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Monday, July 28, 2025

Steroids


Drug class name: Corticosteroids
Subclasses:

  • Glucocorticoids – primarily regulate metabolism, immune function, and inflammation

  • Mineralocorticoids – primarily influence electrolyte and fluid balance

Endogenous origin:

  • Corticosteroids are steroid hormones produced by the adrenal cortex in response to adrenocorticotropic hormone (ACTH).

  • Two primary endogenous hormones:

    • Cortisol (hydrocortisone) – glucocorticoid

    • Aldosterone – mineralocorticoid

Synthetic corticosteroids mimic these actions and are widely used in medicine to manage inflammation, suppress the immune system, and correct adrenal insufficiency.

2. Classification

Glucocorticoids (Anti-inflammatory and immunosuppressive)

Examples:

  • Hydrocortisone

  • Prednisolone

  • Methylprednisolone

  • Dexamethasone

  • Betamethasone

  • Triamcinolone

  • Budesonide

  • Fluticasone

  • Beclometasone

Mineralocorticoids (Salt-retaining)

Examples:

  • Fludrocortisone

  • Deoxycorticosterone

Mixed activity

  • Hydrocortisone (both glucocorticoid and mineralocorticoid activity)

3. Mechanism of Action

Corticosteroids exert their effects by binding to intracellular steroid receptors in the cytoplasm. Upon binding, the complex translocates into the nucleus, where it modulates transcription of target genes.

Glucocorticoid effects:

  • Anti-inflammatory: Suppression of prostaglandins, cytokines (e.g., IL-1, TNF-α), and other mediators

  • Immunosuppression: Reduces lymphocyte, monocyte, and eosinophil activity

  • Metabolic: Increases gluconeogenesis, reduces peripheral glucose uptake, promotes protein catabolism, fat redistribution

  • Anti-proliferative: Inhibits fibroblast activity and collagen formation

Mineralocorticoid effects:

  • Sodium retention in the distal renal tubules

  • Potassium and hydrogen ion excretion

  • Regulated through the renin–angiotensin–aldosterone system (RAAS)

4. Pharmacokinetics

Absorption:

  • Rapid oral absorption (e.g., prednisolone bioavailability ~70–90%)

  • Inhaled, topical, and rectal forms act locally, with limited systemic absorption unless overdosed or skin barrier is compromised

Distribution:

  • Lipophilic nature allows widespread tissue penetration

  • Binds to corticosteroid-binding globulin (CBG) and albumin

Metabolism:

  • Primarily hepatic metabolism via cytochrome P450 enzymes

  • Dexamethasone and betamethasone are long-acting with minimal mineralocorticoid activity

Excretion:

  • Inactive metabolites excreted in urine

5. Indications

5.1 Inflammatory and Autoimmune Diseases

  • Rheumatoid arthritis

  • Systemic lupus erythematosus

  • Vasculitis syndromes

  • Sarcoidosis

  • Polymyalgia rheumatica

  • Ankylosing spondylitis

  • Psoriasis and eczema

5.2 Respiratory Diseases

  • Asthma

  • Chronic obstructive pulmonary disease (COPD)

  • Hypersensitivity pneumonitis

  • Interstitial lung disease

  • Croup (dexamethasone or budesonide)

5.3 Gastrointestinal

  • Inflammatory bowel disease (Crohn’s disease, ulcerative colitis)

  • Autoimmune hepatitis

5.4 Neurological

  • Multiple sclerosis exacerbations

  • Cerebral edema

  • Myasthenia gravis

  • Bell’s palsy

5.5 Endocrine

  • Adrenal insufficiency (Addison’s disease)

  • Congenital adrenal hyperplasia

  • Adrenal crisis

5.6 Neoplastic Diseases

  • Lymphomas, leukemias

  • Multiple myeloma

  • Brain tumors (reduce cerebral edema)

5.7 Allergic and Hypersensitivity Reactions

  • Anaphylaxis (adjunctive)

  • Severe allergic dermatitis

  • Drug-induced hypersensitivity

5.8 Organ Transplantation

  • Prevention and treatment of organ rejection

  • Graft-versus-host disease (GVHD)

5.9 Miscellaneous

  • Nausea and vomiting related to chemotherapy

  • COVID-19 severe pneumonia (dexamethasone)

  • Preterm labor to accelerate fetal lung maturation (betamethasone)

6. Dosage and Formulations

Routes of administration

  • Oral tablets: prednisolone, dexamethasone

  • Injectables: methylprednisolone, hydrocortisone, dexamethasone

  • Topical creams/ointments: hydrocortisone, mometasone, betamethasone

  • Inhalers: beclometasone, fluticasone, budesonide

  • Rectal formulations: hydrocortisone suppositories/enemas

  • Ophthalmic preparations: prednisolone acetate drops

Duration of Action (glucocorticoids)

DrugPotencyHalf-lifeRelative activity
HydrocortisoneLow8–12 hoursBoth glucocorticoid and mineralocorticoid
Prednisone/PrednisoloneMedium12–36 hoursPrimarily glucocorticoid
DexamethasoneHigh36–72 hoursPure glucocorticoid
FludrocortisoneVery high18–36 hoursMostly mineralocorticoid



