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B&L Exam 2 > Anticoagulants & thrombolytics-Mata > Flashcards

Anticoagulants & thrombolytics-Mata Flashcards

1
Q

Heparin

A

MOA: binds to endogenous antithrombin III and irreversibly inactives thrombin

  • Given parenterally
  • Speeds up antithrombin action 1000x
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2
Q

Unfractionated heparin

A
  • Begins working immediately
  • Used in combo w/thrombolytics for revascularization
  • Does NOT cross placental barrier so ok for preggos
  • IV or SC to avoid hematoma
  • Speeds up activity on factor XA
  • Prophylaxis for DVT
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3
Q

Low Molecular Weight (LMW) Heparin & Foundparinux

A
  • Binds antithrombin and has same inhibitory effect on XA as unfractionated heparin
  • More selective (no effect on thrombin)
  • IV or SC (longer half-life after SC)
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4
Q

Heparin toxicity

A
  • Increased bleeding time is common adverse effect of heparin and related molecules
  • Can lead to hemorrhagic stroke
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5
Q

Protamine

A
  • Lessens risk of serious bleeding w/heparin
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6
Q

Major Side Effects of Heparin

A
  1. Non-immune mediated Heparin–associated thrombocytopenia (HAT) Type I - common; direct run b/n heparin and platelets
  2. Immune-mediated Heparin-induced thrombovytopenia (HIT) Type II - FATAL
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7
Q

Rivaroxaban

A
  • MOA: direct inhibitor of factor XA that inhibits both free and clot bound factor XA
  • Uses: prophylaxis for DVT, reducing stroke risk
  • Risk of thrombotic events upon premature discontinuation
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8
Q

Lepirudin

A
  • Direct thrombin inhibitor
  • Recombinant form of hirudin
  • Alternative to heparin
  • Irreversibly binds and inhibits free and fibrin bound thrombin
  • Cons: prolonged half-life in renal compromised pts
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9
Q

Desirudin & Bivalirudin

A
  • Direct thrombin inhibitor
  • Modified forms of hirudin
  • Bivalrudin also inhibits platelet activation
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10
Q

Direct thrombin inhibitors

A

Based on leech protein hirudin that directly binds to thrombin to prevent thrombin-mediated activation of fibrinogen and factor XIII

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11
Q

Argatroban

A
  • Small molecule direct thrombin inhibitor (binds only to active site of thrombin)
  • Used for treatment of patients with heparin-Induced thrombocytopenia (HIT)
  • Safe to be given in renal insufficiency (excrete via biliary route)
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12
Q

Dabigatran

A
  • Small molecule direct thrombin inhibitor (binds only to active site of thrombin)
  • No need to monitor blood levels
  • Greater predictive PK and PD
  • No dose adjustments
  • No significant drug-interactions
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13
Q

Warfarin

A
  • MOA: inhibits Vitamin K epoxide reductase needed for coagulation cascade
  • Affects factor II, VII, IX & X
  • Mimics Vitamin K (Vit K can also reverse it)
  • SE: bleeding, transient period of hypercoagulaility, inhibition of protein C
  • Narrow therapeutic range
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14
Q

Tissue Plasminogen Activator (tPA) (aka - Thrombolytic Agents)

A
  • An enzyme that binds to fibrin in a newly formed clot and directly converts plasminogen to plasmin
  • Toxicity can cause cerebral hemorrhage
  • Increases risk of bleeding with warfarin, heparin, aspirin
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15
Q

Alteplase

A
  • Thrombolytic (fibrinolytic) Agent

- Normal human tPA

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16
Q

Reteplase

A
  • Thrombolytic (fibrinolytic) Agent

- Mutated tPA w/similar effects but faster onset of action and longer duration of action

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17
Q

Tenecteplase

A
  • Thrombolytic (fibrinolytic) Agent

- Mutated form of tPA w/longer half life

18
Q

Anistreplase

A

A preformed complex of streptokinase and plasminogen

19
Q

Platelet Activation

A

Mediated by release of soluble platelet factors (ADP, TxA2)

20
Q

Aspirin

A
  • Irreversible inhibitor of COX1 (which makes TxA2)
  • Efficacy is not dose related
  • High doses can lead to GI bleeding and ulceration
  • So prescribe baby aspirin!
21
Q

