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| Mechanism of Action |
Methimazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
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| Pharmacology |
Methimazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
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| Metabolism |
Methimazole¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Methimazole¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ None or minimal
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| Half-life |
Methimazole¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 5-6 hours
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| Absorption |
Methimazole¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid with an oral bioavailability of 93%.
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| Pharmacokinetics |
MethimazoleÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : °æ±¸ : 30-40 ºÐ
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : °æ±¸ : 12-18 ½Ã°£
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- »ýü³»ÀÌ¿ë·ü : °æ±¸ : Á¤Á¦ : 93 %
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- ¹Ý°¨±â : 2-28 ½Ã°£
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| Biotransformation |
Methimazole¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. Metabolized rapidly, requiring frequent administration.
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| Toxicity |
Methimazole¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
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| Drug Interactions |
Methimazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Anisindione The antithyroid agent causes variations in the anticoagulant effectWarfarin The antithyroid agent causes variations in the anticoagulant effectDicumarol The antithyroid agent causes variations in the anticoagulant effectAcenocoumarol The antithyroid agent causes variations in the anticoagulant effectDigoxin The antithyroid agent increases the effect of digoxin
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Methimazole¿¡ ´ëÇÑ Food Interaction Á¤º¸ Always take at the same moment in regard to meals, food may affect absorption unpredictably.
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| Drug Target |
[Drug Target]
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| Description |
Methimazole¿¡ ´ëÇÑ Description Á¤º¸ 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]
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| Dosage Form |
Methimazole¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Methimazole¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antithyroid Agents
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| Smiles String Canonical |
Methimazole¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C=CNC1=S
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| Smiles String Isomeric |
Methimazole¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C=CNC1=S
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| InChI Identifier |
Methimazole¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C4H6N2S/c1-6-3-2-5-4(6)7/h2-3H,1H3,(H,5,7)/f/h5H
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| Chemical IUPAC Name |
Methimazole¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-methyl-3H-imidazole-2-thione
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| Drug-Induced Toxicity Related Proteins |
METHIMAZOLE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:HLA-DR4 Drug:methimazole Toxicity:insulin autoimmune syndrome. [¹Ù·Î°¡±â] Replated Protein:HLA class II histocompatibility antigen, DRB1-1 beta chain Drug:methimazole Toxicity:insulin autoimmune syndrome. [¹Ù·Î°¡±â]
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