Glucocorticoids

Generic and Brand Names

• Hydrocortisone — Cortef oral, Solu-Cortef injection

• Cortisone acetate — Cortone acetate

• Prednisone — Deltasone, Rayos delayed-release

• Prednisolone — Orapred, Prelone, Solu-Pred, Pred Forte ophthalmic

• Methylprednisolone — Medrol, Solu-Medrol

• Triamcinolone — Kenalog, Aristospan, Nasacort nasal, Triesence ophthalmic

• Dexamethasone — Decadron, DexPak, Maxidex ophthalmic

• Betamethasone — Celestone, Diprolene topical

• Budesonide — Entocort EC, Uceris, Pulmicort inhalation, Rhinocort nasal

• Fluticasone propionate or furoate — Flovent HFA or Diskus, Arnuity Ellipta, Flonase nasal

• Mometasone — Asmanex inhalation, Nasonex nasal

• Ciclesonide — Alvesco inhalation, Omnaris nasal

• Fludrocortisone — Florinef note primary mineralocorticoid with glucocorticoid activity

Class

• Adrenocortical steroids with glucocorticoid activity anti-inflammatory and immunosuppressive

• Varying mineralocorticoid activity and duration of action

• Formulations include oral, intravenous, intramuscular, intra-articular or soft tissue, inhaled, intranasal, ophthalmic, otic, topical, rectal

Mechanism of Action

• Bind cytosolic glucocorticoid receptors → translocate to nucleus → regulate transcription transactivation of anti-inflammatory genes and transrepression of pro-inflammatory pathways including NF-κB and AP-1

• Rapid non-genomic effects on cellular signaling and vasomotor tone

• Systemic effects include lymphocyte redistribution decreased cytokine production reduced capillary permeability and inhibition of arachidonic acid metabolism

Indications

• Replacement in primary and secondary adrenal insufficiency hydrocortisone preferred fludrocortisone for mineralocorticoid replacement

• Anti-inflammatory and immunosuppressive therapy in asthma COPD exacerbations autoimmune and rheumatologic diseases inflammatory bowel disease nephrotic syndrome dermatologic and allergic disorders hematologic malignancies and nonmalignant immune cytopenias neurologic conditions eg cerebral edema MS relapses

• Antiemetic component of chemotherapy regimens dexamethasone

• Fetal lung maturation betamethasone or dexamethasone antenatal

• Covid-19 severe and critical illness dexamethasone systemic per current treatment paradigms

• Local uses intra-articular bursitis tendon sheath injections topical dermatoses ophthalmic and otic inflammation

• Gastrointestinal budesonide controlled-release for Crohn disease and ulcerative colitis

Dosage and Administration

• Individualize by indication disease severity and patient factors using prednisone-equivalent dosing where helpful

• Oral systemic commonly given once daily morning or divided; high-dose pulses eg methylprednisolone 500 to 1000 mg IV daily for 3 days in selected severe flares

• Stress-dose hydrocortisone for adrenal insufficiency major surgery 50 to 100 mg IV at induction then 25 to 50 mg IV every 6 to 8 hours with taper to baseline

• Inhaled corticosteroids standardized device-specific dosing low medium high ranges by product

• Intranasal once daily per product labelling

• Ophthalmic and topical minimal effective dose shortest duration; consider potency class for topical steroids

• Tapering required after prolonged systemic therapy generally if more than 2 to 3 weeks or if high doses to mitigate adrenal suppression and disease flare tailor taper speed to duration and dose

• Pediatric dosing weight-based; avoid growth suppression by using lowest effective inhaled dose with spacers and rinsing

Monitoring

• Blood pressure weight edema glucose A1C lipids

• Bone health calcium vitamin D fracture risk DEXA in long-term or high-risk

• Ophthalmic pressure cataract formation with prolonged use

• Infection surveillance latent TB HBV when applicable

• Growth velocity in children on inhaled or systemic therapy

• Hypothalamic-pituitary-adrenal axis consider morning cortisol or ACTH stimulation when clinically indicated after long courses

• Electrolytes especially with mineralocorticoid activity sodium potassium

• For IV pulses ECG and blood glucose during and after administration

Contraindications

• Systemic fungal infections except where used as adjunct for immune reconstitution complications

• Live or live-attenuated vaccines during high-dose systemic therapy

• Known hypersensitivity to the drug or components

• Ocular herpes simplex for topical ocular steroids relative due to risk of corneal perforation

Precautions

• Use lowest effective dose shortest duration risk mitigation for osteoporosis peptic ulcer disease diabetes hypertension glaucoma cataracts psychiatric disease latent infections heart failure obesity and older age

• Vaccination timing in immunosuppressed avoid live vaccines consider inactivated vaccines before initiating long-term therapy

• Strong CYP3A4 modulators alter exposure; adjust and monitor

• Pregnancy most agents category where benefits may outweigh risks; prefer lowest effective dose; monitor for gestational diabetes and hypertension; avoid fluorinated potent topicals on large areas

• Lactation generally compatible in standard doses; time breastfeeding to avoid peak plasma concentration when feasible

• Perioperative management and stress dosing in adrenal suppression

• Intra-articular aseptic technique limit frequency to avoid cartilage damage and systemic absorption

