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5. Anticoagulants > Anti-Platelets Agents > Flashcards

Anti-Platelets Agents Flashcards

1
Q

Agents belong of Glycoprotein IIb/IIIa Antagonist Class

A
  • Abciximab IV (ReoPro)
  • Tirofibran IV (Aggrastat)
  • Eptifibatide IV (Integrilin)
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2
Q

Glycoprotein IIb/IIIa Antagonist

  • MOA:
  • Precautions/CIs
A
  • MOA: Block fibrinogen binding to GPIIb/IIIa receptor on platelets = prevents platelets from aggregating together

Precautions/CIs

  • Hx of active bleeding/intracranial hemorrhge, surgical procedures or major trauma w/in 1 mo
  • Platelet count < 150000/mm3 (thrombocytopenia)
  • Hypersensitivity
  • Aortic dissection, pericarditis, severe HTN
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3
Q

Glycoprotein IIb/IIIa Antagonist class

  • Agent(s) have short T1/2 and require continuous infusion
  • Agents(s) does (do) not require renal adjustment and cannot shake
  • Require renal adjustment
A

Short half life & require renal adj

- Tirofiban (Aggrastat): Dec dose by 50% if CrCl

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4
Q

Abciximab (ReoPro)

  • Indications:
  • MOA:
  • PK:
A
  • I: Adjust to PTCA (percutaneous transluminal coronary angioplasty). Used as an adjunct w/ heparin when PCI is scheduled w/in 24H
  • MOA: Mouse Ab directed against GPIIb/IIIa receptor (antigenic) irreversible
  • Cross reacts with integrin on endothelial cells
  • PK:
  • ReoPro binds to platelet for many days => inhibition for 24-48H w/ low levels still detectable after 15 days
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5
Q

Tirofiban (Aggrastat)

  • Indications:
  • MOA:
A
  • I: combination w/ heparin, ACS including pts undergoign PTCA
  • Therapey should continue through angiography and for 12-24H after angioplasty
  • MOA: non-peptide tyrosine derivative that blocks arginine-glycine-aspartic binding sites of GP IIb/IIIa
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6
Q

Eptifibatide (Integrilin)

  • Indications:
  • MOA:
A
  • Indication: ACS, PCI

- MOA: Heptapeptide blocks the lysin-glycine-aspartic binding site

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7
Q

Agents belong to ADP receptor Antagonists
=> Inhibitors of P2Y12 (Thiennopyridines)
- MOA:
- Agents that are irreversible:
- Not a prodrug

A
  • Cilostazol (Pletal) =>
  • Ticlopidine (Ticlid) => Irreversible => requires in vivo biotransformation to an unidentified active metabolite
  • Clopidogrel (Plavis) => Irreversible => prodrug
  • Prasugrel (Effient) => Irreversible => prodrug
  • Ticagrelor (Brilinta) => Reversible => not prodrug

=> MOA: Interfere w/ ADP-mediated platelet activation and aggregation. Inhibits platelet aggregation for the lifetime of platelet (5-7 days)

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8
Q

ADP receptor Antagonists

  • Agent use for claudication
  • Dose:
  • ADEs:
A
  • Cilostazol (Pletal)
  • D: 100 mg BID
  • ADEs: HA, palpitations, diarrhea
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9
Q

ADP receptor Antagonists

- Agent cause (severe) neutropenia:

A
  • Ticlopidine (Ticlid): 250 mg BID w/ food
    => Fever, chills sore throat
    Occurs within 1st mo.
    Check CBC w/ diff at baseline and q2w x 3mo, thrombotic thrombocytopenia purpura (TTP), rash, LFT
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10
Q

ADP receptor Antagonists

  • Agent(s) interact w/ CYP2C9
  • Dose:
  • ADEs:
A
  • Clipidogrel (Plavix): a prodrug
  • CYP2C9: the enzyme converts plavix to its active form. Don’t combine w/ CYP2C9 inhibitors
  • Dose: 300-600 mg LD then 75 mg QD
  • ADEs: GI effects, diarrhea, neutropenia, thrombocytopenia, rash, and GI bleeding
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11
Q

