Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator[1]. Proxyphylline inhibits tracheal PDE-activity and half-maximum relaxation of tracheal smooth muscle is obtained with 100 μg/mL proxyphylline[2]. Proxyphylline exhibits bronchodilatory effect[3]. Proxyphylline inhibits cAMP and cGMP hydrolysis in human lung tissue. The apparent inhibition constant of proxyphylline is 0.06-0.7 mM at low cAMP concentrations and it is 1.0 mM at high cAMP concentrations [4]. In guinea pigs (modified Konzett-Rössler method) the reduction in response to metacholine caused by increasing doses of proxyphylline and salbutamol significantly exceeded that of either drug alone. The combination of oral proxyphylline and salbutamol is clinically useful in increasing drug response without increased adverse effects[5].
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