Adverse Effects

• Metabolic and endocrine weight gain Cushingoid features hyperglycemia adrenal suppression menstrual irregularities growth suppression in children with chronic high systemic exposure

• Musculoskeletal osteoporosis vertebral and nonvertebral fractures myopathy tendon rupture especially Achilles avascular necrosis femoral head

• Cardiovascular hypertension fluid retention dyslipidemia arrhythmias with high-dose pulses

• Neuropsychiatric mood changes insomnia euphoria depression psychosis delirium with high doses

• Ophthalmic posterior subcapsular cataracts glaucoma elevated intraocular pressure

• Gastrointestinal dyspepsia peptic ulcer disease gastrointestinal bleeding perforation especially with NSAIDs

• Dermatologic skin atrophy striae ecchymoses acne impaired wound healing

• Immunologic increased infection risk reactivation TB HBV opportunistic infections masking of infection signs

• Local route specific hoarseness dysphonia and oral candidiasis with inhaled use prevent with spacer and mouth rinse; nasal irritation epistaxis; ocular burning and IOP rise with ophthalmic; topical skin atrophy telangiectasia

Drug Interactions

• CYP3A4 inhibitors eg ketoconazole clarithromycin ritonavir increase steroid exposure risk of Cushing syndrome and adrenal suppression

• CYP3A4 inducers eg rifampin carbamazepine phenytoin decrease exposure may precipitate adrenal insufficiency or flare

• Fluoroquinolones increased risk of tendon rupture with systemic steroids

• NSAIDs increased GI bleeding and ulceration risk

• Warfarin variable effects monitor INR closely

• Antidiabetic agents may require dose escalation due to hyperglycemic effect

• Live vaccines contraindicated at immunosuppressive doses; blunted response to inactivated vaccines

• Cyclosporine and tacrolimus mutual metabolism effects and seizure risk with cyclosporine plus steroids at high doses

Overdose

• Acute overdose uncommon; chronic excessive exposure leads to features of hypercortisolism

• Management supportive reduce dose consider gradual taper monitor glucose blood pressure electrolytes and mental status

Patient Counselling

• Take oral systemic dose in the morning with food to reduce insomnia and dyspepsia unless directed otherwise

• Do not stop long-term therapy abruptly; follow prescriber taper plan

• Report signs of infection vision changes severe mood shifts black tarry stools edema shortness of breath or severe muscle or bone pain

• For inhaled use rinse mouth spit after each dose use spacer when appropriate

• Ensure adequate calcium vitamin D weight-bearing exercise smoking cessation limit alcohol

• Carry steroid treatment card or medical alert if on chronic therapy or adrenal suppression risk

• Discuss vaccination schedule before and during therapy

Comparison Table — Systemic Glucocorticoids Potency Duration and Mineralocorticoid Activity

Agent	Approximate Oral Equivalency to Prednisone 5 mg	Relative Anti-inflammatory Potency	Mineralocorticoid Activity	Biologic Half-life Duration	Typical Clinical Notes
Hydrocortisone	20 mg equals Prednisone 5 mg	1	High	Short 8 to 12 h	Preferred for adrenal replacement physiologic dosing and stress dosing
Cortisone acetate	25 mg	0.8	Moderate	Short	Prodrug requires hepatic activation less used currently
Prednisone	5 mg	4	Moderate	Intermediate 12 to 36 h	Common oral systemic choice once daily; prodrug to prednisolone
Prednisolone	5 mg	4	Moderate	Intermediate	Preferred in hepatic impairment and pediatrics liquid forms
Methylprednisolone	4 mg	5	Low	Intermediate	IV pulse use and oral tapers less mineralocorticoid effect
Triamcinolone	4 mg	5	Low	Intermediate	Intra-articular soft tissue injections depot forms topical formulations
Dexamethasone	0.75 mg	25	Minimal	Long 36 to 72 h	Potent long duration cerebral edema chemotherapy antiemetic antenatal steroids Covid-19 severe disease
Betamethasone	0.6 mg	30	Minimal	Long	Antenatal lung maturation dermatologic and intra-articular uses
Fludrocortisone	n a prednisone potency not primary	Weak glucocorticoid strong mineralocorticoid	Very high	Long	Mineralocorticoid replacement in primary adrenal insufficiency orthostatic hypotension off-label

Comparison Table — Inhaled Corticosteroids Selected Profiles

Agent	Delivery	Relative Potency inhaled	Systemic Bioavailability	Typical Adult Low Daily Dose	Key Pearls
Beclomethasone HFA	MDI	Moderate	Higher among ICS older	80 to 160 mcg	Fine-particle HFA deposits peripherally mouth rinse to prevent thrush
Budesonide	DPI or neb	Moderate	Low due to high first-pass	180 to 360 mcg	Nebulized option pediatrics acceptable in pregnancy history
Fluticasone propionate	HFA or DPI	High	Very low	100 to 250 mcg	Potent low systemic exposure watch for local thrush
Fluticasone furoate	DPI	Very high	Very low	100 mcg once daily	Once-daily adherence advantage
Mometasone	DPI or HFA	High	Very low	200 mcg	Low oral bioavailability favorable systemic profile
Ciclesonide	HFA prodrug	Moderate	Very low after activation in lung	80 to 160 mcg	Activated in airway reduced oropharyngeal effects