Antiplatelets Flashcards

0
Q
How are Abciximab (Reopro), Eptifibatide (Integrillin), and Tirofiban (Aggrastat) administered?
A. IV
B. SC
C. IM
D. orally
A

A. IV administration

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1
Q

Adverse effects of dipyridamole + aspirin (Aggrenox)

A
Increased bleeding effects
headache
dizziness
VASODILATION
HYPOTENSION
GI discomfort
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2
Q

What is the MOA of Abciximab (Reopro), Eptifibatide (Integrillin), and Tirofiban (Aggrastat)?

A

bind to GPIIb/IIIa receptor & prevent FIBRINOGEN binding

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4
Q

Cangrelor is a ________________.
A. PAR-1 inhibitor
B. P2Y12 inhibitor
C. Thromboxane receptor inhibitor

A

B

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5
Q

What is the MOA of aspirin?

A

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

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6
Q

What are the therapeutic doses of aspirin for anti-platelet activity?

A

75-325 mg

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7
Q

What is the peak effect time for aspirin?

A

1-3 h

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8
Q

How long does aspirin inhibit platelets?

A

for the life of the platelet (5-7 days)

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9
Q

What are adverse effects of aspirin?

A

bleeding risk
GI irritation of mucosal lining (inhibition of local COX-1)
Hypersensitivity (rare)
Interactions with other nonselective NSAIDs

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10
Q

What are drug interactions with aspirin?

A

Ibuprofen (cleared slower than aspirin and binds to the same site but doesn’t have anti-platelet effect)

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11
Q
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

A,E

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12
Q

What is the MOA of P2Y12 Receptor antagonists?

A

they block ADP binding to P2Y12 receptor and cause an increase in cAMP and PKA activity –> decreases GP …..

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13
Q
[SATA] which of the following block platelet activation?
A. ASA
B. Clopidogrel
C. Ticagrelor
D. Cilostazol
E. Eptifibatide
A

A. ASA
B. Clopidogrel
C. Ticagrelor
D. Cilostazol

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14
Q
What is the half-life of Aggrenox?
A. 2 h
B. 10 h
C. 7 h
D. 30 min
A

B. 10 h

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15
Q
What is the half-life of Clopidogrel?
A. 2 h
B. 10 h
C. 7 h
D. 30 min
A

D. 30 min

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16
Q
What is the half-life of Prasugrel?
A. 2 h
B. 10 h
C. 7 h
D. 30 min
A

C. ~ 7 hours (2-15 hours)

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17
Q

What drug class interacts with Prasugrel and Clopidogrel?

A

PPIs

18
Q
What is the half-life of Ticagrelor?
A. 3 h
B. 10 h
C. 7 h
D. 9 h
A

D. 9 h

19
Q
What is the half-life of Cilostazol?
A. 2 h
B. 10 h
C. 7 h
D. 30 min
A

B. 10 hr

20
Q
What is the half-life of Eptifibatide?
A. 2.5 h
B. 10.5 h
C. 8 h
D. 1.5 h
A

A. 2.5 hours

21
Q
What is the half-life of Tirofiban?
A. 2 h
B. 10 h
C. 7 h
D. 30 min
A

A. 2 hours

22
Q
[SATA] Which of the following blocks GPIIb/IIIa receptors by preventing fibrinogen from bridging adjacent platelets?
A. Cilostazol
B. Eptifibatide
C. Tirofiban
D. Ticagrelor
A

B, C

23
Q

What is the ADR of ASA?

A
bleeding risk
GI irritation (dyspepsia, erosive gastritis, peptic ulcer)
24
Q

What is the ADRs of Clopidogrel and Prasugrel?

A

bleeding risk
GI irritation
N/V/D

25
Q
[SATA] Which of the following are cleared by renal & biliary pathways?
A. Clopidogrel
B. Cilostazol
C. Aggrenox
D. Prasugrel
A

A, D

26
Q
[SATA] Which of the following are renally cleared?
A. Tirofiban
B. Cilostazol
C. Aggrenox
D. Ticagrelor
E. Eptifibatide
A

A. Tirofiban
B. Cilostazol
D. Cilostazol
E. Eptifibatide

27
Q

Name two anti platelets excreted biliary?

A

Aggrenox (glucuronidated and cleared in bile)

Ticagrelor

28
Q

What enzyme(s) activates clopidogrel?

A

2C19

29
Q

What enzyme(s) activates prasugrel?

A

3A4, 2B6

30
Q

What are the ADRs of ticagrelor?

A

SOB

bleeding risk

31
Q
[SATA] Which of the following has irreversible binding?
A. Abciximab
B. Eptifibatide
C. Tirofiban
D. Ibuprofen
E. ASA
A

A, E

32
Q
[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

A, C, D

33
Q

What enzymes metabolize Cilostazol?

A

3A4, minor 2C19

34
Q
[SATA] Which of the  following are adverse effects of Abciximab and eptifibatide?
A. ventricular arrhythmias
B. bleeding risk 
C. hypotension
D. headaches
E. thrombocytopenia
A

B. E

35
Q
[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
A. dizziness
B. bleeding risk 
C. hypotension
D. headaches
F. GI discomfort
36
Q

2C19*2:
A. is the normal “wild” type
B. increases metabolism of Clopidogrel
C. decreases metabolism of Clopidogrel

A

C.

37
Q

2C19*3:
A. is the normal “wild” type
B. increases metabolism of Clopidogrel
C. decreases metabolism of Clopidogrel

A

B

38
Q

If you took verapamil and prasugrel, what would happen to prasugrel levels?

A

less prasugrel would be activated (less active metabolite conc, less effect)

39
Q

Which P2Y12 receptor antagonist does not require bioactivation?

A

Ticagrelor (Brilinta)

40
Q

What is the ROA for GPIIb/IIIa Receptor Antagonists

A

IV