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Pharmacology > Anticoagulants > Flashcards

Anticoagulants Flashcards

1
Q

Antiplatelet drugs

A

Asprin, Clopidogrel

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2
Q

Antithrombin III catalysts

A

Heparin
Enoxaparin
Fondaparinux

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3
Q

Thrombin Inhibitors

A

Dabigatran
Rivaroxaban
(Apixaban) - not on drug list

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4
Q

Clotting factor synthesis inhibitors

A

Warfarin

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5
Q

Heparin chemistry

A

Naturally occuring highly acidic polysaccharide. Available as unfractionated or low molecular weight.

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6
Q

Antithrombin III catalysts mechanisms

A

Activate antithrombin III so it can inactivate IIa and Xa.

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7
Q

Antithrombin III

A

Complexes with and inhibits the activated protease clotting factors.

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8
Q

Unfractionated heparin

A

Long chains - bridges thrombin-antithrombin molecules and serves as a template for interaction of antithrombin III and Factor IIa

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9
Q

Low molecular weight heparin

A

Cannot bridge, but accelerate the interaction of Antithrombin III and Xa

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10
Q

Heparin ADME

A 
IV only
Distributed in blood
Metabolized by reticuloendothelial system (monocytes and macrophages)
Does not cross placenta
Renal Excretion
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11
Q

Enoxaparin - what is it?

A

Low molecular weight heparin

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12
Q

Do you need to routinely monitor activity with Heparin? What about with Enoxaparin? Fondaparinux?

A

Only HEPARIN!

You must monitor anticoagulant action by checking aPTT - 2x control time.

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13
Q

Fondaparinux ADME

A

SC
Long T 1/2 - up to 21 hrs.
Fixed doses without monitoring activity.

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14
Q

Adverse effects of LMW heparins and fondaparinux

A

BLEEDING

Transient thrombocytopenia - 25%

Severe thrombocytopenia - 5%

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15
Q

Heparin induced Thrombocytopenia

A

Antibody-mediated thrombocytopenia - Antibodies to Platetelet-factor 4 complexes - aggregation and embolism.

WARFARIN IS CONTRAINIDICATED IN HIT

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16
Q

Heparin indications

A

Prevention of DVT / PE

Acute MI / unstable angina

Prevention of thrombosis in extracorporeal devices.

17
Q

Heparin Contraindications

A

Hypersensitivity, active bleeding, threatened abortion, infective endocarditis, and surgery.

18
Q

Heparin Antagonist - not on drug list

A

Protamine Sulfate

19
Q

LMW Heparin Indications

A

Prevention of DVT, Thromboembolism

20
Q

Fondaparinux Indications

A

PE, DVT, Antithrombic therapy for Heparin induced thrombocytopenia

21
Q

Warfarin Chemistry

A

Inhibits addition of gamma carboxy groups to clotting factors VII, IX, X, II (prothrombin), making them inactive.

22
Q

Warfarin ADME

A

PO
Protein Bound
Hepatic - CYP2C9
Renal

23
Q

Warfarin Adverse Effects

A

Bleeding
Hemorrhagic disorder in fetus - birth defects
Procoagulant State due to inhibition of protein C and S, leading to cutaneous necrosis during first week of therapy.

24
Q

Warfarin DDI’s

A

All of them

Note - warfarin is a vitamin K antagonist - large amounts of vitamin K can reverse warfarin action.

25
Q

Dabigatran Mechanism

A

Inhibits factor IIa by blocking active site.

26
Q

Rivaroxaban, Apixaban mechanism

A

Inhibits factor Xa by blocking active site.

27
Q

Dabigatran metabolism and adverse effects

A

Prodrug - metabolized to active form

Adverse - bleeding

28
Q

Dabigatran DDI’s

A

P-glycoprotein inhibitors enhance effects (rifampin)

29
Q

Rivaroxaban adverse effects

A

Surprise! Bleeding!

30
Q

Rivaroxaban DDI’s

A

P-glycoprotein inhibitors (rifampin) enhance effects.

Cyp 3A4 inducers decrease effects

31
Q

Clopidogrel mechanism

A

Inhibits activation of platelets via ADP pathway - does not effect prostaglandin pathway so you can use it if you’re allergic to asprin

32
Q

Can you use clopidogrel and asprin together?

A

Yes - they are synergystic

33
Q

Clopidogrel adverse

A

Rash, diarrhea, abd pain, bleeding.

Thrombocytic Thrombocytopenia has been reported.

34
Q

Abciximab mechanism

A

Blocks IIb/IIIa receptors - platelet cell surface proteins that anchor platelets to surfaces and each other when activated.

Pharmacology (11 decks)

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