Prednisone — Drug Monograph

Brand names: Deltasone, Rayos

Drug class: Corticosteroid

Mechanism of Action

Prednisone is an inactive synthetic glucocorticoid prodrug that is rapidly converted by hepatic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) to its active metabolite prednisolone. Prednisolone binds cytoplasmic glucocorticoid receptors (GR-α), and the activated receptor complex translocates to the nucleus to regulate transcription of glucocorticoid-responsive genes. In lymphoid malignancies, it induces apoptosis via upregulation of pro-apoptotic BIM and downregulation of anti-apoptotic BCL-2 and BCL-XL, while suppressing NF-κB-mediated pro-survival signaling. Immunosuppressive effects…

FDA Indications

Common Side Effects

Clinical Pearl

In the CHOP regimen for DLBCL, prednisone 100 mg/day × 5 days serves a dual purpose: direct lymphocytolytic activity via glucocorticoid receptor-mediated apoptosis, and anti-emetic/appetite-stimulating effects that improve tolerability of the other cytotoxic agents. When a patient has uncontrolled diabetes or cannot tolerate prednisone, methylprednisolone (equivalent dose) or dexamethasone can be substituted, though prednisone is the standard per the original CHOP protocol. In elderly or frail…

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