Methods and Findings in Experimental and Clinical Pharmacology 1991-05-01

Pharmacological studies in animals of beta-hydroxyethyltheophylline, the major metabolite of doxofylline in humans.

J S Franzone, R Cirillo, M C Reboani

Index: Methods Find. Exp. Clin. Pharmacol. 13(4) , 289-99, (1991)

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Abstract

beta-HET (beta-Hydroxyethyltheophylline), the major metabolite of the antibronchospastic, antiasthmatic drug doxofylline was studied in several in vitro and in vivo trials to characterize its pharmaco-toxicological profile. When compared to the parent compound, beta-HET was found to be significantly less active. It was also discovered to be a very weak inhibitor of phosphodiesterase activity. Its affinity for A1- and A2-adenosine receptors was even lower than that of doxofylline, which was quite low. The oral toxicity of beta-HET was about three times lower than that of doxofylline. The pharmacological activity of doxofylline is due to the drug in its original form and not to its major metabolite.