The antibacterial activity of a new cephem antibiotic cefluprenam (CFLP), was compared with those of ceftazidime (CAZ), cefuzonam (CZON), cefpirome (CPR) and cefozopran (CZOP). The results are summarized as follows.
1. CFLP had a broad and well-balanced spectrum against gram-positive and gram-negative bacteria including MRSA (DMPPC MIC:≤12.5-50 μg/ml) and Pseudomonas aeruginosa. The in vitro activity of CFLP against Staphylococci, Streptococcus pneumoniae, Enterococcus faecalis, most species of the family Enterobacteriaceae, P. aeruginosa, Haemophilus influenzae and family Neisseria was equivalent to or greater than those of CAZ, CZON, CPR and CZOP.
2. CFLP showed a high bactericidal activity against Staphylococcus aureus Smith and Escherichia coli ML 4707.
3. CFLP was quite stable to various types of β-lactamase, but was hydrolyzed by oxyiminocephalosporinase. Due to this highdegree of stability, CFLP exhibited the potent activity of CFLP against β-lactamase-producing strains of Enterobacter cloacae, Citrobacter freundii and Klebsiella pneumoniae.

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Cefluprenam (CFLP) is a novel parenteral cephalosporin with a wide spectrum of potent antibacterial activity against aerobic and anaerobic gram-positive and gram-negative bacteria. MIC₉₀s of CFLP against clinical isolates of Staphylococcus aureus (49 strains), MRSA (48 strains), CNS (43 strains), Streptococcus pneumoniae (20 strains), Streptococcus pyogenes (48 strains), β-streptococci (15 strains), Enterococcus faecalis (38 strains), Enterococcus faecium (42 strains), Escherichia coli CS 2 (R+)(51 strains), Klebsiella pneumoniae (47 strains), Proteus mirabilis (48 strains), Proteus vulgaris (35 strains), Providencia rettgeri (27 strains), Morganella morganii (50 strains), Citrobacter freundii (50 strains), Serratia marcescens (50 strains), Enterobacter cloacae (50 strains), Acinetobacter calcoaceticus (27 strains), Pseudomonas aeruginosa (50 strains), Xanthomonas maltophilia (48 strains), Pseudomonas cepacia (33 strains), ampicillin (ABPC) resistant Haemophilus influenzae (18 strains), Bacteroides fragilis (38 strains), were 12.5, 25, 6.25, 0.025, 0.025, 0.05, 6.25, >100, 0.05, 12.5, 0.1, 3.13, 0.78, 0.1, 3.13, 3.13, 6.25, 25, 25, > 100, 25, 0.78, > 100μg/ml, respectively. CFLP manifested almost the same activity to S. aureus as cefpirome, however, it showed 2 times stronger anti-MRSA activity than cefpirome (CPR) and cefzonam (CZON). Against E. faecalis, CFLP was the most active one of the cephalosporins tested and was at least 8 fold more active than CPR. CFLP was the most active one of the cephalosporins tested against members of the family Enterobacteriaceae, except for K. pnertinoniae and P. vulgaris. Against P. aeruginosa, CFLP was 2-fold more active than ceftazidime (CAZ), and as active as CPR. CFLP manifested greater binding affinities to PBPs 1, 2, 3 and 4 of S. aureus 209P than ceftazidime, and had a greater affinity to PBP 2' of an MRSA strain 108-1 than CAZ. The binding affinities of CFLP to PBPs 2 and 3 of E. coli NIHJ JC 2, S. marcescens 13 and P. vulgaris 33 were stronger than those of CAZ. CFLP showed greater binding affinities to PBPs IA and 3 of P aeruginosa PAO 1 than those of CAZ. CFLP, at rather low concentration, manifested a strong synergy of bactericidal effect on E. coli NIHJ JC 2 with complement. Cultured mouse macrophages well engulfed and digested E. coli cells in the presence of more than 1/8 MIC of CFLP.

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We investigated the susceptibility and clinical efficacy of cefluprenam (CFLP), a new parenteral cephem antibiotic.
1. The in vitro antibacterial activity of CFLP was examined against 239 strains of clinical isolates of 7 species, and compared with those of cefclidin (CFCL), ceftazidime (CAZ), cefixime (CFIX) and cefpodoxime (CPDX).The MIC₉₀s of CFLP against Staphylococcus aureus (MSSA), Escherichia coli, Klebsiella pneumoniae, Serratia mercescens, Proteus mirabilis, Morganella morganii and Pseudomonas aeruginosa were 0.78, 0.09, 0.09, 3.13, 0.39, 0.09 and 50 μg/ml, respectively.
2. The clinical efficacy and safety of CFLP was evaluated on 12 patients, 10 with respiratory infections and 2 with urinary tract infections.CFLP was injected i.v.at a daily dosage of 2 g for 3-14 days.Clinical response was excellent in 2, good in 8, fair in 1 and unevaluable in 1 patient.No adverse reactions were observed, and mild abnormal changes in laboratory findings, leucopenia and elevation of GOT and GPT, were observed in two patients.

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The antimicrobial effects of a new cephem antibiotic, cefluprenam (CFLP), on pathogens as well as its' clinical effects and utility were assessed as follows: The measeured MIC₅₀ of CFLP of 122 isolated strains were: 0.78 μg/ml for 20 strains of Staphylococcus aureus, 0.1 μg/ml for 23 strains of Streptococcus pneumoniae, ≤0.025 μg/ml for 20 strains of Escherichia coli, 0.05 μg/ml for 20 strains of Klebsiella pneumoniae, 0.05 μg/ml for 20 strains of Haemophilus sp., 0.78 μg/ml for 19 strains of Pseudomonas aeruginosa. CFLP was administered at a dose of 1.0 g twice/day for 9-14 days to 11 patients, including 8 cases of acute pneumonia, 1 case each of lung abscess, chronic bronchitis and secondary infection to bronchiectasis. The clinical result was excellent in 3 cases and good in 8 cases. As for the bacteriological effect, 4 strains of isolated S. pneumoniae and 1 strain of S. dysgalactiae disappeared and 1 strain of P. fluorescens decreased. No side effect was observed in any of the cases. Abnormal laboratory findings were observed in 3 cases; elevation of S-GOT and S-GPT in two cases, elevation of ALP in one case.

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The in vitro antimicrobial activity of cefluprenam (CFLP), a novel perenteral cephalosporin developed in japan, and its therapeutic efficacy in the treatment of respiratory tract infections were evaluated. The minimum inhibitory concentrations (MICs) of CFLP, cefpirome (CPR), ceftazidime (CAZ) and flomoxef (FMOX) against a total of 138 strains consisting of six different species: methicillin-susceptible Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens and Pseudomonas aeruginosa were determined by the micro-broth dilution method using the Dynatech MIC 2000 system.As shown by MICs CFLP was more active than reference antibiotics against MSSA, MRSA, E. cloacae and P.aeruginosa. CFLP was more active than CAZ, and as active as CPR and FMOX against E. coli and K. pneumoniae. Against S. marcescens CFLP was more active than CAZ, but less active than CPR. A dose of 1g (12 cases) and 2g (3 cases) respectively of CFLP was given daily to a total of 15 patients for 4 to 14 days (mean: 11.2 days): 4 patients with pneumonia, 8 patients with infection associated with bronchiectasis, and one patient each with lung abscess, diffuse panbronchiolitis and infection associated with lung cancer. The clinical effects were excellent in one patient, good in nine patients, fair in one patient and poor in three patients (efficacy rate: 71.4%).One case was excluded from clinical evaluation because signs and symtoms of infection were not clear. Six strains were identified as causative organisms: Two strains of P. aeruginosa and one strain each of Streptococcus pneumoniae, Moraxella catarrhalis, Heamophilus influenzae and E. coli. CFLP eradicated all of them except for one strain of P. aeruginosa.Drug fever, drug exanthema et elevation of s-GPT as well as leucocytopenia, elevation of LAP, and a decrease of Hb et Ht were observed in one patient each.All of these adverse effects disappeared after completion of therapy.From the above results, we conclude that CAZ is a useful antibiotic for parenteral use as a first choice in the treatment of respiratory tract infections.

