CHEMOTHERAPY Methicillin-resistant S.aureus(MRSA) coccus epidermidis 105 Streptococcus pyogenes E.faecali senterococcus avium Enterococcus faecium Str
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1 cefaclor(ccl),cefuroxime(cxm),cefixime (CFIX),cefteram(CFTM),cefdinir(CFDN) pneumoniae,streptococcus pyogenes Moraxella catarrhalis,haemophilus influenzae,escherichia coli, Klebsiella pneumoniae,proteus mirabais Propionibacterium acnes Staphylococcus aureus Smith,S.pyogenes C-203,E.coli KC-14,K.pneumoniae KC-1 (+)-(6R,7S)-7[(R)-2-amino-2-phenylacetamido] 3-chloro-8-oxo-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid monohydrate C16H16C1N304 EH20, cefuroxime CXM),cefixime (CFIX),cefteram(CFTM),cefdinir(CFDN),cefpro-
2 CHEMOTHERAPY Methicillin-resistant S.aureus(MRSA) coccus epidermidis 105 Streptococcus pyogenes E.faecali senterococcus avium Enterococcus faecium Streptococcus pneumoniae Escherichia colicitrobac ter freundii siella Imeumoniae Enterobac ter cloacae terobacter aerogenes Serratia marcescens Proteus vulgaris Proteus mirabilis ganella morganii Providencia re ttgeri Pseudomonas aeruginosa Acinetobacter calcoaceti- H.influenzae Moraxella catarrhalis 10 Propionibacterium acnes 8 pneumoniae KC-1,S.marcescens T-55,P.mirabilis HIA,Tryptosoya Agar(TSA),Mueller- Hinton Agar Kprteumoniae KC-1,K.pmeumoniae E.cloacae NCTC9394,S.marcescens 1F03736,Peptostreptococcus magnus ATCC14952,P. acnes
3 Antibacterial spectrum of loracarbef and other antibiotics against standard strains of gram-positive bacteria Medium:Heart infusion agar(nissui) Supplemented with 10% horse blood Method:agar dilution(streak) Inoculum size:106 cells/ml
4 CHEMOTHERAPY Antibacterial spectrum of loracarbef and other antibiotics against standard strains of gram-negative bacteria Medium:Heart infusion agar(nissui) Supplemented with 10% horse blood(chocolate Supplemented with 5% Fildes enrichment Method:agar dilution(streak) Inoculum size:106 cells/ml agar) Antibacterial spectrum of loracarbef and other antibiotics against standard strains of anaerobic bacteria Medium:GAM agar(nissui) Method: agar dilution(streak) Inoculum size:106 cells/ml
5 Antimicrobial activity of loracarbef and other antibiotics against clinical isolates of gram-positive organisms
6 CHEMOTHERAPY AUGUST Antimicrobial activity of loracarbef and other antibiotics against clinical isolates of gram-negative organisms
7 Antimicrobial activity of loracarbef and other antibiotics against clinical isolates of grarn-negative organisms
8 CHEMOTHERAPY Influence of medium on the antibacterial activity of loracarbef and other antibiotics Medium;HIA:Heart infusion agar TSA:Trypto-soy agar MHA:Meuller-hinton agar NTA:Nutrient agar Inoculum size:106 cfutml
9 Influence of horse serum on the antibacterial activity of loracarbef and other antibiotics Inoculum size:106 cfu/ml
10 CHEMOTHERAPY Influence of medium ph on the antibacterial activity of loracarbef and other antibiotics Inoculum size:106 cfu/ml
11 Influence of inoculum size on the antibacterial activity of loracarbef and other antibiotics Inoculum size:106 cfu/ml loracarbef(mic:12.5 jig/ml) cefaclor(mic:50 /g/ml) Bactericidal activity of loracarbef and cefaclor against Staphylococcus aureus No.25.
12 CHEMOTHERAPY loracarbef(mic:25 cefaclor(mic:50 Bactericidal activity of loracarbef and cefaclor against Enterococcus faecalis. loracarbef(mic:0.78 Agtml) cefaclor(mic:0.78 Ag/ml) Bactericidal activity of loracarbef and cefaclor against Escherichia coli K-12. loracarbef MIC:0.78 Agirril) cefaclor(mic:0.78 Ag/m1) Bactericidal activity of loracarbef and cefaclor against Escherichia coli No.35.
