Ceftizoxime (FK 749, CZX) was evaluated in 24 children with a suspicion of bacterial infection.Of the 17 confirmed bacterial infections, 16 were shown to be effective (effective rate, 94.1%).Thedi agnosis included acute pharyngitis (2), pneumonia (6), staphylococcal empyema (1), cervical purulent lymphadenitis (2), acute enterocolitis (2), acute pyelonephritis (1), S S S S (1) and suspected septicemia (2).The etiologic pathogens recovered were Streptococcus anginosus (1), Streptococcus pneumoniae (1), Staphylococcus aureus (2), Haemophilus influenzae (3), enteropathogenic Escherichia coli (1) etc.A case of suspected Pseudomon2s aeruginosa septicemia was not effectively treated with CZX.
The serum half-life of CZX was 1.36 hours after intravenous bolus injection.A cerebrospinal fluid level of CZX was 6.2 mcg/ml 1 hour after intravenous bolus injection of 1 g (23.8 mg/kg) in a child with inflamed meninges.
No severe adverse reaction was encountered with the CZX therapy.The data suggest that CZX is an excellent candidate for the first choice parenteral antibiotic in the pediatric infections.

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Ceftizoxime, a new cephalosporin preparation, was evaluated for its antibacterial activity, absorption, excretion and clinical effectiveness, and the following results were obtained.
The minimum inhibitory concentrations (MICs) of ceftizoxime against 211 clinical isolates were determined in comparison with those of cefazolin, cefmetazole, cefotiam and 6059-S. Against S. pyogenes (50 strains), ceftizoxime was 1 tube inferior to cefazolin inoculum size of 108 cells/ml, but was 2-3 tubes superior to cefmetazole and 6059-S.Against E.coli (50 strains), ceftizoxime and 6059-S were significantly more active than the other drugs. The susceptibility pattern of Klebsiella sp.(50 strains) to ceftizoxime was similar to that to cefotiam and 6059-S.Against Proteus sp.(50 strains), cefotiam and 6059-S were more active than the other drugs. Ceftizoxime was intermediate in activity, and cefazolin was the least active. Against H.influenzae (11 strains), ceftizoxime was the most active, with concentrations of 0.1 mcg/ml required to inhibit 100% of strains with an inoculum size of 10⁸ cells/ml and 10⁶ cells/ml.
A dose of ceftizoxime 10 mg/kg or 20mg/kg was administered to 15 patients aged from 5 years to 12 years, and serum levels and urinary excretion of the drug were measured.Intravenous bolus injection of the drug in dose of 10 mg/kg and 20 mg/kg yielded mean serum levels of 26.6 mcg/ml and 55.7 mcg/ml at 30 minutes, respectively.The serum levels of the drug, thereafter, declined gradually but still remained 1.3 mcg/ml and 2.7 mcg/ml at 6 hours. The serum half-lives (T1/2) were estimated to be 1.17 hours in dose of 10 mg/kg and 1.31 hours in dose of 20mg/kg.When a dose of 20 mg/kg was infused over a period of 30 minutes, the serum levels attained the peak of 72.4 mcg/ml to 82.4 mcg/ml (mean 79.4mcg/ml) at the end of infusion.The levels, thereafter, tapered to mean levels of 45.3mcg/ml at 30 minutes, 24.7 mcg/ml at 1 1/2 hours, and 3.6 mcg/ml at 5 1/2 hours, with a T 1/2 of 1.22 hours. Meanwhile, when the same dose was infused over 1 hour, the serum levels attained the peak of 59.4 mcg/ml to 68.5 mcg/ml (mean 64.2mcg/ml).The mean serum levels after the end of infusion were 41.3 mcg/ml at 30 minutes, 21.6 mcg/ml at 1 hour and 1.9 mcg/ml at 5 hours, with a T 1/2 of0.97 hours. Urinary recovery of the drug was 69.2% to 79.9% after intravenous injection and 62.3% to 79.9% after drip infusion, most of the given drug was excreted in the first 2 hours after administration.
In our clinical study, 27 children with moderate or severe infections (12 cases of bronchopneumonia or bronchitis, 5 of pyelonephritis, 3 of purulent meningitis, etc.) were treated with ceftizoxime at the daily dose of 30-309 mg/kg for 3-23 days.Clinical response was excellent in 10, good in 9, fair in 5 and poor in 3. The drug was proved to be very effective against infections due to H.influenzae, K. pneumoniae, E.coli and S. aureus.
No serious side effects were observed in any case.

