Anti-platelet/fibrinolytic drugs

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Aspirin

Blocks platelet COX-1 (TXA2 synthesis) irreversibly and inhibits platelet aggregation. Used for prophylaxis for of clotting (strokes, MIs) and for acute MIs. Should be avoided in patients with active peptic ulcer, hepatic or renal disease, disorders of coagulation.

Ticlopidine

-Platelet ADP RECEPTOR ANTAGONIST
-Oral, 2 step biotransformation
-Bone marrow toxicity, aplastic anemia, thrombotic thrombocytopenic purpura
-

Clopidogrel

-Platelet ADP RECEPTOR ANTAGONIST
-oral, 2 step biotransformation: less effective if given with inhibitors of CYP2C19 (e.g. omeprazole)
-94% of dose is inactivated by esterases
-slight bone marrow toxicity

Prasugrel

-Platelet ADP RECEPTOR ANTAGONIST
-Activated by estrases rather than CYP2C19

Ticagrelor

-Reversible ADP-RECEPTOR INHIBITOR
-Shorter onset of action (2 hrs) and half life (1 day) vs clopidogrel (4 hr, 3 day)

Abciximab

-Human/mouse chimeric Fab fragment against the fibrin receptor (gp IIb/IIIa) that irriversible blocks the receptor, is given IV short term to prophylactically prevent clots during percutaneous coronary interventions (e.g. angioplasty)

Eptifibatide

-Administered IV to competitively INHIBIT FIBRIN RECEPTOR (Gp IIb/IIIa) on platelets. Analog to rattlesnake venom that mimmics the RGD sequence on fibrin. Used to treat acute coronary syndrome and Percutaneous coronary interventions (coronary angioplasty, stent insertion)

Tirofiban

-IV non-peptide RGD sequence mimetic (Fibrinogen receptor [gp IIb/IIIa] antagonist) approved for treatment of unstable angina and coronary angioplasty

Dipyridamole

-Coronary VASODILATOR and ANTIPLATELET that blocks PDE (elevates cAMP) and Adenosine deaminase (elevates adenosine); used in combo with asprin as prophylaxis against TIAs

Cilostazol

-Oral inhibitor of PDE III (elevates cAMP) used to treat intermittent claudication by INHIBITING PLATELET AGGREGATION and promoting VASODILATION
-Increases heart rate and contractility (via cAMP)
-Contraindicated in CHF patients

Epoprostenol

-Prostacyclin (PGI2) administered IV to raise cAMP and lower Ca++ in platelets to inhibit the release reaction and thus INHIBIT PLATELET aggregation
-Vasodilator primarily used for the treatment of primary pulmonary hypertension; prevents platelet aggregation in extra corporeal circulation of blood (hemodialysis)
-Side effects include a decrease in blood pressure

Delteparin

A heparin

Ardeparin

A heparin

Tinzaperin

A heparin

Fondparinux

-Pentasaccharide that accelerates antithrombin III's inactivation of Xa but NOT THROMBIN
-Dose independent half life of 17-21 hours (renal clearance)

Heparin

-Accelerates antithrombin III's inactivation of thrombin, Xa, IXa, XIa

Unfractionated heparin

Dose dependent half life (1-2 hr at therapeutic doeses)

LMWH

longer (4hr) dose independent half life

Protamine Sulfate

IV antidote to HMWH and less so to LMWH

Enoxaparin

A LMWH

Lepiruden

direct inhibitor of thrombin that is indicated for continous IV infusion for the treatment of HIT type II

Desiruden

A direct inhibitor of thrombin that is administered SC and indicated for DVT prophylaxis in hip replacement surgery

Bivalirudin

Direct, reversible inhibitor of free and clot associated thrombin

Argatroban

highly selective inhibitor of free and clott-associated thrombin

Dabigatran etexilate

-ORAL competitive, reversible thrombin inhibitor

Warfarin

-Inhibits vitamin K recycling and thus the proper production of

Phytonadione (vitamin K1)

Antidote to Warfarin

Rivaroxaban

orally active direct factor Xa inhibitor

e-aminocaproic acid (EACA)

Plasmin inhibitor used in treatment of dental bleeding, pressure dressing, etc.

Tranexamic acid

Plasmin inhibitor used for treatment of cyclic heavy menstrual bleeding.

Streptokinase

-forms a complex with free plasminogen that allows PLASMINOGEN to convert other plasminogen into plasmin
-Administered as loading dose plus contionuous IV infusion (since many people have antibodies to it)

Alteplase

-rtPA that activates plasminogen on the surface of fibrin on the thrombus (fibrinolytic drug); given as a continuous IV infusion

Reteplase

-modified tPA (fibrinolytic drug) that has a longer half life (13-16 min) and therefore given as an IV bolus (not continuous IV)

Tenecteplase

-modified tPA (fibrinolytic drug) that has a longer half life (20-24 min) and therefore given as an IV bolus (not continuous IV)

Urokinase

-Protease that activates plasminogen, which doesn't have antibodies against it; does not have a fibrin depndence

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