-
Dabigatran
- oral direct thrombin inhibitor
- metabolism: 80% renal, 20% hepatic
-
Argatroban
- parenteral direct thrombin inhibitor
- approved for treatment of HIT
- continuous IV infusion
- short half life (1 hr)
- APTT monitoring
- metabolism: hepatic
-
lepirudin and bivalirudin
- parenteral direct thrombin inhibitor
- approved for HIT
- continuous IV infusion
- short half life (1-2 hrs)
- APTT monitoring
- metabolism: renal
-
rivaroxaban
- direct factor Xa inhibitor
- metabolism: mostly hepatic
-
apixaban
- direct factor Xa inhibitor
- metabolism: mostly hepatic
-
idarucizumab
anti-dabigatran monoclonal antibody Fab
-
andexanet
inactive Xa analogue to neutralize factor Xa inhibitors
-
Aspirin
- anti-platelet
- irreversibly inhibits COX1/2, decreases synthesis of thromboxane A2 (potent platelet agonist)
- inhibits platelet fn for the life of the platelet
- adverse effects: bleeding, GI ulceration, allergy and bronchospasm, interstitial nephritis, papillary necrosis, proteinuria, renal failure, Reye's syndrome (rapidly progressive encephalopathy and hepatic dysfunction) in children with viral illness
-
clopidogrel
- thienopyridine
- P2Y12 receptor antagonist (high affinity, essentially irreversible)
- blocks activation of platelets by reducing ADP activation of P2Y12 receptor
- oral
- adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
-
triclopidine
- thienopyridine
- P2Y12 receptor antagonist (high affinity, essentially irreversible)
- blocks activation of platelets by reducing ADP activation of P2Y12 receptor
- oral
- adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
-
prasugrel
- thienopyridine
- P2Y12 receptor antagonist (high affinity, essentially irreversible)
- blocks activation of platelets by reducing ADP activation of P2Y12 receptor
- oral
- adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
-
ticagrelor
- cyclopentyltriazolopyrimidine
- P2Y12 receptor antagonist (noncompetitive inhibitor of P2Y12 - reversible)
- blocks activation of platelets by reducing ADP activation of P2Y12 receptor
- oral
- adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
-
abciximab
- Fab fragment of a monoclonal antibody
- inhibits binding of fibrinogen to glycoprotein IIb/IIIa
- adverse effects: bleeding, thrombocytopenia
-
tirofiban
- small molecule
- inhibits binding of fibrinogen to glycoprotein IIb/IIIa
- adverse effects: bleeding, thrombocytopenia
-
eptifibitide
- cyclic heptapeptide
- inhibits binding of fibrinogen to glycoprotein IIb/IIIa
- adverse effects: bleeding, thrombocytopenia
-
dipyridamole
- multiple mechanisms: stimulates prostacyclin synthesis, inhibits adenosine deaminase and phosphodiesterase
- vasodilatory effects on blood vessels
- oral or IV
- adverse effects: headache
- often used in combination with aspirin
-
streptokinase
- fibrinolytic agent
- single chain polypeptide derived from beta-hemolytic streptococcus
- binds to plasminogen, forming a complex that becomes allosterically active, allowing the streptokinase/plasminogen complex to generate plasmin
- IV or catheter-directed
- not fibrin specific (also cleaves fibrinogen)
- adverse effects: bleeding, allergic rxns, hypotension
-
urokinase (u-PA)
- fibrinolytic agent
- isolated from human urine or kidney cells
- protease that directly cleaves plasminogen to form plasmin
- non-antigenic
- IV
- not fibrin specific: also cleaves fibrinogen
- adverse effects: bleeding
-
tissue plasminogen activator (t-PA)
- recombinant t-PA (alteplase, reteplase, tenecteplase)
- proteases that directly cleaves plasminogen to form plasmin
- relative fibrin-specific (does not cleave fibrinogen, resulting in more localized, rather than systemic fibrinolytic activity)
- short half life (minutes) - must be used in conjunction with heparin
- non-antigenic
- IV
- adverse effects: bleeding
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