Medicinally, wintergreen leaves are taken internally as a decoction to treat nephritis and bladder problems. It is used as a diuretic, for the treatment of neuralgia, as a systemic tonic, to stimulate menses, and to aid in bringing on lactation after childbirth. It has also been used to relieve children's headaches. Leaves have also been used for headaches and other pains, and as a gargle for a sore throat and mouth.

Externally, oil of wintergreen is widely used in liniments for the relief of muscular-skeletal pain, both from sports injuries and arthritis. Because of its aromatic and pain relieving qualities, the oil is used in a number of products in aroma therapy, including stress-reducing pulse point creams, foot scrubs and balms.