Anticoagulation Drugs Cheat Sheet
The drugs used in clotting and bleeding disorders fall into 2 major groups:
(1) drugs used to decrease clotting or dissolve clots already present in patients at risk for vascular occlusion and
(2) drugs used to increase clotting in patients with clotting deficiencies. The first group, the anticlotting drugs, includes some of the most commonly used drugs in the United States. Anticlotting drugs are used in the treatment and prevention of myocardial infarction and other acute coronary syndromes, atrial fibrillation, ischemic stroke, and deep vein thrombosis (DVT). Within the anticlotting group, the anticoagulant and thrombolytic drugs are effective in treatment of both venous and arterial thrombosis, whereas antiplatelet drugs are used primarily for treatment of arterial disease.
DRUG SUMMARY TABLE: Drugs Used for Anticoagulation & for Bleeding Disorders
Anti-coagulation Drugs | ||||
Subclass | Mechanism of Action | Clinical Applications | Pharmacokinetics | Toxicities, Drug Interactions |
Anticoagulants Heparins Unfractionated heparin | Complexes with antithrombin III • irreversibly inactivates the coagulation factors thrombin and factor Xa | Venous thrombosis, pulmonary embolism, myocardial infarction, unstable angina, adjuvant to percutaneous coronary intervention (PCI) and thrombolytics | Parenteral administration | Bleeding (monitor with aPTT, protamine is reversal agent) •thrombocytopenia • osteoporosis with chronic use |
Direct factor X inhibitors Rivaroxaban | Binds to the active site of factor Xa and inhibits its enzymatic action | Venous thrombosis, pulmonary embolism, prevention of stroke in patients with atrial fibrillation | Oral administration • fixed dose no routine monitoring (factor Xa test) | Bleeding • no specific reversal agent |
Direct thrombin inhibitors Lepirudin and dabigatran | Binds to thrombin’s active site and inhibits its enzymatic action | Anticoagulation in patients with heparin-induced thrombocytopenia (HIT) | Lepirudin: IV administration Dabigatran: oral administration | Both: Bleeding (monitor with aPTT) Lepirudin: anaphylactic reactions |
Coumadin anticoagulant Warfarin | Inhibits vitamin K poxide reductase and thereby interferes with production of functional vitamin K-dependent clotting and anticlotting factors | Venous thrombosis, pulmonary embolism, prevention of thromboembolic complications of atrial fibrillation or cardiac valve replacement | Oral administration • delayed onset and offset of anticoagulant activity • many drug interactions | Bleeding (monitor with PT, vitamin K1 is a reversal agent) • thrombosis early in therapy due to protein C deficiency • teratogen |
Thrombolyticdrugs | ||||
Alteplase, recombinant human tissue plasminogen activator (t-PA) | Converts plasminogen to plasmin, which degrades the fibrin in thrombi | Coronary artery thrombosis, ischemic stroke, pulmonary embolism | Parenteral administration | Bleeding, especially cerebral hemorrhage |