Tìm theo
Ethionamide
Các tên gọi khác (15 ) :
  • 2-Ethyl-4-thiopyridylamide
  • 2-ethylthioisonicotinamide
  • ETH
  • Ethinamide
  • Ethionamide
  • Ethionamidum
  • Ethioniamide
  • Ethylisothiamide
  • Ethyonomide
  • Etionamid
  • Etionamida
  • Etionamide
  • Etioniamid
  • ETP
  • Trecator
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 536-33-4
ATC: J04AD03
ĐG : Belgomex Sprl
CTHH: C8H10N2S
PTK: 166.243
A second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. (From Smith and Reynard, Textbook of Pharmacology, 1992, p868)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H10N2S
Phân tử khối
166.243
Monoisotopic mass
166.05646902
InChI
InChI=1S/C8H10N2S/c1-2-7-5-6(8(9)11)3-4-10-7/h3-5H,2H2,1H3,(H2,9,11)
InChI Key
InChIKey=AEOCXXJPGCBFJA-UHFFFAOYSA-N
IUPAC Name
2-ethylpyridine-4-carbothioamide
Traditional IUPAC Name
ethionamide
SMILES
CCC1=NC=CC(=C1)C(N)=S
Độ tan chảy
166
Độ hòa tan
Practically insoluble
logP
0.5
logS
-2.3
pKa (strongest acidic)
11.89
pKa (Strongest Basic)
5
PSA
38.91 Å2
Refractivity
50.19 m3·mol-1
Polarizability
17.99 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ethinamate is bacteriostatic against M. tuberculosis. In a study examining ethionamide resistance, ethionamide administered orally initially decreased the number of culturable Mycobacterium tuberculosis organisms from the lungs of H37Rv infected mice. Drug resistance developed with continued ethionamide monotherapy, but did not occur when mice received ethionamide in combination with streptomycin or isoniazid.
Cơ Chế Tác Dụng : A second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. (From Smith and Reynard, Textbook of Pharmacology, 1992, p868) Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism. Ethionamide, like prothionamide and pyrazinamide, is a nicotinic acid derivative related to isoniazid. It is thought that ethionamide undergoes intracellular modification and acts in a similar fashion to isoniazid. Isoniazid inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. Specifically isoniazid inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis, by forming a covalent adduct with the NAD cofactor. It is the INH-NAD adduct that acts as a slow, tight-binding competitive inhibitor of InhA.
Dược Động Học :
▧ Absorption :
Essentially completely absorbed following oral administration and not subjected to any appreciable first pass metabolism. Bioavailability approximately 100%.
▧ Volume of Distribution :
* 93.5 L [healthy volunteers]
▧ Protein binding :
Approximately 30% bound to proteins.
▧ Metabolism :
Hepatic and extensive. Metabolized to the active metabolite sulfoxide, and several inactive metabolites. The sulphoxide metabolite has been demonstrated to have antimicrobial activity against Mycobacterium tuberculosis.
▧ Route of Elimination :
Less than 1% of the oral dose is excreted as ethionamide in urine. Ethionamide is extensively metabolized to active and inactive metabolites.
▧ Half Life :
2 to 3 hours
Độc Tính : Symptoms of overdose include convulsions, nausea, and vomiting.
Chỉ Định : For use in the treatment of pulmonary and extrapulmonary tuberculosis when other antitubercular drugs have failed.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Sanofi
    Sản phẩm biệt dược : Ethatyl
  • Công ty : Lupin
    Sản phẩm biệt dược : Ethide
  • Công ty : Radicura
    Sản phẩm biệt dược : Ethiokox
  • Công ty : Vesalius Pharma
    Sản phẩm biệt dược : Ethomid
  • Công ty : AC Farma
    Sản phẩm biệt dược : Etionamida
  • Công ty : Macleods
    Sản phẩm biệt dược : Etomid
  • Công ty : Umeda
    Sản phẩm biệt dược : Eton
  • Công ty : Koçak
    Sản phẩm biệt dược : Etyomid
  • Công ty : Panacea
    Sản phẩm biệt dược : Myobid
  • Công ty : Wyeth
    Sản phẩm biệt dược : Trecator
  • Công ty :
    Sản phẩm biệt dược : Trecator-SC
  • Sản phẩm biệt dược : Tubermin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00609
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2761171
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506077
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07665
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00591
ChemSpider
http://www.chemspider.com/Chemical-Structure.2041901.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0008-4117-01
PharmGKB
http://www.pharmgkb.org/drug/PA164768738
Wikipedia
http://en.wikipedia.org/wiki/Ethionamide
RxList
http://www.rxlist.com/cgi/generic2/ethionamide.htm
Drugs.com
http://www.drugs.com/cdi/ethionamide.html
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