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We performed the basic and clinical study on cefluprenam (CFLP), a new parenteral cephalosporin.The in vitro antibacterial activity of CFLP was compared with those of cefozopran (CZOP) and ceftazidime (CAZ) against recent clinical isolates.CFLP showed a broad antibacterial spectrum against gram-positive and gram-negative bacteria.Against Staphylococcus aureus, Enterococcus faecalis, and members of the family Enterobacteriaceae, except for Serratia marcescens and Proteus vulgaris, CFLP was 2-to 4-fold more active than CZOP The activity of CFLP against Pseudomonas aeruginosa was almost the same as that of CZOP and was about 2-fold higher than that of CAZ.The in vitro synergistic activities of CFLP in combination with cefazolin (CEZ), cefotiam (CTM), and fosfomycin were examined against methicillinresistant strains of S.aureus (MRSA). Combinations of CFLP plus CEZ and CFLP plus CTM demonstrated synergy against 70 and 80 % of the MRSA strains, respectively.CFLP was administered to 27 patients with various infections, consisted of 3 with sepsis, 1 with sepsis suspected, 8 with pneumonia, 1 with lung abscess, 3 with bronchopneumonia, 4 with acute bronchitis, 5 with chronic bronchitis, 1 with bronchiectasis and 1 with pyelonephnitis. The overall efficacy rate was 95.5%(21/22).Skin rash was observed in 1 patient. Eosinophilia and elevations in S-GPT were observed in three patients, respectively.

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We performed fundamental and clinical studies on cefluprenam (CFLP), a new parenteral cephalosporin antibiotic, and obtained the following results.
1) The plasma concentrations and urinary excretions of CFLP and ceftazidime(CAZ)were compared by i.v.injection at a dose of 1.0 g each to five healthy adult volunteers.The half-life β-phase was 2.07±0.32 h for CFLP and 1.80±0.11 h for CAZ.The urinary excretion rate within 24 hours was 93.9±2.4% for CFLP and 93.6±3.8% for CAZ.When probenecid was administered to the volunteers before CFLP dosing, plasma levels and urinary excretions were not affected.These results suggested that main excretion route of CFLP was glomerular filtration.
2) Eight patients; three with pneumonia, one with lung abscess, one with acute bronchitis, one with chronic bronchitis, one with bronchiectasis with infection, and one with urinary tract infection, were given 1.0 g of CFLP twice a day by drip infusion for 8 to 14 days.The clinical efficacy was excellent in two cases, good in five cases and unevaluable in one case with untargeted disease.Bacteriologicaly, respiratory infection origin Staphylococcus aureus was eradicated, on the other hand, Pseudomonas aeruginosa was persisted.Urinary tract infection origin Proteus mirabilis was eradicated.A slight elevation of S-GOT was observed, but no adverse reaction was observed.

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The in vitro activity of cefluprenam (CFLP), a newly developed cephalosporin antibiotic in Japan, was studied by determining minimum inhibitory concentration (MIC) using the agar two-fold dilution method. All the strains used for this study were isolated from blood of patients admitted to Keio University Hospital. The range of MIC of CFLP against 31 strains of Staphylococcus aureus with the mecA gene, against which the MIC of methicillin was 25μg/ml or more, was from 25 to 100 μg/ml or more. The MIC of CFLP against one strain of S.aureus, against which the MIC of methicillin was 12.5 μg/ml, was 1.56μg/ml.MIC of CFLP against 15 strains of S. aureus, against which the MICs of methicillin were 0.78 and 1.56μg/ml, ranged from 0.39, μg/ml or less to 1.56μg/ml.Out of these 15 strains, 2 strains had the mecA gene.CFLP was more active than cefpirome and equally active to flomoxef and cefuzonam against these 15 strains.The range of MIC of CFLP against 35 strains of Escherichia coli, 17 of Klebsiella pneumoniae, 11 of Enterobacter cloacae and 17 of Pseudomonas aeruginosa were 0.006 or less to 0.78, ug/ml, 0.01 to 12.5μg/ml, 0.025 to 6.25 μg/ml and 0.39 to 50μg/ml, respectively.CFLP was more active than not only ceftazidime but also cefclidin and equally active to cefpirome against E.coli and K.pneumoniae.CFLP was the most active against E. cloacae among these antibiotics CFLP was more active than ceftazidime and cefpirome but was less active than cefclidin against P.aeruginosa.

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We studied a newly developed cephem antibiotic, cefluprenam (CFLP), and obtained the following results.
1) Clinical pharmacological studies of CFLP were conducted in 12 patients aged 70 to 97 years old.The drug was injected intravenously, in a dose of 1.0 g by drip infusion for 60 minutes, and serum and urine levels of cefluprenam were determined by bioassay and high-performance liguid chromatography (HPLC). patients were classified according to creatinine clearance (Ccr) values into group I (n=5, Ccr 65≤) group II (n=4, 30≤Ccr<65), group III (n=3, Ccr<30).The peak serum levels of CFLP did not differ greatly among those of the three groups and young healthy volunteers.However, the T_1/2β of CFLP in aged patients were prolonged according to creatinine clearance values.
2) The serum and sputum levels of CFLP were determined after 60 minutes drip infusion in a dose of 1.0 or 2.0g CFLP. The peak serum levels of CFLP were 112μg/ml for a dose of 1.0g and 99.3 μg/ml for 2.0g.The peak sputum levels of CFLP were 8.92 μg/ml for a dose of 1.0 g and 9.44μg/ml for 2.0g.
3) CFLP was used to treat 33 patients with respiratory tract infections.Clinical response was excellent in 2, good in 23, poor in 7 and undetermined in 1 patient. Clinical side effects, skin rash and fever, were observed in 1 natient. Abnormal changes in laboratory test values, one case each of elevations of GOT, GPT, Al-p, γ-GTP, LAP and BUN, elevation of Al-p and positive direct coombs', were observed.

