Carbimazole
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| Trade names | Neo-mercazole |
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| Routes of administration |
oral |
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| Pharmacokinetic data | |
| Protein binding | 85% |
| Biological half-life | 5.3h |
| Excretion | >90%Renal |
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| ECHA InfoCard | 100.040.762 |
| Chemical and physical data | |
| Formula | C7H10N2O2S |
| Molar mass | 186.233 g/mol |
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Carbimazole is used to treat hyperthyroidism. Carbimazole is a pro-drug as after absorption it is converted to the active form, methimazole. Methimazole prevents thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4 (thyroxine).
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.
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.
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. Furthermore, breast feeding is possible but only if lowest effective dose is used and neonatal development is closely monitored.
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