PRADAXA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRADAXA (PRADAXA).
Direct thrombin inhibitor; binds reversibly to the active site of thrombin, preventing fibrinogen cleavage and subsequent thrombus formation.
| Metabolism | Undergoes esterase-catalyzed hydrolysis to form active metabolite; not significantly metabolized by CYP450. Conjugated to form acyl glucuronides. |
| Excretion | Renal (80% unchanged); fecal/biliary (20% as inactive metabolites via P-glycoprotein-mediated secretion) |
| Half-life | 12–17 hours (terminal); prolonged to 18–35 hours in severe renal impairment (CrCl <30 mL/min); supports twice-daily dosing |
| Protein binding | 34–35% (bound primarily to albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | 0.7–1.1 L/kg (moderate tissue distribution; high Vd suggests extensive extravascular binding, mainly to thrombin in clot) |
| Bioavailability | 6.5% (oral, after prodrug conversion; absolute bioavailability limited by P-glycoprotein efflux in gut and liver) |
| Onset of Action | Oral: 0.5–2 hours (peak anticoagulant effect at 2–4 hours); IV: Not applicable (no parenteral formulation) |
| Duration of Action | 12–24 hours (anticoagulant effect persists for at least 24 hours after last dose; clinical monitoring via aPTT or TT may show prolongation up to 48 hours) |
| Action Class | Direct thrombin inhibitor- oral |
| Brand Substitutes | Dabigo 110mg Capsule, Dabimend 110 Capsule, Dabiac 110mg Capsule, Dabifib 110 Capsule, Dabipla 110mg Capsule, Dabigo 150mg Capsule, Dabitra 150 Capsule, Dabifib 150 Capsule, Dabipla 150mg Capsule, Goodflo 150mg Capsule, Dabigo 75mg Capsule, Dabiten 75mg Capsule, Dabitra 75mg Capsule, Dabipack 75 Capsule |
150 mg orally twice daily; for patients with CrCl 15-30 mL/min, 75 mg orally twice daily.
| Dosage form | CAPSULE |
| Renal impairment | CrCl >30 mL/min: standard dose; CrCl 15-30 mL/min: 75 mg twice daily; CrCl <15 mL/min or on dialysis: not recommended. |
| Liver impairment | Contraindicated in patients with hepatic impairment or coagulopathy associated with significant bleeding risk. No specific Child-Pugh based adjustments; use caution in mild impairment. |
| Pediatric use | Not approved for pediatric use. Safety and efficacy not established. |
| Geriatric use | No specific dose adjustment required based on age alone; consider renal function (CrCl) which declines with age. Increased bleeding risk in elderly patients. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRADAXA (PRADAXA).
| Breastfeeding | It is not known whether dabigatran is excreted in human milk. In animal studies, dabigatran was present in rat milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. No M/P ratio data available in humans. |
| Teratogenic Risk | Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, dabigatran etexilate has been shown to cause fetal toxicity, including decreased fetal body weight and increased fetal loss, at maternal exposures 2-3 times the human exposure at the maximum recommended dose. Dabigatran crosses the human placenta. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. |
■ FDA Black Box Warning
Discontinuation of dabigatran increases the risk of thrombotic events; premature discontinuation should be avoided. Epidural or spinal hematomas may occur in patients receiving neuraxial anesthesia or spinal puncture.
| Serious Effects |
["Active pathological bleeding","History of serious hypersensitivity reaction to dabigatran","Mechanical prosthetic heart valve requiring anticoagulation","Severe renal impairment (CrCl < 30 mL/min) for some indications"]
| Precautions | ["Increased risk of bleeding, including life-threatening hemorrhage","Spinal/epidural hematoma risk with neuraxial procedures","Discontinuation may increase thrombotic risk","Contraindicated in patients with prosthetic heart valves (increased thromboembolic events)","Serum creatinine monitoring recommended in renal impairment"] |
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| Fetal Monitoring | Monitor for signs of bleeding in the mother and fetus. Consider serial ultrasound to monitor fetal growth and development. Clotting times (e.g., aPTT, ecarin clotting time, dilute thrombin time) may be used to assess anticoagulation status if needed. Monitor maternal hemoglobin and hematocrit. |
| Fertility Effects | No human fertility studies available. In animal studies, dabigatran did not impair fertility in male or female rats at doses up to 2 times the human exposure. |