Clinical pharmacology of antithyroid compounds

Abstract

Successful treatment of hyperthyroidism is predicated upon an understanding of the pharmacology of antithyroid drugs as well as upon a knowledge of their effects on pathways of thyroidal iodide metabolism. Research into the relationship between chemical structure and biologic action of numerous antithyroid compounds has served as a basis for their classification and for selection of those of greatest potency for clinical trial. Biochemical determination of the site and mode of action of compounds affecting thyroid hormonogenesis, although incomplete, allows a tentative working hypothesis which must be periodically revised as further evidence is accumulated. During the 17 years since the introduction of thiouracil, clinical pharmacologic investigations have established optimal dosage schedules, the incidence of toxic reactions, and the indications for the effective use of these drugs. Such studies have further served to develop programs for the management of patients with hyperthyroidism with special emphasis on the use of antithyroid compounds in long‐term therapy, preoperative preparation, and use during childhood or pregnancy. Although refinements in surgical approach and the general availability of radioactive iodine have necessitated modifications in the indications for their use, antithyroid drugs still maintain a secure position as therapeutic agents in the treatment of hyperthyroidism.