Theophylline

Abstract

Theophylline was introduced into clinical medicine almost 50 yr ago for the treatment of asthma. The drug was widely used for 20 yr after its introduction; however, following reports of adverse reactions, including death, there was a pronounced decline of theophylline prescribing, particularly for children. In the mid 1960s and the early 1970s when the pharmacokinetics of the drug began to be elucidated, an increase in the use of theophylline occurred, and it became the most commonly prescribed drug for the treatment of asthma. During the past decade, because of the introduction and widespread use of new potent anti-inflammatory inhaled steroids, doubts about theophylline’s bronchodilatory activity in acute asthma and renewed concern about theophylline toxicity (well characterized in the 1950s and 1960s), prescription of theophylline substantially decreased. Very recently, however, evidence, first based on in vitro and subsequently on clinical studies, has strongly suggested an immunomodulatory role for theophylline even at low (5–10 µg/mL) serum concentrations.