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Cardio II > Pharm-antithromb > Flashcards

Pharm-antithromb Flashcards

1
Q

MOA of aspirin

A

Irreversibly acetylates a serine residue on COX thus reducing the synthesis of TXA2

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2
Q

MOA of ADP receptor blockers

A

Bind to ADP receptor P2Y12 thus preventing ADP-mediated increase in COX and Glycoproteins IIb/IIIa

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3
Q

Irreversible ADP receptor blockers

A

Clopidogrel
Prasugrel
*oral prodrugs with prolonged effect

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4
Q

Clopidogrel is activated by ___ and prasugrel is metabolized by ___

A
  1. CYP2C19

2. CYP3A4 and CYP2B6

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5
Q

Reversible ADP receptor blockers

A

Ticagrelor (oral)

Cangrelor (IV)

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6
Q

Ticagrelor (is/is not) a prodrug and is metabolized by ___. It has a ___ onset of action and it’s half life is ___ hours. It is eliminated by the ___.

A 
Is not
CYP3A4 
Rapid
8-12
Liver
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7
Q

Cangrelor is metabolized by ___. It has a ___ onset of action and it’s half life is ___ hours. It is eliminated by the ___.

A

Dephosphorylation
Rapid
3-6
Urine and feces

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8
Q 
PAR1 antagonists 
Route 
MOA 
Metabolism 
Elimination
Half life
A
  • Vorapaxar (oral)
  • Binds to PAR1 thus blocking thrombin-induced activation of COX1 and GPIIb/IIIa
  • Metabolized by CYP3A4
  • eliminated by feces
  • 159-311 hours
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9
Q

Irreversible GPIIb/IIIa inhibitors

A

Abciximab - a monoclonal antibody

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10
Q

Reversible GPIIb/IIIa inhibitors

A

Eptifibitide - synthetic peptide inhibitor

Tirofiban - synthetic nonpeptide inhibitor

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11
Q

MOA of GPIIb/IIIa inhibitors

A

Bind to GPIIb/IIIa complex and block binding of fibrinogen to GPIIb/IIIa thus inhibiting the final common pathway

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12
Q

Antiplatelet list

A
  1. COX inhibitors
  2. ADP receptor blockers
  3. GPIIb/IIIa inhibitors
  4. PAR1 antagonists
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13
Q

Anticoagulant list

A
  1. Heparin/like agents
  2. Xa inhibitors (indirect thrombin inhibitor)
  3. Thrombin inhibitors (oral direct, IV direct)
  4. Thrombin synthesis inhibitors
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14
Q

Aspirin clinical uses

A
  • prevention of arterial thrombosis
  • acute coronary syndrome
  • long term prevention of arterial thrombosis after PCI
  • prevent TIA and ischemic stroke
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15
Q

Clopidogrel uses

A

Alternative for aspirin

*combo of the two for pts undergoing PCI

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16
Q

Prasugrel uses

A

Prevent PCI-related thrombosis in pts with poor response to clopidogrel

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17
Q

Ticagrelor uses

A

Usually combined with aspirin for same uses as aspirin because it has a rapid onset of action and is reversible

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18
Q

Vorapaxar uses

A

Added to aspirin or clopidogrel to provide secondary prevention of thrombotic CV events (stroke, MI), and need for coronary revascularization

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19
Q

GPIIb/IIIa inhibitors uses

A

Prevent acute arterial thrombosis (PCI-induced) and to treat acute coronary syndrome

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20
Q

Dipyridamole and cilostazol

MOA

A

Inhibit platelet function by reducing adenosine uptake and cGMP phosphodiesterase activity

21
Q

Dipyridamole uses

A
  • Combo with aspirin to prevent cerebrovascular ischemia

- combo with warfarin to prevent thromboemboli in pts with artificial heart valves

22
Q

Cilostazol uses

A

Treat intermittent claudication

23
Q

There are 2 classes of indirect thrombin inhibitors

A

Heparin-like agents

Xa inhibitors

24
Q

Heparin-like agents MOA

A

Accelerate the effects of antithrombin on coagulation factors IIa and Xa by increasing the rate of the antithrombin III-coagulation factor reaction

25
Xa inhibitors do NOT require endogenous antithrombin to produce their effects but ___ do.
Heparin-like agents
26
Heparin-like agents are administered ___ and have a ___ onset of action.
Parenterally (IV) | Rapid
27
UFH MOA Half life Cleared by
High molecular weight heparin - mainly inhibits IIa and Xa - 90 min - reticuloendothelial system
28
``` LMWHs Examples MOA Half life Administered _ Cleared by _ ```
Low molecular weight heparin - enoxaparin, dalteparin, tinzaparin - mainly inhibit Xa - 4-5 hours - IV or subcutaneously - Kidney
29
LMWH vs UFH
LMWH have less chance of non-hemorrhagic side effects AND actions are predictable AND monitoring aPTT and platelet number is not required
30
Fondaparinux (sulfate pentasaccharide) is a synthetic agent that mainly inhibits ____ (and this activity is higher than that of ___). Half life is ___ and it is cleared by the ____. It is administered ___
``` Xa LMWH 17 hours Kidneys Subcutaneously ```
31
___ are the drug of choice for prophylaxis of DVT and PE because they are safe and convenient
LMWHs
32
___ should be initiated in all patients with confirmed acute PE
Parenteral anticoagulant therapy
33
Bleeding is a major side effect for ___, especially in elderly women and those with renal failure
Heparin-like agents
34
Heparin antidote
Protamine sulfate
35
Contraindications for heparin-like agents
Recent brain/eye/spinal cord surgery Lumbar puncture Regional anesthetic block Coagulation abnormalities
36
Xa inhibitors Examples Route Metabolism
``` Rivaroxaban Apixaban Edoxaban *all oral *CYP3A4/p-gp ```
37
Xa inhibitors | Uses
Prevent DVT, PE, stroke (in pts with nonvalvular a fib)
38
Irreversible direct thrombin inhibitors
Lepirudin (renal) Bivalirudin (renal) Argatroban (liver) *IV
39
``` Reversible direct thrombin inhibitor Route Prodrug or not? Elimination Half life Metabolism ```
``` Dabigatran Oral Prodrug Urine 12-17 hours P-gp ```
40
Clinical uses of dabigatran
Primary and secondary prevention of DVT, PE, stroke, and systemic embolism in patients with non-valvular a fib *no INR monitoring required
41
Dabigatran antidote
Idarucizumab
42
Warfarin | MOA
Inhibits synthesis of vitamin K dependent coag factors (II, VII, IX, X, Protein C, and Protein S) by suppressing vitamin K reductase
43
Warfarin is administered ___ and has ___% bioavailability. It has a ___ onset of action
Orally 100% Slow
44
Warfarin | Uses
Primary and secondary prevention of DVT, PE, and thromboembolism associated with a fib, MI, and artificial heart valves -also for recurrence of DVT or PE
45
Contraindications for warfarin
Pregnancy
46
Warfarin antidote
- Vitamin K - Fresh frozen plasma - Prothrombin complex concentrates - recombinant factor VIIa
47
Fibrinolytic antidote
Aminocaproic acid
48
___ can be used to treat heparin-induced thrombocytopenia
Lepirudin | Argatroban

Cardio II (16 decks)

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