Updated: 12/31/2021

Methylxanthines

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  • Snapshot
    • A 17-year-old boy with a history of moderate persistent asthma presents to his pediatrician with continued shortness of breath. He has been prescribed a low-dose fluticasone/salmeterol inhaler with spacer for daily use. He admits his compliance with his inhaler is not perfect and is curious if there is an oral medication that is available. He is prescribed theophylline.
  • Overview
    • One of 7 medications used for asthma aimed to reduce inflammation and obstruction
      • methylxanthines
      • others:
        • corticosteroids
        • β-agonists
        • muscarinic antagonists
        • cromolyn
        • antileukotrienes
        • omalizumab
  • Methylxanthines
    • Mechanism of action
      • bronchodilation via inhibition of phosphodiesterase PDE3
      • anti-inflammatory via inhibition of phosphodiesterase PDE4
      • metabolized by P-450
    • Examples
      • theophylline (oral form)
      • aminophylline (intravenous form)
    • Clinical use
      • moderate persistent asthma
      • chronic obstructive pulmonary disease
      • apnea and bradycardia in neonates
      • requires titrating at initiation and at least annual serum monitoring due to a narrow therapeutic index
    • Adverse effects
      • seizures
      • coarse tremor
      • headaches
      • nausea, vomiting, and abdominal pain
      • arrhythmia
      • hypokalemia
      • hyperglycemia

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