| 词条 | Thiamazole |
| 释义 |
| verifiedrevid = 459829931 | IUPAC_name = 1-Methyl-3H-imidazole-2-thione | image = Methimazole.svg | width = 150px | image2 = Thiamazole ball-and-stick.png | width2 = 250px | synonyms = thiamazole (INN, BAN); methimazole (USAN); MMI | tradename = Tapazole, others | Drugs.com = {{drugs.com|monograph|methimazole}} | MedlinePlus = a682464 | pregnancy_category = D (US) | legal_AU = S4 | legal_US = Rx-only | routes_of_administration = by mouth | bioavailability = 93% | protein_bound = None | metabolism = Liver | elimination_half-life = 5-6 hours | excretion = Kidney | IUPHAR_ligand = 6649 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 60-56-0 | ATC_prefix = H03 | ATC_suffix = BB02 | PubChem = 1349907 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00763 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 1131173 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 554Z48XN5E | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00401 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 50673 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1515 | C=4 | H=6 | N=2 | S=1 | molecular_weight = 114.17 g/mol | smiles = Cn1cc[nH]c1=S | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C4H6N2S/c1-6-3-2-5-4(6)7/h2-3H,1H3,(H,5,7) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = PMRYVIKBURPHAH-UHFFFAOYSA-N | melting_point = 146 | solubility = 275[1] }} Thiamazole, also known as methimazole, is an antithyroid drug,[2] and part of the thioamide group. Like its counterpart propylthiouracil, possible major side effects of treatment include agranulocytosis and liver inflammation. In 2016 it was the 275th most prescribed medication in the United States with more than a million prescriptions.[3] Medical usesThiamazole is a drug used to treat hyperthyroidism such as in Graves' disease, a condition that occurs when the thyroid gland begins to produce an excess of thyroid hormone. The drug may also be taken before thyroid surgery to lower thyroid hormone levels and minimize the effects of thyroid manipulation. {{anchor|feline}}Additionally, thiamazole is used in the veterinary setting to treat hyperthyroidism in cats. Adverse effectsIt is important to monitor any symptoms of fever or sore throat while taking thiamazole; this could indicate the development of agranulocytosis, an uncommon but severe side effect resulting from a drop in the white blood cell count (to be specific, neutropenia, a deficiency of neutrophils). A complete blood count (CBC) with differential is performed to confirm the suspicion, in which case the drug is discontinued.[4] Administration of recombinant human granulocyte colony-stimulating factor (rhG-CSF) may increase recovery. Other known side effects include:
Drug interactionsAdverse effects may occur for individuals who:
Mechanism of actionThiamazole inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I−) to iodine (I2), hypoiodous acid (HOI), enzyme linked hypoiodate (EOI) facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin, a necessary step in the synthesis of triiodothyronine (T3) and thyroxine (T4). It does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate. It acts at CXCL10.[5] References1. ^{{cite web|url=http://www.drugbank.ca/drugs/DB00763|title=DrugBank: Methimazole (DB00763)|work=drugbank.ca|accessdate=21 July 2015}} {{Sulfur compounds}}{{Thyroid therapy}}{{Thyroid hormone receptor modulators}}2. ^{{cite journal |vauthors=Nakamura H, Noh JY, Itoh K, Fukata S, Miyauchi A, Hamada N |title=Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease |journal=The Journal of Clinical Endocrinology and Metabolism |volume=92 |issue=6 |pages=2157–62 |date=June 2007 |pmid=17389704 |doi=10.1210/jc.2006-2135 |url=http://jcem.endojournals.org/cgi/pmidlookup?view=long&pmid=17389704}} 3. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}} 4. ^{{cite journal|last1=Fumarola|first1=A|last2=Di Fiore|first2=A|last3=Dainelli|first3=M|last4=Grani|first4=G|last5=Calvanese|first5=A|title=Medical treatment of hyperthyroidism: state of the art.|journal=Experimental and Clinical Endocrinology & Diabetes|date=Nov 2010|volume=118|issue=10|pages=678–84|pmid=20496313|doi=10.1055/s-0030-1253420}} 5. ^{{cite journal |vauthors=Crescioli C, Cosmi L, Borgogni E, etal |title=Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes |journal=J. Endocrinol. |volume=195 |issue=1 |pages=145–55 |date=October 2007 |pmid=17911406 |doi=10.1677/JOE-07-0240 |url=http://joe.endocrinology-journals.org/cgi/pmidlookup?view=long&pmid=17911406}} 3 : Antithyroid drugs|Imidazoles|Thioureas |
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