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Prednisone

Deltasone | Rayos | Sterapred

FDA ApprovedEndocrine AgentsCorticosteroids
FDA: 1955Half-life: 2-3 hours (plasma); 18-36 hours (biological)Pregnancy: Category C

Overview

Synthetic corticosteroid prodrug converted to prednisolone (active form) in the liver. Binds to glucocorticoid receptors, modulating gene transcription to reduce inflammation and suppress immune respo

Indications

  • Allergic disorders
  • Asthma exacerbations
  • Autoimmune diseases (lupus, rheumatoid arthritis)
  • Inflammatory bowel disease
  • Organ transplant rejection prevention
  • Certain cancers (lymphoma, leukemia)
  • Adrenal insufficiency

Contraindications

  • Systemic fungal infections
  • Administration of live vaccines during immunosuppressive doses

Classification

Endocrine AgentsCorticosteroidsImmune SystemEndocrine System

Mechanism of Action

Synthetic corticosteroid prodrug converted to prednisolone (active form) in the liver. Binds to glucocorticoid receptors, modulating gene transcription to reduce inflammation and suppress immune responses.

Pharmacodynamics

Potent anti-inflammatory and immunosuppressant. 4x glucocorticoid potency of cortisol. Minimal mineralocorticoid activity at therapeutic doses.

Pharmacokinetics

Absorption
Rapidly absorbed from GI tract.
Distribution
Widely distributed. Crosses placenta and enters breast milk.
Metabolism
Hepatic conversion to prednisolone (active metabolite) by 11-beta-hydroxysteroid dehydrogenase.
Excretion
Renal.
Half-life
2-3 hours (plasma); 18-36 hours (biological)
Bioavailability
70-80%
Protein Binding
65-91%

Dosage

Typical dosage: 5-60mg/day (highly variable by condition)

Available Forms

  • Tablet
  • Tablet (delayed-release)
  • Oral solution

Side Effects

Common

  • Increased appetite
  • Weight gain
  • Insomnia
  • Mood changes
  • Fluid retention
  • Elevated blood glucose

Serious

  • Adrenal suppression
  • Osteoporosis
  • Immunosuppression/infection risk
  • Cushing syndrome
  • Avascular necrosis
  • GI bleeding

Rare

  • Psychosis
  • Pancreatitis
  • Tendon rupture
  • Posterior subcapsular cataracts

Drug Interactions

moderate

Increased risk of GI ulceration and bleeding. Use gastroprotective agent if combination necessary.

moderate

Corticosteroids may enhance or diminish anticoagulant effect. Monitor INR closely when initiating, changing dose, or discontinuing.

Warnings

Pregnancy

Category C

Toxicity

LD50 varies by species (very wide safety margin for acute dosing)

Overdose

Acute overdose rarely life-threatening. Chronic overdose causes Cushing syndrome. Treatment: gradual taper (never abrupt discontinuation after prolonged use).

References

Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.