Heparin Anticoagulants II Flashcards

1
Q

What are the main uses of the oral anticoagulants?

A

Prophylactic use: Prevention of thrombotic disorders

Therapeutic use: Treatment of established thrombus

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2
Q

What is the main oral anticoagulant?

A

Warfarin

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3
Q

What are the targets for warfarin action?

A

Factor II, VII, IX and X

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4
Q

What is the MOA of the coumarins (oral anticoagulants)?

A

All agents depress the formation of functional forms of factors II (prothrombin), VII, IX and X by inhibiting the ๐›„-carboxylation of glutamic acid in these proteins which is essential for Ca+2 binding.

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5
Q

How does warfarin inhibit the ๐›„-carboxylation of glutamic acid?

A

Inhibits the action of Vitamin K reductase

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6
Q

What is the onset of action of warfarin like?

A

Slow as it has an effect on the liver with enzyme synthesis

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7
Q

What is the function of Vitamin K?

A

It is essential for the attachment of Ca2+ binding group to prothrombin and for the synthesis of Factor II/VII/IX/X

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8
Q

What is the oral absorption of warfarin?

A

All are well absorbed orally

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9
Q

What is the half life of warfarin like?

A

Long T1/2 of the oral anticoagulants, due to binding to plasma albumin - warfarin is 97% bound

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10
Q

What pathway does warfarin inhibit?

A

Extrinsic Pathway

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11
Q

What is the therapeutic target with warfarin dosing?

A

1.5 times the prolongation of the normal bleed time

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12
Q

What is used to monitor warfarin dosing?

A

PT/INR

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13
Q

What are some factors that can affect warfarin dosing?

A
  • ๔ฐ€Nutrition - too many green leafy vegetables will increase Vitamin K
  • Anemia
    ๔ฐ€- Liver disease - will decrease production of clotting proteins so warfarin will have increased activity
    ๔ฐ€- Biliary obstruction ๔ฐ€
  • Drugs
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14
Q

How can drugs cause warfarin potentiation?

A

a. by causing vitamin K deficiency.
b. by displacing warfarin from protein binding sites.
c. by decreasing clotting-factor synthesis.

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15
Q

How can drugs inhibit the action of warfarin?

A

a. by decreasing warfarin absorption.

b. by enhancing warfarin metabolism.

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16
Q

What are some SE of warfarin?

A
  • Bleeding, coumadin induced necrosis
  • Ecchymosis/purpura/hematuria
  • Has interaction with several medications which results in bleeding due to potentiating the effect of warfarin
  • Bone malformations in the fetus
17
Q

What is warfarin overdose treated with?

A

A. Replacement of 4 factors. Infusion of whole fresh blood or frozen plasma.
B. Recombinant Factor VIIa
C. Vitamin K

18
Q

What are the new oral anticoagulants?

A

Rivaroxaban
Apixaban
Edoxaban
Dabigatran

19
Q

What are the Xa inhibitors of the new oral anticoagulants?

A

Rivaroxaban
Apixaban
Edoxaban

20
Q

What are the antithrombin inhibitors of the new oral anticoagulants?

A

Dabigatran

21
Q

What is the main route of administration of warfarin?

A

Oral

22
Q

What is the site of action of heparin?

A

Blood

23
Q

What is the site of action of warfarin?

A

Liver

24
Q

What is the onset of action of heparin and warfarin like?

A

Heparin has a rapid onset and warfarin has a slow onset

25
Q

What is the MOA of heparin?

A

Activates AT, which inhibits FXa and thrombin

26
Q

What is the MOA of warfarin?

A

Impairs the synthesis of factors II, VII, IX and X (vit. K antagonist

27
Q

How is the effect of heparin reversed?

A

Protamine sulfate

28
Q

How is the effect of warfarin reversed?

A

IV vitamin K and fresh frozen plasma

29
Q

Does heparin cross the placenta?

A

No

30
Q

MOA of Vitamin K

A

Cofactor in the synthesis of functional forms of factors II, VII, IX and X

31
Q

Indications for Vitamin K

A

Hypoprothrombine mia, intestinal disorders and gastrectomy, reverses the effects of warfarin

32
Q

SE of Vitamin K

A

Hemolysis

33
Q

Rivaroxaban and Apixaban MOA

A

Inhibits factor Xa

34
Q

Rivaroxaban and Apixaban Indications

A

Stroke prevention in patients with AF

Rivaroxaban also approved for prophylaxis and treatment of DVT

35
Q

Rivaroxaban and Apixaban SE

A

Bleeding and liver toxicity

36
Q

Dabigatran MOA

A

Inhibits thrombin

37
Q

Dabigatran Indications

A

Stroke prevention in patients with AF

38
Q

Dabigatran SE

A

Bleeding and liver toxicity