Ten patients with moderate or severe bacterial pneumonia with underlying diseases or complications were treated with cefuzonam (CZON) at a daily dose of 2g to 4g.
The clinical effectiveness was good in 9 patients.
No side effects or abnormal laboratory test results were observed in any patient.
These results suggest that CZON may be useful in the treatment of bacterial pneumonia.

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The minimum inhibitory concentrations (MICs) of 5 drugs (ciprofloxacin (CPFX), and 4 drugs used as standard) were determined to investigate antibacterial potencies of CPFX against bacterial strains isolated in 1989 from superficial suppurative foci. The clinical isolates tested included 375 strains from 11 aerobic bacterial species, and 50 strains from 2 anerobic bacterial genera (group) for a total of 425 isolates.
Interpreting MIC level distributions of these drugs as the expression of antibacterial potencies, the results are as follows.
1. When activities of new-quinolone antibiotics were tested, we found that, CPFX expressed far superior antibacterial potency to ofloxacin (OFLX) and norfloxacin (NFLX) against coagulase-negative staphylococci, Enterococcus faecalis, Enterococcus faecium, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Pseudomonas aeruginosa and Peptostreptococcus spp., although the activity of CPFX against Bacteroides fragilis group was weaker than that of OFLX, and CPFX had similar activity against Staphylococcus aureus to OFLX.
2. In comparison to β-lactam antibiotics, CPFX was inferior to amoxicillin (AMPC) against E. faecalis and inferior to AMPC and cefaclor (CCL) against Peptostreptococcus spp. Against all other bacterial species, however, CPFX expressed superior antibacterial potency to AMPC and CCL.
3. Scattered findings of low sensitivity or resistance to CPFX were observed among the S. aureus, E. faecalis, E. faecium, P. vulgaris, M morganii, P. aeruginosa and B. fragilis (group) species, but with an exception of E. faecium, the incidence of resistance strains was low.

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We evaluated combined effects of sulbactam/cefoperazone (SBT/CPZ) with each of imipenem/cilastatin (IPM), cefuzonam, flomoxef, amikacin (AMK) and tobramycin (TOB) against 324 clinical strains.
Through this study, we obtained the following results.
1.Against Serratia marcescens and Enterobacter cloacae, good synergism was obtained by combining SBT/CPZ with IPM, AMK, or TOB.
2.Against Pseudomonas aeruginosa, good synergism was obtained by combining SBT/CPZ with AMK or TOB.
3.When SBT/CPZ was used in combination with IPM, antagonism was observed among about 45% of strains of P. aeruginosa.

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We examined in vitro susceptibilities of 3,109 isolates belonging to 5 species of Proteeae to 2 penicillins, 5 cephems and 2 aminoglycosides. The isolates were collected from 69 hospital laboratories throughout Japan between 1986 and 1988. Minimal inhibitory concentrations were determined using the agar dilution method with inoculation of 10⁸ cells/ml of bacteria.
Proteus mirabilis had marked susceptibilities to the penicillins and cephems tested. Proteus vulgaris and Morganella morganii were similar in their susceptibilities to ampicillin (ABPC), piperacillin (PIPC), cefazolin (CEZ), cefotiam (CTM), latamoxef, gentamicin (GM) and netilmicin (NTL), but M. morganii was slightly more resistant to cefmetazole and ceftizoxime (CZX) than P. vulgaris. Providencia rettgeri also had a susceptibility pattern similar to that of P. vulgaris, except that P. rettgeri showed higher resistances to CZX, GM and NTL. Providencia stuartii had a very similar susceptibility pattern to P. rettgeri, but P. stuartii was much more resistant to GM and NTL than the latter.
Some major defferences on susceptibilities were clearly evident among the 5 species of Proteeae tested. Notable species-specific differences included higher susceptibilities of P. mirabilis to ABPC, PIPC, CEZ and CTM than others and stronger resistances of P. rettgeri and P. stuartii to GM and NTL.

