Pharmacology · Corticosteroids and Sex Hormones (OCPs, Androgens)

A patient develops Cushingoid features while using intranasally administered corticosteroids for chronic rhinitis. The systemic absorption is highest with which agent?

  • A Mometasone furoate — highest lipophilicity ensuring complete GI absorption of swallowed drug
  • B Fluticasone propionate — highest lipophilicity but negligible oral bioavailability due to extensive first-pass hepatic metabolism
  • C Beclomethasone dipropionate — converted to active monopropionate with significant intestinal absorption of swallowed fraction
  • D Budesonide — similar to beclomethasone; both have equivalent systemic absorption
Correct answer: C. Beclomethasone dipropionate — converted to active monopropionate with significant intestinal absorption of swallowed fraction

Explanation

Among intranasal corticosteroids, systemic exposure depends on both direct nasal mucosal absorption and oral bioavailability of swallowed drug. Beclomethasone dipropionate (BDP) has relatively high oral bioavailability (~26% as active beclomethasone-17-monopropionate), making it the agent most associated with systemic effects among older intranasal steroids. Fluticasone propionate (<1% oral bioavailability) and mometasone furoate (<1%) have negligible gut absorption due to extensive first-pass metabolism. Budesonide has ~13% oral bioavailability. For patients requiring long-term therapy, fluticasone or mometasone is preferred to minimize systemic effects.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.

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