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| methimazoleSummarySummary: 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. Top Publications
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- Xie F, Zhou X, Genter M, Behr M, Gu J, Ding X. The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5. Drug Metab Dispos. 2011;39:947-51 pubmed publisherThe antithyroid drug methimazole (MMZ) can cause severe, tissue-specific toxicity in mouse olfactory mucosa (OM), presumably through a sequential metabolic activation of MMZ by cytochrome P450 (P450) and flavin monooxygenases (FMO)...
- Hosseini M, Hadjzadeh M, Derakhshan M, Havakhah S, Rassouli F, Rakhshandeh H, et al. The beneficial effects of olibanum on memory deficit induced by hypothyroidism in adult rats tested in Morris water maze. Arch Pharm Res. 2010;33:463-8 pubmed publisher..03% methimazol was added to drinking water. Group 3 and 4 were treated with 0.03% methimazole as well as 100 and 500 mg/kg olibanum respectively. The animals were tested in Morris water maze...
- Ramos Bonner L, Goldberg T, Moyer S, Anastasopoulou C. Methimazole-induced cholestatic jaundice in an elderly hyperthyroid patient. Am J Geriatr Pharmacother. 2007;5:236-40 pubmedHyperthyroidism is a common disease in the elderly. Antithyroid medications such as methimazole are one of the few treatment options...
- Tsuboi K, Ueshiba H, Shimojo M, Ishikawa M, Watanabe N, Nagasawa K, et al. The relation of initial methimazole dose to the incidence of methimazole-induced agranulocytosis in patients with Graves' disease. Endocr J. 2007;54:39-43 pubmedThe relation between the incidence of methimazole (methylmercaptoimidazole; MMI)-induced agranulocytosis and initial MMI dose was evaluated in a group of 514 patients with Graves' disease who were treated between 1995 and 2005...
- Lombardo F, Messina M, Salzano G, Rabbone I, Lo Presti D, Calcaterra V, et al. Prevalence, presentation and clinical evolution of Graves' disease in children and adolescents with type 1 diabetes mellitus. Horm Res Paediatr. 2011;76:221-5 pubmed publisher..04). The subsequent course with methimazole therapy and after its withdrawal was very similar in both groups. GD prevalence in T1DM patients was 0.53%, i.e...
- Gu X, Zheng L, Chen X, Ruan L, Zhang H, Ge S, et al. Elevated serum IL-16 and RANTES levels in patients with autoimmune thyroid diseases and modulation by methimazole therapy. Horm Metab Res. 2012;44:482-7 pubmed publisher..In conclusion, IL-16 and RANTES might be involved in the pathogenesis of GD and HT, and serum IL-16 levels in GD maybe a potential marker of disease activity and severity...
- Hwang I, Kim I, Kim Y, Yi S, Lee Y, Ju E, et al. Effects of methimazole on the onset of type 2 diabetes in leptin receptor-deficient rats. J Vet Med Sci. 2009;71:275-80 pubmedWe investigated the effects of methimazole, an anti-thyroid drug, on the onset of type 2 diabetes in Zucker diabetic fatty (ZDF) rats. For this, 0...
- Ben Amara I, Fetoui H, Guermazi F, Zeghal N. Dietary selenium addition improves cerebrum and cerebellum impairments induced by methimazole in suckling rats. Int J Dev Neurosci. 2009;27:719-26 pubmed publisher..is to investigate the improving effects of selenium (Se) on cerebrum and cerebellum impairments induced by methimazole (MMI) in suckling rats...
- Emiliano A, Governale L, Parks M, Cooper D. Shifts in propylthiouracil and methimazole prescribing practices: antithyroid drug use in the United States from 1991 to 2008. J Clin Endocrinol Metab. 2010;95:2227-33 pubmed publisherThe thionamide antithyroid drugs methimazole and propylthiouracil are the mainstay of pharmacologic therapy for Graves' disease...
- Rivkees S, Szarfman A. Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children. J Clin Endocrinol Metab. 2010;95:3260-7 pubmed publisherThe antithyroid drugs propylthiouracil and methimazole were introduced for clinical use about 60 yr ago and are estimated to be used in more than 6000 children and adolescents per year in the United States...
- Vallortigara J, Alfos S, Micheau J, Higueret P, Enderlin V. T3 administration in adult hypothyroid mice modulates expression of proteins involved in striatal synaptic plasticity and improves motor behavior. Neurobiol Dis. 2008;31:378-85 pubmed publisher..We used hypothyroid mice, treated with propylthiouracil (PTU) and methimazole (MMI), with or without subsequent administration of T3...
