martes, 19 de abril de 2011

DABIGATRAN

The etexilate dabigatran is a profarmac of small molecule lacking of farmacologic activity, after his oral administration, it is absorbed quickly and transformated in dabigatran by hydrolisis mediated for plasma and liver esterases. Dabigatran is a direct competitive and reversible inhibitor of trombin. Because trombin allows the conversion of fibrinogen to fibrine in the coagulation cascade, his inhibition blocks clots formation. Dabigatran also inhibits free trombin, protein linked trombin and platelet agregation initiated by trombin. Meals doesn't affect his biodisponibility, but delay 2 hours the time required for yield maximum concentrations. Protein link of dabigatran is low (34-35%) it is eliminated principally by kidney (85%), while fecal elimination is about 6%. Dabigatran is conjugated and form active acyl-glucuronids. Dabigatran is eliminated principally in urine in a rate aproximately of 100ml/min.

Indications:Primary prevention of tromboembolism in patients intervened in surgery of total replace of hip or knee.

Dosification: It is administrated VO 220mg day, divided in two takes of 110mg. It is recomended initiate with the administration of the farmac 1-4 hours after surgery. It is continuated for 28-35 days. In CRF is recomendated two takes of 75mg/day.

Contraindication: CRF, pregnancy, lactation, liver failure

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