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Saturday, July 26, 2025

Corticosteroids


Corticosteroids are a class of steroid hormones that are either produced naturally in the adrenal cortex or synthetically manufactured for therapeutic use. These compounds are integral in managing a wide array of inflammatory, autoimmune, and endocrine conditions. Corticosteroids function by mimicking the effects of cortisol, a hormone naturally produced by the adrenal glands. They are categorized primarily into glucocorticoids (which affect carbohydrate metabolism and inflammation) and mineralocorticoids (which regulate salt and water balance).

1. Classification

A. By Type

  • Glucocorticoids

    • Prednisolone

    • Dexamethasone

    • Hydrocortisone

    • Methylprednisolone

    • Betamethasone

    • Triamcinolone

  • Mineralocorticoids

    • Fludrocortisone

    • Deoxycorticosterone

B. By Duration of Action

  • Short-acting (t1/2 < 12 hrs): Cortisone, Hydrocortisone

  • Intermediate-acting (t1/2 12–36 hrs): Prednisone, Prednisolone, Methylprednisolone

  • Long-acting (t1/2 > 36 hrs): Dexamethasone, Betamethasone

2. Mechanism of Action

Corticosteroids enter cells and bind to cytoplasmic glucocorticoid or mineralocorticoid receptors. The receptor-ligand complex translocates to the nucleus and modulates gene expression by:

  • Increasing anti-inflammatory protein synthesis (e.g., lipocortin-1, which inhibits phospholipase A2)

  • Suppressing pro-inflammatory gene transcription, such as IL-1, IL-6, TNF-α, and COX-2

  • Inducing apoptosis in certain immune cells (e.g., eosinophils, T lymphocytes)

This results in immunosuppression, anti-inflammation, reduction of cytokine production, and stabilization of cell membranes, including lysosomes.

3. Pharmacological Actions

  • Anti-inflammatory: By inhibiting inflammatory cytokines and prostaglandins

  • Immunosuppressive: Used in autoimmune disorders and transplant rejection

  • Metabolic effects: Increase gluconeogenesis, cause protein catabolism

  • Fluid-electrolyte balance: Sodium retention, potassium loss (primarily mineralocorticoids)

  • Mood alteration: Can cause euphoria or psychosis

  • Hematologic: Increase neutrophils, decrease eosinophils, basophils, monocytes, and lymphocytes

4. Therapeutic Uses

A. Systemic Use

  • Autoimmune diseases: Rheumatoid arthritis, systemic lupus erythematosus (SLE)

  • Respiratory conditions: Asthma, COPD exacerbations

  • Endocrine disorders: Addison’s disease, congenital adrenal hyperplasia

  • Oncology: Acute lymphoblastic leukemia, multiple myeloma, to prevent chemotherapy-induced nausea

  • Allergic reactions: Anaphylaxis, drug hypersensitivity

  • Organ transplant: Prevention and treatment of graft rejection

B. Topical Use

  • Dermatologic: Psoriasis, eczema, atopic dermatitis, contact dermatitis

  • Ophthalmic: Uveitis, allergic conjunctivitis

  • Otic: Otitis externa with inflammation

C. Inhalational/Nasal Use

  • Inhaled corticosteroids (ICS): Asthma, COPD (e.g., budesonide, fluticasone)

  • Intranasal corticosteroids: Allergic rhinitis, nasal polyps (e.g., mometasone, beclometasone)

D. Local Injection

  • Intra-articular for rheumatoid arthritis, bursitis, tenosynovitis

5. Commonly Used Corticosteroids by Route

  • Oral: Prednisolone, Dexamethasone, Methylprednisolone

  • Intravenous (IV/IM): Hydrocortisone sodium succinate, Dexamethasone phosphate

  • Topical: Betamethasone valerate, Clobetasol propionate

  • Inhaled: Fluticasone, Budesonide, Beclometasone

  • Nasal sprays: Mometasone, Fluticasone

  • Ophthalmic: Prednisolone acetate, Dexamethasone

6. Dosage Considerations

Doses vary widely depending on:

  • Condition treated

  • Severity of disease

  • Route of administration

  • Patient's weight, age, and comorbidities

Tapering is essential after prolonged use to prevent adrenal suppression.