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Fundamental and clinical studies in the pediatric field on ceftizoxime were carried out, and the following results were obtained.
1.In 4 children aged from 3 years to 6 years, the serum concentrations and urinary excretion ofceftizoxime in a dose of 20 mg/kg by intravenous drip infusion over 60 minutes were measured.The peak serum levels were 22.0-84.0 μg/ml (mean 45.0 μg/ml) at the end of infusion. The mean serum levels after the end of infusion were 16.9 μg/ml at 30 minutes, 12.1μg/ml at 1 hour, 6.2 μg/ml at 2 hours, 1.6μg/ml at 4 hours and 0.6 μg/ml at 6 hours, with mean serum half-life (T 1/2) of 1.03 hours. mean urinary recovery rate was 64.9% up to 6 hours.
2.Concentrations of the drug in the cerebrospinal fluid in 1 patient with purulent meningitis at 30 minutes after an intravenous drip infusion of about 33.3 mg/kg were 0.2 to 1.5 μg/ml, which were 8 to 60 times higher than the MICs of the causative organisms.
3.Ceftizoxime was aministered to 38 children with pneumonia, bronchitis, Salmonella enteritis, purulent meningitis, etc. in the daily dose of 44-200mg/kg for 3-19 days.Clinical response was excellent in 24, good in 12, poor in 1 and unknown in 1. The drug was proved to be very effective in 1 case of purulent meningitis due to H. influenzae. As for side effect, eruption was observed in only 1 case.

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Fundamental and clinical studies of ceftizoxime, a new cephalosporin antibiotic, in children led to the following results.
1.Ceftizoxime compared favorably with cefazolin (CEZ) and cefmetazole (CMZ) for in vitro activity against clinically isolated strains of Staphylococcus aureus (31 strains), Escherichia coli (29), Kkbsiella pneumoniae (30) and Pseudomonas aeruginosa (16).While somewhat less active against S. aureus than CEZ and CMZ, ceftizoxime was far more active than these 2 cephalosporin antibiotics against the test strains of E.colt and K. pneumoniai, which included strains resistant to the 2 drugs.Ceftizoxime was not particularly active against Ps.aeruginosa, but this seeming disadvantage was offset by the absolute ineffectiveness of the 2 reference drugs on this obstinate organism.
2.The time course of mean serum ceftizoxime levels in 3 pediatric patients of 5-40 years old given a single intravenous dose of 20 mg/kg was as follows: 45.4 μg/ml at 15 minutes, 40.4μg/ml at 30 minutes, 22.1μEg/m1 at 1 hour, 10.4μg/ml at 2 hours, 2.9μg/ml at 4 hours and 0.9μg/ml at 6 hours. The mean serum half life was 1.12 hours. The mean urinary levels of ceftizoxime at serial 2-hour collection intervals were as follows: 2,477μg/ml for 1-2 hours, 1,235μg/ml for 2-4 hours and 462μg/ ml for 4-6 hours.The mean urinary recovery up to 6 hours was 61.0%.
3.The clinical response of 28 children with infection to ceftizoxime treatment was ‘excellent’ in 22 children, ‘egood’ in 4, and ‘poor’ in 2.These children comprised 11 with acute pneumonia, 3 with acute bronchitis, 4 with acute pyelonephritis, 2 each with acute purulent arthritis and acute enterocolitis, and 1 each with acute purulent tonsillitis, acute purulent lymphadenitis, furunculosis, subcutaneous abscess, subdural abscess and sepsis. The overall rate of effectiveness was 92.9%. Successfully eradicated strains in the bacteriological sense consisted of 4 strains each of H. influenzae and E.coli, 1 strain each of P.morganii, S.pneumoniae and S.pyogenes, 1 of the 2 strains of S.enteritidis, and 1 of the 3 strains of S.aureus. The overall rate of bacteriological effectiveness was 81.3%. No clinical side effects were observed.Changes in laboratory test findings included slightly and transiently elevated GOT and GPT in 1 child and GOT alone in another child.

