Tìm theo
Ethambutol
Các tên gọi khác (12 ) :
  • (+)-2,2'-(ethylenediimino)di-1-butanol
  • (+)-ethambutol
  • (+)-N,N'-bis(1-(hydroxymethyl)propyl)ethylenediamine
  • (+)-S,S-ethambutol
  • (2S,7S)-2,7-Diethyl-3,6-diazaoctane-1,8-diol
  • (S,S)-Ethambutol
  • EMB
  • Etambutol
  • Etambutolo
  • Ethambutol
  • Ethambutolum
  • S,S-Ethambutol
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 74-55-5
ATC: J04AK02
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C10H24N2O2
PTK: 204.3098
An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H24N2O2
Phân tử khối
204.3098
Monoisotopic mass
204.183778022
InChI
InChI=1S/C10H24N2O2/c1-3-9(7-13)11-5-6-12-10(4-2)8-14/h9-14H,3-8H2,1-2H3/t9-,10-/m0/s1
InChI Key
InChIKey=AEUTYOVWOVBAKS-UWVGGRQHSA-N
IUPAC Name
(2S)-2-[(2-{[(2S)-1-hydroxybutan-2-yl]amino}ethyl)amino]butan-1-ol
Traditional IUPAC Name
ethambutol
SMILES
CC[C@@H](CO)NCCN[C@@H](CC)CO
Độ tan chảy
171.5-174.5
Độ hòa tan
7.58e+00 g/l
logP
-0.3
logS
-1.4
pKa (strongest acidic)
14.82
pKa (Strongest Basic)
9.55
PSA
64.52 Å2
Refractivity
57.89 m3·mol-1
Polarizability
24.47 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
4
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
0
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ethambutol is an oral chemotherapeutic agent which is specifically effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Ethambutol inhibits RNA synthesis and decreases tubercle bacilli replication. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of MAC are sensitive to ethambutol.
Cơ Chế Tác Dụng : An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863) Ethambutol inhibits arabinosyl transferases which is involved in cell wall biosynthesis. By inhibiting this enzyme, the bacterial cell wall complex production is inhibited. This leads to an increase in cell wall permeability.
Dược Động Học :
▧ Absorption :
About 75% to 80% of an orally administered dose of ethambutol is absorbed from the gastrointestinal tract.
▧ Protein binding :
20-30%
▧ Metabolism :
Hepatic. Up to 15% of administered drug is metabolized to inactive metabolites. The main path of metabolism appears to be an initial oxidation of the alcohol to an aldehydic intermediate, followed by conversion to a dicarboxylic acid.
▧ Route of Elimination :
During the 24-hour period following oral administration of ethambutol hydrochloride approximately 50 percent of the initial dose is excreted unchanged in the urine, while an additional 8 to 15 percent appears in the form of metabolites. From 20 to 22 percent of the initial dose is excreted in the feces as unchanged drug.
▧ Half Life :
In patients with normal renal function, 3 to 4 hours. In patients with impaired renal function, up to 8 hours.
Độc Tính : The most commonly recognized toxic effect of ethambutol is optic neuropathy, which generally is considered uncommon and reversible in medical literature. Other side effects that have been observed are pruritus, joint pain, gastrointestinal upset, abdominal pain, malaise, headache, dizziness, mental confusion, disorientation, and possible hallucinations.
Chỉ Định : For use, as an adjunct, in the treatment of pulmonary tuberculosis.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Etibi
  • Công ty : Wyeth
    Sản phẩm biệt dược : Myambutol
  • Công ty : Refasa
    Sản phẩm biệt dược : Tibutol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00330
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06984
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50204422
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0923-02
PharmGKB
http://www.pharmgkb.org/drug/PA164784021
Wikipedia
http://en.wikipedia.org/wiki/Ethambutol
RxList
http://www.rxlist.com/cgi/generic2/ethambutol.htm
Drugs.com
http://www.drugs.com/cdi/ethambutol.html
... loading
... loading