Budesonide/Formoterol

Administration

• Type: Inhaled corticosteroid
• Dosage Forms: 80/4.5, 160/4.5 mcg/spray MDI
• Routes of Administration: Inhaled
• Common Trade Names: Symbicort

Adult Dosing

• Asthma, maintenance
  • 2 puffs inhaled BID
    • Start: Dependent on severity of asthma
    • Max: 640 mcg/18 mcg/day
    • May increase to 160 mcg/4.5 mcg/day per spray after 1-2 weeks if started at 80 mcg/4.5 mcg/spray.
    • Taper to lowest effective dose.
• COPD, maintenance
  • 2 puffs (160 mcg/4.5 mcg/ spray) inhaled BID
    • Max: 640 mcg/18 mcg/day

Pediatric Dosing

• 5-11 yo
  • 2 puffs inhaled BID
    • Start: Dependent on severity of asthma
    • Max: 320 mcg/18 mcg/day
    • Taper to lowest effective dose. Use shortest effective treatment duration.
• 12+ yo
  • 2 puffs inhaled BID
    • Start: Dependent on severity of asthma
    • Max: 640 mcg/18 mcg/day
    • Taper to lowest effective dose. Use shortest effect treatment duration.

Special Populations

• Pregnancy Rating: C; Possible risk of delayed ossification based on animal data at 80x MRHD and risk with uterine contractility.
• Lactation risk: L3; Safety unknown

Renal Dosing

• Adult: Not defined
• Pediatric: Not defined

Hepatic Dosing

• Adult: Not defined. Caution in severe hepatic impairment.
• Pediatric: Not defined. Caution in severe hepatic impairment

Contraindications

• Allergy to class/drug
• Asthma, acute
• Bronchospasm, acute
• COPD, acute deteriorating

Adverse Reactions

Serious

• Bronchospasm, paradoxial
• Asthma exacerbation
• Death, asthma-related
• Pneumonia
• Hypersensitivity Reaction
• Anaphylaxis
• Hypertension
• Angina
• Hypotension
• Cardiac arrest
• Arrhythmia
• Hypokalemia
• Hyperglycemia
• Glaucoma in long-term use
• Cataracts in long-term use
• Osteoporosis in long-term use
• Growth suppression in peds pts
• Hypercorticism
• Adrenal suppression
• Behavioral distrubance

Common

• Nasopharyngitis
• Headache
• URI
• Pharyngolaryngeal pain
• Sinusitis
• Influenza
• Back pain
• Nasal congestion
• Dyspepsia
• Nausea
• Vomiting
• Candidiasis, oral
• BP changes
• Chest pain
• Palpitations
• Tachycardia
• Muscle cramps
• Tremor
• Nervousness
• Insomnia
• Cough
• Bronchitis
• Respiratory infection

Pharmacology

• Half-life: Budesonide: 2.3 hr, Formoterol: 10 hr.
• Metabolism: Budesonide: Liver, CYP450: 3A4 substreate. Formoterol: Liver extensively, CYP450: 2A6, 2C9/19, 2D6 substrate.
• Excretion: Budesonide: Urine 60%, feces. Formoterol: Urine 59-62% (10% unchanged), feces 32-24%.

Mechanism of Action

• Budesonide: Inhibits multiple inflammatory cytokine sand produces multiple glucocorticoid and mineralcorticoid effects. Exact mechanism unknown.
• Formoterol: Selectively stimulates beta-2 adrenergic receptors, relaxing airway smooth muscle.

Comments

Black Box Warning: Long acting beta-2 adrenergic agonists (LABA) increase risk of asthma-related death. LABA use may increase risk of asthma-related hospitalization in pediatric and adolescent patients. Do not use corticosteroid/LABA combo if asthma adequately controlled on low-or medium-dose inhaled corticosteroids.

References

Authors

Jonathan Warren