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Budesonide
Budesonide’s targeted delivery minimizes systemic toxicity, making it a cornerstone in managing inflammatory conditions. Adherence to guidelines from the BNF, Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology ensures optimal dosing, monitoring, and safety.
Budesonide is a synthetic glucocorticoid with potent anti-inflammatory and immunosuppressive properties. Its mechanism involves:
- Binding to Glucocorticoid Receptors: Enters target cells and binds to intracellular receptors, modulating gene expression.
- Inhibition of Inflammatory Mediators: Suppresses phospholipase A2, reducing prostaglandin and leukotriene synthesis (Lippincott).
- Immune Cell Suppression: Inhibits cytokine release (e.g., IL-1, TNF-α) and reduces eosinophil, mast cell, and lymphocyte activity.
- Localized Action: Designed for high topical potency with minimal systemic absorption, making it ideal for inhaled, nasal, and enteric formulations.
Budesonide is approved for:
- Respiratory Diseases:
- Asthma: Maintenance therapy via inhaler (often combined with formoterol in Symbicort®).
- Chronic Obstructive Pulmonary Disease (COPD): Reduces exacerbations.
- Allergic Rhinitis: Nasal spray (e.g., Rhinocort®).
- Gastrointestinal Disorders:
- Crohn’s Disease: Enteric-coated tablets (e.g., Entocort®) for ileal and ascending colon inflammation.
- Eosinophilic Esophagitis: Off-label use.
- Dermatological Conditions:
- Topical cream for eczema and inflammatory skin disorders.
- Croup in Children: Nebulized budesonide as an alternative to dexamethasone.
Adults:
- Asthma/COPD (Inhalation): 200–800 mcg twice daily (BNF).
- Allergic Rhinitis (Nasal): 100–200 mcg per nostril once daily.
- Crohn’s Disease (Oral): 9 mg once daily in the morning for up to 8 weeks; taper to 6 mg for maintenance.
Children:
- Asthma (≥6 years): 100–400 mcg twice daily via inhaler.
- Croup (Nebulized): 2 mg single dose.
Special Populations:
- Renal/Hepatic Impairment: No dose adjustment required for inhalation/nasal routes. Use oral forms cautiously in severe liver disease.
- Pregnancy: Category C; use lowest effective dose (BNF).
- Elderly: Monitor for systemic effects (e.g., osteoporosis).
- Local Effects:
- Inhaled/Nasal: Oral thrush, hoarseness, epistaxis, nasal irritation.
- Oral: Dyspepsia, nausea.
- Systemic Effects (rare with topical use):
- Adrenal suppression, hyperglycemia, osteoporosis, growth retardation (children).
- Mood changes, insomnia, glaucoma, cataracts (long-term use).
- Contraindications: Hypersensitivity to corticosteroids, systemic fungal infections.
- Infections: Avoid in active tuberculosis or untreated bacterial/viral infections.
- Monitoring:
- Adrenal Function: For long-term/high-dose therapy.
- Bone Density: In patients at risk for osteoporosis.
- Growth: In pediatric patients.
- Withdrawal: Taper gradually to avoid adrenal crisis.
- CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir): Increase budesonide levels (avoid combination or reduce dose).
- NSAIDs: Increased gastrointestinal ulcer risk.
- Vaccines: Avoid live vaccines (e.g., MMR, varicella) due to immunosuppression.
- Diuretics: Enhanced hypokalemia risk.
- Generic: Budesonide.
- Brand Names:
- Inhaler: Pulmicort®, Symbicort® (with formoterol).
- Nasal: Rhinocort®.
- Oral: Entocort®.
- Topical: Cortifoam®, Budesonide cream.
