Doxofylline: A new generation xanthine bronchodilator devoid of major cardiovascular adverse effects

• Published in: Current medical research and opinion Vol. 16; no. 4; pp. 258 - 268
• Main Authors: DINI, Frank Lloyd, COGO, Roberto
• Format: Journal Article
• Language: English
• Published: Reading Librapharm 01-01-2001; Informa Healthcare
• Subjects: Animals; Arrhythmias, Cardiac - chemically induced; Asthma - drug therapy; Biological and medical sciences; Bronchodilator Agents - chemistry; Bronchodilator Agents - pharmacology; Bronchodilator Agents - therapeutic use; Cardiovascular Diseases - chemically induced; Drug Evaluation, Preclinical; Drug toxicity and drugs side effects treatment; Humans; Lung Diseases, Obstructive - drug therapy; Medical sciences; Pharmacology. Drug treatments; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - pharmacology; Phosphodiesterase Inhibitors - therapeutic use; Pulmonary Heart Disease - drug therapy; Receptors, Purinergic P1 - drug effects; Risk Factors; Safety; Theophylline - analogs & derivatives; Theophylline - chemistry; Theophylline - pharmacology; Theophylline - therapeutic use; Toxicity: cardiovascular system; Treatment Outcome; Xanthines - chemistry; Xanthines - pharmacology; Xanthines - therapeutic use; Heart; Human; Doxofylline; Arrhythmia; Toxicity; Heart disease; Animal; Bronchodilator; Cardiovascular disease; Xanthine derivatives; Review; Theophylline
• ISSN: 0300-7995; 1473-4877
• DOI: 10.1185/030079901750120196

Doxofylline (7-(1,3-dioxalan-2-ylmethyl) theophylline) is a novel xanthine bronchodilator which differs from theophylline in that it contains a dioxalane group in position 7. Similarly to theophylline, its mechanism of action is related to the inhibition of phosphodiesterase activities, but in contrast it appears to have decreased affinities towards adenosine A1 and A2 receptors, which may account for its better safety profile. The bronchodilating activities of doxofylline have been demonstrated in clinical trials involving patients with either bronchial asthma or chronic obstructive pulmonary disease. In contrast to other bronchodilators, experimental and clinical studies have shown that the drug is devoid of direct stimulatory effects. This may be of importance because the arrhythmogenic actions of bronchodilators may have a negative impact on the survival of patients with respiratory diseases.