ADP receptor Antagonists

  • Agent(s) d/c 7 days prior to surgery:
  • Agent(s) d/c 5 days prior to surgery:
A
  • 7 days: Prasugrel (effient)

- 5 days: Clopidogrel (Plavix) & Ticagrelor (Brilinta)

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12
Q

Prasugrel (Effient)

  • Not rec in which population
  • Dose:
A
  • w/ hx of stroke, >/= 75 y.o unless they are at high risk (DM or prior MI)
  • Dose: 10 mg BID
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13
Q

Ticagrelor (Brilinta)

  • PK: OSA
  • Dose:
  • DDI:
  • Boxed warning:
A
  • Rapid onset and rapid off set => require continuous infusion
  • Dose: LD 180 mg (two 90 mg tab). MD 90 mg BID w/ or w/o food
  • DDI: is an inhibitor of P-Glyco-protein transporter & metabolized by 3A4
  • Avoid CYP3A4 inhibitors
  • Inc [ ] of simvastatin and lovastatin
  • Monitor digoxin level (inhibitor of P-GP)
  • Box warning: ASA above 100 mg reduce effectiveness of Brilinta
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14
Q

ADP receptor Antagonists: dose for

  • Cilostazol (Pletal)
  • Ticlopidine (Ticlid)
  • Clopidogrel (Plavis)
  • Prasugrel (Effient)
  • Ticagrelor (Brilinta)
A
  • Cilostazol (Pletal): 100 mg BID
  • Ticlopidine (Ticlid): 250 mg BID w/ food
  • Clopidogrel (Plavis): 300-600 mg LD then 75 mg QD
  • Prasugrel (Effient): 10 mg BID
  • Ticagrelor (Brilinta): LD 180 mg (two 90 mg tab). MD 90 mg BID w/ or w/o food
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15
Q

ASA

  • MOA
  • Dose:
  • ADEs:
  • Precautions:
A
  • MOA: Irreversibly acetylates COX-1, blocking thromboxane synthesis, and inhibiting platelet activation and aggregation for the lifetime of the platelete
  • It inhibits Prostaglandins that produce inflammation and interferes with synthesis of TXA2
  • Dose: 50-325 mg QD
  • ADEs: GI bleed, rash, hypersensitivity, Reye’s synd
  • P: preg cat D, allergy to NSAIDs, hx of asthma, PUD, Alcoholism
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16
Q

ASA

  • Rec low dose for:
  • Benefit:
A
  • 2nd prevention to prevent a 2nd HA or ischemic stroke in pt who already had one
  • MEN age 45-79 and WOMEN age 55-79 and aren’t at high risk for bleeding

Benefit:

  • MEN: prevent a HA
  • WOMEN: preventing an ischemic stroke
17
Q

Reye’s Syndrome

  • What it’s
  • Associated w/
  • Typically occurs
A
  • Accumulation of fat begins to develop in liver and severe increase pressure in brain
  • Ass w/ viral infection along w/ ASA
  • Typically occurs when a pt begin to recover from a viral illness
18
Q

Dipyridamole (Persantine)

  • MOA
  • Indication:
  • Dose:
  • ADEs:
  • Precaution:
A
  • MOA: Reversible inhibitor of platelet aggregation => inc cAMP in platelets
  • Indication: use as an adjunct to warfarin or ASA or cardiac exercise testing for ppl who can’t walk on treadmill
  • Dose: 75-100 mg QID
  • ADEs: infertility, hepatic
  • Precaution: preg B, hypoTN, potential to bleed
19
Q

Can a pt be on warfarin, ASA, and plavix

A

Yes

  • Warfarin: a. fib, DVT, or mechanical heart valves
  • ASA and Plavix: are used after coronary stent
20
Q

Anti-coagulant/anti-platelet work on vein or artery

A
  • Anti-coagulants: work on RBC and fibrin that form in vein or atrium of the heart
  • Antiplatelet drugs: work more specific for platelets that form in the arteries

5. Anticoagulants (9 decks)

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