日本化学療法学会雑誌第51巻第5号
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- ただきよ ひきぎ
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1 Telithromycin 2 3! telithromycin 8 Key words: telithromycin telithromycintel TEL cethromycinabt pikromycin 955 narbomycin 952 erythromycinem EM FigEM EM EM clarithromycincamroxithromycinrxm azithromycinazm Fig. Chemical structures of erythromycin and ketolide. 5
2 PRSPpenicillin resistant Streptococcus pneumoniae ERSPerythromycin resistant S. pneumoniae TEL Fig2 TEL I 3 7 Fig3 Fig2. Chemical structure of telithromycin. Totsuka K.: Medical Practice8(8): 2, 200 Fig3. Mechanism of action antibacterial drugs.
3 70 S 30 S 50 S RNArRNA30 S 6S rrna 2 50 S 5S rrna 23 S rrna 3 RNAmRNA Fig 70 S 30 S mrna fmet trna RNAtRNA 30 S 50 S 70 S 50 S S 2 50 S trna 2 A P 2 3 A trna P trna A trna A P trna 3 trnamrna 70 S ChloramphenicolCP A 3 lincomycinlcm B 35 LCM B 50 S 23 S rrna V 2058 A S rrna V 2058 Fig. Sites action of protein synthesis inhibitors.
4 VOL.5 NO.5 新規ケトライド系抗菌薬の細菌学的検討 28 差耐性を示すことから 化学構造が異なるものの その 用いた rrna の修飾に対する各薬剤の影響を調べた結 結合部位は非常に近いと推定されている 果 TEL は 23 S rrna ド メ イ ン V の 2058 位 お よ び 一方 ケトライド系抗菌薬は マクロライド LCM 2059 位アデニン残基に加えて ドメインⅡの 752 位ア ストレプトグラミン B 系抗菌薬の結合部位に加えて デニン残基の DMS による修飾を抑制した 一方 対照 さらに 23S rrna のドメインⅡに対しても結合親和 の EM は 2058 位および 2059 位アデニン残基の修飾は 性を示すことが footprinting 実験により証明されてい 抑制したが 752 位アデニン残基の修飾はむしろ増強し る 6 8 Fig 5 また 最近その三次元構造が 結晶 解析の結果から明らかにされた3 5 Figs 6 7 Footprinting 実験において 硫酸ジメチル DMS を た また TEL の化学構造からラクトン環の 位にお ける延長構造を除いた RU は 752 位アデニン残 基に対して抑制作用を示さなかった これに対して糖鎖 Hansen L.H. et al.: Mol Microbiol 3: , 999 Fig 5. Binding sites of ketolides and macrolides on the 23 S rrna of the bacterial ribosome. Schluzen F. et al.: Nature 3: 8 82, 200 Fig 6. Binding sites of macrolides. Poehlsgaard J. & Douthwaite S.: Curr Drug Targets Infect Disorders 2: 67 78, 2002 Fig 7. Binding sites of ketolides.
5 RU TEL 752 Table Fig TEL KD EMKD TEL 752 Table 2 TEL 9 II S. pneumoniae Haemophilus influenzae Moraxella catarrhalis Staphylococcus aureus TEL Fig8. Chemical structure of erythromycin and telithromycin and their derivatives. Table Effect on modification of ribosomal RNA by dimethyl sulfate No drug Erythromycin HMR 300 Telithromycin RU RU A 752 A 2058 A 2059 A 2062 G ND Drugs at saturating concentrations00 µmtommwere bound to wild type ribosomes at 00 nm in experiments. Only the positions at which binding of the drugs alters base reactivities are shown here. Each data is based on three to eight independent experiments. Standard deviations are shown in parenthese. ND: not determined. Hansen L H, et al.: Mol Microbiol 3: 62363, 999
6 Drugs Table 2 Dissociation constants for wild type and mutant Escherichia coli ribosomes KdM wild type ratio A 2058G ratio Erythromycin HMR 300 Telithromycin RU RU Values are derived from measurements of antibiotic protection of nucleotides A 2058 and A 2059 based on chemical modification by dimethyl sulfate. RatioKd values relative to erythromycin s. Kd :Kdissociation. Douthwaite S, et al.: Mol Microbiol 36: 8393, 2000 Fig9. Antibacterial spectrum against clinical isolatesmic90 Mycoplasma pneumoniae, Chlamydia pneumoniae Legionella pneumophila 2027 Fig9 TEL III 990 penicillin GPCGEM CP 999 Prospective Resistant Organism Tracking and Epidemiology for the Ketolide TelithromycinPROTEKT Fig 0
7 Felmingham D. et al.: JAC50(S): 25 37, 2002 Fig0. Rates of resistance of Streptococcus pneumoniae to penicillin and macrolide..3.3 PROTEKT TEL MIC mlmic ml TEL NCCLS S: MIC ml 99.9 Table 3 TEL levofloxacinlvfx respiratory quinolone moxifloxacin TEL PRSP ERSP 2003 FDA advisory committee PRSPERSP : 627 Table 29 TEL MIC mlmic ml Table 3 Antibacterial activity against clinical isolates Streptococcus pneumoniae in 25 countries worldwide from 999 to 2000 Drugs MIC50µgmL MIC90µgmL S Penicillin G Cefpodoxime Cefuroxime Erythromycin Clarithromycin Azithromycin Levofloxacin Moxifloxacin Telithromycin RTI strains in 25countries S :Percent of sensitive strains, NCCLS breakpoints for telithromycintentative NCCLS susceptibility breakpoint S is MIC µgml Felmingham D, et al.: JAC 50(S): 2537, 2002 Table Antibacterial activity against clinical isolates of Streptococcus pneumoniae in Japan from 2000 to 200 Drugs MIC50µgmL MIC90µgmL S Penicillin G Cefaclor Cefuroxime Cefpodoxime Erythromycin Azithromycin Clarithromycin Levofloxacin Moxifloxacin Gatifloxacin Telithromycin S :SeeTable3 627 RTI strains in 2 centers Iinuma Y, Inoue M, Farrell D: ICAAC, 2002
