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An antithyroid agent is a hormone inhibitor acting upon thyroid hormones. The main antithyroid drugs are carbimazole (in the UK), methimazole (in the US), and propylthiouracil (PTU). A less common antithyroid agent is potassium perchlorate .
Carbimazole is a pro-drug as after absorption it is converted to the active form, methimazole. Methimazole prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T 3 and T 4 . It is on the World Health Organization's List of Essential Medicines.
The substance is a historically relevant anti-thyroid preparation. Edwin Astwood used it in 1943 as therapy for Graves' disease for the first time. [1] [2] [3] Thiouracil inhibits thyroid activity by blocking the enzyme thyroid peroxidase. [4] Its use in recent times has been replaced by advent of more potent and safer antithyroid drugs.
Thyroid diseases are highly prevalent worldwide, [10] [11] [12] and treatment varies based on the disorder. Levothyroxine is the mainstay of treatment for people with hypothyroidism, [13] while people with hyperthyroidism caused by Graves' disease can be managed with iodine therapy, antithyroid medication, or surgical removal of the thyroid ...
Hypothyroidism is common in pregnancy with an estimated prevalence of 2-3% and 0.3-0.5% for subclinical and overt hypothyroidism respectively. [8] Endemic iodine deficiency accounts for most hypothyroidism in pregnant women worldwide while chronic autoimmune thyroiditis is the most common cause of hypothyroidism in iodine sufficient parts of the world.
Antithyroid drugs (propylthiouracil or methimazole) are used to reduce the synthesis and release of thyroid hormone. Propylthiouracil is preferred over methimazole due to its additional effects on reducing peripheral conversion of T4 to T3, [ 5 ] however both are commonly used.
Antithyroid autoantibodies (or simply antithyroid antibodies) are autoantibodies targeted against one or more components on the thyroid. The most clinically relevant anti-thyroid autoantibodies are anti- thyroid peroxidase antibodies (anti-TPO antibodies, TPOAb), thyrotropin receptor antibodies (TRAb) and thyroglobulin antibodies (TgAb).
Amiodarone inhibits peripheral conversion of thyroxine to triiodothyronine; also interferes with thyroid hormone action. [citation needed] Lithium inhibits thyroid hormone release. [citation needed] Phenobarbitone, phenytoin, carbamazepine, rifampin induce metabolic degradation of triiodothyronine (T 3) and thyroxine (T 4). [citation needed]
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