Antithrombotic Drugs Flashcards
Abciximab
Anti-platelet drug
- glycoprotein IIb/IIIa antagonist
- inhibits binding of fibrinogen to glycoprotein IIb/IIIa
- Fab fragment of a monoclonal antibody
- IV administration
- adverse effects: bleeding, thrombocytopenia
Apixaban
Direct Factor Xa inhibitor
- administered orally (DOAC = teratogen)
- alternative to Warfarin
Argatroban
Direct thrombin inhibitor
- approved for treatment of HIT (heparin-incuded thrombocytopenia)
- administered by IV
- short half live (1 hour)
- monitored by: aPTT
- metabolized by liver (contraindicated in someone w/ liver disease)
Aspirin
Anti-platelet drug
- irreversibly inhibits cyclooxygenases
- decreases synthesis of thromboxane A2 (potent platelet agonist)
- inhibits platelet function for the life of the platelet
- oral administration
- 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 (Plavix)
Anti-platelet drug
- P2Y12 receptor antagonist
- oral administration
- is a Thienopyridine = high affinity binding to P2Y12 (essentially irreversible)
- Adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
Dabigatran
Direct Thrombin inhibitor
- administered orally (DOAC = teratogen)
- alternative to Warfarin
Dipyridamole
Anti- platelet drug
- multiple mechanisms (inhibits phosphodiesterase and adenosine deaminase, stimulates prostacyclin synthesis)
- vasodilatory effects on blood vessels
- administration: IV or oral
- adverse effects: headache
- often used in combination with Aspirin
Heparin-induced Thrombocytopenia (HIT)
prothrombotic condition mediated by IgG antibodies that bind to platelet factor 4 (PF4) when it is complexed with Heparin
- paradoxically causes thrombocytopenia and thrombosis
- surgical patients have higher risk than medical patients
- Heparin carries 5-fold higher risk than LMWH
- thrombocytopenia usually occurs 5-10 days after initiation of heparin
- thromboembolic complications: deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke, skin necrosis at injection sites, peripheral arterial thrombosis that can progress to limb necrosis
Lepirudin
Direct thrombin inhibitors
- approved for treatment of HIT (heparin-induced thrombocytopenia)
- administered by continuous IV infusion
- short half life (1-2 hours)
- monitoring: aPTT
- metabolized by kidney
Rivaroxaban
Direct Factor Xa inhibitor
- Direct oral anticoagulant (DOAC = teratogen)
- alternative to warfarin
Streptokinase
Fibrinolytic Agent
- promote activation of plasminogen to generate plasmin, which degrades fibrin
- single chain polypeptide derived from beta-hemolytic Stretococcus
- binds to plasminogen, forming a complex that is allosterically active, allowing complex to generate plasmin
- administration: IV or catheter-directed
- not fibrin-specific (also cleaves fibrinogen)
Adverse effects: bleeding, allergic rxns (anti-strep antibodies), hypotension
Ticagrelor
Anti-platelet drug
- P2Y12 receptor antagonist
- oral administration
- is a cyclopentyltriazolopyrimidine = noncompetitive inhibitor of P2Y12 (reversible)
- Adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
Tissue Plasminogen activator (t-PA)
Fibrinolytic Agent
- promote activation of plasminogen to generate plasmin, which degrades fibrin
- recombinant t-PA (alteplase)
- variants of recombinant t-PA (reteplase, tenecteplase)
- proteases that directly cleave plasminogen to form plasmin
- relative fibrin-specific (doesn’t cleave fibrinogen = more localized rather than systemic fibrinolytic activity)
- short half life (minutes) - must be in conjunction with heparin
- non-antigenic
- IV administration
Adverse effects: bleeding
Ticagrelor
Anti-platelet drug
- P2Y12 receptor antagonist
- oral administration
- is a cyclopentyltriazolopyrimidine = noncompetitive inhibitor of P2Y12 (reversible)
- Adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
Anti-platelet drugs
- Aspirin
- P2Y12 receptor antagonists
- Glycoprotein IIb/IIIa antagonists
- Dipyridamole (often combined with aspirin)
- Mainly used for arterial thrombosis rather than venous thrombosis*
