Question
Glucocorticosteroids
Answer
Classification (by glucocorticoid:mineralocorticoid potency ratio)
| Group | Examples |
|---|---|
| Short-acting, high mineralocorticoid activity | Hydrocortisone, Cortisone |
| Intermediate-acting, minimal mineralocorticoid activity | Prednisolone, Methylprednisolone |
| Long-acting, negligible mineralocorticoid activity | Dexamethasone, Betamethasone |
| Pure mineralocorticoid | Fludrocortisone |
Mechanism of action: diffuse across the cell membrane and bind cytoplasmic glucocorticoid receptors; the activated complex translocates to the nucleus and alters gene transcription. Key effects: induction of lipocortin-1 (inhibits phospholipase A2, cutting off the eicosanoid cascade at its source), suppression of pro-inflammatory cytokine transcription, reduced leukocyte migration, and lymphocyte suppression.
Therapeutic uses: replacement therapy (Addison’s disease), anti-inflammatory/immunosuppressive use (rheumatoid arthritis, SLE), allergic emergencies, organ transplant rejection prophylaxis, cerebral edema, nephrotic syndrome, antenatal fetal lung maturation.
Adverse effects: Cushingoid features, hyperglycemia, osteoporosis, peptic ulceration, increased infection susceptibility, hypertension, growth retardation in children, cataract/glaucoma, adrenal suppression, psychiatric disturbances, myopathy.