Doxofylline: a new generation xanthine bronchodilator devoid of major cardiovascular adverse effects.
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.
Dini
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Unità Operativa di Cardiologia, Ospedale Villamarina, Via Forlanini, 24, 57025 Piombino, Italy. frankld@tin.it
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D000818:Animals; D001145:Arrhythmias, Cardiac / Q000139:chemically induced*; D001249:Asthma / Q000188:drug therapy*; D001993:Bronchodilator Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002318:Cardiovascular Diseases / Q000139:chemically induced*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008173:Lung Diseases, Obstructive / Q000188:drug therapy*; D010726:Phosphodiesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011660:Pulmonary Heart Disease / Q000188:drug therapy*; D018047:Receptors, Purinergic P1 / Q000187:drug effects; D012307:Risk Factors; D012449:Safety; D013806:Theophylline / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D016896:Treatment Outcome; D014970:Xanthines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D001993:Bronchodilator Agents; D010726:Phosphodiesterase Inhibitors; D018047:Receptors, Purinergic P1; D014970:Xanthines; C008514:methylxanthine; D013806:Theophylline; C029797:doxofylline