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The authors have carried out the laboratory and clinical studies of ceftizoxime (CZX), and obtained the following results.
1.The antibacterial activities of CZX were measured by plate dilution method against clinical isolates of S.aureus, E.coli, K.pneumoniae and P.aeruginosa.CZX inhibited the growth of S. aureus at concentrations less than 12.5μg/ral, and the peak of sensitivity distribution was obtained at 3.13 μg/ml with an inoculum size of 106 cells/ml.
And the peak sensitivity distribution of E.coli and K.pneumoniae were obtained at less than 0.1 g/ml and that of P.aeruginosa was obtained at 6.25μg/ml.
2.Phagocytosis was determined by QUM'S method.Phagocytosis of E. coli and K.pneumoniae by human polymorphonuclear neutrophil was more enhanced in the presence of 1 MIC and 1/2 MIC of CZX than of CEZ at 4 and 6 hours after incubation.
3.As for pharmacokinetic study, CZX was given by intravenous injection and drip infusion for 1 hour at a single dose of 10 mg/kg and 30 mg/kg.After intravenous injection of 10 mg/kg and 30 mg/kg of CZX, the mean peak serum levels were 19.1±3.4μ/ml and 69.1 μg/ml at 30 minutes, and halflife times were 1.20 hours and 1.35 hours, respectively.After 1 hour drip infusion of 10 mg/kg and 30mg/kg of CZX, the mean peak serum levels were 28.8±3.6μg/ml and 60.9±5.9μalml at the end of infusion, and half-life times were 1.40 hours and 1.77 hours, respectively.
The mean urinary excretion rates were between 75.3% and 101% up to 6 hours after intravenous injection and drip infusion.
4.CZX was given to 4 cases with tonsillitis, 3 with pneumonia, 1 with enteritis, 4 with U.T.I., totaling 12 cases.
A daily dose of CZX between 350 mg and 2,000 mg was given for 3 to 5 days.
Clinical results obtained were good in all cases. No side effects and abnormal laboratory findings were observed.

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Ceftizoxime (CZX) was given intravenously to 28 children with the following acute bacterial infections; 15 cases of bronchopneumonia, 4 cases of urinary tract infection, 3 cases of purulent meningitis, 2 cases of acute tonsillitis, each 1 case of purulent cervical lymphulenitis and acute tonsillitis, orbital cellulitis, abscess of eyelid, and perforative peritonitis.Out of 28 patients, good clinical responses were obtained in 26 patients, and bacteriological effectiveness was seen in all 14 cases.
Side effects with CZX were observed in 2 cases;1 case was drug fever, and the other case was eosinophilia.
From the above clinical results, CZX is useful antibiotic for treating the pediatric patients with various kinds of bacterial infections.

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Ceftizoxime was tried in children with various infections and the following results were obtained.
1) Serum levels and urinary recovery of ceftizoxime were studied in 6 patients aged from 6 to 10 years.After intravenous bolus injection of 20 mg/kg, the mean serum concentrations were 113.9μg/ml, 47.6 g/ml, 31.8μg/ml, 18.5μg/ml, 6.3μg/ml and 2.1μg/ml at 5 minutes, 30minutes, 1 hour, 2 μ hours, 4 hours and 6 hours, respectively.The average urinary recovery rates of ceftizoxime were 55.1%, 90.9% and 98.3% at 2 hours, 4 hours and 6 hours after the administration, respectively.
2) The therapeutic efficacy was excellent in 11, good in 9 and poor in 2 patients, the efficacy rate being 91%.
3) As for the side effects, elevation of S-GOT and S-GPT, and drug fever were observed in 1case, but disappeared soon after discontinuation of the therapy.

