PharmaceuticalProdrugGlucocorticoidCorticosteroid

Cortisone

Also known as Cortisone acetate · Cortone

Written by enwyReviewed 5 Aug 20262 sources0 comments

Cortisone is a naturally occurring glucocorticoid prodrug, inactive until the enzyme 11-beta-HSD1 converts it to hydrocortisone (cortisol) in the liver. It was the first glucocorticoid used clinically. Today systemic cortisone is largely superseded by hydrocortisone and synthetics, but 'cortisone shot' remains a colloquial term for corticosteroid joint injections (usually other steroids). Its potency roughly equals cortisol, with mineralocorticoid activity.

01 Overview

Cortisone acetate was the original oral corticosteroid, but because it must be converted to cortisol before it works, hydrocortisone is now preferred for reliable dosing. Cortisone retains historical and occasional replacement use. In popular usage 'cortisone injection' has become a generic label for any corticosteroid joint or soft-tissue shot, most of which actually use methylprednisolone or triamcinolone.

The pharmacology mirrors cortisol: modest anti-inflammatory potency, notable salt-retaining activity, short duration, and the standard glucocorticoid liability of catabolism, immunosuppression and HPA suppression at supraphysiologic doses. WADA restricts systemic administration in-competition.

02 Mechanism

Prodrug reduced by 11-beta-HSD1 to cortisol (hydrocortisone), which then activates glucocorticoid and mineralocorticoid receptors.

03 Dosing

Tier	Dose	Route	Notes
Replacement/anti-inflammatory	25–50 mg/day	Oral	25 mg cortisone approximates 20 mg hydrocortisone.
IM cortisone acetate	25–100 mg	IM	Historical/occasional systemic use.

04 Effects

Effect	Magnitude	Evidence
Anti-inflammatory actionEffective once converted to cortisol; modest potency.	~cortisol equivalent	Clinical
Glucocorticoid replacementCan serve as replacement in adrenal insufficiency where conversion is intact.	physiologic	Clinical

05 Side effects

Effect	Severity	Frequency	Evidence
Fluid retention / hypertensionSalt and water retention from mineralocorticoid activity.	Moderate	Common at higher doses	Clinical
HPA axis suppressionSuppresses endogenous cortisol at supraphysiologic doses.	Moderate	With sustained use	Clinical
Unreliable action if conversion impairedDepends on hepatic 11-beta-HSD1; effect blunted with liver impairment.	Mild	In liver dysfunction	Clinical

06 Legal status

United States

Prescription drug (Rx)

Not controlled; systemic use WADA-restricted in-competition. · as of Jan 2026

United Kingdom

POM

as of Jan 2026

07 References

Cortisone: history and pharmacology of the first corticosteroidMayo Clin Proc

11-beta-HSD1 and glucocorticoid activationEndocr Rev

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.