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The antimicrobial activities of cefluprenam (CFLP) against major pathogenic bacteria of respiratory tract infections were investigated and compared to those of other reference antibiotics.
Serum and sputum levels of CFLP were determinend in two cases with respiratory tract infections.Seven cases with respiratory tract infections were treated with CFLP, and the efficacy and safety of CFLP was evaluated.
1. In vitro activities of CFLP against Staphylococcus aureus (MSSA) and Streptococcus pneumoniae were superior to those of ceftazidime (CAZ), and almost equal to those of cefoperazone (CPZ) and cefmenoxime (CMX).MICs of CFLP against Moraxella catarrhalis and Klebsiella pneumoniae were almost equal to those of imipenem/cilastatin (IPM/CS), CAZ, CPZ, and CMX. MIC of CFLP against Haemophilus influenzae was superior to IPM/CS, and equal to CAZ and CPZ.MIC of CFLP against Pseudomonas aeruginosa was inferior to that of IPM/CS, but superior to those of CPZ and CMX.
2. The peak serum levels (66.4, 101μg/ml) of CFLP in two cases were observed immediately after 60 minutes' infusion of CFLP (1.0g).The peak sputum levels were 5.88 and 3.60 μg/ml, respectively.
3. Clinical efficacy of CFLP in 7 cases with respiratory tract infections were evaluated as excellent in 1 patient, good in 3 patients and poor in 3 patients.Thoraic infiltration was observed in 1 case after three days treatment of CFLP, and eosinophilia was noted in 2 cases, slight and transit elevation of serum GOT and GPT was observed in one case.

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Cefluprenam (CFLP) a new injectable cephem with a broad antibacterial spectrum and potent antibacterial activity, was evaluated in vitro and in vivo antibacterial activities in comparison with those of ceftazidime (CAZ) and cefzonam (CZON).The results were as follows:
1. Antimicrobial activities: Minimal inhibitory concentrations (MICs) against 483 clinical isolated strains including 16 different species were determined by the microbroth dilution method.CFLP showed excellent antimicrobial activities against gram-positive and gram-negative bacteria.The MIC values of CFLP for gram-positive bacteria were almost same as that of CZON, and superior to CAZ. Against gram-negative bacteria, CFLP showed the best antimicrobial activities among the antibiotics tested.
2. The concentrations of CFLP in serum and sputum: CFLP was intravenously administered in a single dose of 1g to a patient with bronchiectasis, and its concentrations in serum and sputum were measured at various intervals by bioassay. The peak concentration of CFLP in serum was 48.4μg/ml at one hour after the administration. The peak concentration in sputum was 6.57μg/ml at 1.5 hours after the administration. The penetration ratio into sputum was 13.6%.
3. Clinical efficacy and adverse reaction: Fifteen patients with respiratory tract infection were treated with CFLP, and overall efficacy rate was 93.3%(excellent in 1 case, good in 13, poor in 1). As to adverse reactions, fever and urticaria were observed in each one patient, and fever, eruption and drug induced pneumonitis in one patient.Whereas, although abnormal laboratory findings were observed in 6 cases, all were mild and transient. From these data, we can conclude that CFLP is a very useful antibiotics for the treatment of respiratory infectious diseases.

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Cefluprenam (CFLP) is a new cephalosporin antibiotic, which possesses potent antipseudomonal and antistaphylococcal activity. We performed laboratory and clinical studies on the drug to evaluate its usefulness in respiratory tract infections. The antibacterial activity of against respiratory pathogenic bacteria was high: its MIC₅₀ and MIC₉₀ of CFLP at 10⁶cfu/ml were 0.013 and 0.05μg/ml against Haemophilus influenzae (42 strains), 0.013 and 0.39μg/ml against Streptococcus pneumoniae (50 strains), 0.39 and 1.56μg/ml against Moraxella catarrhalis (41 strains), 6.25 and >100μg/ml against Staphylococcus aureus (53 strains), 6.25 and 50μg/ml against Pseudomonas aeruginosa (43 strains), respectively. The maximal serum levels of CFLP were 60.3 or 69.3μg/ml after intravenous administration of a single 1 g dose, and 149.7μg/ml after a single 2g dose. The maximal sputum levels of CFLP ranged 3.81μg/ml to 5.75μg/ml in 3 patients with respiratory tract infections and the ratios of maximal sputum levels to peak serum levels were 5.50%, 9.54% and 3.43% in 3 patients during treatment of CFLP. Ten patients with respiratory infections were studied for clinical evaluation of CFLP, which was administered 2, 000mg or 4, 000mg of CFLP daily.Causative organisms were H.influenzae (4), S. pneumoniae (1), M.catarrhalis (1), E.coli (1), and P.aeruginosa (5), 9 out of 12 strains (75%) being eradicated. The clinical therapeutic efficacy was excellent in 3, good in 6, and poor in 1. The overall efficacy rate was 90%(9/10). None of side effect was observed. Laboratory findings showed a slight elevation of eosinophilias. From these results, we concluded that CFLP was one of the effective and useful antibiotic for the treatment of respiratory tract infections.

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We conducted a basic and clinical studies of cefluprenam (CFLP), a new parenteral cephem antibiotic for injection, with the following results.
1. Antibacterial activity:
The minimum growth inhibitory concentrations (MIC) of CFLP against 329 strains of 6 species isolated from clinical materials were measured by the criteria of the Japanese Society of Chemotherapy. Reference drugs were ceftazidime (CAZ), cefuzonam (CZON), flomoxef (FMOX) and imipenem/cilastatin (IPM/CS). CFLP showed potent antibacterial activity, as CZON and FMOX did, against Staphylococcus aureus, Streptococcus pneumoniae and Moraxella catarrhalis. CFLP was the most active among the reference drugs against Escherichia coli and Klebsiella pneumoniae.
2. Serum and sputum levels of CFLP: CFLP (1 g intravenous drip infusion for 60 minutes) were mesured in a patient with acute bronchitis Peak serum level was 66.0μg/ml at the end of drip infusion, and peak sputum level was 2.38μg/ml at 4-5 hour after infusion.
3. Clinical study:
CFLP wan administered 11 patients with respiratory infections at 2g/day b.i.d.for 6-14 days. The clinical efficacy was rated as excellent in 1, good in 5, fair in 2 and poor in 1 patient. No adverse reaction nor abnormal laboratory findings were noted.

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We performed basic and clinical studies on cefluprenam (CFLP), a new cephalosporin antibiotic, and following results were obtained.
1. Antimicrobial activity:
The minimum inhibitory concentrations (MIC) of CFLP against a total of clinically isolated strains of species were measured and compared with those of four cephalosporin (ceftazidime, cefuzonam, ceftizoxime, cefoperazone) using the MIC-2000 System (Dynatech Laboratories).CFLP showed stronger bactericidal activity than other four cephalosporin antibiotics against gram-positive bacteria and gram-negative bacteria. CFLP had wide bactericidal activity against these clinically isolated strains except methicillin-resistant Staphylococcus aureus.
2. 1g of CFLP was drip infused for 30 minutes with pyothorax to measure its serum and sputum levels by bioassay.Peak serum level was 19.1μg/ml at the end of drip infusion.Peak sputum level was 0.87μg/ml at 1-2h after infusion.
3. Clinical study results:
CFLP was given ten patients (pneumonia 7, lung abscess 1, pyothorax 1, bronchiectasis 1) with respiratory infection.The overall efficacy rate was 88.9%(excellent 5, good 3, no change 1, unevaluable 1).Adverse reactions were noted in two patients (Eruption and headache).Mild and trantient elevation in GOT-GPT, and eosinophilia were observed in two patients.
From the above results, we consider that CFLP to be useful antibiotics for the treatment of bacterial respiratory tract infection.

