Pharm: Anti-platelets and Anti-Coagulants Flashcards

1
Q

Warfarin

A

anticoagulant (Coumadin)

  • inhibits vitamin K -dependent posttranslation modification of clotting factors: thrombin, VII, IX, X protein C and S
  • onset is 36-72 hours (t1/2 is 25-60 hours)
  • highly fat soluble, delayed termination
  • taken orally
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2
Q

Unfractionated Heparin

A
  • anticoagulant
  • binds Antithrombin III which inactivates: thrombin, IX, X, XI, XII
  • Given IV or SQ (for surgeries)
  • NOT given orally
  • onset is immediate w/ bolus injection
  • t1/2 = 1-2 hours
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3
Q

Low MW Heparin

A

anticoagulant

ex. Enoxaparin (Lovenox)

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4
Q

Fondaparinux

A

synthetic analog of heparin; injected SQ

indicated: tx of UA/NSTEMI, acute MI, prevention of DVT, tx of PE

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5
Q

Dabigatran

A

= new oral antigoaculant

  • direct thrombin inhibitor
  • used for prevention of stroke
  • monitoring via INR is not required and bleeding is less than warfarin
  • more expensive than warfarin
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6
Q

Aspirin

A

= Anti-platelet

  • irreversibly inhibits thromboxane formation (activator of platelet aggregation), via inhibition of COX-1
  • higher doses inhibit formation of prostacyclin (vasodilator)
  • used to tx MI, stroke and PAD
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7
Q

Clopidogrel

A

= Anti-platelet
-blocks platelet aggregation by inhibiting ADP receptor, thus blocking ADP mediated activation of GPIIB/IIIa complex –> inhibits fibrinogen binding and platelet aggregation

  • indications: prophylaxis of stroke, MI, PAD, ACS
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8
Q

Dipyridamole

A

= Anti-platelet- blocks platelet aggregation through inhibiting cAMP, weak vasodilator
- used to prevent MI and stroke, and thromboembolism

** often used in combo with aspirin **

headaches are a problem

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9
Q

Abciximab

A

= Anti-platelet, GPIIb/IIIa inhibitor

  • prevents fibrinogen from binding to GP IIb-IIIa, thus inhibiting platelet aggregation
  • greater antithrombotic activity than aspirin or heparin

tx: used for acute coronary syndromes, PCI, angiopalsty

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10
Q

Alteplase

A

rt-PA

= thrombolytic

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11
Q

Reteplase

A

= thrombolytic

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12
Q

Tenecteplase

A

= thrombolytic

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13
Q

Streptokinase

A

= thrombolytic

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14
Q

how to prevent pathologic thrombus?

A
  • used to just use heparin/warfarin

- now try to inhibit platelet aggregation with aspirin, clopidogrel or abciximab

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15
Q

white clot vs. red clot?

A

white clot = due to arterial wall damage, atherosclerotic plaque - plugs break away asn arterial thrombus

red clot = due to stasis, see long fibrin tail with central core of RBCs that are clotted. Fibrin tail or red clot breaks away as venous trhombus –> distant embolism

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16
Q

to check UFH?

A

aPTT time: 1.5-2.5
thrombin time
(at high dose it will also increase PT)

17
Q

to check LMWH?

A

no testing necessary

18
Q

to check Warfarin

A

PT test converted to INR

INR should be 2.5-3.5

19
Q

S/E of Heparin?

A
  • hemorrhage
  • thrombocytopenia: HIT syndrome (due to formation of Abs directed against the heparin-platelet factor 4 complexes)

If overdose: stop administration, administer protamine Sulfate (binds to and inactivates heparin, but is not an antidote for warfarin), give fresh-frozen plasma

20
Q

indications of UFH?

A
  • prophylaxis of postop thrombosis (SQ)
  • MI or unstable angina
  • DVT or PE
  • DIC
  • TIA - effective but risky, not used if stroke is in progress

small doses: prevent thromboembolism
medium doses: prevent propogation of thrombus
large doses: inhibit established PE

If prolonged anticoagulation is necessary, the initial heparin therapy is overlapped with and then replaced with oral anticoagulant, i.e., warfarin

21
Q

HIT type 1

A

Heparin induced thrombocytopenia

transient, reversible clumping of platelets
platelet count >100,000
Usually occurs within first few days of therapy
Usually asymptomatic and recover OK even if heparin continued.

22
Q

HIT Type II

A

delayed onset (5-14 days)
severe thrombocytopenia (platelet counts< 100,000).
This is an immune-mediated reaction, a heparin-antibody complex caused significant platelet aggregation.
Recovery can be delayed and consequences of peripheral thrombosis can be severe, including stroke, acute MI, skin necrosis. Amputation is necessary in up to 25% of patients with Type II HIT and mortality approaches 25%.
Incidence of Type II HIT is about 3% of all treated

23
Q

Heparin CI’s?

A

Any site of active or potential bleeding
Severe hypertension or known vascular aneurysm
Recent head, eye, or spinal cord surgery
Head trauma
Lumbar puncture or regional anesthetic block
Tuberculosis, visceral carcinoma, GI ulcers

24
Q

aPTT

A

tests intrinsic pathway: Ca2+ ion is added and charged surface are contacted

used to monitor unfractionated heparin therapy: 1.5 to 2.0 times control

25
Q

Enoxaparin

A

(Lovenox) = LMWH

  • smaller pieces of heparin w/ greater anti-Xa activity
  • less anti-platelet activity
  • used SQ for prophylaxis of DVT assoc. w/ hip, knee or abdominal surgery
  • longer duration
  • clotting tests not necessary
  • unlike UFH, it lasts 2-5 times longer, doesn’t bind proteins, doesn’t bind endothelial cells and is not dose-dependent clearing
26
Q

Toxocity of Warfarin?

A

hemorrhage, anorexia, nausea, vomiting, skin necrosis (due to thrombosis in microcirculation)

27
Q

CI’s of warfarin?

A

pregnant pt, recent bleeding, surgery, aneurysms

** this is the king of drug:drug interactions - can result in serious bleeding

  • pt. variation is high, should not give to unreliable pt.
28
Q

Indications of Warfarin

A

overlap w/ heparin therapy to avoid long delay in onset of action

  • DVT
  • PE
  • Atrial Fib
  • RHD
  • mechanical and prosthetic valves
29
Q

test to monitor warfarin?

A

PT test converted to INR (INR 2.5-3.5)

  • it is administered with heparin until target INR is achieved, and then pt. is just on warfarin
30
Q

Rivaroxaban

A

new drug like warfarin

31
Q

Apixaban

A

new drug like warfarin

32
Q

lepirudin, bivalirudin, argotroban

A

direct thrombin inhibitors - used for HIT and for coronary angioplasty

33
Q

thrombolytic/fibrinolytic agents?

A

alteplase (rt-PA), reteplase, tenecteplase, streptokinase

  • clots are dissolved by plasmin, which is formed from tPA
  • indications: Acute MI, PE, DVT, stroke

adverse effects: serious hemorrhage!

34
Q

PT test

A

used to test extrinsic pathway

  • monitors Warfarin therapy
  • add CA2+ ion and thromboplastin (contains tissue factor)
  • use INR to corret for PT times