Danantizol: Full Drug Profile

Danantizol - General Information

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. [PubChem]

Pharmacology of Danantizol

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.

Danantizol for patients

Patients should be instructed to report to their physicians any symptoms of agranulocytosis, such as fever or sore throat.

Danantizol Interactions

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.

Danantizol Contraindications

Tapazole is contraindicated in the presence of hypersensitivity to the drug and in nursing mothers because the drug is excreted in milk.

Additional information about Danantizol

Danantizol Indication

For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis.

Mechanism Of Action

Danantizol 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 (Tg) 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.

Drug Interactions

Anisindione The antithyroid agent causes variations in the anticoagulant effect

Generic Name

Methimazole

Synonyms

Thymidazole; Thymidazol; Thimazole; Thiamazole; Thiamazol; Metothyrine; Metothyrin; Methimazol; Methiamazole; Methamazole; Metazolo; Merkazolil; Mercazolyl; Mercazole; Mercasolyl; Mercaptazole

Drug Category

Antithyroid Agents

Drug Type

Small Molecule; Approved

Other Brand Names containing Methimazole

Basolan; Danantizol; Favistan; Frentirox; Merkastan; Metizol; Metotirin; Strumazol; Strumazole; Tapazole; Tapuzole; Thacapzol; Thycapsol; Thycapzol;

Absorption

Rapid with an oral bioavailability of 93%.

Toxicity (Overdose)

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.

Protein Binding

None or minimal

Biotransformation

Primarily hepatic. Metabolized rapidly, requiring frequent administration.

Half Life

5-6 hours

Dosage Forms of Danantizol

Tablet Oral

Chemical IUPAC Name

1-methyl-3H-imidazole-2-thione

Chemical Formula

C4H6N2S

Methimazole on Wikipedia

https://en.wikipedia.org/wiki/Methimazole

Organisms Affected

Humans and other mammals