endocrine:drugs:fluticasone
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Corticosteroids
Corticosteroids are synthetic analogs of adrenal cortex hormones used for their potent anti-inflammatory and immunosuppressive effects.
They mimic:
- Cortisol (glucocorticoid activity)
- Aldosterone (mineralocorticoid activity – some agents)
Used across systems:
- Asthma
- Autoimmune disease
- Dermatologic conditions
- Transplant medicine
Classification
Systemic Glucocorticoids
Inhaled / Intranasal
Topical
- Various potency classes
Mechanism of Action
Corticosteroids act via intracellular glucocorticoid receptors.
Stepwise:
1) Drug diffuses across cell membrane 2) Binds cytoplasmic glucocorticoid receptor 3) Complex translocates to nucleus 4) Alters gene transcription
Results:
- ↓ Pro-inflammatory cytokines (IL-1, IL-2, IL-4, IL-5, IL-6, TNF-α)
- ↓ Eosinophil survival
- ↓ T-cell activation
- ↓ Mast cell mediator release
- ↓ Prostaglandin synthesis (via ↓ phospholipase A2)
- ↓ Leukotriene production
Effect:
Broad suppression of inflammation.
Onset:
- Hours to days (genomic mechanism)
Glucocorticoid vs Mineralocorticoid Activity
| Drug | Glucocorticoid Potency | Mineralocorticoid Activity |
|---|---|---|
| Hydrocortisone | Low | Moderate |
| Prednisone | Moderate | Low |
| Methylprednisolone | Moderate | Minimal |
| Dexamethasone | High | None |
Clinical relevance:
- Mineralocorticoid activity → fluid retention, hypertension
- Dexamethasone preferred when fluid retention undesirable
Indications (Allergy Context)
Type I hypersensitivity late-phase control:
Allergic rhinitis:
- Intranasal first-line
Asthma:
- Inhaled maintenance therapy
Severe allergic reactions:
- Adjunct in anaphylaxis (not first-line)
Autoimmune and inflammatory disease:
- Broad use
Adverse Effects
Short-term:
- Mood changes
- Hyperglycemia
- Fluid retention
- Insomnia
Long-term:
- Adrenal suppression
- Osteoporosis
- Cushingoid appearance
- Muscle wasting
- Increased infection risk
- Peptic ulcer disease
Mechanism:
Systemic immunosuppression and metabolic alteration.
Hypothalamic–Pituitary–Adrenal (HPA) Axis Suppression
Chronic steroid use suppresses endogenous cortisol production.
Abrupt withdrawal may cause:
- Adrenal insufficiency
- Hypotension
- Fatigue
- Crisis in severe cases
Taper when:
- High dose
- Prolonged use (>2–3 weeks)
Clinical Pearls
- Intranasal corticosteroids are superior to oral antihistamines for nasal congestion.
- Steroids suppress late-phase allergic inflammation.
- Dexamethasone has no mineralocorticoid activity.
- Always consider HPA suppression with prolonged systemic therapy.
- In anaphylaxis, epinephrine is first-line — steroids are adjunctive.
Related Pages
endocrine/drugs/fluticasone.1770925111.txt.gz · Last modified: by andrew2393cns
