Thiamazolethiamazole tablets, thiamazole
Thiamazole INN or methimazole USAN is an antithyroid drug, and part of the thioamide group Like its counterpart propylthiouracil, possible major side effects of treatment include agranulocytosis and liver inflammation
- 1 Medical uses
- 2 Adverse effects
- 3 Drug interactions
- 4 Mechanism of action
- 5 References
Thiamazole 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 Additionally, thiamazole is used in the veterinary setting to treat hyperthyroidism in cats
It 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 Administration of recombinant human granulocyte colony-stimulating factor rhG-CSF may increase recovery
Other known side effects include:
- skin rash
- abnormal hair loss
- upset stomach
- loss of taste
- abnormal sensations tingling, prickling, burning, tightness, and pulling
- joint and muscle pain
- decreased platelet count thrombocytopenia
- aplasia cutis congenita prenatal exposure
- thyroid gland enlargement prenatal exposure
Adverse effects may occur for individuals who:
- Take anticoagulants 'blood thinners' such as warfarin Coumadin, diabetes medications, digoxin Lanoxin, theophylline Theobid, Theo-Dur, and vitamins
- Have ever had any blood disease, such as decreased white blood cells leukopenia, decreased platelets thrombocytopenia or aplastic anemia, or liver disease hepatitis, jaundice
- Are pregnant, or going to become pregnant, or are breastfeeding
Mechanism of action
Thiamazole 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
- ^ "DrugBank: Methimazole DB00763" drugbankca Retrieved 21 July 2015
- ^ Nakamura H, Noh JY, Itoh K, Fukata S, Miyauchi A, Hamada N June 2007 "Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease" The Journal of Clinical Endocrinology and Metabolism 92 6: 2157–62 doi:101210/jc2006-2135 PMID 17389704
- ^ Fumarola, A; Di Fiore, A; Dainelli, M; Grani, G; Calvanese, A Nov 2010 "Medical treatment of hyperthyroidism: state of the art" Experimental and Clinical Endocrinology & Diabetes 118 10: 678–84 doi:101055/s-0030-1253420 PMID 20496313
- ^ Crescioli C, Cosmi L, Borgogni E, et al October 2007 "Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes" J Endocrinol 195 1: 145–55 doi:101677/JOE-07-0240 PMID 17911406
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