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A narrative review of theophylline: is there still a place for an old friend?

Theophylline has been used for decades in human medicine for its psychostimulant, anti-inflammatory, and bronchodilator effects. Historically, in pulmonary medicine, theophylline has been used in the treatment of obstructive pulmonary diseases such as bronchial asthma (BA) or chronic obstructive pulmonary disease (COPD). This review aims to determine whether theophylline still has its place in the therapy of obstructive pulmonary diseases or whether we can even extend its use to other diagnoses such as atropine-resistant cardiac arrests, apnea of prematurity, or others.

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 Theophylline Toxicity

Around the world, theophylline (1,3-dimethylxanthine) is primarily used as a bronchodilator for patients with asthma and chronic obstructive pulmonary disease (COPD). However, in the United States, asthma and COPD are mainly treated with other agents, and theophylline is predominantly used to treat bradycardia and apnea in premature newborns. Theophylline causes the endogenous release of catecholamines via indirect stimulation of beta-1 and beta-2 receptors, which, at therapeutic levels lead to bronchodilation, the goal of treatment. Unfortunately, theophylline has a narrow therapeutic window, and levels even slightly above the therapeutic range can have adverse effects both acutely and chronically.

Articles of Interest

Theophylline New Perspectives for an Old Drug

Theophylline has been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD) for over 60 years and remains one of the most widely prescribed drugs for the treatment of airway diseases worldwide as it is inexpensive. In many industrialized countries, however, theophylline has recently become a third-line treatment that is only used in some poorly controlled patients. This has been reinforced by various guidelines to therapy. It has even been suggested that theophylline is not indicated in any patients with asthma

Theophylline: Recent Advances in the Understanding of Its Mode of Action and Uses in Clinical Practice

Theophylline, a drug that has been used for several decades, has several different actions at a cellular level, including inhibition of phosphodiesterase isoenzymes, antagonism of adenosine, enhancement of catecholamine secretion, and modulation of calcium fluxes. Recently, theophylline was found to have several immunomodulatory and anti-inflammatory properties, and thus interest in its use in patients with asthma has been renewed. The use of theophylline in the treatment of asthma and chronic obstructive pulmonary disease has diminished with the advent of new medications,but theophylline remains beneficial, especially in the patient with difficult refractory symptoms.

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StatPearls

Theophylline is a drug derived from methylxanthine (a purine derivative) and has smooth muscle relaxant, bronchial dilation, diuretic, cardiac and central nervous system (CNS) stimulant activities. It is naturally present in small amounts in tea and cocoa beans and was initially extracted and synthesized in 1895 and used as a diuretic. In 1922, it came out as a clinical treatment for asthma after identifying its bronchodilator effect.