Isoxsuprine is a β2 adrenoreceptor agonist that causes direct relaxation of uterine and vascular smooth muscle via β2 receptors.

[7] Isoxsuprine may increase the heart rate, cause changes in blood pressure, and irritate the GI tract.

Isoxsuprine is most commonly used to treat hoof-related problems in the horse, most commonly for laminitis and navicular disease, as its effects as a vasodilator are thought to increase circulation within the hoof to help counteract the problems associated with these conditions.

Isoxsuprine is given orally, and many horses find the pills quite palatable.

It is therefore important to check the drug-rules within an animal's given competitive organization, before administering the drug.