State-of-the-Art: Pharmacologic-Therapecitic Update: Theophyllines-A Review
Abstract
Journal of Asthma, 21(4), 243-257 (1984) STATE-OF-THE-ART: PHARMACOLOGIC- THERAPEUTIC UPDATE Theophyllines-A Review Joseph M. Cummiskey, M.D. Associate Professor of Medicine University of California at Davis Dazlis, Califorti in arid Valentin Popa, M.D. Associate Professor of Medicirie University of California at Daziis Dazlis, Cal iforii in am! Chief, Pulrnoiiary Medicine atid Allergy V A Outpatieiit Clinic Sncranrnito, California Director Pirlrnotiary Fuiictioii Laboratory V A Medical Center Martinez, Cdiforiiia INTRODUCTION Theophylline and its ethylenediamine "salt," aminophylline, was introduced in the treatment of asthma in the 1930s (1).In the 1960s, cyclic adenyl monophosphate (AMP) was described as a second mediator and theophylline emerged as an important agent modulating its cellular availability. Improvements in the use of theophyllines over the past decade have been in the areas of dosage and serum concentrations. Measurement of serum concentrations has reduced toxicity and led to the appearance of sustained release theophylline products. A better understanding of the absorption and distribution of theophyllines has led to new dosage guidelines. Copyright @ 1984 by Marcel Dekker, Inc. STRUCTURE AND BIOCHEMICAL ACTION Theophylline is 1,3-dimethylxanthine. Its main pharmacodynamic effects are (a) translocations of intracellular calcium (2), (b) inhibition of phosphodiesterase (3), and (c) blockade of receptors of adenosine