Prednisone

Mechanism of action

Glucocorticoid receptor agonist (corticosteroid)

In plain language

A steroid that turns down inflammation and calms an overactive immune system by acting on receptors inside cells throughout the body.

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ClinicalPlain language

How it works

Prednisone is a synthetic glucocorticoid that itself is largely a prodrug, converted by the liver to its active metabolite, prednisolone. Like other glucocorticoids, it diffuses into cells and binds the cytosolic glucocorticoid receptor; the activated receptor-ligand complex translocates to the nucleus, where it upregulates anti-inflammatory genes (including lipocortin-1, which inhibits phospholipase A2 and downstream eicosanoid synthesis) and represses pro-inflammatory transcription factors such as NF-κB and AP-1. This transcriptional reprogramming suppresses production of cytokines, prostaglandins, and leukotrienes and reduces migration of inflammatory cells, producing the drug's anti-inflammatory and immunosuppressive effects. The manufacturer's label notes that, like other glucocorticoids, prednisone causes profound and varied metabolic effects and modifies the body's immune responses to diverse stimuli.

Therapeutic applications

Indicated across a broad range of conditions responsive to glucocorticoid therapy, including endocrine disorders (primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia of malignancy, nonsuppurative thyroiditis); as short-term adjunctive therapy for acute exacerbations of rheumatic and collagen-vascular diseases such as rheumatoid arthritis, ankylosing spondylitis, acute gouty arthritis, systemic lupus erythematosus, and dermatomyositis; and for severe dermatologic diseases and severe allergic or ophthalmic inflammatory conditions unresponsive to conventional treatment. Also used for respiratory diseases including symptomatic sarcoidosis and aspiration pneumonitis; hematologic disorders such as idiopathic thrombocytopenic purpura and autoimmune hemolytic anemia; palliative management of leukemias and lymphomas; to induce diuresis or remission of proteinuria in nephrotic syndrome; and during acute exacerbations of ulcerative colitis, regional enteritis, and multiple sclerosis.

Class

Small molecule

Therapeutic area

Endocrine / Anti-inflammatory

Source

PubChem CID 5865 ↗FDA label (DailyMed) ↗