Antiplatelets Flashcards
How are Abciximab (Reopro), Eptifibatide (Integrillin), and Tirofiban (Aggrastat) administered? A. IV B. SC C. IM D. orally
A. IV administration
Adverse effects of dipyridamole + aspirin (Aggrenox)
Increased bleeding effects headache dizziness VASODILATION HYPOTENSION GI discomfort
What is the MOA of Abciximab (Reopro), Eptifibatide (Integrillin), and Tirofiban (Aggrastat)?
bind to GPIIb/IIIa receptor & prevent FIBRINOGEN binding
Cangrelor is a ________________.
A. PAR-1 inhibitor
B. P2Y12 inhibitor
C. Thromboxane receptor inhibitor
B
What is the MOA of aspirin?
It inhibits COX-1 (and COX-2 also –> nonselective) by irreversibly acetylating serine AA residue near the active site which prevents PG synthesis from activating TXA2 formation (which normally activates platelets)
So it inhibits platelet activation
What are the therapeutic doses of aspirin for anti-platelet activity?
75-325 mg
What is the peak effect time for aspirin?
1-3 h
How long does aspirin inhibit platelets?
for the life of the platelet (5-7 days)
What are adverse effects of aspirin?
bleeding risk
GI irritation of mucosal lining (inhibition of local COX-1)
Hypersensitivity (rare)
Interactions with other nonselective NSAIDs
What are drug interactions with aspirin?
Ibuprofen (cleared slower than aspirin and binds to the same site but doesn’t have anti-platelet effect)
Which of the following are P2Y12 Receptor antagonists? A. Ticlopiline (Ticlid) B. Aggrenox (Dipyridamol + aspirin) C. Cilostazol (Pletal) D. Tirofiban (Aggrastat) E. Clopidogrel (Plavix)
A,E
What is the MOA of P2Y12 Receptor antagonists?
they block ADP binding to P2Y12 receptor and cause an increase in cAMP and PKA activity –> decreases GP …..
[SATA] which of the following block platelet activation? A. ASA B. Clopidogrel C. Ticagrelor D. Cilostazol E. Eptifibatide
A. ASA
B. Clopidogrel
C. Ticagrelor
D. Cilostazol
What is the half-life of Aggrenox? A. 2 h B. 10 h C. 7 h D. 30 min
B. 10 h
What is the half-life of Clopidogrel? A. 2 h B. 10 h C. 7 h D. 30 min
D. 30 min
What is the half-life of Prasugrel? A. 2 h B. 10 h C. 7 h D. 30 min
C. ~ 7 hours (2-15 hours)
What drug class interacts with Prasugrel and Clopidogrel?
PPIs
What is the half-life of Ticagrelor? A. 3 h B. 10 h C. 7 h D. 9 h
D. 9 h
What is the half-life of Cilostazol? A. 2 h B. 10 h C. 7 h D. 30 min
B. 10 hr
What is the half-life of Eptifibatide? A. 2.5 h B. 10.5 h C. 8 h D. 1.5 h
A. 2.5 hours
What is the half-life of Tirofiban? A. 2 h B. 10 h C. 7 h D. 30 min
A. 2 hours
[SATA] Which of the following blocks GPIIb/IIIa receptors by preventing fibrinogen from bridging adjacent platelets? A. Cilostazol B. Eptifibatide C. Tirofiban D. Ticagrelor
B, C
What is the ADR of ASA?
bleeding risk GI irritation (dyspepsia, erosive gastritis, peptic ulcer)
What is the ADRs of Clopidogrel and Prasugrel?
bleeding risk
GI irritation
N/V/D
[SATA] Which of the following are cleared by renal & biliary pathways? A. Clopidogrel B. Cilostazol C. Aggrenox D. Prasugrel
A, D
[SATA] Which of the following are renally cleared? A. Tirofiban B. Cilostazol C. Aggrenox D. Ticagrelor E. Eptifibatide
A. Tirofiban
B. Cilostazol
D. Cilostazol
E. Eptifibatide
Name two anti platelets excreted biliary?
Aggrenox (glucuronidated and cleared in bile)
Ticagrelor
What enzyme(s) activates clopidogrel?
2C19
What enzyme(s) activates prasugrel?
3A4, 2B6
What are the ADRs of ticagrelor?
SOB
bleeding risk
[SATA] Which of the following has irreversible binding? A. Abciximab B. Eptifibatide C. Tirofiban D. Ibuprofen E. ASA
A, E
[SATA] Which of the following are adverse effects of Cilostazol (Pletal)? A. ventricular arrhythmias B. Shortness of breath C. hypotension D. headaches E. thrombocytopenia
A, C, D
What enzymes metabolize Cilostazol?
3A4, minor 2C19
[SATA] Which of the following are adverse effects of Abciximab and eptifibatide? A. ventricular arrhythmias B. bleeding risk C. hypotension D. headaches E. thrombocytopenia
B. E
[SATA] Which of the following are adverse effects of Aggrenox? A. dizziness B. bleeding risk C. hypotension D. headaches E. thrombocytopenia F. GI discomfort
A. dizziness B. bleeding risk C. hypotension D. headaches F. GI discomfort
2C19*2:
A. is the normal “wild” type
B. increases metabolism of Clopidogrel
C. decreases metabolism of Clopidogrel
C.
2C19*3:
A. is the normal “wild” type
B. increases metabolism of Clopidogrel
C. decreases metabolism of Clopidogrel
B
If you took verapamil and prasugrel, what would happen to prasugrel levels?
less prasugrel would be activated (less active metabolite conc, less effect)
Which P2Y12 receptor antagonist does not require bioactivation?
Ticagrelor (Brilinta)
What is the ROA for GPIIb/IIIa Receptor Antagonists
IV