- Chen L, Zhang X, Wu H, Guo S, Li X. [Relationship between methimazole and antineutrophil cytoplasmic antibody-positive vasculitis]. Zhonghua Er Ke Za Zhi. 2008;46:446-9 pubmedTo study the relationship between methimazole (MMI) and antineutrophil cytoplasmic antibody (ANCA)-positive vasculitis. Thirty-three cases with Graves' disease were tested for serum ANCA before and after taking MMI...
- Leal A, Pantaleão T, Moreira D, Marassi M, Pereira V, Rosenthal D, et al. Hypothyroidism and hyperthyroidism modulates Ras-MAPK intracellular pathway in rat thyroids. Endocrine. 2007;31:174-8 pubmed..We induced hypothyroidism in Wistar rats by methimazole (MMI) treatment (0.03% in the drinking water for 21 days)...
- Rivkees S. Pediatric Graves' disease: controversies in management. Horm Res Paediatr. 2010;74:305-11 pubmed publisher..When ATDs are used in children, only methimazole should be used...
- Yang M, Qu H, Deng H. Acute pancreatitis induced by methimazole in a patient with Graves' disease. Thyroid. 2012;22:94-6 pubmed publisherAntithyroid drugs such as methimazole (MMI), the mainstay of pharmacologic therapy for Graves' disease, can provoke a variety of adverse effects...
- Chattaway J, Klepser T. Propylthiouracil versus methimazole in treatment of Graves' disease during pregnancy. Ann Pharmacother. 2007;41:1018-22 pubmedTo evaluate the evidence supporting the use of propylthiouracil (PTU) versus methimazole for the treatment of Graves' disease during pregnancy. An English-language literature search was conducted using MEDLINE (1966-March 2007)...
- Casallo Blanco S, Valero M, Marcos Sánchez F, de Matías Salces L, Blanco González J, Martín Barranco M. [Methimazole and propylthiouracil induced acute toxic hepatitis]. Gastroenterol Hepatol. 2007;30:268-70 pubmed..Treatment can be either pharmacological, surgical or using radioactive iodine. In Europe methimazole is the antithyroid drug of choice because it can be administered in a single daily dose and has a lower risk of ..
- Alturfan A, Zengin E, Dariyerli N, Alturfan E, Gumustas M, Aytac E, et al. Investigation of zinc and copper levels in methimazole-induced hypothyroidism: relation with the oxidant-antioxidant status. Folia Biol (Praha). 2007;53:183-8 pubmed..On the other hand, GSH and SOD levels remained constant. It may be suggested that Cu and Zn serve as antioxidant molecules and exert their effects in an indirect manner to reduce oxidative stress in experimental hypothyroidism. ..
- Valdez R, Barbero P, Liascovich R, De Rosa L, Aguirre M, Alba L. Methimazole embryopathy: a contribution to defining the phenotype. Reprod Toxicol. 2007;23:253-5 pubmedIt has been suggested that children prenatally exposed to methimazole may present some features in common but the phenotype remains to be defined...
- Heidari R, Babaei H, Eghbal M. Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes. Drug Chem Toxicol. 2013;36:403-11 pubmed publisherb>Methimazole is an antithyroid drug widely used in the treatment of hyperthyroidism...
- Benavides U, Gonzalez Murguiondo M, Harii N, Lewis C, Sakhalkar H, Deosarkar S, et al. Phenyl methimazole suppresses dextran sulfate sodium-induced murine colitis. Eur J Pharmacol. 2010;643:129-38 pubmed publisher..Previously, we have shown that phenyl methimazole (C10) markedly decreases virally-induced TLR-3 expression and signaling and potently inhibits both TNF-alpha-..
- Landex N, Thomsen J, Kayser L. Methimazole increases H2O2 toxicity in human thyroid epithelial cells. Acta Histochem. 2006;108:431-9 pubmed..We further evaluated whether methimazole, an antithyroid drug reported to have antioxidative properties, could counteract the effects of H(2)O(2)...
- Yang J, Zhong J, Zhou L, Hong T, Xiao X, Wen G. Sudden onset agranulocytosis and hepatotoxicity after taking methimazole. Intern Med. 2012;51:2189-92 pubmedAgranulocytosis is a rare adverse effect of methimazole. The usual duration of treatment prior to the onset of agranulocytosis is approximately 1 to 4 months, and can be as long as 1 year...