7. Contraindications

  • Uncontrolled infections (e.g., systemic fungal infections, tuberculosis)

  • Known hypersensitivity to the specific corticosteroid or formulation

  • Cushing’s syndrome (endogenous corticosteroid excess)

  • Recent live vaccinations (when using high-dose systemic steroids)

  • Severe psychosis or psychiatric instability (relative contraindication)

  • Peptic ulcer disease (relative contraindication)

8. Warnings and Precautions

  • Immunosuppression: Prolonged corticosteroid use increases susceptibility to infections; consider prophylaxis (e.g., pneumocystis pneumonia).

  • Adrenal suppression: Long-term use suppresses hypothalamic-pituitary-adrenal (HPA) axis; tapering required to avoid adrenal crisis.

  • Hyperglycemia and diabetes: Increases insulin resistance; monitor glucose levels.

  • Osteoporosis: Accelerates bone resorption and inhibits bone formation; prophylactic calcium and vitamin D advised.

  • Hypertension: Promotes sodium retention and vascular reactivity.

  • Psychiatric effects: May cause mood swings, insomnia, depression, psychosis.

  • Peptic ulcers and GI bleeding: Risk increases with NSAID use; consider gastroprotection.

  • Eye complications: Cataracts, glaucoma with prolonged use; routine ophthalmic monitoring recommended.

  • Myopathy: Especially with high doses or concomitant neuromuscular blockers.

  • Growth suppression: In children on chronic corticosteroids.

9. Adverse Effects

Acute (short-term use)

  • Hyperglycemia

  • Insomnia

  • Fluid retention

  • Mood changes (euphoria, irritability)

  • Increased appetite and weight gain

  • Hypertension

  • Indigestion or peptic symptoms

Chronic (long-term use)

  • Cushingoid appearance (moon face, buffalo hump)

  • Osteoporosis and fractures

  • Skin thinning and easy bruising

  • Cataracts and glaucoma

  • Adrenal suppression and crisis on abrupt withdrawal

  • Diabetes mellitus

  • Central obesity

  • Muscle wasting

  • Delayed wound healing

  • Increased susceptibility to infection

  • Hirsutism or acne

  • Menstrual irregularities

10. Drug Interactions

  • NSAIDs: Increase risk of GI bleeding and ulcers

  • Antidiabetics: Corticosteroids antagonize glycemic control

  • Vaccines: Reduced efficacy of live vaccines and increased risk of dissemination

  • Anticonvulsants (e.g., phenytoin, carbamazepine): Increase steroid metabolism, lowering efficacy

  • Antifungals (e.g., ketoconazole): Reduce steroid metabolism, increasing risk of side effects

  • Warfarin: Effects may be enhanced or reduced; monitor INR closely

  • Diuretics: Risk of hypokalemia when combined with steroids

  • Rifampin: Induces steroid metabolism; may require dose adjustment

11. Special Considerations

Tapering

  • Abrupt cessation after prolonged use (>2 weeks) risks adrenal insufficiency

  • Taper slowly: reduce dose by 10–20% every 5–7 days or as clinically tolerated

  • Assess HPA axis recovery with morning cortisol or ACTH stimulation test when planning full withdrawal

Stress Dosing

  • Patients on long-term steroids may need higher doses during illness, surgery, trauma (“steroid cover”)

  • Example: hydrocortisone 100 mg IV every 8 hours during major surgery in chronic steroid users

Pregnancy and Breastfeeding

  • Prednisolone and hydrocortisone are preferred due to lower placental transfer

  • Monitor for maternal hyperglycemia and fetal growth restriction

  • Breastfeeding: small amounts secreted; generally considered compatible with short-term use

12. Use in Specific Populations

Elderly

  • Increased sensitivity to adverse effects, especially osteoporosis, muscle wasting, diabetes

  • Monitor bone density and metabolic parameters closely

Pediatrics

  • Risk of growth suppression with prolonged systemic use

  • Topical corticosteroids can also cause systemic effects if overused

  • Use the lowest effective dose for shortest time

Hepatic Impairment

  • Metabolism may be impaired in severe hepatic disease

  • Use with caution; monitor closely for signs of toxicity

Renal Impairment

  • Generally safe; no major dose adjustments required

  • Risk of fluid retention and electrolyte imbalance should be monitored

13. Monitoring and Follow-up

  • Blood pressure – particularly during high-dose systemic therapy

  • Blood glucose – in all patients, especially diabetics

  • Bone mineral density (DEXA scans) – baseline and annually if long-term use

  • Ophthalmologic exams – for cataracts and glaucoma

  • Weight and BMI – watch for weight gain and fat redistribution

  • Signs of infection – especially in immunocompromised patients

  • Electrolytes – particularly potassium with mineralocorticoid activity

  • Growth charts – in children on systemic corticosteroids

  • Mood and psychological status – screen for steroid-induced psychiatric effects



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