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Antibacterial activities and clinical efficacy of cefluprenam (CFLP), a new injectable cephalosporin, were studied.The following results were obtained.
1. Antibacterial activities
The antibacterial activities of CFLP against 12 species of 446 clinical isolates from the urine were examined and compared to those of ceftazidime (CAZ), flomoxef (FMOX), cefuzonam (CZON), imipenem (IPM).The antibacterial activities of CFLP against methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coil, Klebsiella pneumoniae, Indol-positive Proteus group and Enterobacter spp. were superior to those of CAZ, FMOX, CZON and IPM. Against Enterococcus faecalis and Pseudomonas aeruginosa, CFLP was as active as IPM, and superior to CAZ, FMOX and CZON. Against methicillin-sensitive Staphylococcus aureus (MSSA) and Serratia marcescens, CFLP was superior to CAZ, FMOX and CZON, but inferior to IPM. CFLP showed a poor activity against Enterococcus faecium, as same as other cephalosporins.
2. Clinical efficacy
The efficacy and safety of CFLP were studied on 2 patients with acute uncomplicated pyelonephritis, 34 patients with complicated urinary tract infections, 1 patient with acute epididymitis, and 2 patients with acute prostatitis. CFLP was administered to patients with complicated urinary tract infections in daily dose of 0.5g to 1.0g for 5 days. In 28 cases satisfying the criteria of Japanese UTI Committee, clinical responses were excellent in 11, moderate in 15 and poor in 2 cases, with the overall efficacy rate of 92.9%. The eradication rate in bacteriological response was 91.9% in 34 out of 37 strains. As for adverse drug reactions, skin eruption was observed in 1 case.Abnormal laboratory changes were observed in 1 cases showing elevation in eosinophilia, and 1 cases showing transient elevation in GOT, GPT, ALP.

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The antibacterial activity of the novel injectable cephem cefluprenam (CFLP) and its clinical study was evaluated.
1) Antibacterial activity
The antibacterial activities of CFLP against 11 species, 248 isolates from the urine were examined and compared with those of ceftazidime (CAZ), flomoxef (FMOX) and imipenem (IPM). CFLP showed good activities against gram-positive cocci, especially, against Enterococcus faecalis. CFLP was as active as IPM, more active than the other cephems. On the whole, CFLP had a great activity against gram-negative rods. In particular, against Escherichia coli, Citrobacter freundii, Serratia marcescens and Morganella morganii, CFLP was more active than other compared antibiotics. Against Pseudomonas aeruginosa, the activity of CFLP was equivalent to that of CAZ.
2) Clinical study
In 10 cases with complicated urinary tract infections, being satisfied the criteria of the Japanese UTI Committee, the clinical efficacies were excellent in 4, moderate in 2 and poor in 4, its overall clinical efficacy rate was 60%. In one case with acute uncomplicate pyelonephritis, the clinical efficacy evaluated according to the criteria of the Japanese UTI Committee was good. In 2 cases with epididymitis, the clinical responses evaluated by the attendant doctor, were excellent in 1 and good in 1. No adverse reaction was observed in 16 cases, but the slight elevation in S-GPT was noted on 1 case, which possibly related to CFLP.

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We performed bacteriological and clinical studies on cefluprenam (CFLP), a new parenternal cephalosporin, in urinary tract infections with the following results.
1. The antibacterial activity of CFLP against clinical isolates from patients with urinary tract infections was compared with that of ceftazidime, cefepime, flomoxef and imipenem, Against Staphylococcus aureus and Enterococcus faecalis, antibacterial activity of CFLP was markedly superior to other cephalosporins. And against gram-negative bacteria including P.aeruginosa, that was similar to that of imipenem.
2. Fourteen patients with complicated urinary tract infections were treated with 0.5g or 1.0g of CFLP twice a day for 5 days. According to the criteria proposed by the Japan UTI Comittee, the overall clinical efficacy of CFLP was 80%. Bacteriologically, 16 of 18 strains (89%) were eradicated. Neither adverse reactions nor abnormal laboratory findings were observed.
We concluded CFLP was a useful drug in the treatnent of urinary tract infections.

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The clinical efficacy of cefluprenam (CFLP), a new cephalosporin, was studied in urological field. The drug was administered to 40 patients, including 39 cases with complicated urinary tract infections (UTI) and 1 with acute prostatitis. The drug was given at a daily dose of 1.0 or 2.0g for 5 days by intravenous drip infusion. According to the Japanese UTI Committee's criteria, the clinical efficacy in 30 complicated UTI was excellent in 8, moderate in 14, poor in 8, with the overall efficacy rate of 73.3%. Bacteriologically, 58 of 65 strains (89.2%) were eradicated, including 11 of 13 strains (84.6%) against Pseudomonas aeruginosa and 14 of 16 strains (87.5%) against Enterococcus faecalis. Bacteriological examinations in complicated UTI were performed on day 1 morning of the therapy. The results were as follows;In 7 of 17 cases, the strains isolated prior to treatment were eliminated on day 1, but, from only 1 case, Enterococcus faecium was replaced on day 5. Meanwhile, in another 10 cases, bacterial counts on day 1 were more than 10³cfu/ml. In 7 of 10 these cases, E. faecium was detected on, day 0, 1 or 5. No adverse drug reactions were observed. Abnormal laboratory findings were noted in 3 patients, but all these changes were mild.

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We studied the antibacterial activity and clinical efficacy of cefluprenam (CFLP), a new injectable cephalosporin antibiotic, in urinary tract infections.
1) Antibacterial activity: The MICs of CFLP were measured against 210 clinical isolates of 14 species from urinary tract infections and compared with those of ceftazidime (CAZ), cefoperazone (CPZ), latamoxef (LMOX) and imipenem (IPM).In general, the antibacterial activity of CFLP was superior to those of other compared cephems except for IPM, but slightly inferior to that of IPM.
2) Clinical efficacy: Fourteen patients with complicated urinary tract infection were treated once or twice a day with 0.5g or 1.0g of CFLP. Out of 14, 12 cases were evaluated according to the criteria of the apanese UTI Committee. The overall clinical efficacy rate was 66.7%(8/12). Bacteriologically, 17 of 20 strains (85%) were eradicated.
3) Side effect: No clinical side effects and no abnormal laboratory changes were observed in any cases.

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We studied in vitro antimicrobial activities and clinical efficacy of cefluprenam (CFLP), a new parenteral cephalosporin developed in Japan, and following results were obtained.
1) in vitro antimicrobial activities of CFLP
The antimicrobial activities of CFLP against 360 strains isolated from patients with urinary tract infection (UTI) were measured by the agar dilution method at an inoculum size of 10⁶ cfu/ml and the results were compared with those of ceftazidime (CAZ), flomoxef (FMOX) and imipenem (IPM).The antimicrobial activities of CFLP against methicillin-susceptible Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, coagulase-negative staphylococci and Enterococcus faecalis were inferior to those of IPM, but superior to CAZ and FMOX.Although CAZ and FMOX were not active against E.faecalis, CFLP showed some activity. Against Escherichia coli, Citrobacter freundii, Klebsiella pneumoniae and Proteus vulgaris, CFLP was the most active among four examined drugs. CFLP was more active than CAZ and FMOX against Enterobacter cloacae, Serratia inarcescens and Pseudomonas aeruginosa.As for the antimicrobial activity against Proteus mirabilis, CFLP was highly active but a little inferior to FMOX and CAZ. Based on the resistance of CFLP to hydrolysis by various types of β-lactamase, CFLP revealed stronger activities than CAZ and FMOX against C.freundii and E. cloacae.
2) Clinical efficacy of CFLP in urogenital infections
The clinical efficacy of CFLP was evaluated in one case with uncomplicated pyelonephritis, 16 cases with complicated UTI, two cases with epididymitis. The efficacy of CFLP judged by the chief doctor in one case with uncomplicated pyolonephritis was fair. In 16 cases with complicated UTI, the efficacy according to the criteria proposed by The Japanese UTI Committee was excellent in 5, moderate in 6, poor in 5, and the overall clinical efficacy rate was 68.8%. The clinical efficacy in 2 patients with epididymitis was evaluated excellent in 1 and good in 1 by the chief doctor.
3) Adverse reaction of CFLP
No adverse reaction was observed in these 19 patients. Elevation of γ-GTP level was noted in one case, which was possibly related with administration of CFLP.
These results indicate that CFLP is one of the most useful antimicrobial drugs in the treatment of urogenital infections.

