ABSTRACT

For decades theophylline was used as a bronchodilator for the relief of

acute asthmatic symptoms, initially in patients unresponsive to injected epinephrine (1), and subsequently as an oral agent in fixed dose combination

with a weak sympathomimetic bronchodilator, ephedrine (2). It had also

been used as a respiratory stimulant for Cheyne-Stokes respirations (3),

as a diuretic in the treatment of acute pulmonary edema (4,5), to prevent

episodes of apnea and bradycardia in premature newborns (6,7), as an aid

in weaning very low birth weight infants from mechanical ventilation (8),

and extensively in the treatment of chronic obstructive pulmonary disease

(COPD) (9,10). It’s most important use eventually became as maintenance therapy for controlling the symptoms of chronic asthma (11). Studies of

the pharmacodynamic and pharmacokinetic characteristics of theophylline,

the development of reliably absorbed slow-release formulations, and the

availability of rapid, specific serum assays improved both the efficacy and

safety of this drug (12). Identification of anti-inflammatory effects for

theophylline has increased current interest in this venerable medication (13).