Methimazole works inside the thyroid gland, where it blocks the making of new thyroid hormone. With less new hormone produced, the gland's overactivity is brought under control. It does not inactivate hormone that is already stored in the gland or moving through the blood. It also leaves thyroid hormone given as a pill or a shot working as usual.
It is absorbed well from the gut, broken down by the liver, and cleared in the urine. Because it lowers hormone production, too much of it can tip the body into an underactive thyroid, so the dose is adjusted over time. It crosses the placenta, so in pregnancy it can cause an enlarged thyroid and lasting thyroid deficiency in the baby. Apart from its thyroid effect, it can rarely cause a dangerous drop in the white blood cells that fight infection.