13 loracarbef(mic:0.39 Bactericidal activity of loracarbef and cefaclor against Klebsiella pneumoniae KC-1. loracarbef(mic:0.05 cefaclor(mic:0.05 Bactericidal activity of loracarbef and cefaclor against Klebsiella pneumoniae No.6. loracarbef(mic:>100 cefaclor(mic:>100 Bactericidal activity of loracarbef and cefaclor against Enterobacter cloacae NCTC9394.
14 CHEMOTHERAPY AUG loracarbef(mic:>100 cefaclor(mic:>100 Bactericidal activity of loracarbef and cefaclor against Serratia marcescens IF loracarbef(mic:0.78 cefaclor(mic:1.56 Bactericidal activity of loracarbef and cefaclor against Pejtostrelptococcus ATCC magnus loracarbef(mic:0.05 cefaclor MIC:1.56 Bactericidal activity of loracarbef and cefaclor against Propionibacterium acnes ATCC
15 Loracarbefのin VOL.41 vitroお よ びin vivo抗 菌 力 45 S μg/ml(MIC) control 1.56μg/ml 0-2μtg/ml 3-13μg/ml 0.39μg/ml Fig. 11. Phase contrast micrographs of Escherichia coli K-12 exposed to loracarbef for 4 h.
16 CHEMOTHERAPY 46 control 1.56 Đg/ml 6.25 Đg/ml 0.2 Đg/ml 0.39 Đg/ml Fig. 12. AUGUST 12.5 Đg/ml (MIC) Phase contrast micrographs of Klebsiella pneumoniae KC-1 exposed to loracarbef for 4 h. 1993
17 Loracarbefのin VOL.41 vitroお よ びin vivo抗 菌 力 S.3 47 control 0.1 ƒêg/ml ƒêg/ml 0.2 ƒêg/ml 0.05 ƒêg/ml Fig. 13. (MIC) Phase contrast micrographs for 18 h ƒêg/ml of Propionibacterium acnes ATCC11827 exposed to loracarbef
18 (): 95% confidence limits a), ddy (18 `20g), std: n=10 b), i. p. c), p. o. 2 h after infection Table 10. Protective effect of loracarbef and other antibiotics on experimental infection in micea) Gram-positive bacteria- - Table 11. Protective effect of loracarbef and other antibiotics on experimental infection in micea) Gram-negative bacteria- - (): 95% confidence limits a), std: ddy (18 `20g), n=10 b), i. p. c), p. o. 2 h after infection
19 Protective effect of loracarbef and other antibiotics on experimental respiratory infectiona) in miceb) ( ):95% confidence limits a),aerozol, 5 ml x 30 min b),std:ddy c),p.o. S.pyogenes,S.pneumoniae E.coli,K.pneumoniae,P.mirabilis,H. influenzae,m.catarrhalis
20 8) Obana Y, Nishino T and Tanino T: Therapeutic efficacy of i9-lactam and aminoglycoside antibiotics on experimental pneumonia caused by Klebsiella pneumoniae B-54 in diabetic mice. J Antibiotics 38: 941 `947, 1985 In vitro and in vivo antibacterial activity of a new oral carbacephem, loracarbef Takeshi Nishino, Masako Otsuki and Tatsuya Yoshino Department of Microbiology, Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi, Yamashina-ku, Kyoto 607, Japan We studied the in vitro and in vivo antibacterial activity of a newly developed oral carbacephem, loracarbef (LCBF), in comparison with cefaclor (CCL), cefuroxime (CXM), cefixime (CFIX), cefteram (CFTM), cefdinir (CFDN) and cefprozil (CFPZ). In vitro studies, LCBF showed wide antibacterial activity equal to CCL and CFPZ against grampositive and gram-negative bacteria. LCBF had better antibacterial activity than CCL and CFPZ against clinical isolates of Streptococcus pneumoniae, Streptococcus pyogenes, Moraxella catarrhalis, Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis. LCBF showed excellent antibacterial activity against the anaerobic bacteria Propionibacterium acnes. In experimental infection in mice, LCBF showed better therapeutic efficacy than CFIX, CFTM and CFDN in some strains.
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