Tìm theo
Diloxanide
Các tên gọi khác (1) :
  • Diloxanide furoate
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 3736-81-0
ATC: P01AC01
CTHH: C14H11Cl2NO4
PTK: 328.147
Diloxanide furoate is an anti-protozoal drug used in the treatment of Entamoeba histolytica and some other protozoal infections. Although it is not currently approved for use in the United States, it was approved by a CDC study in the treatment of 4,371 cases of Entamoeba histolytica from 1977 to 1990.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H11Cl2NO4
Phân tử khối
328.147
Monoisotopic mass
327.006513259
InChI
InChI=1S/C14H11Cl2NO4/c1-17(13(18)12(15)16)9-4-6-10(7-5-9)21-14(19)11-3-2-8-20-11/h2-8,12H,1H3
InChI Key
InChIKey=BDYYDXJSHYEDGB-UHFFFAOYSA-N
IUPAC Name
4-(2,2-dichloro-N-methylacetamido)phenyl furan-2-carboxylate
Traditional IUPAC Name
diloxanide furoate
SMILES
CN(C(=O)C(Cl)Cl)C1=CC=C(OC(=O)C2=CC=CO2)C=C1
Độ hòa tan
3.82e-02 g/l
logP
2.24
logS
-3.9
pKa (strongest acidic)
13.09
pKa (Strongest Basic)
-4.7
PSA
59.75 Å2
Refractivity
78.21 m3·mol-1
Polarizability
30.28 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Diloxanide is a luminal amebicide, however the mechanism of action of diloxanide is unknown. Diloxanide destroys the trophozoites of E. histolytica that eventually form into cysts. The cysts are then excreted by persons infected with asymptomatic amebiasis. Diloxanide furoate is a prodrug, and is hydrolyzed in the gastrointestinal tract to produce diloxanide, the active ingredient.
Cơ Chế Tác Dụng : Diloxanide furoate is an anti-protozoal drug used in the treatment of Entamoeba histolytica and some other protozoal infections. Although it is not currently approved for use in the United States, it was approved by a CDC study in the treatment of 4,371 cases of Entamoeba histolytica from 1977 to 1990. Unknown. Diloxanide may inhibit protein synthesis.
Dược Động Học :
▧ Absorption :
Bioavailability is 90% (in diloxanide parental form), however diloxanide furoate is slowly absorbed from the gastrointestinal tract.
▧ Metabolism :
Hydrolyzed to furoic acid and diloxanide, which undergoes extensive glucuronidation (99% of diloxanide occurs as glucuronide and 1% as free diloxanide in the systemic circulation).
▧ Route of Elimination :
Renal (90%, rapidly excreted as glucuronide metabolite). 10% is excreted in the feces as diloxanide.
▧ Half Life :
3 hours
Chỉ Định : Diloxanide is used alone as a primary agent in the treatment of asymptomatic (cyst passers) intestinal amebiasis caused by Entamoeba histolytica. Diloxanide may also be used concurrently, or sequentially, with other agents such as the nitroimidazoles (eg. metronidazole) in the treatment of invasive or extraintestinal forms of amebiasis.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08792
ChemSpider
http://www.chemspider.com/Chemical-Structure.18400.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958413
Wikipedia
http://en.wikipedia.org/wiki/Diloxanide_furoate
Drugs.com
http://www.drugs.com/mmx/diloxanide-furoate.html
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