Thrombosis

Question 1

Class;Mechanism;Therapeutics;SideEffects

Unfractionated heparin

Answer 1

Indirect thrombin inhibitors Bind antithrombin, potentiating formation of antithrombin-coagulation factor complex (Xa, IIa) Prevention and treatment of venous thromboembolism HIT, osteoporosis (long-term) Bleeding Given parenterally; monitored via PTT (want 2-2.5X normal value); reversed by protamine

Question 2

Class;Mechanism;Therapeutics;SideEffects

Dalteparin (Fragmin)

Answer 2

Indirect thrombin inhibitors LMWH that inhibits thrombin less effectively than Xa Prevent thrombosis and embolism from clots — Bleeding Monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); reversed by protamine

Question 3

Class;Mechanism;Therapeutics;SideEffects

Enoxaparin (Lovenox)

Answer 3

Indirect thrombin inhibitors LMWH that inhibits thrombin less effectively than Xa Drug of choice in pregnancy; prevention and treatment of venous thromboembolism HIT; osteoporosis and thrombocytopenia uncommon Bleeding Can be monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); reversed by protamine

Question 4

Class;Mechanism;Therapeutics;SideEffects

Tinzaparin (Innohep)

Answer 4

Indirect thrombin inhibitors LMWH that inhibits thrombin less effectively than Xa – HIT; osteoporosis and thrombocytopenia uncommon Bleeding Monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); reversed by protamine

Question 5

Class;Mechanism;Therapeutics;SideEffects

Fondaparinux (Arixtra)

Answer 5

Indirect thrombin inhibitors Synthetic polysaccharide that binds active site of antithrombin; inhibits Xa Given for HIT patients — Bleeding No antidote

Question 6

Class;Mechanism;Therapeutics;SideEffects

Warfarin (Coumadin)

Answer 6

Vitamin K antagonist Blocks vitamin K-dependent gamma-carboxylation of factors II, VII, IX, X, Protein C and S (does not affect already synthesized factors) Long-term anticoagulation Thrombosis (Protein C depression) Bleeding Metabolism enhanced by drugs that induce P450 activity (e.g., barbiturates); monitored by PT/INR; reversed by vitamin K and factor concentrates or fresh frozen plasma; contraindicated in pregnancy (teratogen)

Question 7

Class;Mechanism;Therapeutics;SideEffects

Lepirudin (Refludan)

Answer 7

Direct thrombin inhibitor Inactivate fibrinogen-bound AND unbound thrombin; irreversible — — — Administered parenterally; monitored by PTT; no antidote

Question 8

Class;Mechanism;Therapeutics;SideEffects

Bivalirudin (Angiomax)

Answer 8

Direct thrombin inhibitor Inactivate fibrinogen-bound AND unbound thrombin; irreversible — — — Administered parenterally; monitored by PTT; no antidote

Question 9

Class;Mechanism;Therapeutics;SideEffects

Argatroban (Acova)

Answer 9

Direct thrombin inhibitor Inactivate fibrinogen-bound AND unbound thrombin — — — Administered parenterally; monitored by PTT; no antidote

Question 10

Class;Mechanism;Therapeutics;SideEffects

Dabigatran (Pradaxa)

Answer 10

Direct thrombin inhibitor Inactivate fibrinogen-bound AND unbound thrombin; competitive (reversible) — — — Oral; no antidote

Question 11

Class;Mechanism;Therapeutics;SideEffects

Rivaroxaban (Xarelto)

Answer 11

Direct Xa inhibitor Reversible bind active site of Xa — — — Oral; no antidote

Question 12

Class;Mechanism;Therapeutics;SideEffects

Apixaban (Eliquis)

Answer 12

Direct Xa inhibitor Reversible bind active site of Xa — — — Oral; no antidote

Question 13

Class;Mechanism;Therapeutics;SideEffects

Streptokinase (Streptase)

Answer 13

Fibrinolytic Lyse already formed clots by activating circulating plasminogen (not clot specific) Acute MI, acute stroke, central DVT, multiple PE — — —

Question 14

Class;Mechanism;Therapeutics;SideEffects

Urokinase (Kinlytic)

Answer 14

Fibrinolytic Lyse already formed clots by activating circulating plasminogen Acute MI, acute stroke, central DVT, multiple PE — — —

Question 15

Class;Mechanism;Therapeutics;SideEffects

Reteplase (Retavase)

Answer 15

Fibrinolytic Lyse already formed clots; more clot specific, less systemic activation Acute MI, acute stroke, central DVT, multiple PE — — —

Question 16

Class;Mechanism;Therapeutics;SideEffects

Tenecteplase (TNKase)

Answer 16

Fibrinolytic Lyse already formed clots; more clot specific, less systemic activation Acute MI, acute stroke, central DVT, multiple PE — — —

Question 17

Class;Mechanism;Therapeutics;SideEffects

Aspirin

Answer 17

Antiplatelet Irreversibly inhibits platelets, preventing thromboxane A2 formation Often as “baby aspirin” to prevent and treat MI and stroke — — —

Question 18

Class;Mechanism;Therapeutics;SideEffects

Dipyridamole (Persantine)

Answer 18

Antiplatelet PDE inhibitor –> increase in platelet cAMP Weak antiplatelet effect — — Given parenterally

Question 19

Class;Mechanism;Therapeutics;SideEffects

Clopidogrel (Plavix)

Answer 19

Antiplatelet Inhibits platelet ADP receptors — TTP (rare) — Reversed by platelet transfusion

Question 20

Class;Mechanism;Therapeutics;SideEffects

Abciximab (Reopro)

Answer 20

Antiplatelet Monoclonal antibody against GP IIb/IIIa — May elicit immune response — Given parenterally

Question 21

Class;Mechanism;Therapeutics;SideEffects

Eptifibatide (Integrilin)

Answer 21

Antiplatelet Fibrinogen analog which competes with endogenous fibrinogen for IIb/IIIa — — — Given parenterally

Question 22

Class;Mechanism;Therapeutics;SideEffects

Tirofiban (Aggrastat)

Answer 22

Antiplatelet Fibrinogen analogs which compete with endogenous fibrinogen and vWF for IIb/IIIa — — — Given parenterally