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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/01/21 19:52:44」(JST)
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Carbimazole
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Systematic (IUPAC) name |
ethyl 3-methyl-2-sulfanylidene-imidazole-1-carboxylate |
Clinical data |
Trade names |
Neo-mercazole |
AHFS/Drugs.com |
International Drug Names |
Legal status |
|
Routes |
oral |
Pharmacokinetic data |
Protein binding |
85% |
Identifiers |
CAS number |
22232-54-8 Y |
ATC code |
H03BB01 |
PubChem |
CID 31072 |
DrugBank |
DB00389 |
ChemSpider |
28829 Y |
UNII |
8KQ660G60G Y |
KEGG |
D07616 Y |
ChEBI |
CHEBI:617099 Y |
ChEMBL |
CHEMBL508102 Y |
Chemical data |
Formula |
C7H10N2O2S |
Molecular mass |
186.233 g/mol |
|
InChI
-
InChI=1S/C7H10N2O2S/c1-3-11-7(10)9-5-4-8(2)6(9)12/h4-5H,3H2,1-2H3 Y
Key:CFOYWRHIYXMDOT-UHFFFAOYSA-N Y
|
Y (what is this?) (verify) |
|
This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (October 2008) |
Carbimazole is used to treat hyperthyroidism. Carbimazole is a pro-drug as after absorption it is converted to the active form, methimazole. Methimazole prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4 (thyroxine).
Contents
- 1 Clinical use
- 2 Precautions
- 3 Adverse effects
- 4 Brand names
- 5 See also
- 6 References
Clinical use
Therapy for hyperthyroidism generally starts at a high daily dose of 15–40 mg continued until the patient has normal thyroid function, and then reduced to a maintenance dose of 5–15 mg. Treatment is usually given for 12–18 months followed by a trial withdraw.
The onset of anti-thyroid effect is rapid but the onset of clinical effects on thyroid hormone levels in the blood is much slower. This is because the large store of pre-formed T3 and T4 in the thyroid gland and bound to thyroid binding globulin (99% bound) has to be depleted before any beneficial clinical effect occurs.
Precautions
Some people are allergic to azole(s). Some azole drugs have adverse side-effects. Some azole drugs may disrupt estrogen production in pregnancy, affecting pregnancy outcome.[1][verification needed]
Carbimazole should be used judiciously in pregnancy as it crosses the placenta. It has (rarely) been associated with congenital defects, including aplasia cutis of the neonate but is not contra-indicated. However, it more predictably may cause fetal hypothyroidism so (in minimal doses) it can be used in order to control maternal hyperthyroidism. There are reported cases of goiter and choanal atresia in fetus.[2] Furthermore, breast feeding is possible but only if lowest effective dose is used and neonatal development is closely monitored.
Adverse effects
Whilst rashes and pruritus are common, these can often be treated with antihistamines without stopping the carbimazole. For those patients where sensitivity reactions can not be controlled, propylthiouracil may be used as an alternative; cross-sensitivity between these drugs is rare.
Its most serious rare side effect is bone marrow suppression causing neutropenia and agranulocytosis. This may occur at any stage during treatment and without warning; monitoring of white cell count is not useful. Patients are advised to immediately report symptoms of infection, such as sore throat or fever, so that a full blood count test may be arranged. If this confirms a low neutrophil count, discontinuation of the drug leads to recovery. However failure to report suggestive symptoms or delays in considering the possibility of immunosuppression and its testing, can lead to fatalities.
Brand names
See also
- Graves' disease
- Hyperthyroidism
References
- ^ http://informahealthcare.com/doi/abs/10.1081/ERC-120015045
- ^ Goodman & Gilman 12th ed.
