Pharmacology · Corticosteroids and Sex Hormones (OCPs, Androgens)

A cirrhotic patient with severe hepatic dysfunction requires systemic glucocorticoid therapy. Which pair best explains why prednisolone is preferred over prednisone in this setting?

  • A Prednisone is more protein bound, so free drug levels fall in hypoalbuminaemia
  • B Prednisone undergoes extensive first-pass metabolism by CYP3A4, unlike prednisolone
  • C Prednisone has greater mineralocorticoid activity, worsening ascites formation
  • D Prednisone is a prodrug requiring hepatic 11 beta-hydroxysteroid dehydrogenase type 1 for conversion to prednisolone
Correct answer: D. Prednisone is a prodrug requiring hepatic 11 beta-hydroxysteroid dehydrogenase type 1 for conversion to prednisolone

Explanation

Prednisone is the inactive 11-keto form and must be reduced to prednisolone by hepatic 11 beta-hydroxysteroid dehydrogenase type 1. In severe liver disease this bioactivation is unreliable, so the active parent compound prednisolone is given directly. Option B fails because both drugs are cleared hepatically and first-pass metabolism is not the discriminating issue. Options C and A are incorrect since neither drug has meaningful mineralocorticoid activity at these doses and protein binding does not govern the preference.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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