Abstract
The clinical use of theophylline as a first-line bronchodilator has declined during the last two decades. However, in many clinical settings, such as an emergency bronchial asthma attack, theophylline may have a first-line role, in combination with β2-adrenoreceptor agonists and corticosteroids, for improving the asthmatic status. Furthermore, many therapeutic mechanisms of theophylline for bronchial asthma have been reported, and recent studies have suggested that theophylline therapy may have a beneficial role in the management of chronic stable asthma as well as exacerbated disease. However, theophylline has a low therapeutic index because the bronchodilation it produces has a linear relationship with logarithmic increases in serum concentration for the therapeutic range of 5–20 mg/L. Thus, the knowledge of its basic pharmacokinetics and the factors that can alter its clearance is clinically relevant for physicians.
Especially when used in elderly asthmatic patients, dosage adjustment of theophylline is a requisite since the elderly have several risk factors that may increase the plasma theophylline level, such as reduced clearance, various underlying diseases and multiple coadministered drugs. After theophylline treatment has been initiated, therapeutic drug monitoring is required.
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Acknowledgements
The authors are grateful to Dr Tomio Sasaki for his scientific and mathematical assistance in the preparation of this review of the pharmacokinetics of theophylline. There are no sources of funding or conflicts of interest involved in the preparation of this manuscript.
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Ohnishi, A., Kato, M., Kojima, J. et al. Differential Pharmacokinetics of Theophylline in Elderly Patients. Drugs Aging 20, 71–84 (2003). https://doi.org/10.2165/00002512-200320010-00005
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DOI: https://doi.org/10.2165/00002512-200320010-00005