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Clinical efficacy and safety of sultamicillin (SBTPC) in patients with lower respiratory tract infections, mainly pneumonia and bronchitis, have been evaluated in a multicenter trial by 19 institutions in the Kyushu area during a period of 12 months from December 1988 to November 1989.
1. Clinical evaluation was made in 132 patients and efficacy rates of SBTPC were 80.0% (28/35) for pneumonia, 78.5% (73/93) for bronchitis and 100% for the remaining 1 patient with other respiratory tract infections. The overall efficacy rate was 79.1% (102/129).
2. Clinical efficacy rate of SBTPC for respiratory tract infections in patients with underlying diseases such as chronic bronchitis, old pulmonary tuberculosis etc., was 75.0% (60/80) which was not significantly different from the efficacy rate of 85.7% (42/49) in patients without underlying diseases.
3. Of 13 patients who failed to respond to previous antibiotic treatments, 8 (61.5%) were effectively treated with SBTPC.
4. Clinical efficacy rates against infections caused by single species of organisms were 90.9% (10/11) for Haemophilus influenzae, 100% (8/8) for Streptococcus viridans and 100% (3/3) for Staphylococcus aureus. The overall clinical efficacy rate in all cases of monomicrobial infections was 88.6% (31/35), in polymicrobial infection 45.5% (5/11) and the overall efficacy rate in cases in which causative bacteria were identified was 78.3% (35/46).
5. Adverse reactions occurred in 6.8% (9/132) of the patients. The symptoms included allergic reaction in 1 patient, gastrointestinal system disorders in 7 patients and general fatigability in 1 patient. As abnormalities in laboratory test values, elevations of Al-P, GOT, and GPT were observed in 3 patients during the study, but returned to normal after discontinuation of SBTPC administration.
6. SBTPC is a useful antibiotic in the treatment of lower respiratory tract infections under the current medical environment where resistant organisms which produce β-lactamases have been increasing.

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A new injectable cephem antibiotic, cefpirome (CPR), was evaluated clinically in children. CPR was effective in all the 17 evaluable cases with acute bacterial infections including 1 case of purulent meningitis due to Haemophilus influenzae type b. Diarrhea and elevation of serum GOT and GPT were associated with CPR therapy in 2 young infants, although they were mild and transient.
The plasma T1/2 β of CPR was 1.17±0.22 hour safter bolus inlection and mostly excreted in 6 to 8 hours into urine of children with normal renal functions. The data indicate that CPR is safe and efnective, when used in children with susceptible bacterial infbctions.

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Cefpirome (CPR, HR 810), a new parenteral cephalosporin antibiotic, was studied for its pharmacokinetics, bacteriological and clinical effects in the field of pediatrics.
1. CPR was very active against Staphylococcus aureus, Staphylococcus epidermidis, Coagulase-negative staphylococci, Streptococcus pneumoniae among Gram-positive cocci.
Antibacterial activities of CPR were also strong against Branhamella catarrhalis, Haemophilus influenzae, Escherichia coli, Salmonella sp., Klebsiella oxytoca, Enterobacter cloacae, Pseudomonas aeruginosa among Gram-negative rods.
2. The plasma concentration 15 minutes after a bolus intravenous injection of 20 mg/kg was 80.4, ug/ml, and the T 1/2 (β) was 1.03 hours.
Plasma concentrations after intravenous drip infusion over 30 minutes of 20 mg/kg and 25 mg/ kg were 48.3 and 117 μg/ml at the end of infusion, and T 1/2 (8) for these dosage were 1.14 and 1.45 hours.
3. The urinary recovery rates over 6 hours after administration were 45.2-63.9% for CPR.
4. Clinical efficacies of CPR were excellent in 31 patients and good in 30 patients with an efficacy rate of 98.4%.
In bacteriological examinations, causative organisms were eradicated with an eradication rate of 95.7%.
5. As side effects, diarrhea was observed in 5 patients and loose stool in 1 patient with an incidence of 8.2%.
Abnormal values were found in some patients in clinical laboratory tests for eosinophilia, thrombocytosis and an elevation of GOT, GPT and triglyceride.
These findings indicate that CPR will be useful against bacterial infections in pediatrics.

