Also Known As: Methimazole, Tapazole, Thiamazole
Methimazole is a drug used to treat hyperthyroidism, a condition that usually occurs when the thyroid gland is producing too much thyroid hormone. It may also be taken before thyroid surgery to lower thyroid hormone levels and minimize the effects of thyroid manipulation. Methimazole is also used in the veterinary setting to treat hyperthyroidism in cats.
Methimazole inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin, a necessary step in the synthesis of triiodothyronine (T3) and thyroxine (T4).
It does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate.