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 ✓
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
Written and medically reviewed by the StethoPrep medical team.