Mueller-Hinton broth), Streptococcus pneumoniae (S. pneumoniae), Streptococcus faecalis (S. faecalis)
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1 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 acid trihydrate
2 Mueller-Hinton broth), Streptococcus pneumoniae (S. pneumoniae), Streptococcus faecalis (S. faecalis)
3 Fig. 2 MICs of TA-058 and other fl-lactam antibiotics against respiratory pathogenic ABPC-sensitive H. influenzae (27 strains, inoculum size 106 cfu/ml) Fig. 3 MICs of TA-058 and other fl-lactam antibiotics against respiratory pathogenic S. imeumoniae (22 strains, inoculum size 106 cfu/ml)
4 Table 1 MICs of TA-058 and other Ĉ-lactam antibiotics against respiratory pathogenic P. aeruginosa (31 strains, inoculum size 106 cfu/ml) Table 2 MICs of TA-058 and other Ĉ-lactam antibiotics against respiratory pathogenic K. pneumoniae (26 strains, inoculum size 106 cfu/ml) Table 3 MICs of TA-058 and other Ĉ-lactam antibiotics against respiratory pathogenic E. coli (6 strains, inoculum size 106 cfu/ml)
5 Table 4 MICs of TA-058 and other Ĉ-lactam antibiotics against respiratory pathogenic Enterobacter spp. (9 strains, inoculum size 106cfu/ml) Fig. 4 MICs of TA-058 and other Ĉ-lactam antibiotics against respiratory pathogenic S. faecalis (inoculum size 106 cfu/ml) Fig. 5 MICs of TA-058 and other Ĉ-lactam antibiotics against urinary pathogenic S. faecalis (inoculum size 106 cfu/ml)
6 Table 5 MICs of TA-058 combined with Ĉ-lactamase inhibitors against ABPC-resistant H. infiuenzae Fig. 6 MICs of TA-058 alone and with equal concentrations of clavulanic acid (CVA) or CP against 11 strains of respiratory pathogenic B. catarrhalis (inoculum size, 106 cfu/ml)
7 Fig. 7 Bioassay system and standard curves of TA-058 utilizing thin layer cup plate method Table 6 Peak serum levels and maximal sputum levels of TA-058 in 6 patients with respiratory infections
8 Fig. 8 TA-058 concentrations in sputum during 7 consecutive days administered 1 g of TA-058 d. i. over 2 h twice a day and serum and urinary levels of TA-058 after the 13 th dose Fig. 10 Sputum and serum levels of TA-058 K. Y., 71 y.o., F. 38 kg Fig. 11 Concentration of TA-058 in intrabronchiolar lsecretions 60 minutes after a dose of 3 g d. i. over 30 minutes dissolved with 100 ml of isotonic saline in a patient with chronic bronchitis. Fig. 9 Sputum and serum levels of TA-058 S. I., 60 y. o., M. 45 kg Peat serum concentration readied Đg/ml
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13 Table 9 Clinical antibacterial activities of TA-058
14 Fig. 12 Chronic bronchiolitis due to H. influenzae: K. M., 80 y. o., F., 37 kg Fig. 14 H. T., 67y. o., M., 58 kg : Chronic bronchiolitis Fig. 15 Chronic bronchiolitis. H. T., 68 y.o., M., 59.5 kg Fig. 13 The quantitative sputum culture method on a patient with chronic bronchiolitis after the first dose of TA g d. i. K. M., 80 y. o., F., 37 kg
15
16 TANI, H. YOSHIDA & S. OHSHIMA: Pharmaco- kinetic studies of TA-058 in laboratory animals. Current Chemotherapy and Immunotherapy. (Proceeding of the 12 th ICC) Voḷ 3) SHISHIDO, H. ; K. MATSUMOTO, Y. UZUKA, T. NAGATAKE, M. YAMAMOTO, Y. SAKUMA & T. YAMAGUCHI : Phase I clinical study of TA Current Chemotherapy and Immunotherapy. (Proceeding of the 12 th ICC) Vol. I: 29 `331, ) CATLIN, B. W.: Iodometric detection of Haemophilus influenzae beta-lactamase : Rapid 6) SLACK, M. P. E.; D. B. WHELDON & D. C. presumptive test for ampicillin resistance. Antimicrob. Agents Chemother. 7: 265 `270, 1975 TURK : A rapid test for beta-lactamase production by Haernophilus influenzae. Lancet 2 : 906, ) MITSUHASHI, S.(Ed.) : Beta-lactam antibiotics. Japan Scientific Societies Press, Biochemical mechanisms of resistance. Mechanisms of resistance to ƒà-lactam antibiotics (MITSU- HASHI, S. & M. INOUS) 41 `56, ) NISHINO, T. ; N. ISHII, T. TANINO, S. OHSHIMA & T. YAMAGUCHI : In vitro and in vivo antibacterial activity of TA-058, a new broadspectrum semisynthetic penicillin. Current Chemotherapy and Infectious Disease. (Proceedings of the 11th ICC and the 19 th ICA 10) BROWN, A. G. ; D. BUTTERWORTH, M. COLE, G. HANSCOMB, J. D. HOOD, C. READING & G. N. AC) Vol. I: 362 `363, 1980 ROLINASON : Naturally-occurring ƒà-lactamase 2) YAMAGUCHI, T. ; I. MAEZAWA, Y. SAKUMA, K. inhibitors with antibacterial activity. J.
