Prednisone
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Prednisone
Deltasone, Rayos (delayed-release); mostly prescribed generically
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Summary
Pharmacy
Starting dose
0.5-2 mg/kg/d divided or single morning dose for acute conditions; lowest effective dose for chronic conditions, with planned taper
Preparations
1, 2.5, 5, 10, 20, 50 mg tablets; 5 mg/5 mL syrup; 5 mg/mL concentrate
US FDA Max
No fixed maximum; cumulative-dose toxicity drives all chronic decisions
Pharmacology
Routes
Oral
Onset
Hours
Duration
Biologic half-life ~12-36 hours (intermediate-acting); plasma half-life shorter
Half-life
Plasma 3-4 hours; biologic ~12-36 hours[1]
Bioavailability
70-80% (oral)[1]
Pregnancy
Used when benefits outweigh risk; oral cleft signal in first-trimester exposure is debated and small in absolute terms.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Prednisone is an inactive prodrug converted by hepatic 11β-hydroxysteroid dehydrogenase to prednisolone, the active glucocorticoid receptor agonist; the activated receptor translocates to the nucleus and broadly remodels transcription of inflammatory, immune, and metabolic gene programs.0 Effects include suppression of phospholipase A2 (via lipocortin/annexin), NF-κB inhibition, lymphocyte and eosinophil depletion, monocyte/macrophage downregulation, and shifts in carbohydrate, lipid, and protein metabolism. Hepatic insufficiency reduces conversion, an argument for using prednisolone directly in severe liver disease[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, prednisone, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202020s000lbl.pdf