How much theophylline is enough?

Theophylline not only is a bronchodilator but also has other effects (inhibition of mediator release, enhancement of mucociliary clearance, enhancement of diaphragmatic contractility) that are potentially beneficial to asthmatic patients. Recent studies suggest that theophylline pharmacodynamics vary among asthmatic patients. However, on average, most of the total bronchodilatory response occurs at serum theophylline concentrations of 0 to 10 mg/liter. Additional (but less) bronchodilatation occurs at serum theophylline levels between 10 and 20 mg/liter. Pharmacodynamic relationships are not well established for other therapeutic effects of theophylline, such as attenuation of pharmacologically induced bronchoconstriction. An important feature of oral controlled-release theophylline therapy is timing of drug administration. Because airway reactivity increases and airway caliber decreases at night, it has been suggested that the greatest benefit is derived from theophylline when peak serum concentration is reached during the night or the early morning.