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QuickView for Methimazole (compound)
PubChem
| Name: | Methimazole |
|---|---|
| PubChem Compound ID: | 1349907 |
| Description: | A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. |
| Molecular formula: | C4H6N2S |
| Molecular weight: | 114.17 g/mol |
| Synonyms: |
ZINC00896701; AIDS-076131; 2H-Imidazole-2-thione, 1,3-dihydro-1-methyl-; Thiamazol; N-Methyl-2-mercaptoimidazole; 2-Mercapto-1-methylimidazole; Metazolo; KBio3_001489; 1-Metylo 2 merkaptoimidazolem [Polish]; 1-Methyl-1,3-dihydroimidazole-2-thione.
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DrugBank
Identification
| Name: | Methimazole |
|---|---|
| Name (isomeric): | DB00763 |
| Drug Type: | small molecule |
| Description: | A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. |
| Synonyms: |
Thiamazole; Merkazolil; Methiamazole; Methimazol; Mercazolyl; Thiamazol; Thymidazol; Metazolo; Thymidazole; Metothyrine.
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| Brand: | Thycapzol, Basolan, Favistan, Tapazole, Thycapsol, Metotirin, Strumazol, Tapuzole, Merkastan, Frentirox, Thacapzol, Metizol, Strumazole, Danantizol |
| Category: | Antithyroid Agents |
| CAS number: | 60-56-0 |
Pharmacology
| Indication: | For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis. |
|---|---|
| Pharmacology: | Used in the treatment of hyperthyroidism or an overactive thyroid gland, methimazole inhibits the synthesis of thyroid hormones and thus is effective in the treatment of hyperthyroidism. It may also be used to ameliorate hyperthyroidism in preparation for subtotal thyroidectomy or radioactive iodine therapy. |
| Mechanism of Action: |
Methimazole binds to thyroid peroxidase and thereby inhibits the conversion of iodide to iodine. Thyroid peroxidase normally converts iodide to iodine (via hydrogen peroxide as a cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3 and/or 5 positions of the phenol rings of tyrosines found in thyroglobulin....
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| Absorption: | Rapid with an oral bioavailability of 93%. |
| Protein binding: | None or minimal |
| Biotransformation: | Primarily hepatic. Metabolized rapidly, requiring frequent administration. |
| Route of elimination: | Methimazole is excreted in the urine. |
| Half Life: | 5-6 hours |
| Toxicity: | Oral LD50 in rats is 2250 mg/kg. Symptoms of overdose include nausea, vomiting, epigastric distress, headache, fever, joint pain, pruritus, and edema. Aplastic anemia (pancy-topenia) or agranulocytosis may be manifested in hours to days. Less frequent events are hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathies, and CNS stimulation or depression. |
| Affected organisms: | Humans and other mammals |
Interactions
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Targets
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