Tìm theo
Besifloxacin
Các tên gọi khác (2) :
  • Besifloxacin
  • SS734
quinolones, antibiotics
Thuốc Gốc
Small Molecule
CAS: 141388-76-3
ATC: S01AE08
CTHH: C19H21ClFN3O3
PTK: 393.84
Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis. FDA approved on May 28, 2009.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H21ClFN3O3
Phân tử khối
393.84
Monoisotopic mass
393.125547465
InChI
InChI=1S/C19H21ClFN3O3/c20-15-16-12(18(25)13(19(26)27)9-24(16)11-4-5-11)7-14(21)17(15)23-6-2-1-3-10(22)8-23/h7,9-11H,1-6,8,22H2,(H,26,27)/t10-/m1/s1
InChI Key
InChIKey=QFFGVLORLPOAEC-SNVBAGLBSA-N
IUPAC Name
7-[(3R)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Traditional IUPAC Name
7-[(3R)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid
SMILES
N[C@@H]1CCCCN(C1)C1=C(F)C=C2C(=O)C(=CN(C3CC3)C2=C1Cl)C(O)=O
Độ hòa tan
Not soluble in water
logP
0.54
logS
-3.4
pKa (strongest acidic)
5.64
pKa (Strongest Basic)
9.67
PSA
86.87 Å2
Refractivity
101.75 m3·mol-1
Polarizability
39 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
6.0-7.0
Dược Lực Học : Besifloxacin tear concentrations were higher than MIC90 (minimum inhibitory concentration) values for common bacterial pathogens and sustained for 24 hours or longer. Mean residence time in the conjunctiva was 4.7 hours.
Cơ Chế Tác Dụng : Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis. FDA approved on May 28, 2009. Besifloxacin is a bactericidal fluroquinolone-type antibiotic that inhibits bacterial enzymes, DNA gyrase and topoisomerase IV. By inhibiting DNA gyrase, DNA replication, transcription, and repair is impaired. By inhibiting topoisomerase IV, decatenation during cell devision is impaired. Inhibiting these two targets also slows down development of resistance.
Dược Động Học :
▧ Absorption :
Although ocular surface concentrations are high, average systemic concentrtions after three-times daily dosing was less than 0.5 ng/mL. This indicates that besifloxacin is not appreciably absorbed into the systemic and has a very low risk of systemic side effects.
▧ Volume of Distribution :
Not absorbed into the systemic
▧ Protein binding :
None
▧ Metabolism :
No appreciable metabolism
▧ Route of Elimination :
N/A
▧ Half Life :
The average elimination half-life of besifloxacin in plasma following multiple dosing was estimated to be 7 hours.
▧ Clearance :
N/A
Độc Tính : LD50, rat: >2000 mg/kg. The most common adverse reaction reported in 2% of patients treated with besifloxacin was conjunctival redness.
Chỉ Định : Treatment of bacterial conjunctivitis. Bacterial isolates that are susceptible to besifloxacin include: CDC coryneform group G; Corynebacterium pseudodiphtheriticum; Corynebacterium striatum; Haemophilus influenzae; Moraxella lacunata; Staphylococcus aureus; Staphylococcus epidermidis; Staphylococcus hominis; Staphylococcus lugdunensis; Streptococcus mitis group; Streptococcus oralis; Streptococcus pneumoniae; Streptococcus salivarius*
Liều Lượng & Cách Dùng : Suspension / drops - Ophthalmic - 0.6%
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06771
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08872
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-6282-0
Wikipedia
http://en.wikipedia.org/wiki/Besifloxacin
RxList
http://www.rxlist.com/besivance-drug.htm
Drugs.com
http://www.drugs.com/besivance.html
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