Methimazole

Các tên gọi khác (14 ) :

1-METHYL-1,3-dihydro-2H-imidazole-2-thione
1-Methylimidazole-2(3H)-thione
Danantizol
Favistan
Mercazolyl
Methimazole
Strumazol
Tapazole
Thacapzol
Thiamazol
Thiamazole
Thiamazolum
Tiamazol
USAF el-30

antithyroid agents

Thuốc Gốc

Small Molecule

CAS: 60-56-0

ATC: H03BB02

ĐG : AAIPharma Inc. , http://www.aaipharma.com

CTHH: C₄H₆N₂S

PTK: 114.169

A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. [PubChem]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₄H₆N₂S

Phân tử khối

114.169

Monoisotopic mass

114.025168892

InChI

InChI=1S/C4H6N2S/c1-6-3-2-5-4(6)7/h2-3H,1H3,(H,5,7)

InChI Key

InChIKey=PMRYVIKBURPHAH-UHFFFAOYSA-N

IUPAC Name

1-methyl-2,3-dihydro-1H-imidazole-2-thione

Traditional IUPAC Name

methimazole

SMILES

CN1C=CNC1=S

Độ tan chảy

146 °C

Độ sôi

280 °C

Độ hòa tan

275 g/L

logP

-0.34

logS

-1

pKa (strongest acidic)

10.41

pKa (Strongest Basic)

-3

PSA

15.27 Å²

Refractivity

33.23 m³·mol^-1

Polarizability

11.64 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Dược Lực Học : Used in the treatment of hyperthyroidism or an overactive thyroid gland, methimazole inhibits the synthesis of thyroid hormones and thus is effective in the treatment of hyperthyroidism. It may also be used to ameliorate hyperthyroidism in preparation for subtotal thyroidectomy or radioactive iodine therapy.

Cơ Chế Tác Dụng : A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. [PubChem] Methimazole binds to thyroid peroxidase and thereby inhibits the conversion of iodide to iodine. Thyroid peroxidase normally converts iodide to iodine (via hydrogen peroxide as a cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3 and/or 5 positions of the phenol rings of tyrosines found in thyroglobulin. Thyroglobulin is degraded to produce thyroxine (T4) and tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland. So methimazole effectively inhibits the production of new thyroid hormones.

Dược Động Học :

▧ Absorption :
Rapid with an oral bioavailability of 93%.
▧ Protein binding :
None or minimal
▧ Metabolism :
Primarily hepatic. Metabolized rapidly, requiring frequent administration.
▧ Route of Elimination :
Methimazole is excreted in the urine.
▧ Half Life :
5-6 hours

Độc Tính : Oral LD₅₀ in rats is 2250 mg/kg. Symptoms of overdose include nausea, vomiting, epigastric distress, headache, fever, joint pain, pruritus, and edema. Aplastic anemia (pancy-topenia) or agranulocytosis may be manifested in hours to days. Less frequent events are hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathies, and CNS stimulation or depression.

Chỉ Định : For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis.

Tương Tác Thuốc :

Acenocoumarol The antithyroid agent, methimazole, may decrease the anticoagulant effect of acenocoumarol.
Anisindione The antithyroid agent, methimazole, may decrease the anticoagulant effect of anisindione.
Dicoumarol The antithyroid agent, methimazole, may decrease the anticoagulant effect of dicumarol.
Digoxin The antithyroid agent increases the effect of digoxin
Tamoxifen Methimazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
Tamsulosin Methimazole, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Methimazole is initiated, discontinued, or dose changed.
Warfarin Methimazole may decrease the anticoagulant effect of warfarin. Monitor for changes in the therapeutic and adverse effects of warfarin if methimazole is initiated, discontinued or dose changed.