8 TEL NCCLS S: MIC ml 00 PCGcefaclor CCLcefuroximeCXMcefpodoximeCPDX MIC90 28 ml NCCLS EMAZMCAM MIC ml NCCLS LVFXmoxifloxacingatifloxacin MIC ml NCCLS TEL MIC90 TEL TEL LVFX III 30 3 TEL ermb MIC mlmic ml 3 mefa efflux ermb mefa TEL MIC90: ml EMCAMAZM ermb ermb mefa MIC90: 326 mlmefa EMCAM AZM MIC90 6 ml Table 5 PROTEKT LVFX: MIC8 ml35 TEL MIC mlmic ml LVFXmoxifloxacinciprofloxacin MIC90 66 ml EMCAMAZM MIC ml MIC90 PCG: mlccl: 28 mlcpdx: 8 mlcxm: 6 ml Table 6 5 ermb TEL L RU 6987Fig8 EM spiramycin 32 TEL TEL Table 6 Antibacterial activity against quinolone resistant Streptococcus pneumoniae isolated worldwide from 999 to 2000 Drugs MIC50µgmL MIC90µgmL Range Penicillin G Cefaclor Cefpodoxime Cefuroxime Erythromycin Clarithromycin Azithromycin Levofloxacin Moxifloxacin Ciprofloxacin Telithromycin RTI strains PROTEKT, Table 5 Antibacterial activity against macrolide resistant Streptococcus pneumoniae isolated worldwide from 999 to 2000 Mechanism of resistance MIC 5090µgmL EM CAM AZM TEL ermbn mefan368 6 Bothn EM: erythromycin, CAM: clarithromycin, AZM: azithromycin, TEL: telithromycin Farrell D L, et al.: JAC 50(S ): 397, 2002 Fig. Clarebout G, Huet C, Leclercq R: ICAAC, 2000 Lack of induction of resistance to telithromycin.
9 BMLSB FigRU 6987 EM erm B ermb TEL TEL MIC8 ml TEL ermb TEL mefa TEL TEL V TEL ermb S. aureus ermb ermb 33 V 2058 TEL 3 TEL IV Table 7 Table 7 Differences between macrolides and ketolides Properties Mechanism of action Inhibition of protein synthesis Interaction with domain Interaction with domain Induction of MLSB resistance Pneumococci Activity against macrolide resistant isolates Activity against lactam resistant isolates Activity against FQ resistant isolates Macrolides Ketolides Andrews J MWeller T MAshby J Pet al.: The in vitro activity of ABT 773a new ketolide antimicrobial agent. J Antimicrob Chemother 6: Bryskir A: Novelties in the field of anti infective compounds in 999. Clin Infect Dis 3: Champney W STober C L: Structure activity relationships for six ketolide antibiotics. Curr Microbiol 2: Brockmann HHenkel W: Pikromycinein bitter schmeckendes antibioticum aus Actinomyceten. Chem Ber 8: Allen N E: Macrolide resistance in Staphylococcus aureus : Inducers of macrolide resistance. Antimicrob Agents Chemother : Pestka SVince RLeMahier Ret al.: Induction of erythromycin resistance in Staphylococcus aureus by erythromycin derivatives. Antimicrob Agents Chemother 9: : Medical Practice 8: Shinabarger D LMarotti K RMurray R Wet al.: Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother : Lin A HMurray R WVidmar T Jet al.: The oxazolidinone eperezolid binds to the 50 S ribosomal subunit and competes with the binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother : Swaney S MAoki HGonoza M Cet al.: The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria. Antimicrob Agents Chemother 2: Brodersen D EClemons J W MCarter A Pet al.: The structural basis for the action of the antibiotics tetracyclinepactamycinand hygromycin B on the 30 S ribosomal subunit. Cell 03: Recht M IPuglisi J D: Aminoglycoside resistance with homogeneous and heterogeneous populations
10 of antibiotic resistant ribosomes. Antimicrob Agents Chemother 5: Schlunzen FZarivach RHarms Jet al.: Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria. Nature 3: Porse B TGarrett R A: Sites of interaction of streptogramin A and B antibiotics in the peptidyl transferase loop of 23 S rrna and the synergism of their inhibitory mechanisms. J Mol Biol 286: Poehlsgaard JDouthwaite S: The macrolide binding site on the bacterial ribosome. Current Drug Targets Infectious Disorders 2: Xiong LShah SMauvais Pet al.: A ketolide resistance mutation in domain II of 23 S rrna reveals the proximity of hairpin 35 to the peptidyl transferase centre. Mol Microbiol 3: Hansen L HMauvais PDouthwaite S: The macrolide ketolide antibiotic binding site is formed by structures in domains II and V of 23 S ribosomal RNA. Mol Microbiol 3: Douthwaite SHansen L HMauvais P: Macrolide ketolide inhibition of MLS resistant ribosomes is improved by alternative drug interaction with domain II of 23 S rrna. Mol Microbiol 36: : telithromycin in press 20 : Telithromycin in press 2 : Telithromycin in press 22 : Telithromycin in press 23 :Telithromycin Legionella in vitro in press 2 : Telithromycin in vitro in vivo in press 25 Ubukata KIwata SSunakawa K: In vitro activities of new ketolidetelithromycin and eight other macrolide antibiotics against Streptococcus pneumoniae having ermam and mefe genes that mediate macrolide resistances. J Infect Chemother. in press 26 Yamaguchi THirakata YIzumikawa Ket al.: In vitro activity of telithromycinhmr 367a new ketolideagainst clinical isolates of Mycoplasma pneumoniae in Japan. Antimicrob Agents Chemother : Miyashita NFukano HNiki Yet al: In vitro activity of telithromycina newketolideagainst Chlamydia pneumoniaej. Antimicrob. Chemother 8: Felmingham DReinert R RHirakata Yet al.: Increasing prevalence