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Basic and clinical study on cefluprenam (CFLP) in the field of surgical infections, especially intraabdominal infections and skin and soft tissue infections were conducted.The activities of CFLP against recent clinical isolates of MSSA, Enterococcus faecalis and Pseudomonas aeruginosa were superior to those of ceftazidime, cefpirome, cefotaxime, cefuzonam, cefepime, cefoperazone and flomoxef.Against Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Serratia marcescens and Citrobacter freundii, CFLP was as active as these reference drugs.Sixteen targeted diseases consisted of peritonitis, cholangitis, wound infection, periproctal abscess, lymphangitis, phlegmon and pneumonia.The severity of infections was severe for 8, moderate for 7 and mild for 1 case.Clinical efficacy judged by presiding doctors in 16 cases was excellent for 2, good for 11, fair for 2, poor for 1 case, showing the efficacy rate of 81.3%. Causative organisms were detected bacteriologically in 15 of 16 cases.Clinical efficacy by isolated organisms in 15 cases was excellent for 2, good for 10 and fair for 2, poor for 1 case, showing the efficacy rate of 80.0%.Bacteriological responses in 15 cases were eradication for 5, replacement for 6, partial eradication for 3 and unchanged for 1 case, with the eradication rate of 73.3%.Five of 7 cases showing no response to preceding chemotherapies responsed to CFLP regimen.No adverse drug reaction was noted.Abnormal laboratory change was noted in 1 case showing eosinophilia.

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The pharmacokinetics and clinical studies were undertaken to evaluate the effect of intravenously administered cefluprenam (CFLP) on the surgical infections.
1.Peritoneal exudate was collected for 3 consecutive days through a Foley's balloon catheter inserted to the subphrenic space at the end of surgery.One g of CFLP was administered twice a day to 3 patients after gastrectomy for gastric cancer.CFLP levels in exudate at 1, 2 and 3 postoperative days were 8.0, 11. 1 and 11.1μg/ml in avarage respectively.The relative mean concentration of CFLP was 5.1μg/ml and belonged to the high value group among 30 β-lactams.
2.Concentration of CFLP in choledocus bile was studied on 1 patient of choledocolithiasis after cholecytectomy and T-tube drainage.Bile levels at 1, 2, 4, 6 and 8 hours after CFLP (1.0g) administration were 0.3, 0.3, 1.9, 4.0 and 4.7μg/ml respectively.
3.In the clinical study, 16 patients received intravenous CFLP (1 or 2g), bid for 4-16 days.Sixteen patients consisted of 2 cholangitis, 2 panperitonitis, 5 localized peritonitis, 3 postoperative wound infection, 1 burn wound infection, 1 ileopsoas abscess, 1 abdominal wall abscess and 1 periproctal abscess.The clinical effects were excellent in 2 cases, good in 12 cases, fair in 1 case and poor in 1 case;overall clinical response rate in 16 cases was 87.5%.No adverse drug reaction was noted but slight abnormal laboratory finding in S-GPT was recognized in 1 case.
These results suggested CFLP may be useful drug to surgical infections including intraperitoneal infections.

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We performed basic and clinical studies on cefluprenam (CFLP).The antibacterial activity of CFLP against clinical isolates was compared with those of piperacillin (PIPC), cefoperazone (CPZ), cefpiramide (CPM), ceftazidime (CAZ) and cefuzonam (CZON).MICs of CFLP against coagulase negative Staphylococci (CNS) were ranged from 0.2 to > 100μg/ml and MIC₅₀ was 3.13μg/ml.Against CNS, CFLP showed better antimicrobial activity compared with PIPC, CPZ, CPM and CAZ.Antimicrobial activity of PIPC against Enterococcus faecalis was superior to all other tested antibiotics and CFLP was next. Antimicrobial activities of CFLP against Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa were superior to all other tested antibiotics. One gram of CFLP was administered by drip infusion for 30 minutes to two patients with PTCD and measured serum and bile concentrations.Bile concentrations of CFLP were 10.5 and 10.8μg/ml 1 hour after administration. CFLP was administered to eighteen patients with surgical infections.The cases were 10 cases of peritonitis, 5 of wound infections and 1 of periproctal abscess, cholecystitis and infected biliary fistula.Clinial responses were excellent in 1 case, good in 11 cases, fair in 1 and poor in 5 cases, being an efficacy rate of 66.7%. No side effect was noted except slight increase of eosinophile and serum GPT.

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We investigated the clinical efficacy of cefluprenam (CFLP), a newly developed injectable antibiotic, against various surgical infections.We also studied the drug distribution into wound exudate and bile. The CFLP concentrations in exudate were 13.4±3.2 μg/ml after 1 hour and 6.26μg/ml after 6 hours.The concentration of CFLP in bile was 23.8μg/ml after 1 hour with 30 min drip infusion of 1 g of CFLP. The clinical efficacy of CFLP was evaluated in 10 cases.There was seen good in all cases.The bacteriological response was investigated in 14 strains Gram-positive bacteria (6 strains), Gram-negative bacteria (5 strains), and anaerobes (3 strains) exhibiting 92.9 % of the eradication rate.Although no adverse drug reaction was recognaized, mild abnormal laboratory findings were noted in 1 case.

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We performed bacteriological and clinical studies on cefluprenam, a new parenteral cephalosporin antibiotic, in the field of surgery to determine its antibacterial activity and clinical efficacy.The results were as follows:
(1) Antibacterial activity: The MIC₅₀/MIC₉₀ values (μg/ml) of cefluprenam against surgical lesion isolates of Staphylococcus aureus, Escherichia coil, Klebsiella pneumoniae, and Pseudomonas aeruginosa were 25/50, ≤0.2≤0.2, ≤0.2≤0.2, 1.56/12.5, respectively.
(2) Transport to bile: After intravenous administration of cefluprenam (1 g) to 2 subjects, its maximum concentration in bile was 22.0μg/ml and 6.35μg/ml.
(3) Clinical efficacy: In 5 patients with surgical infections treated with cefluprenam, the response was excellent in 1 patient, good in 2 and fair in 1.In the bacteriological study, the causative pathogens were isolated from 3 patients and eradicated in 2, replaced in 1, and unknown in 2 cases.Neither subjective nor objective side effects were observed.Abnormal laboratory test findings were observed in 1 case with elevated GOT, GPT and ALP.