Thienopyridines

A
  • MOA: irreversible inhibitors of platelet ADP receptors

- BBW: bleeding

22
Q

Ticlopidine

A
  • Thienopyridine
  • Converts to thiol metabolites that accumulate (therefore delay in action)
  • Takes 8-11 days for max effect
  • Shorten delay w/aspirin or loading dose
  • BBW: life threatening hematological adverse runs including neutropenia, TTP, and aplastic anemia
23
Q

Clopidogrel

A
  • Thienopyridine
  • Metabolized by CYP2C19
  • Poor metabolizers may show higher rates of CV SEs
  • BBW: diminished effectiveness in poor metabolizers
24
Q

Prasugrel

A
  • Thienopyridine
  • More effectively metabolized than clopidogrel so greater P2Y ADP antagonism
  • Metabolized via CYP3A4
25
Q

Ticagelor

A
  • Thienopyridine
  • Parent drug and major metabolite reversibly interact w/P2Y12 ADP receptor
  • Both parent and metabolite are equipotent
  • Metabolized via CYP3A4
  • BBW: bleeding risk
26
Q

Abciximab

A
  • Platelet glycoprotein IIb/IIIa receptor blocker
  • MOA: bind to IIb/IIIa and prevent interaction w/fibrinogen
  • Chimeric mouse/human monoclonal Ab
27
Q

Eptifibatide & Tirofiban

A
  • Platelet glycoprotein IIb/IIIa receptor blockers
  • MOA: bind to IIb/IIIa and prevent interaction w/fibrinogen
  • Small molecule inhibitors
28
Q

Phosphodiesterase Inhibitors

A

2 MOAs:

  1. Block uptake of adenosine which stimulate platelet adenylyl cyclase
  2. Inhibits platelet phosphodiesterase which leads to increased intracellular cAMP and decreased platelet aggregation
29
Q

Cilostazol

A
  • Phosphodiesterase Inhibitor
  • Used to treat intermittant claudication (manifestation of peripheral arterial disease)
  • Not for pts w/CHF!
30
Q

Dipyridamole

A
  • Phosphodiesterase Inhibitor
  • Used + Warfarin to prevent thrombus on prosthetic heart valves
  • Used + Aspirin to lower incidence of thrombotic diathesis
31
Q

Fibrinolytic Inhibitors

A

MOA: lysine analog that blocks plasmin fibrin interaction

32
Q

Aminocaproic Acid

A
  • Fibrinolytic Inhibitor
  • Used to reduce bleeding in hemophiliacs after prostatic surgery or tooth extractions
  • Thrombi that form during drug treatment do not get lysed
33
Q

Tranexamic Acid

A
  • Fibrinolytic Inhibitor

- Used to control heavy menstrual bleeding

34
Q

Vitamin K

A
  • Hemostatic agent
  • MOA: essential cofactor required in γ-carboxylation of several clotting factors (II, VII, IX and X)
  • Used in reversing bleeding episodes induced by oral anticoagulants
  • Caution: fast IV infusion can lead to dyspnea, chest pain and death
35
Q

Which drugs are anticoagulants? (4)

A
  1. Heparin
  2. Unfractionated Heparin
  3. LMW Heparin & Foundparinux
  4. Rivaroxaban
36
Q

Which drugs are Direct Thrombin Inhibitors? (4)

A
  1. Lepirudin
  2. Desirudin & Bivalrudin
  3. Argatroban
  4. Dabigatran
37
Q

Which drugs are Thrombolytic Agents? (3)

A
  1. Ateplase
  2. Reteplase
  3. Tenecteplase
38
Q

Which drugs are Thienopyridines? (4)

A
  1. Ticlopidine
  2. Clopidogrel
  3. Prasugrel
  4. Ticagelor
39
Q

Which drugs are Platelet Glycoprotein IIb/IIIa receptor blockers? (2)

A
  1. Abciximab

2. Eptifibatide & Tirofiban

40
Q

Which drugs are Phosphodiesterase Inhibitors? (2)

A
  1. Cilostazol

2. Dipyridamole

41
Q

Which drugs are Fibronlytic Inhibits? (3)

A
  1. Aminocaproic Acid
  2. Tranexamic Acid
  3. Vitamin K

B&L Exam 2 (8 decks)

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