of antimicrobial resistance among isolates of Streptococcus pneumoniae from the PROTEKT surveillance studyand comparative in vitro activity of the ketolidetelithromycin. J Antimicrob Chemother 50 Sup. : Iinuma YInoue MFarrell D: Longitudinal surveillance of antibiotic resistance among clinical isolates of community acquired respiratory tract pathogens collected in Japan during the winters of and In program and abstracts of the 2 nd Interscience Conference on Antimicrobial Agents and ChemothrapySan Diego Abstract C 2 6p.3. American Society for MicrobiologyWashington DCUSA 30 : Telithromycin 600 mg 300 mg in press 3 Farrell D JMorrissey SBakker Set al.: Molecular characterization of macrolide resistance mechanisms among Stretococcus pneumoniae and Streptococcus pyogenes isolated from the PROTEKT study. J Antimicrob Chemother 50 Sup. : Clarebout GHuet CLeclercq R: A convenient fluorescence assay to study the capacity of macrolides and related antimicrobials to induced resistance by ribosomal methylation. In program and abstracts of the 0 th Interscience Conference on Antimicrobial Agents and Chemotherapy Toronto Abstract 92p.7. American Society for MicrobiologyWashingtonDCUSA 33 Kaieda SYano HOkitsu Net al.: In vitro isolation of a Streptococcus pneumoniae mutant constitutively resistant to macrolide lincosamidemland characteroization of its altered attenuator of the ermb gene. In program and abstracts of the 2 nd Interscience Conference on Antimicrobial Agents and ChemotherapySan Diego Abstract C 580p. 72. American Society for Microbiology WashingtonDCUSA 3 Liu MDouthwaite S: Activity of the ketolide telithromycin is refractory to erm monomethylation of bacterial rrna. Antimicrob Agents Chemother 6:
11 Novel ketolide antibacterial agents With special reference to telithromycin Matsuhisa Inoue Mitsuo Kaku 2 Takeshi Nishino 3 Yoichi Hirakata and Shigeru Kohno 5 Department of MicrobiologyKitasato University School of Medicine 5 Kitasato Sagamihara Japan 2 Department of Molecular DiagnosticsTohoku University Graduate School of Medicine 3 Department of MicrobiologyKyoto Pharmaceutical University Clinical LaboratoryNagasaki University Hospital 5 Department of Molecular Microbiology & ImmunologyNagasaki University Ketolide antibacterial agents have been under development worldwide as a new class of antibacterial agents. Initial research and development of ketolide antibacterials has been aimed at identifying characteristic properties of ketolide compoundsand telithromycin, the agent that has been developed the furthest has been used clinically in many countries. The chemical structure of ketolides is characterized by a ketone group at position 8and bacteriologicaly they exhibit potent antibacterial activity against pathogenic bacteria of respiratory and otorhinological infections, such as gram positive coccihaemophilus atypical microorganisms, and intracellularly parasitic bacteria. Telithromycins characterized by potent activity against penicillin macrolide and quinolone resistant Streptococcus pneumoniaeand there is no cross resistance with other antibacterial agents.
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THE JAPANESE JOURNAL OF ANTIBIOTICS 57 5 425( 1 ) Telithromycin 7 20 PROTEKT (Prospective Resistant Organism Tracking and Epidemiology for the Ketolide Telithromycin) Telithromycin (TEL) TEL ermb mefa
Table 1.Resistance criteria Fig.1.The resistance rates of piperacillin,ceftazidime, cefsulodin,imipenem,aztreonam,gentamicin,tobramycin,amikacin,isepamicin,fosfomycin and ofloxacin against 2,793 strains
Table 1.Quality control of MICs for reference strains Table 2.Antimicrobial activity of gatifloxacin against aerobic bacteria Table 4.Antimicrobial activity of gatifloxacin and other quinolones against
172( 38 ) THE JAPANESE JOURNAL OF ANTIBIOTICS 57 2 Apr. 2002 1 19 6 2002 5 8 4 254 254 (PBP) 90 83 65 142 PBP pbp1a, pbp2x, pbp2b 121 (49%), pbp1a, pbp2x 30 (12%), pbp2x, pbp2b 16 (6%), pbp2x 61 (24%),
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CHEMOTHERAPY VOL.41 S-2 Laboratory and clinical evaluation of teicoplanin CHEMOTHERAPY AUG. 1993 VOL.41 S-2 Laboratory and clinical evaluation of teicoplanin Table 1. Comparative in vitro activity of teicoplanin
1272 CHEMOTHERAPY MAR. 1975
1272 CHEMOTHERAPY MAR. 1975 VOL. 23 NO. 3 CHEMOTHERAPY 1273 Fig. 2 Minimal inhibitory concentration of aminoglycosides against 50 strains of Klebsiella Fig. 1 Minimal inhibitory concentration of aminoglycosides
Fig. 1 Chemical structure of DL-8280
Fig. 1 Chemical structure of DL-8280 Fig. 2 Susceptibility of cl in ical isolates to DL4280 Fig. 5 Susceptibility of clinical isolates to DL-8280 Fig. 3 Susceptibility of clinical isolates to DL-8280 Fig.
