Dabigatran etexilate is an oral prodrug; esterase hydrolysis in gut/liver/plasma yields active dabigatran, a reversible, competitive direct thrombin inhibitor that binds both free and fibrin-bound thrombin. Absorption from the gut requires an acidic microenvironment — hence the tartaric-acid pellet formulation and the tendency for dyspepsia. ~80% renal elimination makes creatinine clearance the dominant determinant of exposure. Specific reversal agent: idarucizumab.
Half-Life (t½)
PO: 13h
Dosing Guidelines
PO: Typical 150 mg (Range: 150–150 mg)
Target Organ Systems
renal
immune-hematologic
Interactions
Warfarin (caution): Do not co-administer; transition per protocol only.
Aspirin (caution): Additive bleeding risk; use only for defined indications. [Holbrook 2005]
NSAIDs (caution): Additive GI bleeding; avoid chronic combination. [Holbrook 2005]