7. Adverse Effects

A. Short-Term Use

  • Increased appetite, weight gain

  • Fluid retention

  • Mood changes, insomnia

  • Hyperglycemia

  • Hypertension

B. Long-Term Use

  • Cushingoid features (moon face, central obesity, buffalo hump)

  • Osteoporosis

  • Cataracts, glaucoma

  • Peptic ulcers

  • Growth retardation in children

  • Myopathy

  • Skin thinning, easy bruising

  • Adrenal suppression (HPA axis suppression)

  • Increased infection risk

  • Avascular necrosis (especially femoral head)

8. Contraindications

  • Systemic fungal infections (absolute contraindication for systemic corticosteroids)

  • Hypersensitivity to the drug

  • Live or attenuated vaccines in immunocompromised individuals

  • Use with caution in:

    • Diabetes mellitus

    • Hypertension

    • Psychiatric disorders

    • Peptic ulcer disease

    • Osteoporosis

    • Glaucoma

9. Precautions and Monitoring

  • Monitor:

    • Blood glucose levels

    • Blood pressure

    • Weight

    • Bone mineral density (especially in postmenopausal women)

    • Eye exams (for cataract/glaucoma)

  • Supplement calcium and vitamin D during chronic therapy

  • Consider bisphosphonates to prevent steroid-induced osteoporosis

  • Assess for latent infections (e.g., TB) before initiation

10. Drug Interactions

A. Pharmacokinetic Interactions

  • Enzyme inducers (e.g., rifampicin, phenytoin, carbamazepine): ↓ corticosteroid efficacy

  • Enzyme inhibitors (e.g., ketoconazole, itraconazole): ↑ corticosteroid levels

B. Pharmacodynamic Interactions

  • NSAIDs: ↑ risk of GI bleeding

  • Diuretics (loop, thiazides): ↑ risk of hypokalemia

  • Antidiabetics: Corticosteroids counteract glycemic control

  • Vaccines: Reduced immune response; live vaccines contraindicated

11. Withdrawal and Tapering

Abrupt discontinuation of corticosteroids after prolonged use can cause:

  • Adrenal crisis (potentially fatal)

  • Fatigue, weakness, hypotension, hypoglycemia

  • Disease flare-up

Tapering schedule depends on:

  • Duration and dose of therapy

  • Underlying condition

For example:

  • Prednisolone 40 mg daily >2 weeks requires slow tapering over weeks/months

12. Special Populations

A. Pregnancy

  • Corticosteroids cross the placenta

  • Can be used for fetal lung maturity (e.g., betamethasone at 24–34 weeks gestation)

  • Long-term use may result in fetal adrenal suppression, growth restriction

B. Lactation

  • Low amounts excreted in breast milk

  • Generally considered compatible with breastfeeding (monitor infant)

C. Pediatrics

  • Long-term use risks: growth retardation, HPA axis suppression, osteoporosis

D. Elderly

  • Increased risk of osteoporosis, diabetes, psychiatric effects, and infection

13. Examples of Fixed Combination Corticosteroid Products

  • Salmeterol + Fluticasone: Asthma, COPD

  • Formoterol + Budesonide: Asthma, COPD

  • Clotrimazole + Beclomethasone: Fungal skin infections with inflammation

  • Mupirocin + Mometasone: Infected eczema

14. Steroid-Sparing Agents

Because of the side effects associated with long-term corticosteroid use, alternative or adjunctive therapies known as steroid-sparing agents are used:

  • Methotrexate

  • Azathioprine

  • Mycophenolate mofetil

  • Biologics (e.g., infliximab, adalimumab)

  • Calcineurin inhibitors (e.g., tacrolimus, cyclosporine)

These help reduce the required corticosteroid dose and minimize toxicity.

15. Corticosteroid Sensitivity and Testing

  • Patients suspected of adrenal insufficiency undergo ACTH stimulation test

  • Late-night salivary cortisol and dexamethasone suppression test are used in diagnosing Cushing’s syndrome

  • Corticosteroid hypersensitivity (rare) may require alternative formulations or desensitization

16. Recent Advances and Trends

  • Liposomal corticosteroids: Better tissue penetration, fewer systemic effects

  • Once-daily inhaled corticosteroids: Improved compliance

  • Topical steroid alternatives: Calcineurin inhibitors (e.g., pimecrolimus) in dermatology

  • Biomarker-based personalization: Tailoring steroid use in asthma based on eosinophil levels

17. Abuse and Doping in Sports

Some athletes misuse corticosteroids for:

  • Anti-inflammatory effects to mask pain

  • Enhancing endurance by reducing fatigue-related inflammation

World Anti-Doping Agency (WADA) regulates systemic corticosteroid use in competitive sports.

18. Steroid Phobia and Patient Education

Many patients fear corticosteroids due to their side effects. Healthcare professionals must:

  • Educate on the necessity and benefits

  • Discuss tapering plans

  • Emphasize regular follow-up and lab monitoring



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