coccus aureus Corynebacterium sp, Haemophilus parainfluenzae Klebsiella pneumoniae Pseudornonas aeruginosa Pseudomonas sp., Xanthomonas maltophilia, F
VOL.43 S-1 coccus aureus Corynebacterium sp, Haemophilus parainfluenzae Klebsiella pneumoniae Pseudornonas aeruginosa Pseudomonas sp., Xanthomonas maltophilia, Flavobacter- Table 1. Concentration of grepafloxacin
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moxifloxacin in vitro moxifloxacin in vitro 17 9 6 17 11 21 moxifloxacinmflx in vitro cefdinir CFDNclavulanic acidamoxicillincvaampcclarithromycincamclindamycincldm levofloxacinlvfx 1MFLX Clostridium clostridiiformeclostridium
Table 1. Antibacterial activitiy of grepafloxacin and other antibiotics against clinical isolates
Table 1. Antibacterial activitiy of grepafloxacin and other antibiotics against clinical isolates Table 2-1. Summary of patients treated with grepafloxacin for respiratory infection 1) Out: outpatient,
E Societe de Pathologie Infectieuse de Langue Francaise (, 1991) E Spanish Thoracic Society (1992) E American Thoracic Society (ATS : 1993. ü ù2001 ) E British Thoracic Society (1993, ü è2001 ) E Canadian
CHEMOTHERAPY FEB Table 1. Activity of cefpirome and others against clinical isolates
VOL.39 S-1 CHEMOTHERAPY FEB. 1981 Table 1. Activity of cefpirome and others against clinical isolates VOL.39 S-1 CHEMOTHERAPY FEB. 1991 72 M, 55.5 kg 66 F, 53 kg Chronic bronchitis Bronchopneumonia Peak
Table 1 Survival rates of infected mice given antibiotic doses producing peak serum a) S. aurcus Smith Challenge dose :7 ~10 (5% mucin) CFU/mouse. LD50: 1 ~103 (5% mucin) CFU/mouse. Table 2 Survival rates
Key words : R-plasmid, Urinary tract infection, E. coli Fig. 1. MIC distribution against E. coli isolated from urinary tract (366 strains) and isolation - frequencies of drug-resistant strains Table 1.
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VOL.35 S-2 CHEMOTHERAPY Fig.1 Chemical structure of carumonam CHEMOTHERAPY JUNE 1987 Table1 Media used *BHIB, brain heart infusion broth (Difco); /3 -NAD, S -nicotinamidoadeninedinucleotide (Sigma Chemical
Clostridium difficile ciprofloxacin, ofloxacin, norfloxacin Bifidobacterium Lactobacillus Lactobacillus Bacteroides fragilis B. fragilis C. difficile
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CHEMOTHERAPY aureus 0.10, Enterococcus faecalis 3.13, Escherichia coli 0.20, Klebsiella pneumoniae, Enterobacter spp., Serratia marcescens 0.78, Prote
aureus 0.10, Enterococcus faecalis 3.13, Escherichia coli 0.20, Klebsiella pneumoniae, Enterobacter spp., Serratia marcescens 0.78, Proteus mirabilis 3.13, Proteus vulgaris 1.56, Citrobacter freundii 0.39,
180 ( 64 ) THE JAPANESE JOURNAL OF ANTIBIOTICS June 2011 A b group A Streptococcus: GAS GAS 10 meta-analysis 1) 2,3) GAS potential pathogens Tab
June 2011 THE JAPANESE JOURNAL OF ANTIBIOTICS 64 23 179 ( 63 ) A b cefditoren pivoxil 5 amoxicillin 10 1,2) 1,3) 1) 1) 1) 4) 5) 6) 7) 1) 2) 3) 4) 5) 6) 7) 2011 4 8 2007 5 2009 4 A b GAS cefditoren pivoxil
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Fig.1 Chemical structure of BAY o 9867
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CHEMOTHERAPY Proteus mirabilis GN-79 Escherichia coli No. 35 Proteus vulgaris GN-76 Pseudomonas aeruginosa No. 11 Escherichia coli ML-1410 RGN-823 Kle
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VOL.42 S-1
CHEMOTHERAPY APR. 1994 VOL.42 S-1 CHEMOTHERAPY APR. 1994 Table 1. Criteria for evaluation of clinical efficacy by the Japanese Society of Oral and Maxillo-Facial Surgeons Grades of symptoms and numerical
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VOL. 34 S-3 CHEMOTHERAPY Fig. 1 Structural formula of L-105 CHEMOTHERAPY JUNE 1986 VOL. 34 S-3 CHEMOTHERAPY Table 1 Antibacterial spectra of L-105 against gram negative anaerobic rods Inoculum 106 cells/ml
VOL.48 NO.7 lase negative staphylococci, Escherichia coli, Klebsiella spp., Citrobacter freundii, Enterobacter spp., indole-positive Proteus, Serratia
ceftazidime, cefpirome, cefepime, cefoperazone/sulbactam (2: 1), imipenem Staphylococcus aureus oxacillin coagulase negative staphylococci Escherichia coli piperacillin Klebsiellac spp. Citrobacter Pseudomonas
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β Moraxella catarrhalis Escherichia coli Citrobacter Klebsiella pneumoniae Enterobacter cloacae Serratia marcescens Proteus Pseudomonas aeruginosa Acinetobacter Bacteroides fragilis β Haemophilus influenzae
CHEMOTHERAPY APRIL 1992 Acinetobacter calcoaceticus Staphylococcus aureus, Escherichia coli P. aeruginosa E. eoli, Klebsiella pneumoniae Serratia marc
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VOL.30 NO.12 CHEMOTHERAPY Fig. 1 Effect of temperature on the growth curve of A. calcoaceticus A. calcoaceticits Ac 54 A. calcoacetictts Ac 164 Fig. 2 Effect of medium ph on the growth curve of A. calcoaceticus
15) Egawa, R., Sawai, T. and Mit.uhashi, S.: Jap. J. Microbiol., 11 : 173-178, 1967. 16) Tanaka, T. and Hashimoto, H., Nagai, Y. and Mitsuhashi, S.: Jap. J. Microbiol., 11: 155-162, 1967. 17) Mitsuhashi,
VOL. 23 NO. 3 CHEMOTHERAPY 1067 Table 2 Sensitivity of gram positive cocci isolated from various diagnostic materials Table 3 Sensitivity of gram nega
1066 CHEMOTHERAPY MAR. 1975 Table 1 Sensitivity of standard strains VOL. 23 NO. 3 CHEMOTHERAPY 1067 Table 2 Sensitivity of gram positive cocci isolated from various diagnostic materials Table 3 Sensitivity
b) Gram-negative bacteria Fig. 2 Sensitivity distribution of clinical isolates : E. coli Fig. 3 Sensitivity distribution of clinical isolates : Pseudomonas Fig. 1 Sensitivity distribution of clinical isolates
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β β Moraxella catarrhalisescherichia colicitrobacter Klebsiella pneumoniaeenterobacter cloacaeserratia marcescens Proteus Providencia Pseudomonas aeruginosaacinetobacter Bacteroides fragilis β β E. colik.
