Anticoagulant Agents Table Flashcards

1
Q

Heparin (Unfractionated [UFH])

Mechanism of Action?

A

Binds ATIII –> inactivates IIa and Xa

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2
Q

Heparin (Unfractionated [UFH])

Onset of action?

A

Rapid (minutes if IV w/ LD)

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3
Q

Heparin (Unfractionated [UFH])

Administration route?

A

Parenteral (IV / SC)

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4
Q

Heparin (Unfractionated [UFH])

Elimination?

A

Dose-dependent t1/2 – cleared by reticuloendothelial system

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5
Q

Heparin (Unfractionated [UFH])

Monitoring lab test

A

aPTT

can use anti-factor Xa prn

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6
Q

Heparin (Unfractionated [UFH])
Adverse Effects?
narrow therapeutic index

A

Bleeding / thrombocytopenia

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7
Q

Heparin (Unfractionated [UFH])

Safety in pregnancy?

A

Safe

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8
Q

Heparin (Unfractionated [UFH])
DDIs
NSAIds Incr bleeding risk with all anticoagulants?

A

Antiplatelet agents

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9
Q

Heparin (Unfractionated [UFH])

Overdose Treatment?

A

Protamine

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10
Q

Heparin (Unfractionated [UFH])

Uses

A

ACS / VTE

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11
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Mechanism of Action?

A

Binds ATIII –> inactivates Xa

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12
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Onset of action

A

3-5 hours SC

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13
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Administration route

A

Parenteral (IV / SC)

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14
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Elimination

A

Renal clearance (decr dose in renal failure)

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15
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Monitoring lab test

A

Not needed, action predictable
Dosed on mg/kg basis
(can use anti-factor Xa prn)

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16
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Adverse Effects?
narrow therapeutic index

A

Bleeding / thrombocytopenia

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17
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Safety in pregnancy

A

Safe

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18
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
DDIs
NSAIds Incr bleeding risk with all anticoagulants?

A

Antiplatelet agents

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19
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Overdose Treatment Protamine

A

Protamine

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20
Q

Low-Molecular Weight Heparin [LMWH],
(Enoxaparin - Dalteparin)
Uses

A

ACS / VTE

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21
Q

Warfarin

Mechanism of Action

A
Inhibits liver synthesis of Vit K-
dep factors (II, VII, IX, and X)
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22
Q

Warfarin

Onset of action

A

Delayed (hours to days)

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23
Q

Warfarin

Administration route

A

Oral

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24
Q

Warfarin

Elimination

A

Hepatic metabolism – CYP2C9

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25
Q

Warfarin

Monitoring lab test

A

INR (from PT)

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26
Q

Warfarin
Adverse Effects?
narrow therapeutic index

A

Bleeding, skin necrosis

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27
Q

Warfarin

Safety in pregnancy

A

NOT safe –> Category X

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28
Q

Warfarin
DDIs
NSAIds Incr bleeding risk with all anticoagulants?

A

incr effect: CYP450-inhibitors, abx,

decr effect: CYP450 inducers, dietary Vit K

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29
Q

Warfarin

Overdose Treatment Protamine

A

Phytonadione (Vit K1) – FFP

30
Q

Warfarin

Uses

A

A Fib / VTE prophylaxis

31
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Mechanism of Action

A

[D] Direct thrombin (IIa) inhibitor

[R]-[A] Direct factor Xa inhibitor

32
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Onset of action

A

[R]-[A]: peak action 2.5-4h

33
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Administration route

A

[D] Oral – administered as prodrug

[R]-[A] Oral

34
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Elimination

A

[D] Primarily renal (decr dose if renal impairment) - BID

[R]-[A] hepatic CYP3A, [A] BID

35
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Monitoring lab test

A

[D]-[R] not routinely monitored

for [D] can use ECT-precise or aPTT qualitative if needed

36
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Adverse Effects

A

[D] Bleeding, gastritis symptoms

[R] Bleeding

37
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Safety in pregnancy

A

[D]-[R]-[A] Category C– not studied

38
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
DDIs
NSAIds Incr bleeding risk with all anticoagulants?

