BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
|Preparation method||Human thrombin is dose-dependently and competitively inhibited by dabigatran (Table 2). This inhibition with a Ki of 4.5 nmol/L compares well to the Ki of melagatran (11.2 nmol/L). Real-time binding kinetics using surface plasmon resonance showed a rapid and reversible binding of dabigatran to thrombin.7 The concentration of dabigatran required tom double the in vitro coagulation time (EC2) in platelet poor plasma is species dependent and varies with the type of test (Table 3).|
|Animal models||rabbit model of venous thrombosis|
|Dosages||a single IV administration of 5, 10, 20, and 30 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans.
Blech et al. Drug Metab Dispos. 2008 Feb;36(2):386-99. PMID: 18006647.
Population pharmacokinetic analysis of the new oral thrombin inhibitor dabigatran etexilate (BIBR 1048) in patients undergoing primary elective total hip replacement surgery.
Trocóniz et al. J Clin Pharmacol. 2007 Mar;47(3):371-82. PMID: 17322149.
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