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200( 96 ) THE JAPANESE JOURNAL OF ANTIBIOTICS 58 2 Apr. 585 1 17 MIC 1. (Transtracheal aspiration: TTA) TTA TTA TTA 1400 TTA (diffuse panbronchiolitis, DPB) 1) erythromycin(em) EM 12.5% 87.5% 2,3) EM EM
epidermidis, Enterococcus faecalis, Enterococcus Klebsiella pneumoniae, Proteus mirabilis, indolepositive Proteus spp., Enterobacter spp., Serratia
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366 12 THE JAPANESE JOURNAL OF ANTIBIOTICS 65 6 Dec. 2012 1 8 DNA 2,3 16 12 20 171 2008 12 2010 11 2 3,558 4.44% 1.65% 1.17% 90% 9 Escherichia coli -
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CHEMOTHERAPY CHEMOTHERAPY Table 1 Antibacterial activity of BRL 28500 against standard strains of bacteria Fig, 1 Sensitivity distribution of ABPC-resistant E. coli isolated from urinary tract Fig. 2 Sensitivity
400 46 THE JAPANESE JOURNAL OF ANTIBIOTICS 65 6 Dec. 2012 LVFX 100 mg 3 / 7 150 mg 2 / 7 2 2006 2008 9 LVFX PK PD 2009 7 100 mg 1 3 500 mg 1 1 AUC/MIC
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THE JAPANESE JOURNAL OF ANTIBIOTICS 68 3 June 2015 Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis % 2 S. pneumon
June 2015 THE JAPANESE JOURNAL OF ANTIBIOTICS 68 3 189 49 1 : 14 1 2 2 3 1 2 3 2015 4 3 1 : 14 CVA/AMPC 1 : 14 27 CVA/AMPC 1 : 14 88.5% Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis
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13 11 30 14 4 22 Streptococcus pneumoniae Haemophilus influenzae amoxicillin AMPC cefditoren pivoxil CDTR AMPC 50 mg kg day CDTR 9mg kg day CDTR 18 mg kg day S. pneumoniae H. influenzae 8 17 25 1 25 S.
CHEMOTHERAPY JUN Citrobacter freundii 27, Enterobacter aerogenes 26, Enterobacter cloacae 27, Proteus rettgeri 7, Proteus inconstans 20, Proteus
VOL. 32 S-4 CHEMOTHERAPY Fig. 1 Chemical structure of sodium cefoperazone Fig. 2 Chemical structure of sodium cefoperazone CHEMOTHERAPY JUN. 1984 Citrobacter freundii 27, Enterobacter aerogenes 26, Enterobacter
Table 1 Antibacterial spectra of CPM and other antimicrobials against anaerobes Fig. 1 In vitro activity of CPM and other antibiotics against B. fragilis (136 strains) Fig. 2 In vitro activity of CPM and
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242 ( 36 ) THE JAPANESE JOURNAL OF ANTIBIOTICS 63 _ 3 prulifloxacin * ** ** CMC * ** 2010 2 22 Prulifloxacin ulifloxacin (UFX) 3 1 2003 12 2004 5 19 534 2 2005 12 2006 5 19 805 3 THE JAPANESE JOURNAL OF
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Feb. 2016 THE JAPANESE JOURNAL OF ANTIBIOTICS 69 1 1 1 2013 69 11,762 2015 11 16 1994 2013 69 19 11,762 FQ 33 Streptococcus pyogenes, Streptococcus pneumoniae, Moraxella catarrhalis, Haemophilus influenzae
Fig. 1. Structures of NM394, NAD-358 and NAD-245 Fig. 2. Typical HPLC chromatograms of NM394 in human plasma by organic solvent extraction method (a): Blank plasma (b): Plasma spiked with NM394 and internal
988 CHEMOTHERAPY NOV. 1971
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CHEMOTHERAPY OCT. 1994 Tazobactam Piperacillin Fig. I. Chemical structures of tazobactam and piperacillin. Table 1. Media used for preculture and MIC determination BHIB: Brain heart infusion broth (Difco),
VOL.47 NO.5 Table 1. Susceptibility distribution of Ĉ- lactams against clinical isolates of MRSA MRSA: rnethicillin- resistant Staphylococcus aureus
MAY 1999 VOL.47 NO.5 Table 1. Susceptibility distribution of ƒà- lactams against clinical isolates of MRSA MRSA: rnethicillin- resistant Staphylococcus aureus (oxacillin MIC: 4ƒÊg/ ml) FMOX: flomoxef,
Table 1. Antibacterial spectrum SBT ABPC ABPC CPZ : sulbactamiampicillin : ampicillin : cefoperazone
Table 1. Antibacterial spectrum SBT ABPC ABPC CPZ : sulbactamiampicillin : ampicillin : cefoperazone (inoculum size= 106 CFU/ml) (Ĉ-lactamase producer : 2 strains) Fig. 1. Sensitivity distribution of
Staphylococcus sp. K.pneumoniae P.mirabilis C.freundii E. cloacae Serratia sp. P. aeruginosa ml, Enterococcus avium >100ƒÊg/ml
CHEMOTHERAPY SEPT. 1992 cefoperazone ceftazidime (CAZ), imipenem (IPM) Staphylococcus sp., Enterococcus (CPZ), faecalis, Escherichia coli, Klebsiella pneumoniae, Citrobacter freundii, Enterobacter cloacae,
