1
Q
Agents belong of Glycoprotein IIb/IIIa Antagonist Class
A
- Abciximab IV (ReoPro)
- Tirofibran IV (Aggrastat)
- Eptifibatide IV (Integrilin)
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
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
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
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
6
Q
Eptifibatide (Integrilin)
- Indications:
- MOA:
A
- Indication: ACS, PCI
- MOA: Heptapeptide blocks the lysin-glycine-aspartic binding site
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)
8
Q
ADP receptor Antagonists
- Agent use for claudication
- Dose:
- ADEs:
A
- Cilostazol (Pletal)
- D: 100 mg BID
- ADEs: HA, palpitations, diarrhea
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
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
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)
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
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
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
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
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
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