Pharmacology · Anticoagulants, Antiplatelets and Thrombolytics

A 68-year-old woman on dabigatran 110 mg twice daily for atrial fibrillation has eGFR 35 mL/min. Her physician warns that her bleeding risk is higher than with apixaban mainly because dabigatran:

  • A Has approximately 80 percent renal excretion of active drug
  • B Is a prodrug requiring renal activation
  • C Is a potent inducer of CYP3A4
  • D Accumulates in hepatic failure rather than renal failure
Correct answer: A. Has approximately 80 percent renal excretion of active drug

Explanation

Dabigatran etexilate is converted to the active compound by esterases, and about 80 percent of the active drug is cleared unchanged by the kidneys, the highest renal fraction among DOACs. Renal impairment therefore causes marked accumulation and bleeding risk, mandating dose reduction or avoidance. Apixaban is only about 27 percent renally cleared. Dabigatran is not a CYP3B4 substrate or inducer, ruling out C.

Reference: Katzung's Basic and Clinical Pharmacology, 16th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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