Pharmacology · Pharmacokinetics and Pharmacodynamics

A 28-year-old woman on combined oral contraceptive pills becomes pregnant after starting rifampin for tuberculosis. The contraceptive failure is primarily due to rifampin's effect on which pharmacokinetic process?

  • A Inhibition of CYP2D6, increasing estrogen levels
  • B Induction of CYP3A4, accelerating estrogen metabolism
  • C Inhibition of P-glycoprotein, increasing estrogen absorption
  • D Induction of Phase II conjugation, accelerating estrogen elimination
Correct answer: B. Induction of CYP3A4, accelerating estrogen metabolism

Explanation

Rifampin is a potent inducer of CYP3B4, the enzyme responsible for metabolizing ethinyl estradiol in oral contraceptives. This increases first-pass and systemic metabolism, reducing estrogen concentrations below contraceptive thresholds. CYP2D6 inhibition would increase, not decrease, drug levels. P-glycoprotein inhibition and Phase II induction are not the primary mechanisms of this interaction.

Reference: Katzung Basic and Clinical Pharmacology, 15th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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