Carbimazole   中文名称: 仲丁威

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Carbimazole is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Doses of carbimazole of 30 mg daily or 50 mg weekly have not adversely affected the few breastfed infants studied. Carbimazole is a prodrug for methimazole which has been studied extensively during breastfeeding; maternal methimazole therapy does not affect thyroid function or intellectual development in breastfed infants with doses up to 20 mg daily. Some experts now recommend that methimazole should be considered the antithyroid drug of choice in nursing mothers.
The American Thyroid Association recommends only monitoring infants for appropriate growth and development during routine pediatric health and wellness evaluations and routine assessment of serum thyroid function in the child is not recommended. Rare idiosyncratic reactions (e.g., agranulocytosis) might occur, and the infant should be watched for signs of infection. Monitoring of the infant's complete blood count and differential is advisable if there is a suspicion of a drug-induced blood dyscrasia.
◉ Effects in Breastfed Infants
Eleven mothers were taking oral carbimazole in dosages ranging from 5 to 20 mg daily during pregnancy and 5 to 15 mg daily during breastfeeding (extent not stated). None of the 12 infants, including one set of twins, had a serum thyroxine (T4) concentration below the lower limit of normal on day 4 of life. Thyrotropin (TSH) concentrations were normal in all infants when measured at various times over the first 21 days postpartum.
Four women were receiving 10 to 20 mg of carbimazole daily. Infant blood samples were obtained on days 4, 7, 10, and 42 and at 3 and 6 months postpartum. Thyroid function was normal in 3 infants. In one infant, the TSH was elevated for the first 10 days of life.
A mother with twins began taking carbimazole 30 mg daily 2 months postpartum. The dosage was lowered as she became euthyroid. The infants were breastfed (extent not stated) and clinical and laboratory examinations were performed over the following 4 months. There was no evidence of alterations in thyroid function.
Fifteen mothers received carbimazole 10 to 20 mg daily for 12 to 40 weeks during pregnancy and 9 continued to take the drug during 2 to 26 weeks of lactation. Their infants were monitored for up to 18 months. Infant thyroid function was within nornml over this period, the range of mean values for individual infants being TSH 1.4 to 5.9 millliunits/L, free T3 6.2 to 9.3 pmol/L and T4 104 to 189 nmol/L. Physical examination at intervals for 2 to 18 months was normal in all infants who received carbimazole and Griffiths mental development scales were normal in all 6 infants who were assessed at 18 months.
A mother was taking carbimazole 50 mg once weekly during pregnancy and postpartum. Her infant was exclusively breastfed for the first 84 days of life and had clinical and laboratory examinations performed over the first 4 months of life. Although the infant's tone and deep tendon reflexes were slightly increased and she was easily irritable, serum thyroid hormone levels were normal as was her growth. No symptoms or signs of hypothyroidism were observed.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
85%

[1]. Carbimazole is an inhibitor of protein synthesis and protects from neuronal hypoxic damage in vitro. J Pharmacol Exp Ther. 2013 Dec;347(3):781-93.

[2]. Effects of Dose Level of Anti-thyroid Drug Carbimazole on Thermoregulation and Blood Constituents in Male Rabbits (Oryctolagus cuniculus). Advances in Research, 2014, 2(3), 129–144.

[3]. Nakashima, T. and A. Taurog, Rapid conversion of carbimazole to methimazole in serum; evidence for an enzymatic mechanism. Clin Endocrinol (Oxf), 1979. 10(6): p. 637-48.

Carbimazole is a member of the class of imidazoles that is methimazole in which the nitrogen bearing a hydrogen is converted into its ethoxycarbonyl derivative. A prodrug for methimazol, carbimazole is used for the treatment of hyperthyroidism. It has a role as a prodrug and an antithyroid drug. It is a carbamate ester and a member of 1,3-dihydroimidazole-2-thiones.
An imidazole antithyroid agent. Carbimazole is metabolized to methimazole, which is responsible for the antithyroid activity.
An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.

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Drug Indication
For the treatment of hyperthyroidism and thyrotoxicosis. It is also used to prepare patients for thyroidectomy.

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Mechanism of Action
Carbimazole is an aitithyroid agent that decreases the uptake and concentration of inorganic iodine by thyroid, it also reduces the formation of di-iodotyrosine and thyroxine. Once converted to its active form of methimazole, it 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.

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Pharmacodynamics
Carbimazole is a carbethoxy derivative of methimazole. Its antithyroid action is due to its conversion to methimazole after absorption. It is used to treat hyperthyroidism and thyrotoxicosis.

C7H10N2O2S

186.229

186.046

22232-54-8

31072

White to off-white solid powder

1.3±0.1 g/cm3

240.4±23.0 °C at 760 mmHg

124°C

99.2±22.6 °C

0.0±0.5 mmHg at 25°C

1.612

0.34

68.25

0

3

2

12

240

0

CFOYWRHIYXMDOT-UHFFFAOYSA-N

InChI=1S/C7H10N2O2S/c1-3-11-7(10)9-5-4-8(2)6(9)12/h4-5H,3H2,1-2H3

ethyl 3-methyl-2-sulfanylideneimidazole-1-carboxylate

Neomercazole Neo-Tireol CarbimazoleCarbimazole 3-Methyl-2-thionoimidazoline-1-carboxylic acid ethyl ester

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~536.97 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (13.42 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (13.42 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (13.42 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。