Rapidly absorbed following oral administration. Peak plasma concentrations reached in 1 hr (2 hr if given with food). 35% plasma protein bound. Dabigatran etexilate is a prodrug, converted to active form by plasma and hepatic esterases. Hepatic glucuronidation to active metabolites. Excreted 80% via urine. Half-life: 12–17 hr; elderly: 14–17 hr; mild-to-moderate renal impairment: 15–18 hr; severe renal impairment: 28 hr.
Conversion from a parenteral anticoagulant: Initiate dabigatran ≤2 hr prior to the time of the next scheduled dose of the parenteral anticoagulant or at the time of discontinuation for a continuously administered parenteral drug; discontinue parenteral anticoagulant at the time of dabigatran initiation.
Hypersensitivity to dabigatran or any component of the formulation. May cause fatal bleeding. No specific antidote exists for dabigatran reversal; protamine and vitamin K do not reverse or impact anticoagulant effects of dabigatran. Use in patients with severe renal and hepatic impairment and valvular heart disease is not recommended. Use with extreme caution in elderly patients. Avoid use in patients taking other anticoagulants and P-glycoprotein inducers/inhibitors.
A monoclonal antibody that binds to the interleukin-2 (IL-2) receptor complex, inhibiting the IL-2-mediated activation of T lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection.
Rapidly and completely absorbed after PO administration. Unbound to plasma proteins. Well distributed in saliva. Minimally metabolized in liver. Primarily excreted unchanged (90%) in urine. CYP2E1 is the major isoenzyme responsible for the 3-hydroxylation of dalfampridine. Half-life: 5.2–6.5 hr.
Prevention of deep vein thrombosis (DVT) following abdominal surgery, treatment of life-threatening conditions such as unstable angina, non–Q-wave MI; prevention of ischemia complications caused by blood clot formation in patients on aspirin therapy; in combination with warfarin in deep vein thrombosis with or without pulmonary embolism (PE)
An antithrombotic agent that inhibits thrombin formation through factor antiXa and antiIIa effects. Does not significantly influence bleeding time, PT, aPTT, or platelet function. Possesses greater antithrombotic activity than anticoagulant activity.
Severe hemorrhagic diathesis (hemophilia, idiopathic thrombocytopenic purpura), active major bleeding state, including hemorrhagic stroke in the acute phase, type II phase thrombocytopenia associated with positive in vitro test for antiplatelet antibody in presence of danaparoid, hypersensitivity to pork products, danaparoid, or any component of the formulation
! Accidental overdosage may lead to bleeding complications ranging from minor ecchymosis to major hemorrhage. An unexplained fall in HCT or fall in B/P should lead to consideration of a hemorrhagic event. The antidote protamine sulfate only partially neutralizes danaparoid activity and is incapable of reducing severe nonsurgical bleeding during treatment. If serious bleeding occurs, discontinue danaparoid; give blood or blood product transfusions.
A testosterone derivative that suppresses the pituitary-ovarian axis by inhibiting the output of pituitary gonadotropins. Causes atrophy of both normal and ectopic endometrial tissue in endometriosis. Follicle-stimulating hormone (FSH) and luteinizing hormone (LH) are depressed in fibrocystic breast disease. Inhibits steroid synthesis and binding of steroids to their receptors in breast tissues. Increases serum levels of esterase inhibitor.