Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents. Reference of 60-56-0.
Cozzolino, Alessia research published 《 [“Block and replace” of sodium levothyroxine therapy].》, the research content is summarized as follows. We present the case of a 65 years old patient with Graves disease associated with hyperthyroidism and a medical history of bipolar disorder treated with lithium. Hyperthyroidism was initially treated with high-dose methimazole monotherapy and later the patient developed overt hypothyroidism (clinical and biochemical), but without remission of the underlying autoimmune disease. A “block and replace” therapeutic regimen was then started with reduced methimazole doses in combination with levothyroxine, which resulted in a short time in normalization of the hormonal profile and significant improvement of the clinical picture. Therefore, the “block and replace” regimen represents a valid therapeutic alternative to anti-thyroid drugs monotherapy in the treatment of hyperthyroidism due to Graves disease in selected cases.
60-56-0, Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.
Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.
Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.
Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.
Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).
Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., Reference of 60-56-0
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem