Pharmacology: Pharmacodynamics: Methimazole inhibits the synthesis of thyroid hormones by blocking the oxidation of iodine in the thyroid gland. As a result, methimazole inhibits the ability of iodine to combine with tyrosine to form thyroxine (T4) and triiodothyronine (T3). It is effective in the treatment of hyperthyroidism. It does not inactivate existing thyroxine (T4) and triiodothyronine (T3), which are stored in the thyroid or which circulate in the blood.
Pharmacokinetics: Methimazole is rapidly absorbed from GI tract following oral administration with peak plasma concentrations occurring within about 1-2 hours. Onset of action is 12-18 hours. Methimazole readily crosses the placenta and is distributed into milk in concentrations approximately equal to those in maternal serum. This drug concentrated in thyroid gland. Protein binding of methimazole is 0%. Methimazole metabolized in the liver. The elimination half-life of methimazole reportedly ranges from about 5-13 hours. The drug is excreted in urine. In one study, about 12% of a dose was excreted in urine within 24 hours. Bioavailability of this drug is 80-95%.
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