Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative,[5] skeletal muscle relaxant, motor skill-impairing or amnestic[6] properties.

[7][8] Tofisopam is indicated for the treatment of anxiety and alcohol withdrawal, and is prescribed in a dosage of 50–300 mg per day divided into three doses.

Tofisopam is not reported as causing dependence to the same extent as other benzodiazepines, but is still recommended to be prescribed for a maximum of 12 weeks.

However, Vela Pharmaceuticals of New Jersey is developing the D-enantiomer (dextofisopam) as a treatment for irritable bowel syndrome,[9] with moderate efficacy demonstrated in clinical trials so far.

[11] Tofisopam has been shown to act as an inhibitor of the liver enzyme CYP3A4,[12][13] and some researches suspect that this could cause dangerous drug interactions with other medications metabolised by this enzyme,[14][15] although the clinical significance of these findings remains unclear.