Coagulation Pathway Inhibitors Flashcards
Unfractionated Heparin
Class: Indirect thrombin inhibitor
Mech: Binds antithrombin, potentiating formation of antithrombin-coagulation factor complex (Xa, IIa)
Thera: Prevention and treatment of venous thromboembolism
Tox: HIT, bleeding, osteoporosis
Misc: Given parenterally, monitored via PTT (want 2-2.5 times normal value), reversed by protamine
Dalteparin
Class: Indirect thrombin inhibitor
Mech: LMWH that inhibits thrombin less effectively than Xa
Thera: Prevent thrombosis and embolism from clots
Tox: Bleeding
Misc: Monitored by heparin assay (anti-factor Xa), longer half-life than heparin (1-2/day), reversed by protamine
Enoxaparin
Class: Indirect thrombin inhibitor
Mech: LMWH that inhibits thrombin less effectively than Xa
Thera: Drug of choice in preg; prevention and treatment of venous thromboembolism
Tox: HIT, bleeding, osteoporosis, and thrombocytopenia (uncommon)
Misc: Monitored by heparin assay (anti-factor Xa), longer half-life than heparin (1-2/day), reversed by protamine
Tinzaparin
Class: Indirect thrombin inhibitor
Mech: LMWH that inhibits thrombin less effectively than Xa
Thera: N/A
Tox: HIT, bleeding, osteoporosis, and thrombocytopenia (uncommon)
Misc: Monitored by heparin assay (anti-factor Xa), longer half-life than heparin (1-2/day), reversed by protamine
Fondaparinux
Class: Indirect thrombin inhibitor
Mech: Synthetic polysaccharide that binds active site of antithrombin; inhibits Xa
Thera: Given for HIT
Tox: Bleeding
Misc: No antidote
Warfarin
Class: Vitamin K antagonist
Mech: Blocks vitamin K dependent gamma carboxylation of factors II, VII, IX, X, Protein C, Protein S (does not affect already synthesized factors)
Thera: Long-term anticoagulation
Tox: Thrombosis (Protein C depression)
Misc: Metabolism enhanced by drugs that induce P450 activity (barbituates), monitored by PT/INR, reversed by vitamin K, and factor concentrates, contraindicated in pregnancy (teratogen)
Bivalirudin
Class: Direct thrombin inhibitor
Mech: Inactivate fibrinogen-bound and unbound thrombin; irreversible
Thera: Percutaneous coronary intervention
Tox: Bleeding
Misc: Administered parenterally, monitored by PTT; no antidote
Argatroban
Class: Direct thrombin inhibitor
Mech: Inactivate fibrinogen-bound and unbound thrombin; irreversible
Thera: Percutaneous coronary intervention, HIT
Tox: Bleeding
Misc: Administered parenterally, monitored by PTT; no antidote
Dabigatran
Class: Direct thrombin inhibitor
Mech: Inactivate fibrinogen-bound and unbound thrombin; competitive (reversible)
Thera: DVT/PE; A-fib
Tox: Bleeding
Misc: Oral, no antidote, renal fixed dose clearance
Rivaroxaban
Class: Direct Xa inhibitor
Mech: Reversible bind active site of Xa
Thera: DVT/PE prophylaxis
Tox: Bleeding
Misc: Oral, no antidote, renal fixed dose clearance
Apixaban
Class: Direct Xa inhibitor
Mech: Reversible bind active site of Xa
Thera: DVT/PE prophylaxis
Tox: Bleeding
Misc: Oral, no antidote, renal fixed dose clearance
