Propentofylline has been shown to increase blood flow, particularly of the heart and skeletal muscle. It also increases the blood flow of the brain and therefore its oxygen supply, without increasing the brain's glucose demand. It has a modest positive chronotropic effect and a marked positive inotropic effect. In addition, it has been shown to have an anti-arrhythmic effect in dogs with myocardial ischemia and a bronchodilator action equivalent to that of aminofylline.

Propentofylline inhibits platelet aggregation and improves the flow properties of erythrocytes.

It has a direct effect on the heart and reduces peripheral vascular resistance thereby lowering cardiac load.

After oral administration, propentofylline is rapidly and completely absorbed and quickly distributed into the tissues. Maximum plasma levels are reached by 15 minutes following oral dosing in dogs.

The half-life is approximately 30 minutes and the bioavailability of the parent compound is approximately 30%.

There are a number of effective metabolites and biotransformation takes place mainly in the liver.

80-90% of propentofylline is excreted in the form of metabolites via the kidneys. The rest is eliminated with the faeces.

There is no bioaccumulation.