Anticoagulants (Drugs)

Question 1

Warfarin

Answer 1

Vitamin K Reductase Antagonist
- Anticoagulant

MOA:
- Reduced Vit K is needed for carboxylation of glutamic acid
–> Without Reduced Vit K clotting factors remain inactivated (remains +)
–> Can not bind to negatively charged surfaces of platelets via Ca2+

• Only affects new clotting factors, have to wait for old active clotting factors to go away

Question 2

Unfractionated Heparin

Answer 2

Endogenous anticoagulant
- Anticoagulant

MOA:
- Binds Antithrombin III (ATIII)
–> Induces conformation change in antithrombin
–> Increases affinity for active site of serine proteases of coagulation cascade
= ATIII binds Thrombin (IIA)

Question 3

Low Molecular Weight Heparin

Answer 3

Endogenous anticoagulant
- Anticoagulant

MOA:
- Binds Antithrombin III (ATIII)
–> Induces conformation change in antithrombin
–> Increases affinity for active site of serine proteases of coagulation cascade
= ATIII binds Xa

• Longer Half Life, predictable anticoagulation effects

Question 4

Rivaroxaban

Answer 4

Xa Inhibitor
- Anticoagulant

MOA:
- Reversible, direct competitive inhibitor of Xa
–> Prevents Prothrombin to Thrombin conversion

Question 5

Apixaban

Answer 5

Xa Inhibitor
- Anticoagulant

MOA:
- Reversible, direct competitive inhibitor of Xa
–> Prevents Prothrombin to Thrombin conversion

Question 6

Edoxaban

Answer 6

Xa Inhibitor
- Anticoagulant

MOA:
- Reversible, direct competitive inhibitor of Xa
–> Prevents Prothrombin to Thrombin conversion

Question 7

Dabigatran Etexilate

Answer 7

Prodrug, converted to Dabigatran by plasma esterases

MOA:
- Reversible, direct competitive inhibitor of Thrombin (IIa)
–> Prevents Fibrinogen conversion to Fibrin

Question 8

Hirudins

Answer 8

Anticoagulant Protein
- Anticoagulant

MOA:
- Slowly reversible, inhibits Thrombin (IIa) does not need ATIII
–> Prevents fibrinogen conversion to fibrin

Question 9

Lepirudin

Answer 9

Recombinant Hirudin
- Anticoagulant

MOA:
- Slowly reversible, inhibits Thrombin (IIa) does not need ATIII
–> Prevents fibrinogen conversion to fibrin

Question 10

Bivalirudin

Answer 10

Contains the 20 amino acids that allow for inhibition of thrombin from Hirudin
- Anticoagulant

MOA:
- Slowly reversible, inhibits Thrombin (IIa) does not need ATIII
–> Prevents fibrinogen conversion to fibrin

Question 11

Alteplase

Answer 11

Recombinant Tissue-Plasminogen Activator (r-tPA)
- Destroys clots

MOA:
Converts plasminogen to plasmin
- Plasmin breaks down fibrin

Question 12

Duteplase

Answer 12

Recombinant Tissue-Plasminogen Activator (r-tPA)- Destroys clots

MOA:
Converts plasminogen to plasmin
- Plasmin breaks down fibrin

Question 13

Reteplase

Answer 13

Recombinant Tissue-Plasminogen Activator (r-tPA)
- Destroys clots

MOA:
Converts plasminogen to plasmin
- Plasmin breaks down fibrin

Question 14

Streptokinase

Answer 14

Thrombolytic (Fibrinolytic) Drug
- Destroys clots

MOA:
- Forms complex with plasminogen
–> Forces conformational change in plasminogen
–> Plasminogen gains enzymatic activity
–> Plasminogen can now break down fibrin

• Plasminogen can now be deactivated by anti-streptokinase antibodies