- ^ http://www.nicholas.co.id/product/?module=detailberita&id=128&act=neo-mercazole.html/
- British National Formulary 45 March 2003
Thyroid therapy (H03)
|
|
Thyroid hormones |
- Levothyroxine#
- Liothyronine
- Liotrix
- Tiratricol
- Thyroid gland preparations
|
|
Antithyroid preparations |
Thyroid peroxidase
inhibitors (thioamide)
|
- Thiouracils: Propylthiouracil#
- Methylthiouracil
- Benzylthiouracil
- Sulfur-containing imidazole derivatives: Carbimazole
- Methimazole
|
|
Block conversion of
T4 to T3
|
- Propylthiouracil#
- Ipodate
|
|
Sodium-iodide symporter
inhibitor
|
- Perchlorate (Potassium perchlorate)
- Pertechnetate (Sodium pertechnetate)
|
|
Other
|
- Diiodotyrosine
- Dibromotyrosine
|
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
|
|
Description |
- Glands
- Hormones
- Physiology
- Development
|
|
Disease |
- Diabetes
- Congenital
- Neoplasms and cancer
- Other
- Symptoms and signs
|
|
Treatment |
- Procedures
- Drugs
- calcium balance
- corticosteroids
- oral hypoglycemics
- pituitary and hypothalamic
- thyroid
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UpToDate Contents
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English Journal
- [Pharmacotherapy of hyperthyreosis - adverse drug reactions.]
- Perger L, Burgi U, Fattinger K.SourceUniversitatsklinik fur Allgemeine Innere Medizin Inselspital, Universitatsspital Bern und Universitat Bern.
- Therapeutische Umschau. Revue therapeutique." abstractLink="yes" alsec="jour" alterm="Ther Umsch.2011 Jun;68(6):303-308.
- The antithyroid drugs mainly include thioimidazole (carbimazole, methimazole = thiamazole) and propylthiouracil. After absorption, carbimazole is rapidly metabolized to methimazole and thus switching between these two drugs should not be considered in case of side effects. Furthermore, in case of si
- PMID 21656488
- Risk of adverse perinatal outcomes with antithyroid treatment during pregnancy: a nationwide population-based study.
- Chen CH, Xirasagar S, Lin CC, Wang LH, Kou Y, Lin HC.SourceDepartment & Institute of Physiology, National Yang-Ming University, Taipei, Taiwan Department of Thoracic Surgery, Mackay Memorial Hospital, Taipei, Taiwan Mackay Medicine, Nursing, and Management College, Taipei, Taiwan Department of Health Services Policy and Management, University of South Carolina, Columbia, SC, USA School of Health Care Administration, Taipei Medical University, Taipei, Taiwan School of Pharmacy, Taipei Medical University, Taipei, Taiwan.
- BJOG : an international journal of obstetrics and gynaecology." abstractLink="yes" alsec="jour" alterm="BJOG.2011 May 31. doi: 10.1111/j.1471-0528.2011.03019.x. [Epub ahead of print]
- Please cite this paper as: Chen C-H, Xirasagar S, Lin C-C, Wang L-H, Kou Y, Lin H-C. Risk of adverse perinatal outcomes with antithyroid treatment during pregnancy: a nationwide population-based study. BJOG 2011; DOI: 10.1111/j.1471-0528.2011.03019.x Objective? To compare, using two large nationwi
- PMID 21624036
Japanese Journal
- Propylthiouracil and carbimazole associated-antineutrophil cytoplasmic antibodies (ANCA) in patients with Graves' disease
- Acute Pancreatitis, Hepatic cholestasis, and Erythema Nodosum Induced by Carbimazole Treatment for Graves' Disease
- MARAZUELA Monica,PACO Graciano Sanchez de,JIMENEZ Isabel,CARRARO Rafael,FERNANDEZ-HERRERA Jesus,PAJARES Jose Maria,GOMEZ-PAN Antonio
- Endocrine journal 49(3), 315-318, 2002-06-01
- NAID 10008701480
Related Links
- Carbimazole is used to treat hyperthyroidism. Carbimazole is a pro-drug as after absorption it is converted to the active form, methimazole. Methimazole prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine ...
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