- Devine C, Brennan G, Lanusse C, Alvarez L, Trudgett A, Hoey E, et al. Effect of the metabolic inhibitor, methimazole on the drug susceptibility of a triclabendazole-resistant isolate of Fasciola hepatica. Parasitology. 2009;136:183-92 pubmed publisher..The flavin monooxygenase system (FMO) was inhibited using methimazole (MTZ) to see whether a TCBZ-resistant isolate could be made more sensitive to TCBZ action...
- Kobayashi M, Higuchi S, Ide M, Nishikawa S, Fukami T, Nakajima M, et al. Th2 cytokine-mediated methimazole-induced acute liver injury in mice. J Appl Toxicol. 2012;32:823-33 pubmed publisher..However, the mechanisms leading to DILI are unknown in most cases. Methimazole (MTZ) is used as an antithyroid drug and is well known to have induced liver injuries such as cholestatic ..
- Sato H, Sasaki N, Minamitani K, Minagawa M, Kazukawa I, Sugihara S, et al. Higher dose of methimazole causes frequent adverse effects in the management of Graves' disease in children and adolescents. J Pediatr Endocrinol Metab. 2012;25:863-7 pubmed publisherb>Methimazole (MMI) is used as a first-line antithyroid drug in children and adolescents with Graves' disease (GD)...
- Ahmed K, Rao S, Simha V. Antineutrophil cytoplasmic antibody-positive vasculitis in a patient with graves disease: cross-reaction between propylthiouracil and methimazole. Endocr Pract. 2010;16:449-51 pubmed publisher..To alert clinicians about the risk of vasculitis and cross-reactivity of antithyroid medication...
- Suzukawa K, Kondo K, Kanaya K, Sakamoto T, Watanabe K, Ushio M, et al. Age-related changes of the regeneration mode in the mouse peripheral olfactory system following olfactotoxic drug methimazole-induced damage. J Comp Neurol. 2011;519:2154-74 pubmed publisher..Mice at postnatal ages of 10 days, 3 months, and 16 months were given an intraperitoneal injection of methimazole to produce damage in the olfactory neuroepithelium...
- Coady K, Marino T, Thomas J, Currie R, Hancock G, Crofoot J, et al. Evaluation of the amphibian metamorphosis assay: exposure to the goitrogen methimazole and the endogenous thyroid hormone L-thyroxine. Environ Toxicol Chem. 2010;29:869-80 pubmed publisher..exposure studies with Xenopus laevis tadpoles were conducted with two known thyroid-active compounds, namely, methimazole or L-thyroxine, for a total of 21 d...
- Pedro A, Romaldini J, Takei K. Changes of serum cytokines in hyperthyroid Graves' disease patients at diagnosis and during methimazole treatment. Neuroimmunomodulation. 2011;18:45-51 pubmed publisher..factor (TNF)-? concentrations in 29 untreated GD patients before and after restoration of euthyroidism with methimazole (MMI) treatment compared to 25 control subjects...
- Kahmann C, Wunderlich G, Freudenberg R, Zophel K, Oehme L, Kotzerke J. Radioprotection of thyroid cells mediated by methimazole. Int J Radiat Biol. 2010;86:811-6 pubmed publisher..Adherent thyroid cells were irradiated following incubation with the mediators methimazole and perchlorate using either X-ray tube or Re-188-perrhenate...
- Chang C, Chen Y, Huang H, Lee F, Chang F, Lin H, et al. Methimazole alleviates hepatic encephalopathy in bile-duct ligated cirrhotic rats. J Chin Med Assoc. 2006;69:563-8 pubmed..Three weeks after BDL, rats were randomized to receive either tap water (control) or 0.04% methimazole in drinking water for 3 weeks...
- Lau E, So S, Chan E, Kwok J, Ma J, Kung A. Methimazole-induced antineutrophil cytoplasmic antibody-associated diffuse alveolar haemorrhage in a Chinese woman with Graves' disease. Hong Kong Med J. 2009;15:209-12 pubmedWe report on a case of diffuse alveolar haemorrhage in a Chinese woman due to methimazole-induced antineutrophil cytoplasmic antibodies...
- Hasebe M, Matsumoto I, Imagawa T, Uehara M. Effects of an anti-thyroid drug, methimazole, administration to rat dams on the cerebellar cortex development in their pups. Int J Dev Neurosci. 2008;26:409-14 pubmed publisherIn the present study, the effects of methimazole (a major anti-thyroid drug) administration to rat dams on the development of cerebellum of their pups were investigated with morphological, morphometrical and functional procedures...
