thus reduces platelet activation

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5
Q

contradictions to aspirin

A

use in children and teens with viral infections (reyes syndrome)

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6
Q

ADR of aspirin

A

1) GI bleeds

2) hemorrhagic stroke

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7
Q

Clopidogrel (Plavix) indications:

A

1) acute coronary syndrome (STEMI and NSTEMI)
2) ischemic stroke
3) peripheral atherosclerotic disease

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8
Q

US box warning: Clopidogrel (Plavix)

A

diminished effects in CYP2C19 poor metabolizers

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9
Q

MOA Clopidogrel (Plavix)

A

irreversibly blocks P2Y12 component of ADP receptors on the platelet surface- effects last the duration of the platelet’s life (7-10 days)

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10
Q

Contraindications of Clopidogrel (Plavix)

A

Active pathological bleeding (peptic ulcer, intracranial hemorrhage)

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11
Q

Dosage for aspirin

A

1) 81 mg- maximal effects on platelet function

2) 325 mg- indicated in initial treatment of an acute event (chew 4 aspirin)

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12
Q

ADR of Clopidogrel (Plavix)

A

Bleeding

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13
Q

Metabolism/excretion of Clopidogrel (Plavix)

A

1) must be metabolized by CYP2C19 into active drug
2) CYP2C19 is inhibited by. PPI (drugs used to reduce stomach acid and protect the stomach from GI bleeding)
3) american college of cardiology, aha, etc. issued a consensus document that PPIs may reduce the antiplatelet effects but NOT diminish the effects

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14
Q

Prasugrel indications

A

Acute coronary syndrome

  • slightly more effective than clopidogrel- BUT also had a higher risk of major bleeding
  • bleeding significantly is increased in patients undergoing a CABG
  • may also increase the risk of cancer
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15
Q

DRUG INTERACTIONS OF CLOPIDOGREL

A
  • PPIs are used to reduce stomach acid production and to protect the stomach from GI bleeding. But, the 2c19 it inhibited by ppis.
  • however, we found out that ppis might reduce the antiplatelet effect but not enough to diminish the effects
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16
Q

Prasugrel MOA

A

irreversibly blocks P2Y12. component of ADP receptors on the platelet surface- effects last the duration of the platelets life (7-10. days)

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17
Q

Prasugrel contradictions

A

active pathological bleeding (peptic ulcer, intracranial hemmorhage) prior TIA or stroke

18
Q

ADR Prasugrel

A

Bleeding

19
Q

Prasugrel US box warning

A

Bleeding risk

1) significant sometimes fatal bleeding- avoid in patients with active pathological bleeding or a hx of TIA or stroke
2) in patients 75+ use is generally not recommended
3) do not use in patients likely need urgent CABG sx- d/c 7 day prior to sx (most agents are 5)
4) additional risk factors for bleeding, low body weight, propensity to bleed or hx of bleeding, concomitant medications that increase risk of bleeding
5) suspect bleeding in any patient who is hypotensive
6) IF POSSIBLE, MANAGE BLEEDING WITHOUT D/C PRASUGREL- D/C INCREASES THE RISK OF A SECONDARY EVENT

20
Q

Ticagrelor Indications

A

ACS, primary prevention of. ischemic cv events in CAD, minor ischemic stroke or high risk TIA
-more effective than clopidogrel (but fatal IC hemorrhage)

21
Q

US box warning ticagrelor

IMPORTANT

A

1) bleeding risk
2) ASPIRIN DOSES >100 MG CAN REDUCE THE EFFECTIVENESS OF TICAGRELOR AND SHOULD BE AVOIDED ( USE 81MG DOSE ASPIRIN INSTEAD)

22
Q

MOA of ticagrelor

A

reversible P2Y12 inhibition-reduces platelet aggregation

-inhibition of platelet aggregation is around 60% 24 hours after d/c of maintenance dosing

23
Q

contraindications of ticagrelor

A

active pathological bleeding or hx of ich

24
Q

ADR of ticagrelor

A

dyspnea

25
Q

cangrelor indications

A

used in patients who remain a high risk of thrombotic event and cannot tolerate a P2Y12 or at times used in cardiogenic shock

26
Q

cangrelor moa

A

Reversible P2Y12 inhibition- reduces platelet activation

  • activation in 2 minutes (ONLY IV AGENT)
  • total effects end about 1 hour after d/c
  • transition to p2y12 (stop cangrelor and immediately start oral agent)
27
Q

contradictions of cangrelor

A

signficant active bleeding

28
Q

ADR cangrelor

A

bleeding

29
Q

vorapaxar indications

A

history of MI or established peripheral artery disease

-reduce thrombotic event in combination with clopidogrel or aspirin (or both)

30
Q

vorapaxar MOA

A

PAR-1 antagonist- inhibit platelet aggregation

31
Q

contradictions of vorapaxar

A

hx of stroke, tia,ic hemm

32
Q

ADR vorapaxar

A

bleeding

33
Q

glycoprotein iib/iiia inhibitors

A

eptifibitide and tirofibam

34
Q

glycoprotein iib/iiia inhibitors indications

A

the most effective antiplatelet drugs
- prevent ischemic events in those undergoing PCI- prevent re-occlusion following coronary artery revascularization with PCI- typically used on primary PCI facilities

35
Q

US box warnings: glycoprotein iib/iiia inhibitors

A

none

36
Q

glycoprotein iib/iiia inhibitors MOA

A

reversible blockade of GP iib/iiia receptors on platelets and thereby inhibit the final step of aggregation
- prevent aggregation stimulated by all factors including collagen…

37
Q

contraindications: glycoprotein iib/iiia inhibitors

A

1) active abnormal bleeding within the previous 30 days or a hx of bleeding diathesis
2) hx of stroke within 30 days or hx of hemorrhagic stroke
3) severe HTN
4) major sx within the preceding 6 weeks

38
Q

dipyridamole/aspirin (aggrenox) indications

A

prevent. recurrent stroke or tia

- shown more effective than either drug alone - the clinical trial was tainted by scientific scandal

39
Q

dipyridamole/aspirin (aggrenox) us box warnings

A

none

40
Q

dipyridamole/aspirin (aggrenox) MOA

A

dipyridamole inhibits the uptake of adenosine into platelets- prevents platelet activation/ aggregation

41
Q

dipyridamole/aspirin (aggrenox) contradictions

A

same as aspirin

42
Q

route dipyridamole/aspirin (aggrenox)

A

oral capsules

- note: there is not enough aspirin for primary prevention of MI (ony 50mg and you need > 80 mg)