Anticoagulation therapy Flashcards

1
Q

Classes of antithrombotic drugs

A
  1. Heparin, oral anticoagulants
  2. Fibrinolytic agents
  3. Antiplatelets
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2
Q

Antithrombotic drug needs to balance between ____ and ____

A

efficacy

toxicity

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3
Q

Heparin is normally in _________

A

granules of mast cells

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4
Q

Difference in 3 forms of heparin:

A

Size

Antithrombin binding to Xa (all) or both Xa and THrombin (unfractionated)

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5
Q

Heparin binds to ______ and it’s effect is ______

A

antithrombin;

INcrease rate by 1000x

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6
Q

Unfractionated heparin is given ______, has ____ pharmacokinetics

A

IV/SC (immediate/delayed)
Poor - poor bioavailability, short half life
(requires hospital admission)

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7
Q

Unfractionated heparin and pregancy

A

Drug of choice - does NOT cross placenta

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8
Q

LMWH/Fondaparinux is given ____ and has _____ pharmacokinetics

A

SC
Better - (bioavail + predictable dose response)
(outpatient treatment)

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9
Q

Heparin is used for

A
DVT/PE + oral anticoag + FIbrinolytic drugs
Unstable angina/A. MI
Coronary angioplasty/stent placement
Surgery + cardiopulm. bypass
Kidney dialysis
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10
Q

Heparin toxicity

A

Bleeding
HIT (heparin induced thrombocytopenia)
Allergic events

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11
Q

Heparin bleeding toxicity fixed by:

A

–> reverse with protamine sulfate (positively charged)

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12
Q

HIT is caused by

A

platelet factor 4/heparin complex (antibody - to platelets)

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13
Q

LMWH Heparin examples

A

lovenox, enoxaprin, dalteparin, nadroparin

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14
Q

Pentasaccharide heparin examples

A

Fondaparinux, Arixtra

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15
Q

Warfarin (oral anticoagulant) acts by:

A

Vit K analogue - blocks vit K reductase

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16
Q

Warfarin Pharmacokinetics

A

90 min absorbed
36-48 half life
full effect needs to wait 2-3 days

17
Q

Wafarin used to prevent:

A

Venous thromboembolism
Systemic embolisms (prosthetic heart valves, atrial fibrillation)
Stroke/recurrent infarction/AMI

18
Q

Warfarin adverse effects

A

hemorrhage

Teratogenic

19
Q

Warfarin and pregancy

A

DO NOT USE - cross placenta

20
Q

Reverse warfarin effect:

A

stop drug, give vit K

Plasma transfused - replace coagulation factors

21
Q

Warfarin DDI (list a few examples to enhance effect)

A

platelet function - aspirin
Decrease vit K absorption - antibiotics
Displace warfarin - clofibrate/phenytoin
Reduce metabolism/elimination - cimetidine, amiodorone, phenylbutazone

22
Q

Warfarin DDI (list a few examples to decrease effect)

A

increase metabolism - barbituates/ripamin

Decrease warfarin absorption - cholestyramine

23
Q

What are the “new oral anticoagulants” do?

A

DIrect thrombin/Factor Xa inhibitors

24
Q

New oral anticoagulants advantages

A

rapid onset
no food interaction
no monitoring

25
Q

New oral anticoagulatns disadvantages

A
bad with kidney disease
short t1/2
more GI bleed
High cost
No antidote
26
Q

Examples of new anticoagulants

A
Dabigatran Etexilate (Pradaxa)
Apixaban (Eliquis)
Rivaroxaban (Xarelto)
27
Q

Dabigatran Etexilate (Pradaxa) uses + notes

A

atrial fibrillation
Less intracranial hemmorhage - increase MI
NOT in pt with prosthetic heart valves

28
Q

Apixaban (Eliquis) used for

A

atrial fibrillation

29
Q

Rivaroxaban (Xarelto) used for + notes

A

Atrial fib + VTE
DIrectly inhibits Xa
Prevent strokes/emboli better than warfarin

30
Q

Fibrinolytic agents include

A

tPA (alteplase)
uPA (abbokinase)
Streptokinase (Streplase)

31
Q

Differences between tPA and uPA agents

A

tPA binds to fibrin –> cleaves plasminogen

uPA does NOT bind fibrin - converts plasminogen directly

32
Q

How does streptokinase work?

A

non-enzymatic protein - complex w/ plasminogen –> activate/convert

33
Q

Fibrinolytic agent uses:

A

AMI + aspirin
Ischemic stroke (w/in 3 hr)
DVT
PE

34
Q

Fibrinolytic agent side effects

A

hemorrhage
Systemic lytic state - increase plasmin
Allergic reaction/Ab to streptokinase

35
Q

Antiplatelet drugs target:

A

platelet production, ADP receptor (activation/aggregation), block adhesion proteins

36
Q

ADP receptor antongists examples:

A

thienopyridines (clopidogrel/ticlopidine/prasugrel) - slow - need metabolism to activate
Ticagrelor - ATP analoge

37
Q

ADP receptor antagonists bind:

A

ADP receptor P2Y12

38
Q

Glycoprotein IIb/IIIa inhibitors include

A

abciximab - mAb
Eptifibatide - cyclic peptide inhibitor
Tirofiban - small molecule inhib

39
Q

Glycoprotein IIb/IIIa inhibitors adverse effect/fix

A

bleeding/thrombocytopenia

Reverse with platelet infusions