A

decr effect: [D]-[R]-[A] P-glycoprotein inducers (rifampin, dronedarone)

incr effect: [D]-[R]-[A] P-glycoprotein inhibitors;
[R] CYP3A4 inhibitors

39
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Overdose Treatment

A

[D]-[R]-[A] no specific antidote

hemostatic measures: FFP, RBCs

40
Q

Dabigatran [D]
Rivaroxaban [R] – Apixaban [A]
Uses

A
[D] A Fib (FDA approved), VTE
(non-FDA approved)
[R] A Fib, DVT-PE prevention after
total hip or knee replacement
[A] A Fib
41
Q

Aspirin

Mechanism of Action

A

Low dose (81 mg) “selective”
inhibition of platelet COX-1
(irreversible)

42
Q

Aspirin

Onset of action

A

Can be rapid

43
Q

Aspirin

Administration route

A

Oral-once daily

44
Q

Aspirin

Elimination

A

Hepatic

45
Q

Aspirin

Adverse Effects

A

Gastric upset, bleeding

46
Q

Aspirin

Safety in pregnancy

A

Pregnancy category C/D (3rd)

47
Q

Aspirin

DDIs

A

incr bleeding risk w/anticoagulants

48
Q

Aspirin

Uses

A

Acute MI-Unstable angina (ACS)

PCI / 2° prevention MI-stroke

49
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Mechanism of Action

A

Inhibition of platelet ADP
(P2Y12) receptor
[C]-[P] irreversible
[T] reversible

Efficacy ([P]-[T] > [C])

50
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Onset of action

A

Onset-2 hrs; peak 2-5 hrs if loading

dose used, otherwise 3-7 days

51
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Administration route

A

[C]-[P] Oral prodrug-once daily

[T] Oral – twice daily

52
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Elimination

A
 then renal and fecal excretion  [P]: activated by CYP3A4/2B6 [T]: CYP3A4 metabolism to active metabolite
53
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Adverse Effects

A

Bleeding ([P]-[T] > [[C])
[C]: Dyspepsia, gastritis, HA
[T]: Dyspnea, bradyarrhythmias

54
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Safety in pregnancy

A

[C] Pregnancy category B

[P]-[T] Pregnancy category C

55
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
DDIs

A

NO DDI with [P] + PPIs

56
Q

Ticagrelor [T]
Clopidogrel [C]-Prasugrel [P]
Uses

A

Acute MI-Unstable angina,

PCI

57
Q

Dipyridamole

Mechanism of Action

A

Inhibits phosphodiesterase in platelets –>
incr cAMP –> incr PGI2
anti-aggregation effect

58
Q

Dipyridamole

Onset of action

A

dfdf

59
Q

Dipyridamole

Administration route

A

Oral

60
Q

Dipyridamole

Elimination

A

Hepatic: phase II conjugation

61
Q

Dipyridamole

Adverse Effects

A

Dizziness, HA, nausea, GI upset

62
Q

Dipyridamole

Safety in pregnancy

A

Pregnancy category B

63
Q

Dipyridamole

DDIs

A

dfdf

64
Q

Dipyridamole

Uses?

A

2° prevention MI-stroke

65
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Mechanism of Action

A
Blocks platelet GIIb/IIIa receptor 
     preventing fibrinogen binding and 
      platelet aggregation
[A]: monoclonal antibody
[E]: cyclic peptide 
[T]: non-peptide
66
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Onset of action

A

Rapid onset

67
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Administration route

A

Parenteral infusion

68
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Elimination

A
69
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Adverse Effects

A

Bleeding

70
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Safety in pregnancy

A
71
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
DDIs

A

kjk

72
Q

Abciximab [A]–Eptifibatide [E]
Tirofiban [T]
Uses

A

PCI