Tìm theo
Tinidazole
Các tên gọi khác (1) :
  • Timidazole
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 19387-91-8
ATC: J01XD02, P01AB02
ĐG : Apotheca Inc.
CTHH: C8H13N3O4S
PTK: 247.272
A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H13N3O4S
Phân tử khối
247.272
Monoisotopic mass
247.062676609
InChI
InChI=1S/C8H13N3O4S/c1-3-16(14,15)5-4-10-7(2)9-6-8(10)11(12)13/h6H,3-5H2,1-2H3
InChI Key
InChIKey=HJLSLZFTEKNLFI-UHFFFAOYSA-N
IUPAC Name
1-[2-(ethanesulfonyl)ethyl]-2-methyl-5-nitro-1H-imidazole
Traditional IUPAC Name
tinidazole
SMILES
CCS(=O)(=O)CCN1C(C)=NC=C1[N+]([O-])=O
Độ tan chảy
127-128 °C
Độ hòa tan
1.99E+004 mg/L
logP
-0.35
logS
-1.9
pKa (Strongest Basic)
3.1
PSA
97.78 Å2
Refractivity
57.66 m3·mol-1
Polarizability
23.27 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
5
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Tinidazole is a synthetic antiprotozoal agent. Tinidazole demonstrates activity both in vitro and in clinical infections against the following protozoa: Trichomonas vaginalis, Giardia duodenalis (also termed G. lamblia), and Entamoeba histolytica. Tinidazole does not appear to have activity against most strains of vaginal lactobacilli.
Cơ Chế Tác Dụng : A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections. [PubChem] Tinidazole is a prodrug and antiprotozoal agent. The nitro group of tinidazole is reduced in Trichomonas by a ferredoxin-mediated electron transport system. The free nitro radical generated as a result of this reduction is believed to be responsible for the antiprotozoal activity. It is suggested that the toxic free radicals covalently bind to DNA, causing DNA damage and leading to cell death. The mechanism by which tinidazole exhibits activity against Giardia and Entamoeba species is not known, though it is probably similar.
Dược Động Học :
▧ Absorption :
Rapidly and completely absorbed under fasting conditions. Administration with food results in a delay in Tmax of approximately 2 hours and a decline in Cmax of approximately 10% and an AUC of 901.6 ± 126.5 mcg hr/mL.
▧ Volume of Distribution :
* 50 L
▧ Protein binding :
Plasma protein binding of tinidazole is 12%.
▧ Metabolism :
Hepatic, mainly via CYP3A4. Tinidazole, like metronidazole, is significantly metabolized in humans prior to excretion. Tinidazole is partly metabolized by oxidation, hydroxylation and conjugation. Tinidazole is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.
▧ Route of Elimination :
Tinidazole crosses the placental barrier and is secreted in breast milk. Tinidazole is excreted by the liver and the kidneys. Tinidazole is excreted in the urine mainly as unchanged drug (approximately 20-25% of the administered dose). Approximately 12% of the drug is excreted in the feces.
▧ Half Life :
Elimination half-life is 13.2 ± 1.4 hours. Plasma half-life is 12 to 14 hours.
Độc Tính : There are no reported overdoses with tinidazole in humans. In acute studies with mice and rats, the LD 50 for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration. In rats, the LD 50 was > 2,000 mg/kg for both oral and intraperitoneal administration.
Chỉ Định : For the treatment of trichomoniasis caused by T. vaginalis in both female and male patients. Also for the treatment of giardiasis caused by G. duodenalis in both adults and pediatric patients older than three years of age and for the treatment of intestinal amebiasis and amebic liver abscess caused by E. histolytica in both adults and pediatric patients older than three years of age.
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Fasigyn
  • Công ty :
    Sản phẩm biệt dược : Tindamax
  • Công ty :
    Sản phẩm biệt dược : Tindazole
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00911
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5479
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506396
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01426
ChemSpider
http://www.chemspider.com/Chemical-Structure.5279.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0178-8250-40
PharmGKB
http://www.pharmgkb.org/drug/PA10813
Wikipedia
http://en.wikipedia.org/wiki/Tinidazole
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tin1701.shtml
Drugs.com
http://www.drugs.com/cdi/tinidazole.html
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