Dabigatran Etexilate (Pradaxa)

byAbdelwahab Ward, BS Pharm, PharmD - last updated
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PRADAXA...
CLASS: Direct Oral Anticoagulant (DOAC).
DOSAGE FORMS: Oral Capsule: 75 mg, 110 mg, 150 mg.

  • Treatment and prevention of initial or recurrent DVT and PE: 150 mg po bid (after 5-10 d treatment with parenteral anticoagulant).
  • Prevention of stroke and systemic embolism in patient with nonvalvular atrial fibrillation: 150 mg po bid.
  • Prevention of deep venous thromboembolism and PE after hip replacement: 110 mg po 1-4 h postoperatively, then 220 mg po daily × 28-35 day.
  • Prevention of deep venous thromboembolism and PE after knee replacement: 110 mg po 1-4 h postoperatively, then 220 mg po daily × 28-35 d.
  • Dabigatran is a competitive, reversible, direct thrombin inhibitor.
  • Because thrombin enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus.
  • Both free and clot-bound thrombin and thrombin-induced platelet aggregation are inhibited.

Table (1). Drug Characteristics (Pradaxa)
Dose Adjustment Hepatic Not required Absorption F = 3-7%, no effect of food on absorption
Dose Adjustment Renal CrCl 15-30 mL/min, 75 mg po bid; CrCl <15 mL/min, avoid use Distribution Vd = 50-70 L; 35% protein bound
Dialyzable Use in ESRD should be avoided; hemodialysis removes 60% of drug in 2-3 h Metabolism Extensive hepatic metabolism but not by CYP; substrate of P-glycoprotein
Box Warnings Use in elderly; risk of stroke at discontinuation; spinal epidural hematoma Elimination Renal 80% with a half-life of 12-17 h
Contraindications Active bleeding, prosthetic heart valve, hypersensitivity Pharmacogenetics None known
Briggs Pregnancy Recommendation No human data—animal data suggest moderate risk
Briggs Breastfeeding Recommendation No human data—potential toxicity

REFERENCES

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