Tìm theo
Pefloxacin
Các tên gọi khác (6 ) :
  • Labocton
  • Pefloxacin
  • Pefloxacine
  • Pefloxacino
  • Pefloxacinum
  • PFLX
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 70458-92-3
ATC: J01MA03
CTHH: C17H20FN3O3
PTK: 333.3574
A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H20FN3O3
Phân tử khối
333.3574
Monoisotopic mass
333.148869726
InChI
InChI=1S/C17H20FN3O3/c1-3-20-10-12(17(23)24)16(22)11-8-13(18)15(9-14(11)20)21-6-4-19(2)5-7-21/h8-10H,3-7H2,1-2H3,(H,23,24)
InChI Key
InChIKey=FHFYDNQZQSQIAI-UHFFFAOYSA-N
IUPAC Name
1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Traditional IUPAC Name
pefloxacin
SMILES
CCN1C=C(C(O)=O)C(=O)C2=CC(F)=C(C=C12)N1CCN(C)CC1
Độ tan chảy
271 dec °C
Độ hòa tan
11.4 mg/mL at 25 °C
logP
0.27
logS
-2.4
pKa (strongest acidic)
5.66
pKa (Strongest Basic)
6.47
PSA
64.09 Å2
Refractivity
90.77 m3·mol-1
Polarizability
34.42 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pefloxacin is a fluoroquinolone antibiotic. Flouroquinolones such as pefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.
Cơ Chế Tác Dụng : A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria. [PubChem] The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Dược Động Học :
▧ Absorption :
Well absorbed by the oral route.
▧ Protein binding :
20-30%
▧ Metabolism :
Hepatic. Primary metabolites are pefloxacin N-oxide and norfloxacin.
▧ Half Life :
8.6 hours
Độc Tính : Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.
Chỉ Định : For the treatment of uncomplicated gonococcal urethritis in males and for gram-negative-bacterial infections in the gastrointestinal system and the genitourinary tract.
Tương Tác Thuốc :
  • Aminophylline Pefloxacin may increase the effect of aminophylline.
  • Calcium Formation of non-absorbable complexes
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
  • Oxtriphylline Pefloxacin may increase the effect of oxtriphylline.
  • Theophylline Pefloxacin may increase the effect of theophylline.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Labocton
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00487
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=51081
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507338
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02306
ChemSpider
http://www.chemspider.com/Chemical-Structure.46291.html
PharmGKB
http://www.pharmgkb.org/drug/PA164742856
Wikipedia
http://en.wikipedia.org/wiki/Pefloxacin
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