Liều Lượng & Cách Dùng : Tablet - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Tapazole 10 mg tablet

Giá bán buôn : USD >1.45

Đơn vị tính : tablet
Biệt dược thương mại : Methimazole 20 mg tablet

Giá bán buôn : USD >1.9

Đơn vị tính : tablet
Biệt dược thương mại : Methimazole powder

Giá bán buôn : USD >9.49

Đơn vị tính : g
Biệt dược thương mại : Northyx 5 mg tablet

Giá bán buôn : USD >0.29

Đơn vị tính : tablet
Biệt dược thương mại : Methimazole 5 mg tablet

Giá bán buôn : USD >0.45

Đơn vị tính : tablet
Biệt dược thương mại : Northyx 10 mg tablet

Giá bán buôn : USD >0.47

Đơn vị tính : tablet
Biệt dược thương mại : Tapazole 5 mg tablet

Giá bán buôn : USD >0.66

Đơn vị tính : tablet
Biệt dược thương mại : Methimazole 10 mg tablet

Giá bán buôn : USD >0.78

Đơn vị tính : tablet
Biệt dược thương mại : Northyx 15 mg tablet

Giá bán buôn : USD >0.82

Đơn vị tính : tablet
Biệt dược thương mại : Northyx 20 mg tablet

Giá bán buôn : USD >0.94

Đơn vị tính : tablet

Nhà Sản Xuất

Công ty : Gador S.A.

Sản phẩm biệt dược : Danantizol
Công ty : Temmler

Sản phẩm biệt dược : Favistan
Công ty : ICN

Sản phẩm biệt dược : Metizol
Công ty : Organon

Sản phẩm biệt dược : Strumazol
Công ty :

Sản phẩm biệt dược : Strumazole
Công ty : Paladin

Sản phẩm biệt dược : Tapazole
Công ty : Recip

Sản phẩm biệt dược : Thacapzol
Công ty : Sandoz

Sản phẩm biệt dược : Thycapzol
Công ty : Merck

Sản phẩm biệt dược : Thyrozol
Công ty : Merck

Sản phẩm biệt dược : Tirozol

Đóng gói

Công ty : AAIPharma Inc.

Website : http://www.aaipharma.com
Công ty : Actavis Group

Website : http://www.actavis.com
Công ty : Amerisource Health Services Corp.

Website : http://www.amerisourcebergen.com
Công ty : Caraco Pharmaceutical Labs

Website : http://www.caraco.com
Công ty : Cedar Pharmaceuticals LLC

Website : http://www.cedarpharma.com
Công ty : Centrix Pharmaceuticals

Website : http://www.cenrx.com
Công ty : Dispensing Solutions

Website : http://www.drxdispensing.com
Công ty : Eon Labs
Công ty : Heartland Repack Services LLC
Công ty : Kaiser Foundation Hospital
Công ty : King Pharmaceuticals Inc.

Website : http://www.kingpharm.com
Công ty : Medisca Inc.

Website : http://www.medisca.com
Công ty : Mikart Inc.

Website : http://www.mikart.com
Công ty : Murfreesboro Pharmaceutical Nursing Supply

Website : http://www.unitdosesupply.com
Công ty : Mylan

Website : http://www.mylan.com
Công ty : Nucare Pharmaceuticals Inc.

Website : http://www.nucarerx.com
Công ty : Par Pharmaceuticals

Website : http://www.parpharm.com
Công ty : Philopharm GmbH
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com
Công ty : Remedy Repack

Website : http://www.remedyrepack.com
Công ty : Resource Optimization and Innovation LLC
Công ty : Southwood Pharmaceuticals

Website : http://www.southwoodhealthcare.com
Công ty : United Research Laboratories Inc.

Website : http://www.urlpharma.com
Công ty : Vangard Labs Inc.

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00763

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=1349907

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506536

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00401

ChemSpider

http://www.chemspider.com/Chemical-Structure.1131173.html

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0677-1945-01

PharmGKB

http://www.pharmgkb.org/drug/PA450422

Wikipedia

http://en.wikipedia.org/wiki/Methimazole

RxList

http://www.rxlist.com/cgi/generic3/methim.htm

Drugs.com

http://www.drugs.com/cdi/methimazole.html

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