prednisone
Brand: Deltasone, Rayos
Prototype Drug
Drug Class: corticosteroid
Drug Family: corticosteroid
Subclass: synthetic glucocorticoid (intermediate-acting)
Organ Systems: endocrineimmunology
Mechanism of Action
Prodrug converted to active prednisolone by 11-beta-HSD1; activates cytosolic glucocorticoid receptors, translocating to nucleus to transactivate anti-inflammatory genes (lipocortin-1) and transrepress pro-inflammatory transcription factors (NF-kB, AP-1); reduces synthesis of prostaglandins, leukotrienes, and cytokines.
glucocorticoid receptor (GR)
Indications
- autoimmune diseases (rheumatoid arthritis, lupus, IBD, vasculitis)
- allergic reactions and anaphylaxis (adjunct)
- asthma exacerbations
- COPD exacerbations
- adrenal insufficiency (with fludrocortisone)
- organ transplant rejection prophylaxis
- anti-emetic (CINV — high-dose)
- cerebral edema (IV dexamethasone preferred for brain tumors)
Contraindications
- systemic fungal infections (without concurrent antifungal therapy)
- live vaccines in immunocompromised doses
Adverse Effects
Common
- hyperglycemia
- weight gain / increased appetite
- insomnia
- mood changes (euphoria, anxiety, depression)
- GI irritation
- fluid retention / hypertension
Serious
- HPA axis suppression (adrenal insufficiency on abrupt withdrawal)
- osteoporosis (long-term)
- Cushing's syndrome (iatrogenic)
- immunosuppression / opportunistic infections
- myopathy
- avascular necrosis of the femoral head
- cataracts and glaucoma (long-term)
Pharmacokinetics (ADME)
| Absorption | Well absorbed orally; converted to prednisolone in liver |
| Distribution | Widely distributed; protein binding ~70%; crosses placenta, BBB |
| Metabolism | Converted to prednisolone by hepatic 11-beta-HSD1; further metabolism by CYP3A4 |
| Excretion | Renal |
| Half-life | Biological half-life 18–36 hours (HPA suppression); plasma half-life ~3–4 hours (prednisolone) |
| Onset | 1–2 hours |
| Peak | 2 hours |
| Duration | 12–36 hours (biological effect) |
| Protein Binding | 70% |
| Vd | ~1 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP3A4 inducers (rifampin, phenytoin, carbamazepine) | reduce prednisolone levels by 50–60%; may require dose doubling | major |
| NSAIDs | additive GI irritation and peptic ulcer risk | moderate |
| live vaccines | immunosuppression increases risk of vaccine-strain dissemination; avoid with doses >20 mg/day for >14 days | major |
Nursing Considerations
- Administer with food to reduce GI irritation; take in the morning to mimic physiologic cortisol peak and minimize insomnia and HPA suppression
- Never abruptly discontinue after more than 2 weeks of therapy — taper dose gradually to allow HPA axis recovery; warn patient about signs of adrenal insufficiency (fatigue, nausea, dizziness) during tapering
- Monitor blood glucose, blood pressure, weight, electrolytes, and mood; screen for osteoporosis with DEXA scan for long-term therapy; prescribe calcium and vitamin D with any chronic steroid course
- Patient education: take with food; don't abruptly stop; avoid sick contacts; report any signs of infection; stress dosing may be needed during major illness or surgery
Clinical Pearls
- Prednisone is a prodrug that requires hepatic conversion to prednisolone — in severe hepatic disease, prednisolone should be used directly to ensure reliable drug activation
- The Beers-like maxim of 'lowest dose for shortest duration' applies strictly to glucocorticoids — even short burst courses (1 week of 40 mg) cause measurable bone density loss and insulin resistance; these effects accumulate with repeated courses
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.
Adrenal Insufficiency (with Fludrocortisone) Allergic Reactions And Anaphylaxis (adjunct) Anti-emetic (CINV — High-dose) Asthma Exacerbations Autoimmune Diseases (rheumatoid Arthritis, Lupus, IBD, Vasculitis) Cerebral Edema (IV Dexamethasone Preferred For Brain Tumors) COPD Exacerbations Corticosteroid Organ Transplant Rejection Prophylaxis