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Methimazole
drug data and news
Methimazole drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Methimazole | ||
| Brand Names/Synonyms | Basolan; Danantizol; Favistan; Frentirox; Mercaptazole; Mercasolyl; Mercazole; Mercazolyl; Merkastan; Merkazolil; Metazolo; Methamazole; Methiamazole; Methimazol; Methimazole; Methylmercaptoimidazole; Metizol; Metothyrin; Metothyrine; Metotirin; Propyl-Thyracil; Strumazol; Strumazole; Tapazole; Tapuzole; Thacapzol; Thiamazol; Thiamazole; Thimazole; Thycapsol; Thycapzol; Thymidazol; Thymidazole; Usaf El-30 | ||
| Indication | For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis. | ||
| Sponsored links | Description | Not Available | |
| 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. Thyroglobulin is degraded to produce thyroxine (T4) and tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland. So Methimazole effectively inhibits the production of new thyroid hormones. | ||
| Methimazole News (When available) |
Tulsa World (subscription), She recently started taking an anti-thyroid medication, methimazole, and is under doctors orders to rest for another six weeks until her body is not so toxic. ... The lowdown on thyroid slowdown Dec 11, 2005 ITP.net, ...certain types of leukemia and other cancers; and the cancer drug interleukin-2. Drugs taken to treat an overactive thyroid — methimazole (Tapazole, Thiamazole ... | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Antithyroid Agents; ATC:H03B | ||
| Absorption | Rapid, oral bioavailability = 93% | ||
| Interactions |
-->Interactions for Methimazole: Anticoagulants (oral): The activity of oral anticoagulants may be potentiated by anti-vitamin-K activity attributed to methimazole. ß-adrenergic blocking agents: Hyperthyroidism may cause an increased clearance of beta ratio. A dose reduction of beta-adrenergic blockers may be needed when a hyperthyroid patient becomes euthyroid. Digitalis glycosides: Serum digitalis levels may be increased when hyperthyroid patients on a stable digitalis glycoside regimen become euthyroid; reduced dosage of digitalis glycosides may be required. Theophylline: Theophylline clearance may decrease when hyperthyroid patients on a stable theophylline regimen become euthyroid; a reduced dose of theophylline may be needed.
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| Toxicity | LD50 = 2250 mg/kg (rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-methyl-1H-imidazole-2-thiol | ||
| Chemical Formula | C4H6N2S | ||
| Molecular Weight | 114.17 g/mol | ||
| Smiles String | CN1C=CN=C1S | ||
| Melting Point | 146 °C | ||
| Water Solubility | 275 g/L | ||
| State | Solid | ||
| LogP/Hphobicity | 0.905 (Hansch LogP is -0.34) | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Primarily hepatic | ||
| Half Life | 5-6 hours | ||
| Protein Binding [%] | None or minimal | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Methimazole.html http://www.rxlist.com/cgi/generic3/methim.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00002 | ||
| CAS Registry Number | 60-56-0 | ||
| KEGG Compound ID | C07190 | ||
| PubChem ID | SID:9399 | ||
| PharmGKB ID | PA450422 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2258935 |
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