17 Antibiotics 29 : 668 `669, 1976 ENGLISH, A. R. ; J. A. RETSEMA, A. E. GIRARD, J. E. LYNCH & W. E. BARTH : CP-45899, a beta-lactamase inhibitor that extends the antibacterial spectrum of beta-lactams : Initial bacteriological characterization. Antimicrob. Agents Chemother. 14 : 414 `419, ) WISE, R. ; J. M. ANDREWS & K. A. BEDFORD : Clavulanic acid and CP : A comparison of their in vitro activity in combination with penicillin. J. Antimicrob. Chemother. 6 : ) PERLMAN, D., (Ed.) : Structure-activity relationships among the semisynthetic antibiotics. Academic Press, New York, ) MATSUMOTO, K. & Y. UZUKA : Concentration of antibiotics in bronchiolar secretions of the patients with chronic respiratory infections. Chemotherapy 4: 73 `78, 1976
18 CLINICAL AND LABORATORY EVALUATION OF TA-058 KEIZO MATSUMOTO, HARUMI SHISHIDO, MASASHI YAMAMOTO, YOSHIO UZUKA, TSUYOSHI NAGATAKE, TOMOYUKI HARADA, ATSUSHI TAKAHASHI, MASAKAZU TAKASUGI, SHIGEO KAIDA and KIWAO WATANABE Department of Internal Medicine, Institute for Tropical Medicine, Nagasaki University HISAO KIMURA Department of Internal Medicine, Fukushima Rosai Hospital Respiratory KUNIO KUDO Division, Sendai National Hospital SIGERU TAMAKI Department of Internal Medicine, Fujita General Hospital TA-058 is a new semisynthetic penicillin which has a unique chemical structure containing an amino-acyl (N-methyl-asparaginyl) function in its side chain. Clinical and laboratory study has been performed on TA-058 in order to evaluate its usefulness mainly in respiratory tract infections. Minimal inhibitory concentrations (MICs) of TA-058 against 27 strains of respiratory pathogenic H. influenzae sensitive to ampicillin were `0.1 Đg/ml. MICs of TA-058 against 22 strains of S. pneumoniae were `0.1 Đg/ml. MICs of TA-058 against respiratory pathogenic P. aeruginosa and K. pneumoniae were 0.39 `>100 Đg/ml and 0.78 `>100 Đg/ml, respectively. The synergistic effects were demonstrated between TA-058 and clavulanic acid or CP against respiratory pathogenic ampicillin-resistant H. influenzae and B. catarrhalis. Ratios of maximum sputum level to peak serum concentration ranged from 3.07 % to 7.45% in 6 patients with chronic respiratory infections, while ratio of maximum intrabronchiolar level to peak serum concentration was as high as 20.1 % in a patient with chronic bronchitis. TA-058 was administered by the intavenous drip infusion of a dose of 1 g twice a day. Eighteen respiratory tract infections and 10 urinary tract infections were subjected to clinical evaluation of TA-058, indicating favorable clinical response, i. e., the rates of clinical therapeutic efficacy were 94.4% and 80 %, respectively. None of them showed adverse effects. The safety of this penicillin antibiotic was very good. From the above results, it was concluded that TA-058 is one of the most effective and useful antibiotics for the treatment of the respiratory bacterial infections, particularly for those due to H. influenzae and S. pneumon iae.