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As part of a two-part investigation, a pharmacokinetic study was performed with four patients after choledocholithotomy as the subjects.One gram of cefluprenam, a new semi-synthetic parenteral cephem, was administered intravenously over a 30-min period and serial samples of blood and bile were taken. The peak levels of cefluprenam in the plasma were 50.8-124μg/ml at 0.5h after the start of administration, and the levels decreased to 5.4-20.3μg/ml at 6h.The peak levels in the bile were 4.1-16.5μg/ml at 0.5-3.0h.
In the second part of the study, 32 patients were treated.Clinical efficacy was excellent in 20 (62%) infections, good in 4 infections, fair in 4 infections, and poor in 4 infections with an efficacy rate of 75%.
The bacteriological response 34 strains of 24 bacterial species isolated was evaluated.Twenty-nine strains were eradicated and five strains persisted, with an eradication rate of 85%. The bacteriological response of the host was evaluated in 19 infections. Bacteria were eradicated in 10 infections, decreased in two, were replaced in four and persisted in three with an eradication rate of 74%.
The MIC was calculated for 37 strains isolated, and 10 strains (27%) of them required the MIC of 12.5μg/ml to be inhibited.
Abnormal changes in laboratory test results were found in nine. Six such changes involved liver enzymes and of the six patients, five had intra-abdominal infection.Cefluprenam seemed to be effective for surgical infection.

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Pharmacokinetics and clinical effects of cefluprenam (CFLP), a new injectable cephalosporin whch has high activities against Gram-positive cocci to Gram-negative rods, on surgical infections were evaluated in 28 patients.
1) After intravenous drip infusion of CFLP 1g, the tissue levels of CFLP to 7 hours were 5.9-31.3μg/g in the gallbladder tissne, 14.2-46.8μg/ml in the gallbladder bile, 1.6-11.5 in the abdominal skin, 2.5-4.9 in the subcutaneous fat, 2.4-20.5 in the parietal peritonium, 4.0 in the omentum, 3.6-5.2 in the liver, and 10.5μg/g in the stmach.
2) The biliary concentration was determined at a dose of 1g in each patient with an indwelling T-tube or PTCD-tube, showing that peak levels were 4.5 and 12.1μg/ml.
3) When 1g of CFLP was intravenously given to a patient twice a day for 3 days, the ascitic levels after 1 to 6 hours were 18.4-25.1 in the first day, 4.9-19.7 in the second day, and 1.1-16.9μg/ml in the third day.
4) CFLP was administered at doses of 0.5-1g twice a day for 4-10 days to 20 patients including 8 with biliary tract infection, 6 with peritonitis, 1 with intraabdominal abscess, 2 with wound infection, 2 with periproctal abscess, and 1 with suspected sepsis.The clinical efficacy was excellent in 8 cases, good in 10, poor in 1, and unevaluable in 1.The total clinical efficacy rate was 94.7%.Although no side effect was observed, eosinophile in 1 case, increase of GOT and GPT in 1, and increase of GOT, GPT and γ-GTP in 1 were found.It may be said that CFLP is a highly useful drug in the treatment of surgical infections.

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The antibacterial activity and clinical efficacy of cefluprenam (CFLP), a new injectable cephalosporin, were evaluated in the treatment of surgical infections.
1. Antibacterial activity
CFLP showed potent activity against methicillin sensitive Staphylococcus aureus (methicillin, MIC:≤6.25 μg/ml), but the activity against methicillin resistant S. aureus (methicillin, MIC:≥12.5μg/ml) was inferior. The MIC₅₀ of CFLP against coagulase negative Staphylococcus and Enterococcus sp. were 6.25μg/ml. CFLP showed potent activity against gram-negative rods, Escherichia coli, Klebsiella pneuroniae, Klebsiella oxytoca, Enterobacter cloacae, Enterobacter aerogenes and Citrobacter freundii. Against Serratia marcescens, Pseudomonas aeruginosa and Acinetobacter calcoaceticus, the MIC₉₀ of CFLP were 12.5, 50 and 6.25μg/ml, respectively.
2. Clinical study
The clinical efficacy of CFLP in 12 patients: 4 with wound infection, 2 with cholangitis, 2 with phlegmon, 1 with cholecystitis, 1 with panperitonitis, 1 with intraabdominal abscess and 1 with periproctal abscess: was excellent in 3 and good in 9 cases. Neither subjective nor objective side effects were observed. Abnormal laboratory findings were observed with eosinophilia, leukopenia and elevation of BUN.

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We conducted basic and clinical studies on cefluprenam (CFLP), a new injectable cephem antibiotics, in the obstetric and gynecological field. It was found that CFLP penetrate sufficiently in the genital organs (various regions in the uterus, ovary and oviduct) after d.i.v. of 1 g.
Clinically CFLP was administered to 3 patients with obstetrical and gynecological infection at 2g daily for 4-6 days. Clinical efficacy was good in 3. Bacteriological response were eradicated in 1, replaced in 1 and unkown in 1. No adverse drug reaction and abnormal laboratory findings were recognized.

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Fundamental and clinical studies of cefluprenam (CFLP), a new parenteral cephalosporin, in the fields of obstetrics and gynecology were performed, and the following results were obtained.
1. The MICs of CFLP for 90% of the clinical isolates tested were as follows: 0.10μg/ml for Streptococcus agalactiae, 12.5μg/ml for Enterococcus faecalis, 0.025μg/ml for Escherichia coli, 1.56μg/ml for Peptostreptococcus magnus. The MICs of CFLP for 50% of the clinical isolates tested were as follows: 6.25μg/ml for Bacteroides fragilis, 25μg/ml for Prevotella bivia.
2. According to the effects of CFLP on intrauterine infections caused by E. coli in the newly designed rat model, CFLP markedly eradicated E. coli from the genital tissue. And according to the penetration studies of antimicrobial agents, CFLP showed better penetration into the genital tissue than aztreonam and cefotaxime.
3. A clinical study, given 1.0g of CFLP drip infusion twice a day for 5-10 days, was carried out in patients with obstetric and gynecological infections. Clinical efficacy rate was 83.3%(5/6) and bacteriological efficacy rate was 100%(2/2). There were no side effects. As for abnormal laboratory findings, the mild and transient elevation of GOT, GPT, ALP and decrease of WBC were observed.

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Fundamental and clinical studies of cefluprenam (CFLP), newly developed cephalosporin, were performed, and following results were obtained. In the fundamental study, concentrations of CFLP in the serum, female genital organs and retroperitoneal exudate were examined after the intravenous infusion of CFLP. When 1.0g of CFLP was administered by one shot iv injection, peripheral blood consentration of CFLP were 58.7μg/ml to 41.1μg/ml at 13 to 90 minutes after administration. In these cases, CFLP penetarated into the female genital organs at levels 37.5% to 111.6% those of peripheral blood concentration. Peripheral blood concentration of CFLP were determined to 80.6μg/ml to at the termination of drip infusion of 1.0 g of CFLP over a period of 30 minutes, and gradually decreased thereafter. Concentration of CFLP in retroperitoneal exudate reached there maximum levels, 26.6μg/ml, at 120 minutes after drip infusion. In a clinical study, CFLP was administered to 2 patients with obstetrical and gynecological infections such as puerperal endometritis and parametritis following the radical hysterectomy. Clinical efficacy was good in both cases. Bacteriologically, 5 organisms were isolated and except methicillin-resistant Staphylococcus aureu, 4 were eradicated. No side effects were observed, and no abnormal change of laboratory data was observed.

