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药品详细

Besifloxacin(贝西沙星)

化学结构式图
中文名
贝西沙星
英文名
Besifloxacin
分子式
C19H21ClFN3O3
化学名
7-[(3R)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
分子量
Average: 393.84
Monoisotopic: 393.125547465
CAS号
141388-76-3
ATC分类
S01A 抗感染药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis. FDA approved on May 28, 2009.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. O’Brien TP: Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90. doi: 10.1007/s12325-012-0027-7. Epub 2012 Jun 20. Pubmed
    2. Proksch JW, Granvil CP, Siou-Mermet R, Comstock TL, Paterno MR, Ward KW: Ocular pharmacokinetics of besifloxacin following topical administration to rabbits, monkeys, and humans. J Ocul Pharmacol Ther. 2009 Aug;25(4):335-44. doi: 10.1089/jop.2008.0116. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication 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*
    Pharmacodynamics 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.
    Mechanism of action 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.
    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
    Toxicity LD50, rat: >2000 mg/kg. The most common adverse reaction reported in 2% of patients treated with besifloxacin was conjunctival redness.
    Affected organisms
    • Gram negative and gram positive bacteria
    Pathways Not Available
    理化性质
    Properties
    State liquid
    Experimental Properties
    Property Value Source
    water solubility Not soluble in water MSDS
    pKa 6.0-7.0 MSDS
    Predicted Properties
    Property Value Source
    water solubility 1.43e-01 g/l ALOGPS
    logP 0.7 ALOGPS
    logP 0.54 ChemAxon
    logS -3.4 ALOGPS
    pKa (strongest acidic) 5.64 ChemAxon
    pKa (strongest basic) 9.67 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 86.87 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 101.75 ChemAxon
    polarizability 39 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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