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VOL. 30 S-3 CHEMOTHERAPY imeumoniae, Serratia marcescens, Proteus sp, CHEMOTHERAPY DEC. 1982 Table 1 Antibacterial spectra of T-1982, CTT, CMZ, CTX, CPZ and CEZ 106 CFU/ml Note: P; Peptococcus, S; Streptococcus,
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
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
CHEMOTHERAPY APRIL 1992 Acinetobacter calcoaceticus Staphylococcus aureus, Escherichia coli P. aeruginosa E. eoli, Klebsiella pneumoniae Serratia marc
APRIL 1992 Acinetobacter calcoaceticus Staphylococcus aureus, Escherichia coli P. aeruginosa E. eoli, Klebsiella pneumoniae Serratia marcescens P. aeruginosa P. aeruginosa Streptococcus pyogenes Streptococcus
Table 1. Concentration of ritipenem in plasma, gallbladder tissue and bile after ritipenem acoxil administration (200 mg t.i.d., 3 days) N.D.: not det
Table 1. Concentration of ritipenem in plasma, gallbladder tissue and bile after ritipenem acoxil administration (200 mg t.i.d., 3 days) N.D.: not detected *: time after last administration Table 2. Concentration
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,
CHEMOTHERAPY JUNE 1986
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
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,
Fig. 1 Chemical structure of norfioxacin (AM-715)
Fig. 1 Chemical structure of norfioxacin (AM-715) Table 1 Serum and biliary concentration of norfloxacin (AM-715) Table 2 Protocol for clinical evaluation of norfloxacin (AM-715) in the treatment of biliary
123 昭 和49年4月20日 写 真4 写 真1 写 真2 指摘 が最 初 の もの と思 わ れ る. イ菌 感 染症 は イ菌 が 抗 生 剤 に 感 受 性 を 有 す る限 り,そ の化 学 療 法 効 果 が 期 待 出 来 るが,化 学 療 法 を 中 止す る と再 度 出現 す る症 例 が 多 い こ とに気 付 き,エ コ ロジ カル に検 討 した と ころ,三 病型 に分
Table 1 Patients with various renal function * Ccr, Creatinine clearance ml/min per 1. 48 m2 ** C.V.D., Cerebral vascular disease ; C.R F., Chronic renal failure ; H.D., Hemoclialysis ; D., Dialyzer ;
CHEMOTHERAPY DEC (NFLX), ofloxacin (OFLX), ciprofloxacin (CPFX) Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Enterococcus faecali
CHEMOTHERAPY DEC. 1988 (NFLX), ofloxacin (OFLX), ciprofloxacin (CPFX) Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Enterococcus faecalis Pseudomonas aeruginosa, Serratia ma- Fig. 1. Chemical
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,
VOL.27S-1 CHEMOTHERAPY 109 Klebsiella, Proteus, Pseudomonas Streptococcus Fig. 1 Concentration in blood and in CSF after intravenous drip infusion of
VOL.27S-1 CHEMOTHERAPY 109 Klebsiella, Proteus, Pseudomonas Streptococcus Fig. 1 Concentration in blood and in CSF after intravenous drip infusion of 4.9 g Mezlocillin Streptococcus pneumonzae pneumoniae
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,
Table 1. Influence of urine ph on MBCs of new quinolones against Escherichia coli NIHJ JC-2 and Pseudomonas aeruginosa 18S; MBCs in urine were compared with those in Miieller-Hinton broth. Table 2. Influence
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.39 S-3
VOL.39 S-3 CHEMOTHERAPY SEPT.1991 Table 1. Background of characteristics and allocation of 5 healthy male volunteers in a multiple-dose study on panipenem/betamipron Day 1 Fig. 1. Schedule of multiple-dose
CHEMOTHERAPY APR. 1982
VOL.30 S-1 CHEMOTHERAPY Table 1 Dose of CTT and subjects i. v.: Intravenous bolus injection d. i. v.: Intravenous drip infusion i. m.: Intramuscular injection Fig. 1 Schedule for examination of CTT, 1.0g
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)
