Dabigatran (Pradaxa)
Prodrug of a direct thrombin inhibitor; dabigatran etexilate converts to dabigatran (active form) via sequential carboxylesterase hydrolysis. Dabigatran directly and reversibly inhibits thrombin. Rapidly absorbed in stomach/small intestine (tmax 1-2h); very low oral bioavailability (6.5%) due to ester metabolism and low membrane permeability; compensated by high dosing (110-150 mg BID). Primarily renally eliminated (>80% unchanged); use with caution in renal impairment. Half-life 14-17h. Fixed dosing. May cause more dyspepsia than other DOACs. Reversal agent (idarucizumab) available. Higher risk of GI bleeding compared to apixaban/rivaroxaban.
Projected serum levels — 150 mg, once daily
Maintenance schedule: 150 mg once daily (oral).
Loading schedule: 215 mg on day 1, then 150 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~1 days: peak ≈ 13.0 mg, trough ≈ 4.3 mg body load. Population-based estimate over 15 days for a 150 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Anticoagulant
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 14 h
- Common dose
- 150 mg
- Suggested maximum
- 150 mg/day
- Reference dose range
- 75–150 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 150 mg oral — Cmax 0.17 mg/L at 1.5 h
Documented interactions
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warning
St. John's Wort (Hypericum perforatum) + Dabigatran (Pradaxa)
CYP3A4 induction reduces DOAC levels, compromising anticoagulation.
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caution
Prednisone + Dabigatran (Pradaxa)
Prednisone may induce dabigatran metabolism.
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moderate
Carvedilol (Coreg) + Dabigatran (Pradaxa)
Carvedilol (Coreg) inhibitor of P-gp may alter Dabigatran (Pradaxa) absorption / distribution
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moderate
CBD (Cannabidiol) + Dabigatran (Pradaxa)
CBD (Cannabidiol) inhibitor of P-gp may alter Dabigatran (Pradaxa) absorption / distribution
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moderate
Efavirenz (Sustiva) + Dabigatran (Pradaxa)
Efavirenz (Sustiva) inducer of P-gp may alter Dabigatran (Pradaxa) absorption / distribution
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moderate
Fisetin + Dabigatran (Pradaxa)
Fisetin inhibitor of P-gp may alter Dabigatran (Pradaxa) absorption / distribution
Serum checks 19 modeled interaction pairings for dabigatran (pradaxa) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Clinical Pharmacokinetics and Pharmacodynamics of the Oral Direct Thrombin Inhibitor Dabigatran Etexilate
Comprehensive PK/PD review of dabigatran etexilate prodrug, carboxylesterase hydrolysis to active dabigatran, bioavailability 6.5%, renal elimination >80%, and thrombin inhibition kinetics.
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Carboxylesterase-2 plays a critical role in dabigatran etexilate active metabolite formation
Molecular study showing carboxylesterase-2 (intestinal) and carboxylesterase-1 (hepatic) sequentially convert prodrug dabigatran etexilate to active dabigatran via ester hydrolysis.
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The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects
Phase I study establishing dabigatran etexilate dosing, PK profile, rapid thrombin inhibition, dose proportionality, and tolerability in healthy volunteers.
3 published studies referenced in the app, each with a plain-language summary.