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药品详细

Roxithromycin(罗红霉素)

化学结构式图
中文名
罗红霉素
英文名
Roxithromycin
分子式
C41H76N2O15
化学名
(3R,4S,5S,6R,7R,9R,11S,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-3,5,7,9,11,13-hexamethyl-10-(2,4,7-trioxa-1-azaoctan-1-ylidene)-1-oxacyclotetradecan-2-one
分子量
Average: 837.0465
Monoisotopic: 836.524569772
CAS号
80214-83-1
ATC分类
J01F 未知
药物类型
small molecule
阶段
approved
商品名
ROX;Rulid;Rulide;Surlid;
同义名
基本介绍

Roxithromycin is a semi-synthetic macrolide antibiotic. It is very similar in composition, chemical structure and mechanism of action to erythromycin, azithromycin, or clarithromycin. Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. It can treat respiratory tract, urinary and soft tissue infections.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Link
    2. Gentry LO: Roxithromycin, a new macrolide antibiotic, in the treatment of infections in the lower respiratory tract: an overview. J Antimicrob Chemother. 1987 Nov;20 Suppl B:145-52. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    antibacterials 抗细菌;
    药理
    Indication Used to treat respiratory tract, urinary and soft tissue infections.
    Pharmacodynamics Roxithromycin is a semi-synthetic macrolide antibiotic. It is very similar in composition, chemical structure and mechanism of action to erythromycin, azithromycin, or clarithromycin. Roxithromycin has the following antibacterial spectrum in vitro: Streptococcus agalactiae, Streptococcus pneumoniae (Pneumococcus), Neisseria meningitides (Meningococcus), Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydia trachomatis, Ureaplasma urealyticum, Legionella pneumophila, Helicobacter (Campylobacter), Gardnerella vaginalis, Bordetella pertussis, Moraxella catarrhalis (Branhamella Catarrhalis), and Haemophilus ducreyi. Roxithromycin is highly concentrated in polymorphonuclear leukocytes and macrophages, achieving intracellular concentrations greater than those outside the cell. Roxithromycin enhances the adhesive and chemotactic functions of these cells which in the presence of infection produce phagocytosis and bacterial lysis. Roxithromycin also possesses intracellular bactericidal activity.
    Mechanism of action Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila.
    Absorption Very rapidly absorbed and diffused into most tissues and phagocytes.
    Volume of distribution Not Available
    Protein binding 96%, mainly to alpha1-acid glycoproteins
    Metabolism
    Hepatic. Roxithromycin is only partially metabolised, more than half the parent compound being excreted unchanged. Three metabolites have been identified in urine and faeces: the major metabolite is descladinose roxithromycin, with N-mono and N-di-demethyl roxithromycin as minor metabolites. The respective percentage of roxithromycin and these three metabolites is similar in urine and faeces.

    Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

    Substrate Enzymes Product
    Roxithromycin
      		descladinose roxithromycin Details
      Roxithromycin
        		N-di-demethyl roxithromycin Details
        Roxithromycin
          		N-mono roxithromycin Details
          Route of elimination Not Available
          Half life 12 hours
          Clearance Not Available
          Toxicity Most common side-effects are gastrointestinal; diarrhoea, nausea, abdominal pain and vomiting. Less common side-effects include headaches, rashes, abnormal liver function values and alteration in senses of smell and taste.
          Affected organisms
          • Enteric bacteria and other eubacteria
          Pathways
          Pathway Name SMPDB ID
          Smp00251 Roxithromycin Pathway SMP00251
          理化性质
          Properties
          State solid
          Experimental Properties
          Property Value Source
          water solubility 0.0189 mg/L at 25 °C (SRC PhysProp estimated -- MEYLAN,WM et al. (1996)) Not Available
          logP 1.7 Not Available
          Predicted Properties
          Property Value Source
          water solubility 1.87e-01 g/l ALOGPS
          logP 2.9 ALOGPS
          logP 3 ChemAxon
          logS -3.6 ALOGPS
          pKa (strongest acidic) 12.45 ChemAxon
          pKa (strongest basic) 9.08 ChemAxon
          physiological charge 1 ChemAxon
          hydrogen acceptor count 16 ChemAxon
          hydrogen donor count 5 ChemAxon
          polar surface area 216.89 ChemAxon
          rotatable bond count 13 ChemAxon
          refractivity 211.24 ChemAxon
          polarizability 91.84 ChemAxon
          药物相互作用
          Drug Interaction
          Cyclosporine The macrolide, roxithromycin, may increase the effect of cyclosporine.
          食物相互作用
          Not Available

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