VOL.27 S-3 CHEMO THERAPY mido)-3-[[[1- (2-dimethylaminoethyl)-1H-tetrazol-5-yl] -thio] methyl]-ceph-3-em-4-carboxylic acid dihydro- S. aureus 209-P JC
![VOL.27 S-3 CHEMO THERAPY mido)-3-[[[1- (2-dimethylaminoethyl)-1H-tetrazol-5-yl] -thio] methyl]-ceph-3-em-4-carboxylic acid dihydro- S. aureus 209-P JC](/thumbs/95/124246112.jpg "VOL.27 S-3 CHEMO THERAPY mido)-3-[[[1- (2-dimethylaminoethyl)-1H-tetrazol-5-yl] -thio] methyl]-ceph-3-em-4-carboxylic acid dihydro- S. aureus 209-P JC")
VOL.27 S-3 CHEMO THERAPY mido)-3-[[[1- (2-dimethylaminoethyl)-1H-tetrazol-5-yl] -thio] methyl]-ceph-3-em-4-carboxylic acid dihydro- S. aureus 209-P JC, E. coli NIHJ JC-2 pneumoniae E. coli 106, K. pneumoniae
CHEMOTHERAPY SEPT. 1970
CHEMOTHERAPY SEPT. 1970 VOL. 18 NO. 5 CHEMOTHERAPY CHEMOTHERAPY SEPT. 1970 VOL. 18 NO. 5 CHEMOTHERAPY 691 692 CHEMOTHERAPY SEPT. 1970 VOL. 78 NO. CHEMOTHERAPY 5 写 真1 第1病 693 写 真4 日 In vitroの しCEZの 第22病
VOL.42 S-1 methicillin-susceptible Staphylococcus aureus (MSSA), Staphylococcus epidermidis, Enterococcus faecalis, Escherichia coli, Klebsiella pneum
VOL.42 S-1 methicillin-susceptible Staphylococcus aureus (MSSA), Staphylococcus epidermidis, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae methicillin-resistant Staphylococcus
VOL. 21 NO. 2 CHEMOTHERAPY 395
394 CHEMOTHERAPY MAR. 1973 VOL. 21 NO. 2 CHEMOTHERAPY 395 396 CHEMOTHERAPY MAR. 1973 VOL. 21 NO. 2 CHEMOTHERAPY 397 398 CHEMOTHERAPY MAR. 1973 VOL. 2 1 NO. 2 CHEMOTHERAPY 399 400 CHEMOTHERAPY MAR. 1973
Jan THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Table 1. Outline of administering doses, routes and sampling times *: 4 ml/hr/kg Bacillus subtilis
THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Jan. 1987 Jan. 1987 THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Table 1. Outline of administering doses, routes and sampling times *: 4 ml/hr/kg Bacillus subtilis
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
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
CHEMOTHERAPY APR. 1984
VOL.32 S-3 CHEMOTHERAPY dihydro-4-oxo-7-(1-piperazinyl)-1, 8-naphthyridine- CHEMOTHERAPY APR. 1984 VOL.32 S-3 CHEMOTHERAPY Table 1 Implantation rates and post- implantation survival rates in females mated
CHEMO THER APY Table 1. Background of the volunteers in the phase I clinical trial of ME1207 Table 2. Methods for Phase I clinical trial of ME1207 All doses are expressed in terms of potency as ME1206
Key words:group D streptococci,classification,enterococcal infections, Antibiotic susceptibility,vancomycin
Key words:group D streptococci,classification,enterococcal infections, Antibiotic susceptibility,vancomycin Table 1 Differentiation of group D streptococcia aderived from R.R.Facklam1,2),K.C.Gross-et al3),and
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
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.
1) Chemical name: Fig. 1 Chemical structure of TE-031 (-)-(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-4-[(2, PYranosyl)oxy]-14-ethyl-12,13-dihydroxy-7-meth 6-dideoxy-3-C-methyl-3-O-methyl-a-L-ribo-hexo- oxy-3,5,7,9,11,13-hexamethy1-6-[[3,4,6-trideoxy-3-
CHEMOTHERAPY DEC phvlococcus aureus Staphylococcus Enterococcus faecalis Escherichia Klebsiella pneumoniae Serratia marcescens Pseudomonas cepac
CHEMOTHERAPY DEC. 1988 phvlococcus aureus Staphylococcus Enterococcus faecalis Escherichia Klebsiella pneumoniae Serratia marcescens Pseudomonas cepacia 1 Bacteroides bivius Propionibacterium granulosum
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