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Pharmacology > Antithrombotics > Flashcards

Antithrombotics Flashcards

1
Q

Antiplatelet drug classes (4)

A

COX-1 inhiitors
PDE inhibitors
ADP receptor antagonists
GP IIb/IIIa antagonists

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2
Q

ADP-recpetor antagonist

A

clopidogrel

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3
Q

GP IIb/IIIa antagonist

A

abciximab

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4
Q

MOA of clopidogrel

A

Irriversibly antagonizes ADP receptor reducing inactivation of AC, increasing cAMP and increasing PKA, leading to reduced platelet aggregation

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5
Q

MOA of abciximab

A

binds to GP to prevent them from crosslinking through fibrinogen bridge

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6
Q

Pharmaco genetics of clopidogrel

A

prodrug metabolized by CYP2C19. Black boxed warning

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7
Q

Pharmacokinetics of clopidogrel

A

orally effective, maximal efficacy 8-11 days

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8
Q

Therapeutic use of colpidogrel

A

alternative to low dose asprin
reduces rate of stroke, MI and death in those with recent stroke, MI, ACS, PAD
In combination with asprin for prevention of coronary stent thrombosis and ACS

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9
Q

Adverse effects of colpidogrel

A

bleeding

thrombotic thrombocytopenic purpura

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10
Q

Drug interactions with colpidogrel

A

avoid NSAIDS

CYP2C19 inhibitors, omeprazole

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11
Q

Pharmacokinetics of abciximab

A

half life 10 min duration of action 48 hours due to irreversible binding

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12
Q

Therapeutic use of abciximab

A

most effective, most expensive

short term in combo with asprin to prevent ischemic events in hospital setting

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13
Q

Adverse effects of abciximab

A

bleeding, anaphylaxis

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14
Q

Heparin MOA

A

indirect inhibitors of thrombin and/or Xa through antithrombin

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15
Q

Enoxaparin MOA

A

~17 saccharide heparin

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16
Q

Fondaparinux MOA

A

pentasaccharide heparin

17
Q

Pharmacokinetics of heparin

A

immediate onset
parenteral
“sticky,” must monitor aPTT
LMWH/fondaparinux- don’t need to monitor aPTT

18
Q

Selectivity of heparins

A

Heparin inactivates thrombin and Xa
LMWH inactivates Xa well, thrombin poorly
Fondaparinux inactivates Xa only

19
Q

Therapeutic use of heparin

A

initial treatment of DVT/PE
transition to warfarin
safe in pregnancy

20
Q

Adverse effects of heparin

A

bleeding, protamine sulfate antidote

HIT/HITT - CBC needed

21
Q

Alternative anticoagulants in HIT

A

bivalirudin, fondaparinux

22
Q

Vitamin K antagonist

A

warfarin

23
Q

MOA of warfarin

A

inhibits synthesis of K-dependent clotting factors by inhibiting VKOR1C in the liver

24
Q

Pharmacokinetics of warfarin

A

oral
delayed onset, dependent on clotting factor turnover
metabolized by CYP2C9

25
Q

Dosing of warfarin

A

must be monitored by PT/INR

26
Q

Therapeutic use of warfarin

A

prevent progression of recurrence of DVT or PE
Prevention of thromboembolism in patient with prosthetic heart valves
not useful in an emergency

27
Q

Adverse effects of warfarin

A

boxed warning for bleeding
antidote is vitamin K, takes hours, for immediate need- prothrombin complex concentrate (PPC) or plasma.
Teratogen

28
Q

Drug interactions with warfarin

A

CYP inhibitors
displacement of plasma albumin
broad spectrum antibiotics
anything that promotes bleeding

Reduce warfarin effect
CYP inducers
excessive vitamin K

29
Q

Direct inhibitors of thrombin

A

bivalirudin- parenteral

dabigatran etexilate- oral

30
Q

bivalirudin MOA

A

binds to and inhibits thrombin

31
Q

Pharmacokinetics of bivalirudin

A

given IV and monitored by aPTT, short half life, excreted by the kidney

32
Q

Therapeutic use of bivalirudin

A

used for HITT and during PCI

33
Q

Adverse effect of bivalirudin

A

bleeding

34
Q

Pharmacokinetics of dabigatran etexilate

A

orally active
onset 2-3 hrs
dosed 2x per day without monitoring

35
Q

Therapeutic use of dabigatran

A

“warfarin replacement”

no monitoring required

36
Q

Adverse effect of dabigatran

A

bleeding with no antidote

37
Q

Thrombolytic agents

A

t-PA

38
Q

MOA of t-PA

A

activates plasminogen and breaks up fibrinogen clot.

39
Q

Therapeutic use of t-PA

A

within the first three hours after MI

Pharmacology (35 decks)

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