- Gallelli L, Staltari O, Palleria C, De Sarro G, Ferraro M. Hepatotoxicity induced by methimazole in a previously healthy patient. Curr Drug Saf. 2009;4:204-6 pubmedWe report a case of hepatotoxicity induced by methimazole treatment in a patient affected by hyperthyroidism...
- Clementi M, Di Gianantonio E, Cassina M, Leoncini E, Botto L, Mastroiacovo P. Treatment of hyperthyroidism in pregnancy and birth defects. J Clin Endocrinol Metab. 2010;95:E337-41 pubmed publisherClinical hyperthyroidism is not uncommon in pregnancy, with a reported prevalence of 0.1 to 0.4%. The available antithyroid drugs are propylthiouracil and methimazole/carbimazole.
- Ismail H. Reversible pulmonary hypertension and isolated right-sided heart failure associated with hyperthyroidism. J Gen Intern Med. 2007;22:148-50 pubmed..We report a case of hyperthyroidism presenting with signs and symptoms of isolated right heart failure, tricuspid regurgitation, and pulmonary hypertension, which resolved with treatment of hyperthyroidism. ..
- Crescioli C, Cosmi L, Borgogni E, Santarlasci V, Gelmini S, Sottili M, et al. Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes. J Endocrinol. 2007;195:145-55 pubmed..Treatment with methimazole (MMI) reduces serum CXCL10 in patients with Graves' disease...
- Barbero P, Valdez R, Rodriguez H, Tiscornia C, Mansilla E, Allons A, et al. Choanal atresia associated with maternal hyperthyroidism treated with methimazole: a case-control study. Am J Med Genet A. 2008;146A:2390-5 pubmed publisher..Several case reports have suggested a relationship between the prenatal use of methimazole (MMI) and choanal atresia in the offspring...
- Tripodi P, Ruggeri R, Campenni A, Cucinotta M, Mirto A, Lo Gullo R, et al. Central nervous system vasculitis after starting methimazole in a woman with Graves' disease. Thyroid. 2008;18:1011-3 pubmed publisher..Here we describe the first patient with central nervous system (CNS) vasculitis that developed shortly after the start of methimazole (MMI) treatment for GD.
- Virdis A, Colucci R, Fornai M, Polini A, Daghini E, Duranti E, et al. Inducible nitric oxide synthase is involved in endothelial dysfunction of mesenteric small arteries from hypothyroid rats. Endocrinology. 2009;150:1033-42 pubmed publisher..Male Wistar rats were treated with methimazole (MMI; 0.003%) or placebo up to 16 wk...
- Cano Europa E, Perez Severiano F, Vergara P, Ortiz Butron R, Rios C, Segovia J, et al. Hypothyroidism induces selective oxidative stress in amygdala and hippocampus of rat. Metab Brain Dis. 2008;23:275-87 pubmed publisher..Hypothyroidism was induced by administering methimazole in drinking water (60 mg/kg/day)...
- Weng Q, Saita E, Watanabe G, Takahashi S, Sedqyar M, Suzuki A, et al. Effect of methimazole-induced hypothyroidism on adrenal and gonadal functions in male Japanese quail (Coturnix japonica). J Reprod Dev. 2007;53:1335-41 pubmed..was induced in male adult Japanese quail by daily administration of 2-Mercapto-1-methylimidazole (methimazole) in their drinking water...
- Ceballos L, Moreno L, Alvarez L, Shaw L, Fairweather I, Lanusse C. Unchanged triclabendazole kinetics after co-administration with ivermectin and methimazole: failure of its therapeutic activity against triclabendazole-resistant liver flukes. BMC Vet Res. 2010;6:8 pubmed publisher..and clinical efficacy of TCBZ administered alone or co-administered with ivermectin (IVM, efflux modulator) and methimazole (MTZ, metabolic inhibitor) in TCBZ-resistant F. hepatica-parasitized sheep...
- Osman A, Nemnem M, Abou Bakr A, Nassier O, Khayyal M. Effect of methimazole treatment on doxorubicin-induced cardiotoxicity in mice. Food Chem Toxicol. 2009;47:2425-30 pubmed publisher..The present study was undertaken to find out the chemo protective role of methimazole against doxorubicin-induced cardiotoxicity in experimental animals...
- Sakamoto T, Kondo K, Kashio A, Suzukawa K, Yamasoba T. Methimazole-induced cell death in rat olfactory receptor neurons occurs via apoptosis triggered through mitochondrial cytochrome c-mediated caspase-3 activation pathway. J Neurosci Res. 2007;85:548-57 pubmedThe administration of methimazole is known to induce cell death in rat olfactory receptor neurons (ORNs)...
