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Theophyllines
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  • AHFS Monographs

Theophyllines

Class: Respiratory Smooth Muscle Relaxants
ATC Class: R03DA01
VA Class: RE104
CAS Number: 317-34-0
Brands: Dy-G, Dylix , Dyphylline-GG, Elixophyllin, Lufyllin, Lufyllin GG, Theo-24, Theochron, Uniphyl

Introduction

Xanthine derivative; respiratory smooth muscle relaxant, bronchodilator.

Uses for Theophyllines

Symptomatic management or prevention of asthma and reversible bronchospasm associated with COPD, including chronic bronchitis and emphysema.

Aminophylline and dyphylline generally share the same indications as theophylline.

Bronchospasm in Asthma

Symptomatic management or prevention of bronchospasm in patients with reversible, obstructive airway disease (e.g., asthma).

In the stepped-care approach recommended in current asthma management guidelines, a selective, short-acting, inhaled β2-adrenergic agonist is used as needed to control acute asthma symptoms in all patients; use of such a β2-adrenergic agonist alone generally sufficient for patients with intermittent asthma.

Consider short-acting theophylline (if extended-release theophylline not already used) as less-effective alternative to short-acting inhaled β2-agonist for relief of acute asthma symptoms (i.e., as temporary measure if inhaled or parenteral β2-agonist not available); theophylline has slower onset of action and greater risk of adverse effects.

Consider extended-release theophylline as less-effective alternative to low-dose inhaled corticosteroid for long-term control and prevention of symptoms in adults and children ≥5 years of age with mild persistent asthma. Also consider extended-release theophylline as less-effective alternative to long-acting inhaled β2-adrenergic agonist for use as adjunct to inhaled corticosteroid therapy in adults and children ≥5 years of age with moderate persistent asthma. Some clinicians do not recommend use of extended-release theophylline as alternative or add-on long-term control therapy in children <5 years of age with mild persistent asthma. (See Pediatric Use under Cautions.)

Consider extended-release theophylline as add-on therapy in adults and children ≥5 years of age with severe persistent asthma inadequately controlled by high dosages of an orally inhaled corticosteroid and a long-acting inhaled β2-adrenergic agonist.

IV theophylline and aminophylline are FDA-labeled for use as an adjunct to inhaled β2-adrenergic agonists and systemic corticosteroids in the treatment of acute asthma exacerbations. However, some experts do not recommend theophylline derivatives for treatment of severe, acute asthma exacerbations because such therapy does not appear to provide additional benefit to optimal therapy with inhaled short-acting β2-adrenergic agonists and is associated with an increased risk of adverse effects. Other experts suggest consideration of IV theophylline or aminophylline as add-on therapy for treatment of severe, acute exacerbations of asthma in hospitalized patients not responding adequately to oxygen, inhaled short-acting β2-adrenergic agonists, and systemic corticosteroids.

Dyphylline not indicated for the management of status asthmaticus.

Bronchospasm in COPD

Management of symptoms and reversible airflow obstructi...