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Carbimazole

Carbimazole structure

CAS No:
22232-54-8
Formula:
C7H10N2O2S
Chemical Name:
Carbimazole
Synonyms:
1H-Imidazole-1-carboxylic acid,2,3-dihydro-3-methyl-2-thioxo-,ethyl ester;4-Imidazoline-1-carboxylic acid,3-methyl-2-thioxo-,ethyl ester;Tyrazol;Carbimazole;1-Ethoxycarbonyl-3-methyl-2-thio-4-imidazoline;Ethyl 3-methyl-2-thioimidazoline-1-carboxylate;1-Methyl-3-carbethoxy-2-thioglyoxalone;Athyromazole;CG 1;3-Carbethoxymercapto-1-methylimidazole;Carbethoxymethimazole;3-Carbethoxythio-1-methylglyoxaline;3-Carbethoxythio-1-methyliminazole;Neomercazole;Ethyl 3-methyl-2-thioxo-Δ4-imidazoline-1-carboxylate;Basolest;Carbimazol;Neo-Thyreostat
Categories:
Active Pharmaceutical Ingredients > Hormones and the Endocrine System

Description

Carbimazole is an imidazole antithyroid agent. Target: OthersCarbimazole is an effective thyroid hormone inhibitor under a class of drugs known as pro-drugs. It is considered a pro-drug because it converts to methimazole after being absorbed by the body, generating an antithyroid action that works against hyperthyroidism (excessive production of thyroid hormones) and thyrotoxicosis (inflammation of the thyroid gland) [1]. Methimazole prevents the thyroid peroxidase enzyme from coupling a

Solid

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.

Carbimazole Basic Attributes

Molecular Weight：

186.23

Exact Mass：

186.23

BRN：

144339

EC Number：

244-854-4

UNII：

8KQ660G60G

NSC Number：

758966

DSSTox ID：

DTXSID9022736

ATC Code：

H - Systemic hormonal preparations, excl. sex hormones and insulins

HScode：

2933290090

Characteristics

PSA：

64.9

XLogP3：

0.7

Appearance：

white to beige

Density：

1.3±0.1 g/cm3

Melting Point：

123.5 °C

Boiling Point：

240.4°C at 760 mmHg

Flash Point：

99.2±22.6 °C

Refractive Index：

1.612

Water Solubility：

soluble in water, ethanol, chloroform and acetone. Sightly soluble in water.DMSO: soluble 5mg/mL, clear (warmed)

Storage Conditions：

Refrigerator

Vapor Pressure：

0.038mmHg at 25°C

Collision Cross Section：

134.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

3335

wgk germany：

hazard class code：

22-36-43

safety instructions：

22-36/37/39

RTECS Number：

NJ2441000

Precautionary statement(s)：

P201, P202, P260, P263, P264, P270, P281, P308+P313, P314, P405, P501

Hazard Statements：

H360D

GHS Classification：

|Danger|H302 (18.6%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P264, P270, P272, P273, P280, P281, P301+P312, P302+P352, P305+P351+P338, P308+P313, P314, P321, P330, P333+P313, P337+P313, P363, P391, P405, and P501|Aggregated GHS information provided by 43 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H360D: May damage the unborn child [Danger Reproductive toxicity]|P201, P202, P260, P263, P264, P270, P281, P308+P313, P314, P405, and P501

Toxicity

Protein Binding：

85%

Drug Information

Drug Indication：

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

Pharmacology：

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.

MeSH：

Agents that are used to treat hyperthyroidism by reducing the excessive production of thyroid hormones. (See all compounds classified as Antithyroid Agents.)

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.

MeSH Entry Terms：

Carbimazole

Carbimazole Use and Manufacturing

Uses

Carbimazole, a prodrug of Methimazole (M260300), is used in the treatment of hyperthyroidism.

Use Classification：

Pharmaceuticals -> Animal Drugs -> Approved in Taiwan

Computed Properties

Molecular Weight:186.23
XLogP3:0.7
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:186.04629874
Monoisotopic Mass:186.04629874
Topological Polar Surface Area:64.9
Heavy Atom Count:12
Complexity:240
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Pyridine

1-Methylimidazole

Drug Function and Efficacy

This product is an anti-thyroid drug. Its mechanism of action is to inhibit thyroid peroxidase, thereby hindering the oxidation of iodide absorbed into the thyroid gland and the coupling of tyrosine, and hindering the synthesis of thyroxine (T4) and triiodothyronine (T3). Animal experiments have observed that it can inhibit the synthesis of antibodies by B lymphocytes, reduce the level of thyroid stimulating antibodies in the blood circulation, and restore the function of inhibitory T cells to normal.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Carbimazole tablets
Ingredients	The main ingredient of this product is carbimazole, and its chemical name is: 3-methyl-2-thio-2,3-dihydro-1H-imidazole-1-carboxylic acid ethyl ester
Indication	1. When used in combination with anticoagulants, it can enhance the anticoagulant effect. 2. Intake of high-iodine foods or drugs can aggravate hyperthyroidism, increase the amount of antithyroid drugs required or prolong the duration of medication. Therefore, avoid taking iodine before taking this product. 3. Sulfonamides, para-aminosalicylic acid, phenylbutazone, barbiturates, phentolamine, tolazoline, vitamin B12, sulfonylureas, etc. all have the effect of inhibiting thyroid function and thyroid enlargement, so be careful when using this product in combination.
Specifications	5mg
Manufacturer	Chengdu First Pharmaceutical Co., Ltd.

Carbimazole tablets
Ingredients	The main ingredient of this product is carbimazole, and its chemical name is: 3-methyl-2-thio-2,3-dihydro-1H-imidazole-1-carboxylic acid ethyl ester
Indication	1. When used in combination with anticoagulants, it can enhance the anticoagulant effect. 2. Intake of high-iodine foods or drugs can aggravate hyperthyroidism, increase the amount of antithyroid drugs required or prolong the duration of medication. Therefore, avoid taking iodine before taking this product. 3. Sulfonamides, para-aminosalicylic acid, phenylbutazone, barbiturates, phentolamine, tolazoline, vitamin B12, sulfonylureas, etc. all have the effect of inhibiting thyroid function and thyroid enlargement, so be careful when using this product in combination.
Specifications	5mg
Manufacturer	Handan Berlin Pharmaceutical Co., Ltd.

Carbimazole tablets
Ingredients	Carbimazole. Chemical name: 3-methyl-2-thioxo-2,3-dihydro-1H-imidazole-1-carboxylic acid ethyl ester.
Indication	1. When used in combination with anticoagulants, it can enhance the anticoagulant effect. 2. Intake of high-iodine foods or drugs can aggravate hyperthyroidism, increase the amount of antithyroid drugs required or prolong the duration of medication. Therefore, avoid taking iodine before taking this product. 3. Sulfonamides, para-aminosalicylic acid, phenylbutazone, barbiturates, phentolamine, tolazoline, vitamin B12, sulfonylureas, etc. all have the effect of inhibiting thyroid function and thyroid enlargement, so be careful when using this product in combination.
Specifications	5mg
Manufacturer	Jinyao Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

MAITHRI DRUGS PRIVATE LTD

United States
Active
SUZHOU RYWAY BIOTECH CO LTD

United States
Active
MACLEODS PHARMACEUTICALS LIMITED

European Union
Active

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Carbimazole22232-54-8

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Content: 99%

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