Carbimazole

Carbimazole

Systematic (IUPAC) name
ethyl 3-methyl-2-sulfanylidene-imidazole-1-carboxylate
Clinical data
Trade names	Neo-mercazole
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	oral
Pharmacokinetic data
Protein binding	85%
Identifiers
CAS number	22232-54-8
ATC code	H03BB01
PubChem	CID 31072
DrugBank	APRD00503
ChemSpider	28829 Y
UNII	8KQ660G60G Y
KEGG	D07616 Y
ChEBI	CHEBI:617099 Y
ChEMBL	CHEMBL508102 Y
Chemical data
Formula	C7H10N2O2S
Mol. mass	186.233 g/mol
SMILES	eMolecules & PubChem
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)

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).

Clinical use

Therapy for hyperthyroidism generally starts at a high daily dose of 15 - 40mg continued until the patient has normal thyroid function, and then reduced to a maintenance dose of 5 - 15mg. 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]

Side 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.

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. Patients are advised to immediately report symptoms of infection, especially sore throats, so that a full blood count test may be arranged. If this confirms a low neutrophil count then the drug must be discontinued immediately, allowing for usually a prompt recovery. However failure to report suggestive symptoms or delays in considering the possibility of immunosuppression and its testing, can lead to fatalities. Should be used with caution in pregnancy as crosses the placenta barrier.

Brand names

• Neomercazole
• Vidalta
• Camazol

See also

• Graves' disease
• Hyperthyroidism

References

• British National Formulary 45 March 2003

This hormonal preparation article is a stub. You can help Wikipedia by expanding it.v · Categories: Antithyroid drugs Imidazoles Thioureas Carbamates Systemic hormonal preparation stubs Wikimedia Foundation. 2010. Игры ⚽ Нужно решить контрольную? Mentadent Elektrichka Look at other dictionaries: carbimazole — n. a thionamide used to reduce the production of thyroid hormone in cases of overactivity of the gland (thyrotoxicosis); it is the most commonly used antithyroid drug in the UK. A prodrug, it is administered by mouth and converted to its… …   The new mediacal dictionary carbimazole — Used in the treatment of hyperthyroidism. * * * n. a drug used to reduce the production of thyroid hormone in cases of overactivity of the gland (thyrotoxicosis). It is administered by mouth; some allergic reactions may occur and high dosage may… …   Medical dictionary Карбимазол (Carbimazole) — лекарственное вещество, применяемое для уменьшения выработки гормонов щитовидной железой при ее гипсрактивности (тиреотоксикозе). Назначается внутрь; после приема у больного могут возникать различные аллергические реакции, а прием больших доз… …   Медицинские термины КАРБИМАЗОЛ — (carbimazole) лекарственное вещество, применяемое для уменьшения выработки гормонов щитовидной железой при ее гипсрактивности (тиреотоксикозе). Назначается внутрь; после приема у больного могут возникать различные аллергические реакции, а прием… …   Толковый словарь по медицине Carbimazol — Strukturformel Allgemeines Freiname Carbimazol Andere Namen …   Deutsch Wikipedia Antithyroid drug — A drug directed against the thyroid gland. The antithyroid drugs include carbimazole, methimazole, and propylthiouracil (PTU). These drugs are used to treat hyperthyroidism (overactivity of the thyroid gland) in order to reduce the excessive… …   Medical dictionary Drug, antithyroid — A drug directed against the thyroid gland. The antithyroid drugs include carbimazole, methimazole, and propylthiouracil (PTU). These drugs are used to treat hyperthyroidism (overactivity of the thyroid gland) in order to reduce the excessive… …   Medical dictionary Hyperthyroidism — Classification and external resources Triiodothyronine (T3, pictured) and thyroxine (T4) are both forms of thyroid hormone. ICD 10 …   Wikipedia Thyroid — Infobox Anatomy Name = Thyroid Latin = glandula thyroidea GraySubject = 272 GrayPage = 1269 Caption = Endocrine system Caption2 = Thyroid and parathyroid. Precursor = 4th Branchial pouch System = endocinal jubachina system Artery = superior… …   Wikipedia Graves' disease — Classification and external resources Photo showing the classic finding of proptosis and lid retraction in Graves disease ICD 10 …   Wikipedia 18+ © Academic, 2000-2024 Contact us: Technical Support, Advertising Dictionaries export, created on PHP, Joomla, Drupal, WordPress, MODx. Mark and share Search through all dictionaries Translate… Search Internet Share the article and excerpts Direct link … Do a right-click on the link above and select “Copy Link”