Feb THE JAPANESE JOURNAL OF ANTIBIOTICS Tebipenem pivoxil 1 1, Meiji Seika 2 Meiji Seika G 3 Meiji Seika Tebipen
Feb. 2016 THE JAPANESE JOURNAL OF ANTIBIOTICS 69 1 53 53 Tebipenem pivoxil 1 1, 3 2 2 1 1 Meiji Seika 2 Meiji Seika G 3 Meiji Seika 2015 12 15 Tebipenem pivoxil 10% 2010 4 2013 3 3,547 3,540 3,540 3,331
1.Streptococcus pneumoniae, Streptococcus pyogenes JC-1,S.aureus Smith,methicillin (DMPPC)- susceptible S. aureus subsp. aureus (MSSA) TR101, DMPPC-resistant S. aureus subsp. aureus (MRSA) TR102, Staphylococcus
VOL. 37 NO. 3 Key words: Drug allergy, LMIT, Penams, Cephems, Cross-reactivity
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Fig.2. Sensitivity distribution of clinical isolates of S. epidermidis (24 strains, 106 CFU/ml) Staphylococcus aureus Staphylococcus epider- midis Ent
Fig.2. Sensitivity distribution of clinical isolates of S. epidermidis (24 strains, 106 CFU/ml) Staphylococcus aureus Staphylococcus epider- midis Enterococcus faecalis Klebsiella pneumoniae, Morganella
Streptococcus pneumoniae,streptococcus pyogenes,streptococcus agalactiae,neisseria gonorrhoeae,h.influenzae,moraxella subgenus Branhamella catarrharis
Streptococcus pneumoniae,streptococcus pyogenes,streptococcus agalactiae,neisseria gonorrhoeae,h.influenzae,moraxella subgenus Branhamella catarrharis, E.coil,Klebsiella pneumoniae,klebsiella oxytoca,proteus
日本化学療法学会雑誌第59巻第5号
Streptococcus pneumoniae Haemophilus influenzae Moraxella catarrhalis S. pneumoniae H. influenzae M. catarrhalis S. pneumoniae H. influenzae M. catarrhalis S. pneumoniae H. influenzae M. catarrhalis S.
The clinical characteristics of Mycoplasma pneumoniae pneumonia in children younger than 6 years old Nobue Takeda1,2),Tomomichi Kurosaki1),Naruhiko Ishiwada2),Yoichi Kohno2) 1)Department of Pediatrics,Chiba
VOL. 40 S- 1 Table 1. Susceptibility of methicillin-resistant Staphylococcus aureus to meropenem Table 2. Coagulase typing of methicillin-resistant St
CHEMOTHERAPY VOL. 40 S- 1 Table 1. Susceptibility of methicillin-resistant Staphylococcus aureus to meropenem Table 2. Coagulase typing of methicillin-resistant Staphylococcus aureus CHEMOTHERAPY Table
VOL.32 S-7 CHEMOTHERAPY Table 1 MIC of standard strains of CTRX Fig. 2 Cumulative curves of MIC S. aureus (26 strains )
CHEMOTHERAPY OCT. 1984 Fig. I Chemical structure of CTRX VOL.32 S-7 CHEMOTHERAPY Table 1 MIC of standard strains of CTRX Fig. 2 Cumulative curves of MIC S. aureus (26 strains ) CHEMOTHERAPY Fig. 3 Cumulative
Feb THE JAPANESE JOURNAL OF ANTIBIOTICS ,4 2,4 2,4 2,3,4 2,3,4 2,3, ,3, Garenoxacin GRNX Levofloxacin LV
Feb. 2016 THE JAPANESE JOURNAL OF ANTIBIOTICS 69 1 27 27 1,4 2,4 2,4 2,3,4 2,3,4 2,3,4 2 1 2,3,4 1 2 3 4 2015 10 21 9 Garenoxacin GRNX Levofloxacin LVFX Sitafloxacin STFX Moxifloxacin MFLX Pharmacokinetics-Pharmacodynamics
VOL.32 S-9 CHEMOTHERAPY Table 1 Minimum inhibitory concentrations of AC-1370, CPZ and CAZ Table 2 Efficacy of AC-1370 and CPZ against systemic infections in mice *Inoculum size: 106 cells/ml * 95% confidence
VOL.35 S-2 CHEMOTHERAPY Table 1 Sex and age distribution Table 2 Applications of treatment with carumonam Table 3 Concentration of carumonam in human
CHEMOTHERAPY Fig. 1 Chemical structure of carumonam Disodium(+)-(Z)-CCE1-(2-amino-4-thiazoly1)-2-[[(2S, -(carbamoyloxymethyl)-4-oxo-1-sulfonato-3-azetidinyll -2-oxoethylidene] amino] oxy] acetate 3S)-2
Oct THE JAPANESE JOURNAL OF ANTIBIOTICS Pseudomonas aeruginosa 186 P. aeruginosa piperacillin PIPC, taz
Oct. 2016 THE JAPANESE JOURNAL OF ANTIBIOTICS 69 5 327 27 2013 2014 2016 7 5 2013 2014 Pseudomonas aeruginosa 186 P. aeruginosa piperacillin PIPC, tazobactam/piperacillin TAZ/PIPC, ceftazidime CAZ, cefepime
Table 1. Antibacterial activity of azithromycin and other agents against gram-positive anaerobic bacteria and facultative anaerobic bacteria a Facultative anaerobic bacteria. Table 2. Antibacterial activity
VOL. 23 NO. 3 CHEMOTHERAPY 1379 Table 1 Susceptibility of clinical isolated strains to Tobramycin
VOL. 23 NO. 3 CHEMOTHERAPY 1379 Table 1 Susceptibility of clinical isolated strains to Tobramycin 1380 CHEMOTHERAPY MAR. 1975 Table 2 Susceptibility of isolated Pseudomonas aeruginosa to various antibiotics
CHEMOTHERAPY APR Fig. 1 Chemical structure of cefotetan (CTT, YM09330)
