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.

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.
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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)
Thrown off course  Dec 21, 2005
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.

 


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
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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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