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Thionamides in the treatment of Graves' disease

Douglas S Ross, MD
Section Editor
David S Cooper, MD
Deputy Editor
Jean E Mulder, MD


The thionamides, methimazole, carbimazole, and propylthiouracil are effective treatment of patients with Graves' hyperthyroidism. They are actively transported into the thyroid gland where they inhibit both the organification of iodine to tyrosine residues in thyroglobulin and the coupling of iodotyrosines (figure 1) [1]. (See "Pharmacology and toxicity of thionamides".)

Methimazole is usually preferred to propylthiouracil (except during the first trimester of pregnancy) because it can reverse the hyperthyroidism more quickly and it has fewer side effects (figure 2 and table 1). We usually begin with 10 to 15 mg of methimazole once daily; this low-dose regimen appears to be as effective as higher doses except in patients with large goiters and severe hyperthyroidism who should be treated with 20 to 30 mg daily (figure 3).

The clinical use and efficacy of the thionamides in the treatment of Graves' hyperthyroidism will be reviewed here; the pharmacology and toxicity of these drugs are reviewed separately. (See "Pharmacology and toxicity of thionamides".)


Thionamides are often started in patients with Graves' hyperthyroidism to attain a euthyroid state rapidly in preparation for radioiodine therapy or thyroidectomy. However, patients who want to avoid or defer ablative therapy with radioiodine or surgery can continue the thionamide for prolonged periods. Although hyperthyroidism can almost always be controlled as long as the drug is taken, overall, only about 20 to 30 percent of patients achieve a permanent remission. (See 'Rate of prolonged remission' below.)

The approach outlined below is largely consistent with Hyperthyroidism Management Guidelines from the American Thyroid Association (ATA) and the American Association of Clinical Endocrinologists (AACE) [2].


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Literature review current through: Sep 2016. | This topic last updated: May 5, 2016.
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