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We performed basic and clinical studies on cefluprenam (CFLP), a newly developed cephem antibiotics, in obstetric and gynecological fields and obtained the following results.
1) The levels of CFLP in the serum of the uterine artery and cubital vein were 54.4μg/ml and 57.0μg/ml in the maximum, respectively at 40 min., after the beginning of CFLP 1g drip infusion for 30 min., and then declined gradually. The tissue concentrations of CFLP in genital organs ranged from 17.2μg/ml to 61.0μg/ml in the maximum after CFLP 1 g drip infusion, followed by a gradual decline, and remaining above 2μg/ml for about 5 hours. The concentration of CFLP transfered into retroperitoneal fluid was reached at the maximum level of 19.4μg/ml at 4 hours after CFLP 1 g drip infusion, then declined and remained at 11.1μg/ml for 12 hours.
2) In our clinical study, CFLP was administered to 11 patients with obstetrical and gynecological infection. The clinical results were good in 9 cases and poor in 2 cases, showing the total effective rate of 81.8%. No clinical adverse reactions were observed in any cases.
These results indicate that CFLP is effective for obstetrical and gynecological infection.

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Basic and clinical studies on cefluprenam (CFLP), a new cephalosporin antimicrobial agent in otorhinolaryngological infections were performed. In basic study, serum and tissue (middle ear mucosa in 17, maxillary sinus mucosa in 3, tonsil, submandibular gland and parotid gland in 1) concentration of CFLP were mesured after intravenous administration of ig at 23 cases of otorhinolaryngological operations. The concentration of CFLP in serum, middle ear mucosa, maxillary sinus mucosa, tonsil, submandibular gland and parotid gland were 17.2-14.0μg/ml, 3.1-64.4μg/g, 4.35-9.8μg/g, 16.1μg/g, 11.8μg/g and 1.8μg/g. In clinical study, a total of 16 patients with otorhinolaryngological infections, comprising acute purulent otitis media, chronic purulent otitis media with acute exacerbation, mastoid abscess, chronic paranasal sinusitis with acute exacerbation, chronic paranasal sinusitis, acute lacunar tonsillitis, peritonsillar abscess, and acute sialoadenitis were administered. Clinical efficasy was excellent in 6, good in 5, fair in 3. Overall efficacy rate was 78.6% excluding 2 cases of unknown. Bacteriologically, 12 strains were isolated in 14 patients, a high eradication rate of 91.7% was achieved. One case of eruption was observed and elevation of GOT in 2 and elevation of basophil in one case with abnormal laboratory findings.

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Pharmacokinetic and clinical studies were carried out with cefluprenam in otorhinolaryngological infection. The results were as follows. The concentration of cefluprenam to the mucousmembrane of middle ear was 11.6μg/g, to the mucousmembrane of maxillary sinus 22.7-33.3μg/g, to the tonsil 7.6-32.4μg/g. The drug was administered to 28 patients. Overall clinical efficacy was very high, 95.7%. There were two patients who had moderate side effect, one was eruption, and the other was abdominal pain. And there was one patient with transient elevation in GPT.

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The effectiveness and safety of the new cephem antibiotic, cefluprenam (CFLP), for infections in the otorhinolaryngological field were evaluated. CFLP was administered to 29 patients at a dose of 1g once or twice a day by intravenous drip infusion. Clinical efficacy rate was 96.2% and as for bacteriological efficacy, the eradication rate was 95.2% in 20 cases. As for adverse drug reactions, rash and nausea were elicited in 1 case. No abnormal laboratory finding was observed in all cases. These results indicate that CFLP is promising for the treatment of infections in the otorhinolaryngological field.

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We conducted a pharmacokinetic and clinical study of cefluprenam (CFLP) against the cases with infectious diseases in otorhinolaryngological field. The results obtained were as follows.
1. The concentration ratios of CFLP in tissue versus serum were 25.7% for palatine tonsil (n=18), 36.8% for maxillary sinus mucosa (n=3), 52.0% for submandibular gland (n=6) and 36.2% for parotid gland (n=3) after i. v. injection of CFLP at a dose of one gram.
2. In the clinical study, patients were given CFLP at a dose of 1 g twice a day by intravenous or drip infusion. In 19 patients with otorhinolaryngological infectious diseases, the overall efficacy rate was 94.1%: excellent in 11 cases, good in 5 cases, fair in 1 case and unevaluable in 1 case. The bacteriological eradication rate was 100%. In laboratory findings, an elevation in GOT and GPT was observed in one case. No adverse drug reactions were observed in all cases.

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We conducted a basic and clinical evaluation on a newly injectable cephalosporin, cefluprenam (CFLP) in the ophthalmological field and results were obtained as follows.
1) CFLP had broad spectrum against Gram-positive and negative bacteria. The susceptibility distribution of clinical isolates of Staphylococcus aureus (20 strains) stayed with in≤0.19-1.56μg/ml, showing the maximum distribution at 0.39μg/ml. The susceptibility distribution of clinical isolates of Pseudomonas aeruginosa (20 strains) stayed between 0.39-≥100μg/ml.
2) When CFLP was administered intravenously to matured white rabbits at a dose of 50mg/kg, the peak aqueous humor level was 4.1-4.2μg/ml after 15-30 minutes. At the time of 30 minutes after dosing, the ocular tissue levels were 6.8±0.1-53.4±0.4μg/g in extraocular tissues and 0.6-16.6±1.2μg/g in intraocular tissues.
3) Penetration of CFLP into human aqueous humor of anterio chamber were detected that the concentrations were 0.69-2.7μg/ml at 60-120 minutes after CFLP administration 1g dose d.i.v. High CFLP concentration in lacrimal sac of human was obtained as 15.6μg/g at 3 hours after CFLP administration 1g dose d.i.v.
4) CFLP was administered intravenously 1 g twice a day to 29 cases consisting of 1 blepharitis, 7 dacryosystitis, 13 corneal ulcer, 1 endophthalmitis, 4 panophthalmitis and 3 orbital cellulitis. Clinical responses were excellent in 11 cases, good in 13 cases, poor in 4 cases and unevaluable in 1 case showing the efficacy rate of 85.7%. Adverse drug reactions noted in 2 cases and abnormal laboratory findings recognized in 6 case.

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The clinical efficacy and safety of cefluprenam (CFLP), a newly developed cephalosporin antibiotic, on infections associated with hematologic disorders were investigated in 1 patient with sepsis, 4 with sepsis suspected, 3 with acute pharyngitis, 1 with acute bronchitis and 1 with bronchopneumonia. CFLP was administered by intravenous drip infusion at a dose of 1.0 or 2.0 g twice a day for 6-19 days. Clinical responses were excellent in 4, good in 1, fair in 1 and poor in 2 cases. Skin rash was observed in 1 patient. Abnormal laboratory findings were observed in 2 patients.

