ATC Group: R03DA Xanthines

Aminophylline is a soluble derivative of theophylline and is given for its theophylline activity. Aminophylline relaxes smooth muscle and relieves bronchial spasm. It stimulates the myocardium and reduces venous pressure in congestive heart failure, leading to a marked increase in cardiac output.

Bamifylline is a methylxanthinic derivative with two side chains in position 7 and 8, distinguishing it clearly from theophylline. Bamifylline carries out a bronchospasmolytic action on the smooth musculature and also blocks the action of the bronchoconstriction mediators. Unlike theophylline, bamifylline usually has no exciting effects on the central nervous system.

Bufylline is a combination of theophylline and aminoisobutanol used as a bronchodilator. It also acts and may be used as a diuretic.

Choline theophyllinate is the choline salt of theophylline. It has a strong bronchodilator action, due to the relaxation of the smooth muscle fibers of the bronchi.

Diprophylline is a xanthine derivative with pharmacologic actions similar to theophylline and other members of this class of drugs. Its primary action is that of bronchodilation, but it also exhibits peripheral vasodilatory and other smooth muscle relaxant activity to a lesser degree. The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of the bronchial smooth muscle. Diprophylline exerts its bronchodilatory effects directly and, unlike theophylline, is excreted unchanged by the kidneys without being metabolized by the liver. Because of this, dyphylline pharmacokinetics and plasma levels are not influenced by various factors that affect liver function and hepatic enzyme activity, such as smoking, age, congestive heart failure, or concomitant use of drugs which affect liver function.

Theophylline is a bronchodilator. In addition it affects the function of a number of cells involved in the inflammatory processes associated with asthma and chronic obstructive airways disease. Theophylline stimulates the myocardium and produces a diminution of venous pressure in congestive heart failure leading to marked increase in cardiac output.