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We conducted a pharmacokinetic and clinical study on cefpirome (HR 810, CPR), an aminothiazolylmethoxyiminoacetamido cephalosporin (ATOIC), and obtained the following results.
1. Concentrations in blood/excretion in urine
We studied pharmacokinetic in children upon intravenous bolus injections and 30-minute and 1-hour intravenous drip infusions in single dosages of lO, 20, and 40mg/kg, andobtained virtually the same results as those found inadult subjects. Upon intravenous bolus injections, mean blood concentrations 30 minutes after administration of 10, 20, and 40mg/kg were26.1, 47.8, and 82.8 μg/ml, respectively, and half-liveswere 1.13, 1.43, and 1.26 hours, respectively. Upon 30-minute intravenous drip infUsion, mean blood concentrations on completion of the drip infusions of 10, 20, and 40mg/kg were 43.2, 106.9, and l63.0μg/ml, respectively, and half4ives were1.15, 1.09, and 1.15 hours, respectively. In addition, upon 1-hour intravenous drip infusion, mean blood concentrations on completion of infusion were27.1μg/ml for 10mg/kg and 475μg/ml for 20mg/kg, and half-lives were l.09 and 1.40 hours, respectively. A clear dose response was observed at all dosages for either administration method. Mean excretion rates in urine in the first 8 hours after administration were 60.6-71.1% upon intravenous bolus injections of 10-40mg/kg, and upon intravenous drip infusion, thevalues were 50.2-83.8% for administration of 10-40mg/kg 6 or 7 hours after completion of drip infusion.
2. Concentrations in the cerebrospinal fluid
Penetration into the cerebrospinal fluid was studied in 2 subjects, and a concentration of 0.28-5.19μg/ml was observed upon administration of 50mg/kg, a moderate degree of penetration compared to the penetration of cephalosporins of group 5 studied up to now.
3. Clinical results
Evaluation of clinical effects of CPR on various types of bacterial infections was conducted in 56 subjects, excluding 3 subjects who had diseases which were excluded from the study. The breakdown was as follows: 3 cases of meningitis, 1 case of septicemia, 25 cases of bronchial pneumonia, 1 case each of tonsillitis and infection of the external acoustic meatus, 2 caseseach of scarlet fever and phlegmon, 8 cases each of lymphadenitis and urinary tract infections, and 5 cases of staphylococcal scalded skin syndrome. Results of excellent or good were obtained in 54 subjects for an efficacy rate of 96.4%.
There were 6 cases of mixed infections (2 cases of Haemophilus influenzae+Staphylococcus aureus, 1 case each of H.ifluenzae+Streptococcus pyogenes and H.influenzae+Branhamella catarrhalis, and 2 cases of H.influenzae+Streptococcus pneumoniae), 37 cases of single infections, 22 cases of Gram-positive cocci (12 cases of S. aureus, 4 cases of S. Pyogenes, and 6 cases of S.pneumoniae), and 15 cases of Gram-negative bacilli (1 case each of B. catarrhalis, Proteus mirabilis, Haemophilus parainfluenzae, Pseudomonas fluorescens, 6 cases of H. influenzae and 5 cases of Escherichia coli). Causative bacteria were confirmed in 43 of 56 cases, eradication of the bacteria was observed during the course of the study in 40 cases, excluding 1 case each of single infections with S. aureus, S. pneumoniae and P. fluorescens which were unevaluable, thus an eradication rate of 100% was obtained. From these clinical results according to individual types of bacteria isolated, it appears that CPR was effective in all cases except pneumonia resulting from S. pneumoniae, for a total of 42 of 43 cases with an efficacy rate of 97.7%.
4. Side effects and clinical laboratory findings
A study of safety was conducted on a total of 59 subjects, including 3 subjects with mycoplasmal pneumonia who were excluded.

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Pharmacokinetics and clinical effects of cefpirome (CPR, HR 810) in children were studied. When 20 mg/kg and 40 mg/kg doses of CPR were administered to 4 children through 30 minutes' drip infusion, half-lives were 1.23±0.23 (mean±S.D.) hours and 1.37±0.35 (mean±S.D.) hours, respectively for the 2 dose levels, and recovery rates in urine in the first 6 hours after administration were 74.8% and 56.1%, respectively. CPR was administered to 15 cases (3 tonsilitis, 3 bronchitis, 5 bronchopneumonia, 1 acute cystitis, 1 coxoiliatitis, 1 otitis media, 1 otitis externa). The efficacy rate was 86.7%. Seven strains of bacteria were isolated and identified 4 Haemophilus influenzae, 3Staphylococcus aureus, 1 Pseudomonas sp. from these cases. These bacteria in children were followed after administration of CPR. Six strains were eradicated and one was reduced in number. No adverse effects of CPR were observed except in 2 cases, one of which showed transient eosinophilia and the other showed a transient increase of transaminase.
These results suggest that CPR may be an effective and safe drug to use on children clinically.

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Pharmacokinetic and clinical studies of cefpirome (CPR) in children were carried out, and the following results were obtained.
1. Peak serum levels were obtained at the end of drip infusion of 20.0, 17.5 and 6.8 mg/kg for 30 minutes and the half-lives were 1.93, 1.91 and 0.48 hours, respectively.
2. Urinary excretion rates in 6 hours were 40.0-96.2%.
3. Thirty-two patients including 17 with respiratory infections, 7 with urinary tract infections and 8 with skin and soft tissue infections were treated with CPR at 52.2-92 mg/kg per day by intravenous administration. Clinical effects were excellent in 12 cases, good in 13 cases, fair in 3cases and unknown in 4 cases, and the overall efficacy rate was 89.3% (25 cases/28 cases).
4. Bacterial eradication rate was 93.8% (15 strains/16 strains).
5. Rash and diarrhea were found in 1 case each, and abnormal laboratory test values were found in 7 cases.

