Anticoagulants & Fibrinolytics
Generic |
Brand |
Class |
Form |
Heparin |
UFH (abbreviation) |
HMWH |
PAR |
Enoxaparin |
Lovenox |
LMWH |
PAR |
Dalteparin |
Fragmin |
LMWH |
PAR |
Warfarin |
Coumadin |
Coumarin Derivative (Vit K Antag.) |
PO |
Dabigatran |
Pradaxa |
Direct Thrombin Inhibitor |
PO |
Fondaparinux |
Arixtra |
Xa Inhibitor |
PAR |
Apixaban |
Eliquis |
Xa Inhibitor |
PAR |
Rivaroxaban |
Xarelto |
Xa Inhibitor |
PO |
Edoxaban |
Savaysa |
Xa Inhibitor |
PO |
Betrixaban |
Bevyxxa |
Xa Inhibitor |
PO |
Alteplase t-PA |
Activase Cathflo |
Fibrinolytic |
IV Bolus & Infusion |
Reteplase rPA |
Retavase |
Fibrinolytic |
IV Bolus |
Tenecteplase TNK-tPA |
TNKase |
Fibrinolytic |
IV Bolus |
Drug Site of Action in Coagulation Cascade
Class |
Drugs |
Site of Action |
Unfractionated Heparin |
Heparin |
ATIII, Xa, IIa, VIIa, IXa, XIa, & XIIa |
LMWH |
Enoxaparin, Dalteparin |
ATIII, Xa, IIa |
Factor Xa Inhibitor |
Fondaparinux |
ATIII, Xa |
Vit K Antagonist |
Warfarin |
II, VII, IX, & X |
Oral Xa Inhibitors |
Apixaban, Rivaroxaban, Edoxaban, Betrixaban |
Xa |
Direct Thrombin Inhibitors |
Dabigatran |
IIa (Thrombin) |
Fibrinolytics |
Alteplase Reteplase Tenectaplase |
Fibrin |
|
|
MOA for Therapies
Drug |
MOA |
Result |
Heparin |
fxn of ATIII Significant inhibition of Xa & IIa Minor Inhibitor of VIIa, IXa, XIa, & XIIa |
ACF become inactivated |
Enoxaparin Dalteparin |
fxn of ATIII Significant inhibition of Xa Some inhibition of IIa |
ACF become inactivated |
Fondaparinux |
fxn of ATIII Significant inhibition of Xa Inhibition specific to Xa |
ACF become inactivated |
Warfarin |
Targets Vit K dependent clotting factors (II, VII, IX, & X) Inhibits VKORC1
|
KH2 KH2 is needed as a cofactor for carboxylase enzyme to activate dependent clotting factors Vit K dependent clotting factors are produced F II, VII, IX, & X |
Apixaban Rivaroxaban Edoxaban Betrixaban |
Blocks the active site for Factor Xa Does not affect antithrombin |
Direct inhibition of Factor Xa |
Dabigatran |
Directly inhibits Factor IIa (Thrombin) |
No conversion of fibrinogen to fibrin Prevents development of a thrombus |
Alteplase (t-PA/r-tPA) |
Converts plasminogen to plasmin |
Breaks up clot |
ACF: Active Clotting Factors
VKORC1: Vit K Epoxide Reductase - Enzyme responsible for converting Vit K epoxide to its reduced and active form (KH2)
KH2: Active Vit K
|