CHEMOTHERAPY APR. 1982 Fig. 1 Chemical structure of cefotetan (CTT, YM09330) VOL.30 S-1 CHEMOTHERAPY Fig. 2 Comparison of standard curves of CTT on various test organisms by cylinder plate method Column
CHEMOTHERAPY APRIL 1992 VOL. 40 S- 1 Table 1-1. Comparative in vitro activity of meropenem against clinical isolates CNS: coagulase-negative staphylococci CHEMOTHERAPY APRIL 1992 Table 1-2. Comparative
Fig. 1 Chemical structure of TE-031 Code number: TE-031 Chemical name: (-) (3R, 4S, 5S, 6R, 7R, 9R, 11R, 12R, 13S, 14R)-4-[(2, 6-dideoxy-3-C-methyl-3-
Fig. 1 Chemical structure of TE-031 Code number: TE-031 Chemical name: (-) (3R, 4S, 5S, 6R, 7R, 9R, 11R, 12R, 13S, 14R)-4-[(2, 6-dideoxy-3-C-methyl-3-O-methyl-a-L-ribo-hexopyranosyl) oxy]-14-ethyl-12,
Key words: E. coli O 157: H7, fosfomycin, verotoxin, mouse infection
Key words: E. coli O 157: H7, fosfomycin, verotoxin, mouse infection Table 1. Bacterial cell counts in feces of mice infected with Esclwrichia coli O 157: H7 NK2 before and during oral dosing with fosfomycin
2 CHEMOTHERAPY JAN. 1976 VOL. 24 NO. 1 CHEMOTHERAPY 3 Table 1 Antibacterial spectra of Cephacetrile, Cephalothin, Cephaloridine and Cefazolin 4 CHEMOTHERAPY JAN. 1976 Fig. 1 In vitro activity of Cephacetrile,
CHEMOTHERAPY Fig. 1 Chemical structure of CXM-AX
Fig. 1 Chemical structure of CXM-AX NOV. 1986 Fig. 2 Sensitivity distribution of clinical isolates organisms (106 cells/ml) a Smurcus 27 strains d) P.m irabilis 15 strains b Ecol i 27 strains 111.morganii
Table 1 Sensitivity distribution of clinical isolates 1. Escherichia coli Inoculum size: 106cells/ml 2. Klebsiella pneumoniae 3. Enterobacter cloacae 4. Serratia marcescens Inoculum size: 106cells/nil
Table 1. Antibacterial activity of cefdinir, cefixime, cefteram, cefuroxime, cefaclor and amoxicillin against standard strains Inoculum size: 108 cells/ml CFDN: cefdinir, CFIX: cefixime, CFTM: cefteram,
日本化学療法学会雑誌第60巻第4号
Streptococcus pneumoniae Haemophilus influenzae S. pneumoniae H. influenzae Key words β Streptococcus pneumoniae Haemophilus influenzae S. pneumoniae H. influenzae μ μ S. pneumoniae H. influenzae S. pneumoniae
VOL.30 S-1 CHEMOTHERAPY Table 1 Antibacterial activity of CTT against standard strains Table 2 Antibacterial activity of CTT against standard strains
CHEMOTHERAPY APR. 1982 Fig. 1 Chemical structure of cefotetan (CTT, YM09330) VOL.30 S-1 CHEMOTHERAPY Table 1 Antibacterial activity of CTT against standard strains Table 2 Antibacterial activity of CTT
CHEMOTHERAPY JUNE 1993 Table 1. Background of patients in pharmacokinetic study
CHEMOTHERAPY JUNE 1993 Table 1. Background of patients in pharmacokinetic study VOL. 41 S 1 Table 2. Levels (Đg/ml or Đg/g) of S-1006 in serum, bile, and tissue (gallbladder) after oral administration
VOL. 36 S-3 CHEMOTHERAPY 437
VOL. 36 S-3 CHEMOTHERAPY 437 438 CHEMOTHERAPY JULY 1988 Fig. 1 Contractile response of gastrointestinal tract to intravenous administration of saline and EM in interdigestive state in dogs (a) : Saline,
Table 1. Antimicrobial drugs using for MIC
Table 1. Antimicrobial drugs using for MIC Table 2. Susceptibilities determined with the VITEK 2 system and agar dilution reference by interpretive eategory for Staphylococcus aureus Table 3. Interpretive
Table 1.Distribution and number of cases with acute upper respiratory tract infections classified according to antimicrobial agents administered Table 2. Distribution of cases which were enrolled to set
Key words:fatty acid,plant oil,staphylococcus aureus,skin care, atopic dermatitis
Key words:fatty acid,plant oil,staphylococcus aureus,skin care, atopic dermatitis growth was monitored at 660 nm with a biophotorecorder. Table 1.Relative inhibitory effects of fatty acids,plant oils,
CHEMOTHERAPY MAY. 1988
CHEMOTHERAPY MAY. 1988 CHEMOTHERAPY Fig. 1 Chemical structure CHEMOTHERAPY MAY. 1988 VOL.36 5-1 CHEMOTHERAPY CHEMOTHERAPY MAY. 1988 VOL.36 S-1 CHEMOTHERAPY CHEMOTHERAPY MAY. 1988 VOL.36 S-1 CHEMOTHERAPY
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173 Table 1.Detection rates of Neisseria gonorrhoeae, Chlamydia trachomatis, Mycoplasma genitalium, Ureaplasma urealyticum, Haemophilus influenzae and adenovirus from male urethritis in Urethritis No.
