L25 Flashcards
What are the 2 most potent factors to upregulate GP2b3a receptor for platelet aggregation and thrombus formation?
Thrombin
Collagen
Aspirin mechanism
COX inhibitor
X TXA2 synthesis - no platelet aggregation
Permanently inhibits that platelet - must wait for liver to make more
“Weak” anti-platelet
Aspirin:
- Dose dep inhibition?
- When does drug become bioavail
- t1/2
Dose dep inhibition of COX
Works in pre-hepatic circulation after GI absorption
- Drug doesn’t need to reach systemic circulation
t1/2 doesn’t really matter - matters how long it takes to make new platelets
3 times to use aspirin
Can take 81mg daily to prevent a 1st CV event - really only for high risk pts (stable angina)
- ↓MI mortality - chew baby aspirin when you have chest pain!
- CABG graft patency, stents
- Prior stroke to ↓risk another
SE aspirin
Could be allergy
GI
What is the mechanism of aspirin resistance?
TXA made b/c platelets express COX2
Dx by ↑TXA in urine
These pts have baseline ↑risk MI, stroke, etc
Dipyridamole mechanism
cAMP phosphodiesterase inhibitor on platelets
X TXA2
Not 1st line choice
What are the 3 ADP receptor antagonists? Which is already in active form?
Clopidogrel - 2 time cyp2C19 activation
Prasugrel - 1 time “ “
Ticagrelor - active form
Mechanism of ADP receptor antagonists
X ADP receptor binding
- No ADP - P2Y12 binding
No Gp2b3a receptor upregulation for platelet aggregation
Action of ADP receptor antagonists - which is an important extra
Uses: prevent re-events
↓stent thrombosis
↓N/STEMI recurrence
**TICAGRELOR ↓s CV DEATH RATE
What is standard ADP receptor antagonist therapy?
Dual anti-platelet therapy
X + aspirin
What should you consider when dosing prasugrel?
End stage renal disease - only get about 1/2 amt of active metabolite you’re exposed to
3 situations in which to use prasugrel > clo
Cerebrovasc
Over 75 yo
Pts w/ stents placed should be on what type of therapy
Anti-PLATELET for at least a year until stent has been fully endothelialized
What are the 2 Gp2a3b receptor antagonists
Abciximab - irreversible
Eptifibatide