Gb IIb/IIIa Inhibitors (STEMI/NSTEMI/UA) Flashcards

1
Q

GP IIb/IIIa Inhibitors

Indications

A

Conformational changes in receptor allow binding with

  • Fibrin
  • Thrombin
  • VWF
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2
Q

Binding triggers:

A
  • Adhesion
  • Activation
  • Aggregation of platelets
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3
Q

Efficacy order!

  1. anti platelet
  2. UA/NSTEMI
A

Receptor blocking determines antiplatelet efficacy (abciximab>eptifibatide>tirofiban),
Clinical efficacy (UA/NSTEMI): (eptifibatide = tirofiban > abciximab),
and bleeding

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4
Q

GP IIb/IIIa Inhibitors

CI

A
CI: active or recent bleed 4-6weeks
Hemorrhagicaccident
CVA in 30 days- 2 ys
Severe HTN >180/110
Major surgery/trauma in past 4-6 weeks
Thrombocytopenia
Bleeding diathesis/warfarin with elevated INR
Renal insufficiency/failure
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5
Q

Eptifibatide MOA

A

Cyclic, small molecule
GP IIb/IIIa receptor antagonist

Selective
Reversible
Competitive inhibition

Temporarily blocks fibrin cross linking btwn active Gp Receptors

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6
Q

Eptifibatide Indications

A

Medical therapy in NSTEMI ACS with herparin, ASA +/- PCI and stenting

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7
Q

Eptifibatide Metabolism

A

Half life 1.1-2.5 hrs
(2 half lives at 5 hrs is 75% gone.. 90% gone is 3.3 half lives)
RENAL elimination

Platelet function returns within 4-12 hrs of D/C

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8
Q

Eptifibatide DI/CI/ Caution

A

Caution: aPTT>/= 45 seconds

CrCl less than 50

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9
Q

Eptifibatide SE

A

Bleeding (10%)

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10
Q

Eptifibatide considerations

A

Reduce MI/death by 20% after PCI for ACS when used with ASA

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11
Q

Tirofiban MOA

A
Nonpeptide, small molecule
GP IIb/IIIa receptor antagonist
Selective
Reversible
Competitive inhibition

Temporarily blocks fibrin cross linking btwn active Gp Receptors

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12
Q

Tirofiban Indications

A

Medical therapy in NSTEMI ACS with herparin, ASA +/- PCI and stenting

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13
Q

Tirofiban Metabolism

A

Infusion runs for up to 24 hours after PCI

Half life is 2 hrs

RENAL elimination

Platelet function returns within 4-12 hours of D/C

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14
Q

Tirofiban DI/CI/ Caution

A

Caution:
Platelets /= 45 secs
CrCl less than 30

Tiro Thirty- TT

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15
Q

Tirofiban considerations

A

Reduce MI/death by 20% after PCI for ACS when used with ASA

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16
Q

Abciximab MOA

A

Mouse monoclonal antibody gragment
Binds platelet GP IIb/IIIa receptor to inhibit activation and aggregation via fibrin crosslinking—steric hinderance prevents interactions btwn GP and vironectin recptors and other molecules (VW factor)
Binds platelet GP ab3 mediated thrombin generation
Clot retraction and smooth muscle cell proliferation

17
Q

Amiximab Indications

A

Use with heparin and ASA in NSTMEI and STEMI ACS

Only in cath lab!

(to go home use asa, clipidogrel, adp inhibitors, prasugril, tacagrilor)

18
Q

Amiximab Metabolism

A

Platelet inhibition exceeds 90% during infusion

binds and dissociates rapidly
steric hindrance of GP receptor

half life 10-30 min

platelet function returns in 48 hrs

19
Q

Amiximab CI/DI/Precaution

A

CI: active bleeding
GI/GU bleed, trauma, surgery within 6 weeks
Anticoag in last 7 days

Precaution:
-Hypersensitivity reactions, TCP, rebound thrombosis observed with abciximab antibodies
-Heparin doses adjusted to minimize bleeding
increased risk of bleeding events when used with clopidogrel, lytics, longer PCI procedure

20
Q

Amiximab Considerations

A

*50% reduction in total CV events but mortality is offset by adverse bleeding events
antibody remains bound to receptor aIIbB3
major hemorrhage varies and with heparin intensity, surgical pts at risk
reverse with platelets when needed
TCP in 2% of pts