CHEMOTHERAPY 52 MAY d a a. Normal S. aureus d Đg/ml, 2h; e b b Đg/ml, Abnormal e. division lh; Abnormal thickening division cross f c. 1
Levloxacin V.:1 Z iiiir fa L CHEMOTHERAPY 52 MAY d a a. Normal S. aureus d. 0.39 Đg/ml, 2h; e b b. 0.10 Đg/ml, Abnormal e. division lh; Abnormal thickening division cross f c. 1992 0.39 Đg/ml, and Fig.
VOL. 43 NO. 4
VOL. 43 NO. 4 Fig. 1. Frequency of Enterococcus species from complicated UTI, 1988-1992. the number * of Enterococcus species/the number of cases with complicated UTI. Fig. 3 Epidemiologic characteristics
Fig. 1 Chemical structure of KW-1070
Fig. 1 Chemical structure of KW-1070 Fig. 2 Sensitivity distribution of clinical isolates Fig. 4 Sensitivity distribution of clinical isolates Fig. 3 Sensitivity distribution of clinical isolates Fig.
THE JAPANESE JOURNAL OF ANTIBIOTICS 48-8 Enterococcus avium 5Š, Corynebacterium xerosis 10Š, Corynebacterium pseudodiphtheriticum 10Š, Corynebacterium
THE JAPANESE JOURNAL OF ANTIBIOTICS 48-8 Enterobacter spp., Serratia spp., Burkholderia cepacia, Flavobacterium spp., Alcaligenes spp. THE JAPANESE JOURNAL OF ANTIBIOTICS 48-8 Enterococcus avium 5Š, Corynebacterium
pneumoniae 30, C. freundii 32, E. aerogenes 27, E. cloacae 32, P. mirabilis 31, P. vulgaris 34, M. morganii 32, S. marcescens 31, H. influenzae 27, P.
pneumoniae 30, C. freundii 32, E. aerogenes 27, E. cloacae 32, P. mirabilis 31, P. vulgaris 34, M. morganii 32, S. marcescens 31, H. influenzae 27, P. aeruginosa 30, P. maltophilia pyogenes 32, Escherichia
Key words: change serotype, Pseudomonas aeruginosa anti-pseudomonal drug,
Key words: change serotype, Pseudomonas aeruginosa anti-pseudomonal drug, Table 1 Incidence of changes in serotype of Pseudomonas aeruginosa isolates induced by anti-pseudomonal drugs Number of isolates
CHEMOTHERAPY Table 1 Urinary excretion of mezlocillin Fig. 4 Urinary excretion of mezlocillin Fig. 3 Blood levels of mezlocillin
CHEMOTHERAPY Fig. 2 Urinary excretion of mezlocillin Fig. 1 Blood levels of mezlocillin CHEMOTHERAPY Table 1 Urinary excretion of mezlocillin Fig. 4 Urinary excretion of mezlocillin Fig. 3 Blood levels
Mueller-Hinton broth), Streptococcus pneumoniae (S. pneumoniae), Streptococcus faecalis (S. faecalis)
Fig. 1 Chemical structure of TA-058 (2S, 5R, 6R)-6- k2r-2- (2R-2- amino-3-n- methyl carbamoylpropionamido) -2- (4- hydroxyphenyl) acetamido l-3, 3-dimethy1-7-oxo- 4-thia-1- azabicycio k3.2,0 l heptane-2-carboxylic
CHEMOTHERAPY Table 2 Clinical response of 6059-S by infection Table 3 Effect of 6059-S on blood chemistry *Normal range : S-GOT 20 `60 mu/ml, S-GPT 5 `25 IU/L, Al-Pase 30 `85 mu/ml In oilier cases : S-GOT
抗IV-薬剤耐性（6912）.indd
解説 報告 動物用抗菌性物質を取り巻く現状 (Ⅳ) 薬剤耐性機構 小澤真名緒 (農林水産省動物医薬品検査所検査第二部安全性検査第一領域主任研究官 ) 1 はじめに 2 耐性の獲得 DNA S rrna tet 3 耐性機構 キノロン耐性マクロライド耐性 感受性菌 変異 抗菌剤使用による選択圧 耐性菌 耐性遺伝子の獲得 抗生物質産生菌 大腸菌や腸球菌など常在する菌の薬剤耐性菌 耐性遺伝子の供給源 セファロスポリン耐性テトラサイクリン耐性
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β β β β β Streptococcus pneumoniaehaemophilus influenzaemoraxella catarrhalismycoplasma pneumoniaechlamydia pneumoniae β Key wordsβ mys nilc laci ngis Table. Assessmentschedule Parameters Patientcharacteristics
Pseudomonas aeruginosa S-827 Fig. 1. Method of biofilm formation. Table 1. Susceptibilities of antimicrobial agents on agar plate and in broth against Pseudomonas aeruginosa S-827 JULY CHEMOTHERAPY 888
03-b-„FŒ{›xŒ¾-4.02
518( 30 ) THE JAPANESE JOURNAL OF ANTIBIOTICS 58 6 Dec. 25 2003 1. * * Dec. THE JAPANESE JOURNAL OF ANTIBIOTICS 58 6 519( 31 ) 9 5 2003 8 2004 7 14 565 701 258 (36.8%) 443 (63.2%) Staphylococcus aureus
1) i) Barber, M. et al.: Brit. Med J, 2, 565, 19'49. ii) Barber, M.F.G. J. Hayhoe and J. E. M. Whithead: Lancet, 1120 `1125, 1949.-2) Bergey: Bergey's Manual of Determinative Bacteriology 7 th Ed: (1958).-3)
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Mycoplasma pneumoniae M. pneumoniae M. pneumoniae M. pneumoniae M. pneumoniae M. pneumoniae Key words Mycoplasma pneumoniae Mycoplasma pneumoniae M. pneumoniae I M. pneumoniae M. pneumoniae M. pneumoniae