Budison F

Approved Uses:

• Asthma (Maintenance Treatment):
• Indicated for patients aged ≥6 years whose symptoms are not controlled on inhaled corticosteroids alone.
• Chronic Obstructive Pulmonary Disease (COPD):
• For maintenance treatment and reduction of exacerbations in adults with moderate to very severe COPD, including chronic bronchitis and/or emphysema.

Clinically Accepted Off-Label Uses:

• Exercise-Induced Bronchospasm:
• Used as part of maintenance therapy in individuals with exercise-induced airway constriction.
• SMART Regimen (Single Maintenance and Reliever Therapy):
• For adult asthma patients using the same combination inhaler for both maintenance and symptom relief, where regional guidelines support this approach.

Route of Administration: Inhalation only (via DPI or MDI). Not for oral ingestion.

Asthma (Adults & Adolescents ≥12 years):

• Maintenance dose: 160 mcg Budesonide + 4.5 mcg Formoterol, 1–2 inhalations twice daily.
• Maximum dose: Up to 640 mcg Budesonide + 18 mcg Formoterol daily in divided doses.

Asthma (Children 6–11 years):

• 80 mcg Budesonide + 4.5 mcg Formoterol, 1–2 inhalations twice daily depending on severity.

COPD (Adults only):

• 160 mcg Budesonide + 4.5 mcg Formoterol, 2 inhalations twice daily.

Special Populations:

• Elderly: No adjustment needed; monitor for cardiovascular or CNS side effects.
• Hepatic Impairment: Use cautiously; monitor systemic effects.
• Renal Impairment: No dosage adjustment necessary.

Important Notes:

• Rinse mouth after each dose to minimize oral candidiasis.
• Consistent use is essential for effectiveness; not for acute symptom relief.

This fixed-dose combination contains Budesonide, an inhaled corticosteroid that binds to intracellular glucocorticoid receptors, suppressing pro-inflammatory gene expression and cytokine release, thereby reducing bronchial inflammation. Formoterol, a long-acting β₂-adrenergic receptor agonist (LABA), stimulates adenylate cyclase, increasing intracellular cAMP in airway smooth muscle, resulting in bronchodilation. Their synergistic action enhances both control of airway inflammation and sustained bronchodilation, improving asthma and COPD symptoms.

• Absorption: Budesonide oral bioavailability is ~39%; Formoterol is rapidly absorbed via lungs.
• Peak Plasma Concentration:
• Budesonide: ~15–45 minutes
• Formoterol: ~1–2 hours
• Distribution:
• Budesonide: Vd ~3 L/kg; protein binding ~90%.
• Formoterol: Vd ~4 L/kg; protein binding ~60%.
• Metabolism:
• Budesonide is extensively metabolized by CYP3A4.
• Formoterol is metabolized by CYP2D6 and conjugation.
• Half-life:
• Budesonide: ~2–3.6 hours
• Formoterol: ~10–14 hours
• Excretion:
• Budesonide: 60% urine (as metabolites)
• Formoterol: ~62% urine, ~24% feces

• Pregnancy:
• Budesonide: Category B (inhaled form)
• Formoterol: Category C
• Use only if clearly needed. Prefer Budesonide monotherapy when possible.
• Lactation:
• Budesonide is excreted in breast milk in minimal amounts.
• Limited data on Formoterol; caution advised.
• Monitor infants for systemic corticosteroid or beta-agonist effects if used during breastfeeding.

• Primary Class: Combination Inhaled Respiratory Agent
• Subclasses:
• Inhaled Corticosteroid (ICS): Budesonide
• Long-Acting Beta₂-Agonist (LABA): Formoterol

• Hypersensitivity to Budesonide, Formoterol, or any excipients
• Primary treatment of acute bronchospasm or status asthmaticus
• Monotherapy with LABA in asthma (increases risk of asthma-related death)

• Asthma-Related Death Risk (LABA): Always use with ICS; never as monotherapy.
• Adrenal Suppression: Risk with high-dose corticosteroids.
• Paradoxical Bronchospasm: Discontinue immediately if this occurs.
• Systemic Corticosteroid Effects: Risk of hypercortisolism, growth suppression in children.
• Ocular Risks: May increase risk of cataracts or glaucoma with prolonged use.
• Infections: Higher risk of respiratory and oral fungal infections.

Common:

• Oral thrush, sore throat, cough
• Headache, dizziness
• Tremor, palpitations

Less Common:

• Hypertension, tachycardia
• Hyperglycemia
• Anxiety, restlessness

Serious/Rare:

• Paradoxical bronchospasm
• Adrenal insufficiency
• Growth retardation (in pediatrics)
• Hypokalemia
• QT prolongation (Formoterol)

• CYP3A4 Inhibitors (e.g., ketoconazole): Increase Budesonide levels.
• Beta-blockers: May antagonize Formoterol’s effects.
• Diuretics: Risk of hypokalemia when used with Formoterol.
• MAOIs and Tricyclics: May enhance cardiovascular effects.
• Live Vaccines: Immunosuppressive effect of Budesonide may reduce efficacy.

• GINA 2024 Update: Supports ICS-Formoterol for both maintenance and reliever therapy in mild asthma (SMART approach).
• FDA & EMA: Reinforce warnings against LABA monotherapy.
• Labeling Clarifications: Updated precautions for growth monitoring in children and systemic corticosteroid effects.

• Temperature: Store at 20–25°C (68–77°F).
• Humidity/Light: Protect from moisture and sunlight.
• Handling:
• DPI: Keep dry and closed tightly.
• MDI: Shake well before use. Avoid spraying into eyes.
• Do Not Freeze.
• Discard after labeled number of actuations or expiry, whichever comes first.