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We conducted a study on the pharmacokinetics and clinical application of cefpirome (CPR) in children.
1. A single intravenous injection of 20 mg/kg of CPR was given to a two-month-old boy, and the concentration of the drug in the blood was measured. Fifteen minutes after administration, the concentration was 53.3μg/ml, and it gradually decreased thereafter, reaching a level of 5.18 μg/ml after 8 hours with a half-life in the plasma of 2.36 hours.
2. A single intravenous injection of 700 mg (50 mg/kg) of CPR and that of cefotaxime (CTX) were given to a girl with suppurative meningitis (3 years old, 14 kg, causative bacteria, Haemophilus influenzae), and concentrations of the drugs in plasma and cerebrospinal fluid after 1 hour were measured. On the second day of illness, the concentration of CTX in the plasma was 39.4μg/ml and the concentration of desacetyl-CTX (D-CTX) was 25.2μg/ml, while concentrations in the cerebrospinal fluid were 6.22μg/ml(15.8%) for CTX and 3.94μg/ml (15.6%) for D-CTX. On the third day of illness, concentration of CPR in the plasma was 59.3μg/ml, while its concentration in the cerebrospinal fluid was 7.44μg/ml (12.5%).
3.CPR was intravenously administered in daily dosages of 37.7-75.0mg/kg in 2-3 portions for periods of 4-15 days to 2 patients with septicemia (causative bacteria, Klebsiella pneumoniae in 1 case and Escherichia coli in the other), 1 patient with bronchitis (K.pneumoniae), 9 patients with pneumonia (1 case of Staphylococcus aureus, 3 cases of H.influenzae, 2 cases of Haemophilus parainfluenzae, 1 case of K. pneumoniae+Pseudomonas cepacia, 2 cases of H. infuenzae+Branhamella catarrhalis), 2 patients with cellulitis (1 case of S.aureus, 1 case, causative agent unknown), 1 patient with suppurative lymphadenitis (causative agent, unknown), 1 patient with staphylococcal scalded skin syndrome, 1 patient with renal abscess (causative agent, unknown), and 1 patient with a urinary tract infection (E. coli), for a total of 18 patients, with excellent results in 9 cases and good results in 9 cases, hence an emcacy rate of 100% was obtained.
4. As an accompanying side-effect, eruption was observed in 1 of the 18 patients, but when administration was discontinued, the symptom gradually receded, and it disappeared by the 4th day. Abnormal laboratory test values observed were 3 cases of eosinophilia, 1 case of thrombocytosis, 1case of elevated GPT, and 2 cases of elevated GOT/GPT, but all of these findings were mild, noneof them required administration to be discontinued, and they normalized after the study was completed.
5. Based on the abovere sults, CPR may be considered effective in the treatment of general infections, and the expected results may be achieved with 3 daily administrations of 20mg/kg.

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This study describes the pharmacokinetic characteristics and clinical usefulness of cefpirome (CPR) in children. Mean half-lives of 20mg/kg and 40 mg/kg of CPR injected intravenously in one shot were 1.18 and 1.34 hours, respectively, and their mean recovery rates into urine were 69.8 and 72.2%, respectively. Minimum inhibitory concentrations of CPR against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Escherichia coli and Haemophilus influenzae were the same as or lower than those of ceftazidime. CPR was clinically effective in 14/15 of patients with bacterial infections; 8/9 of pneumonia, 2/2 of bronchitis, 1/1 of pharyngitis, 1/1 of tonsillitis, 1/1 of osteomyelitis, 1/1 of urinary tract infection. No clincally overt side effects of CPR were found, while an increase of eosinophils in blood was observed in 2 cases, and an increase of platelet in blood in 1 case and an elevation of serum GPT activity in 1 case were also observed. These findings indicate that CPR is useful for the treatment of bacterial infections in children.

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The clinical efficacy and the pharmacokinetics of cefpirome (CPR, HR 810), a new semisynthetic cephalosporin derivative, were investigated in children with various infectious diseases.
CPR showed high blood peak levels, relatively long half-life and high levels in urine.
Excellent clinical efficacy was obtained in 2/3 cases with pneumonia, 3/4 cases with upper respiratory infection, 2/2 cases with cutaneous and soft tissue infection and 1/1 case with urinary tract infection. The overall efficacy rate was 80%.
No clinical adverse effects were observed while slightly elevated GPT and GOT, decreased platelet were detected in 4 cases without clinical problems.
CPR should be an useful and safe drug in treating infectious diseases in children.

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