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We evaluated the clinical efficacy and safety of cefluprenam (CFLP), a new injectable cephem antibiotic, at a dose of 1.0 g twice daily for 4-15 days in 7 patients with bacterial pneumonia.The clinical efficacy was excellent in 1 patient, good in 5 and poor in 1. Streptococcus pneumoniae were isolated from 3 patients, and all strains were eradicated after CFLP administration. Two cases of skin rash were observed, and a mild elevation of GOT and GPT was observed in 1 case.

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Clinical efficacy and safety of cefluprenam (CFLP), a new cephem antibiotic for injection, was investigated in 6 patients with respiratory tract infections.CFLP was administered to the patients by intravenous drip infusion at a dose of 1 g twice a day for 4 to 11 days.Clinical response was good in 3 patients and poor in 3 patients.Two strains of causative organisms were isolated from one patient.One of two strains, Acinetobacter calcoaceticus was eradicated, and the other strain Staphylococcus aureus (MRSA) was persisted. Skin rashes were observed in 2 patients, and mild abnormal laboratory findings were observed in 2 patients.

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We evaluated the clinical efficacy of cefluprenam (CFLP), a new injectable cephalosporin antibiotic, on 7 cases of respiratory tract infections. CFLP was injected i.v.at a daily dosage of 2.0 g on 2 patients with pneumonia, 1 with acute bronchitis, 3 with chronic bronchitis and 1 with pulmonary fibrosis with infection. Clinical response was good in all patients. Haemophilus influenzae and Staphylococcus aureus were isolated as causative organisms, and H.influenzae was eradicated, but S.aureus was persisted.Loose bowel and rash were observed in two different patients.Eosinophilia was noticed in 3 patients.

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Clinical efficacy and safty of cefluprenam (CFLP) was evaluated on 3 patients with bronchiectasis, bronchiectasis+pyothorax and chronic bronchitis.CFLP was administered intravenously at the dosage of 1 g twice a day in the morning and evening.Clinical response was good in 1 case and poor in 2 cases. The causative organisms isolated were 1 Klebsiella pneumoniae and 2 Pseudomonas aeruginosa. K.pneumoniae was eradicated, but 2 P.aeruginosa were decreased or replaced with Pseudomonas cepacia and Staphylococcus. aureus.Any adverse drug reactions and abnormal laboratory changes were not noted.

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We studied the clinical usefulness of cefluprenam (CFLP), a newly semi-synthesized injectable cephem antibiotic, on 18 infection episodes of 16 patients with respiratory tract infections.The clinical efficacy was evaluable on 15 episodes, and was excellent in 4, good in 7, and poor in 3.In 1 infection episode, it was unevaluable because of side effect.The causative organism was eradicated in 7, decreased in 2, and no change in 2. Side effect was observed in 2, eruption in 1 and nausea and diarrhea in 1. No abnormal laboratory findings were noticed.These results suggested that CFLP is one of the most useful antibiotics for the treatment of respiratory tract infections.

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The clinical efficacy and safety of cefluprenam were evaluated in 6 patients with respiratory tract infections: 2 with pneumonia, 3 with chronic bronchitis and 1 with bronchiectasis.The drug was administered to 6 patients in a daily dose of 2 g for 8-14 days.The clinical efficacy was “good” in 1 and “poor” in 1 with pneumonia, “good” in 3 with chronic bronchitis, and “good” in 1 with bronchiectasis. Bacteriologically, 2 strains of Streptococcus pneumoniae and 1 strain of Haemophilus pneumoniae were detected in sputum, and all strains were eradicated.One strain of Acinetobacter junii was detected after the treatment. Skin rash was observed in 1 case, and slight increase of eosinophils in 2 cases.

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We evaluated the clinical efficacy and safety of cefluprenam, a new injectable cephem antibiotic, on 4 patients with pneumonia, 1 with interstitial pneumonia with infection, 2 with diffuse panbronchiolitis, 2 with pyelonephritis and 1 with phlegmon.Clinical effects were excellent in 1 patient, good in 8 and poor in 1. Exanthema was observed in 1 patient.Abnormal laboratory findings were observed in 2 patients.

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We evaluated the clinical efficacy and safety of cefluprenam, a new injectable cephalosporin antibiotic. Cefluprenam was administered to 10 patients at a dose of 1.0 g twice daily for 7-21 days.Clinical response was good in 9 patients and fair in 1 patient.Adverse reactions were observed in two patients, and eosinophilia was observed in one patient.

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Cefluprenam is a new injectable cephalosporin antibiotic with a broad and potent antimicrobial activities against gram-positive and negative organisms.Cefluprenam was administered to 8 patients with pneumonia and 1 with cholecystitis at a dose of 1.0 g twice a day for 5-14 days by intravenous instillation. Six of the seven patients responded well to the therapy.As to adverse reaction, skin eruptions were observed in three patients, but it was alleviated rapidly following a cessation of the therapy.As to abnormal laboratory findings, a mild elevation of S-GOT and a eosinophilia were observed.

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A newer injectable cephalosporin, cefluprenam (CFLP) was evaluated on 8 patients (6 males, 2 females) aged 43-84 years old with their consent for enrollment in this trial.Enrolled diseases were consist of 7 bacterial pneumonia and 1 mycoplasma pneumonia.When excluding 1 mycoplasma pneumonia case and 1 case of with ileus, clinical responses were as follows, excellent in 2 cases, good in 3 cases, fair in 1 case.A causative organism was not detected in all cases.As for adverse drug reactions, a skin rash was noted in 2 cases and drug fever was noted in 1 case.On the basis of these results, CFLP seemed useful in the treatment of bacterial pneumonia but its light adverse reactions.

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Clinical efficacy and safety of cefluprenam (CFLP), a newly developed injectable cephalosporin, on respiratory infections were investigated.The subjects were 9 patients with pneumonia, 1 with lung abscess, 1 with pleurisy and 3 with bronchiectasis.One of 14 patients was excluded from subjects, because the patient was clarified to pulmonary tuberculosis during the treatment.All the 13 patients received CFLP at a dose of 1.0 g twice a day for 7-12 days.Clinical efficacy was excellent in 2 patients, good in 10 patients and fair in 1 patient.Skin rash and drug fever was observed in one patient, and mild abnormal laboratory findings were observed in 2 patients.

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Laboratory and clinical studies were conducted for cefluprenam (CFLP), a new injectable cephem, with the following results.
1) Antibacterial activity: The antibacterial activity of 181 strains of 7 species (clinical isolates) were compared with those of ceftazidime (CAZ), flomoxef (FMOX).Antibacterial activity of CFLP against Staphylococcus aureus was superior to that of CAZ and was equal to that of FMOX.Antibacterial activities of CFLP against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Morganella morganii were superior to those of CAZ, FMOX, and it was superior to that of FMOX and equal to that of CAZ against Serratia marcescens, but it was weak against Pseudomonas aeruginosa.
2) Clinical study: Ten cases of respiratory infections (pneumonia 5, pulmonary abscess 1, bronchiectasis 2, secondary infection of pulmonary emphysema 1, secondary infection of pulmonary fibrosis 1) were studied in a clinical evaluation of CFLP.Clinical responses were excellent in 2, good in 5, poor in 2 cases, and not evaluated in 1 case.As for adverse reactions, eruption in 1 case and diarrhea in 1 case were observed. Eosinocytosis was noted in 1 case and an elevation of transaminase was noted in 1 case and an elevation of GOT, direct Coobms (+) was noted in 1 case.

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