- Bilu Martin D, Deng A, Gaspari A, Pearson F. Perinuclear antineutrophil cytoplasmic antibody-associated vasculitis in a patient with Graves' disease treated with methimazole. Skinmed. 2006;5:302-5 pubmed..She had a medical history of Graves' disease, diagnosed in 1999, for which she was taking methimazole (MMI)...
- Cooper D. Antithyroid drugs. N Engl J Med. 2005;352:905-17 pubmed
- Tsai M, Chang Y, Wu V, Chang C, Huang T. Methimazole-induced pulmonary hemorrhage associated with antimyeloperoxidase-antineutrophil cytoplasmic antibody: a case report. J Formos Med Assoc. 2001;100:772-5 pubmed..vasculitis manifesting as a skin lesion and hemoptysis with hypoxic respiratory failure after taking methimazole. An open lung biopsy was consistent with acute capillaritis...
- Guma M, Salinas I, Reverter J, Roca J, Valls Roc M, Juan M, et al. Frequency of antineutrophil cytoplasmic antibody in Graves' disease patients treated with methimazole. J Clin Endocrinol Metab. 2003;88:2141-6 pubmed..The aim of this study was to determine ANCA in Graves' disease patients at diagnosis and after treatment with methimazole and to evaluate the relationship between ANCA and hyperthyroidism evolution...
- Barbero P, Ricagni C, Mercado G, Bronberg R, Torrado M. Choanal atresia associated with prenatal methimazole exposure: three new patients. Am J Med Genet A. 2004;129A:83-6 pubmedWe report three patients with bilateral choanal atresia in children prenatally exposed to methimazole (MMI) in order to define a MMI embryopathy clinical pattern...
- Bonaci Nikolic B, Nikolic M, Andrejevic S, Zoric S, Bukilica M. Antineutrophil cytoplasmic antibody (ANCA)-associated autoimmune diseases induced by antithyroid drugs: comparison with idiopathic ANCA vasculitides. Arthritis Res Ther. 2005;7:R1072-81 pubmed..of 16/72 patients who became ANCA-positive during ATD therapy (12 receiving propylthiouracil and four receiving methimazole)...
- Aragoni M, Arca M, Demartin F, Devillanova F, Garau A, Isaia F, et al. Anti-thyroid drug methimazole: X-ray characterization of two novel ionic disulfides obtained from its chemical oxidation by I(2). J Am Chem Soc. 2002;124:4538-9 pubmedInteraction of methimazole (MMI, 1-methyl-imidazole-2-thione) with I2 in solvents having different polarity gives two new stable compounds containing a dication disulfide and a monocation disulfide arranged in dimers, respectively...
- Bergman U, Ostergren A, Gustafson A, Brittebo B. Differential effects of olfactory toxicants on olfactory regeneration. Arch Toxicol. 2002;76:104-12 pubmed..in the olfactory mucosa of NMRI mice after exposure to the olfactory toxicants dichlobenil (a herbicide) or methimazole (an antithyroid drug). Three and six months after exposure to dichlobenil (2x or 1 x 25 mg/kg i.p...
- Diav Citrin O, Ornoy A. Teratogen update: antithyroid drugs-methimazole, carbimazole, and propylthiouracil. Teratology. 2002;65:38-44 pubmed
- Zhang L, Parratt J, Beastall G, Pyne N, Furman B. Streptozotocin diabetes protects against arrhythmias in rat isolated hearts: role of hypothyroidism. Eur J Pharmacol. 2002;435:269-76 pubmed..This protection was prevented by treatment with either triiodothyronine or insulin. Hearts from methimazole-hypothyroid rats also showed no ventricular fibrillation during reperfusion...
- Ciulla M, Paliotti R, Cortelazzi D, Tortora G, Barelli M, Buonamici V, et al. Effects of thyroid hormones on cardiac structure: a tissue characterization study in patients with thyroid disorders before and after treatment. Thyroid. 2001;11:613-9 pubmed
- Mizutani T, Yoshida K, Murakami M, Shirai M, Kawazoe S. Evidence for the involvement of N-methylthiourea, a ring cleavage metabolite, in the hepatotoxicity of methimazole in glutathione-depleted mice: structure-toxicity and metabolic studies. Chem Res Toxicol. 2000;13:170-6 pubmedIn mice depleted of GSH by treatment with buthionine sulfoximine (BSO), methimazole (2-mercapto-1-methylimidazole, MMI) causes liver injury characterized by centrilobular necrosis of hepatocytes and an increase in serum alanine ..