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Clinical studies on ceftizoxime, a new cephalosporin, were carried out in our department.The following results were obtained.
1.Antibacterial activity
Antibacterial activity of ceftizoxime against 7 strains of E.coli, 6 strains of Klebsiella, 6 strains of H.influenzae, 7 strains of E.cloacae and 10 strains of S.aureus, recently isolated from patients, was compared with that of cefotiam, cefmetazole and cefazolin.Ceftizoxime was more active than the other antibiotics against E.coli, Klebsiella, H.influenzae and E.cloacae, but less active against S.aureus.
2.Urinary excretion
Urinary excretion was measured in 2 cases with normal renal function after dosing with 750 mg (35 mg/kg) and 350 mg (17mg/kg) of ceftizoxime by intravenous injection. Urinary recovery rates within 6 hours were 97% and 82% respectively.3.Clinical study
Eighteen children with the following bacterial infections were treated with ceftizoxime;respiratory tract infection (13), acute otitis media (1), acute intervertebral chondritis and tonsillitis (1), chronic cystitis (1), subcutaneous abscess (1) and chronic bacteremia (1).
The dosage was 69-147mg/kg q.i.d.by intravenous injection.The duration of administration was from 3 to 32 days.
The clinical results were excellent in 4 cases, good in 13 cases and fair in 1 case of chronic bacteremia.The overall effectiveness rate was 94%.
Slight elevation of GPT in 1 case and leukopenie (neutropenie) in 1 case were observed, but returned to the normal range immediately after discontinuation of dosing.
It is considered that ceftizoxime is one of the useful first choice antibiotics used for children with bacterial infections.

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Pharmacokinetics and clinical effects of ceftizoxime (CZX), a new cephalosporin antibiotic, were investigated and following results were obtained.
1) Ceftizoxime was given by intravenous injection or drip infusion for1hour at a single dose of30mg/kg.
After intravenous injection, the mean peak serum level of3children was 95.9mcg/ml at15minutes and half-life time was 1.18 hours.
After1hour drip infusion, the mean peak serum level of 3 children was 79.5mcg/ml at the end of infusion and half-life time was1.20hours.
The urinary level was high and the mean urinary recovery rate was69.6%and63.4%up to6 hours after intravenous injection and 1 hour drip infusion, respectively.
2) CZX was administered in dose of39-76mg/kg to7pediatric patients (4cases of purulent meningitis, 2of septicemia with purulent meningitis, and1of aseptic meningitis) by a single intravenous injection.In patients with purulent meningitis, passage into the cerebrospinal fluid was relatively as good as30%of serum level at the same time in the presence of remarkable signs of inflammation, but poor in cases of mild inflammation or aseptic meningitis.
3) Cerebral puncture fluid level in1patient with cerebral abscess was as good as65.5%of serum level at the same time.
4) CZX was given to28cases of respiratory tract infection, 1of tonsillitis with otitis media, 6of scarlet fever, 1each of maxillary sinusitis and bacterial endocarditis, 6of purulent meningitis, 2of septicemia, 5of septicemia suspected, 2ofsepticemia with purulent meningitis, 1each of osteomyelitis, typhoid fever, peritonitis and biliary tract infection, 16of urinary tract infection, 14of skin and soft tissue infection, and1of external otitis, totaling87cases.The mean daily dose of101.6mg/kg wasadministered for an kverage of10days mainly by intravenous injection4times daily.Clinical results obtained were excellent in34cases, and good in46.Bacteriological effectiveness rate was100%.
As for side effects, fever, fever with rash, fever with cough and diarrhea appeared in1each case out of182cases incl, uding95drop out cases.
As for laboratory findings, eosittoPhilia, thrombocytopenia, elevation of GOT, that of GOT with GPT, and that of GOT with LDK appeared in10, 2, 2, 3and1cases, repectively.

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The clinical efficacy of ceftizoxime, a new cephem antibiotic, was evaluated in bacterial infections in children and blood and cerebrospinal fluid concentrations and urinary excretion of ceftizoxime were determined.
1.Blood cencentrations of the drug were determined in6children: 2of them received a single intravenous injection of about50mg/kg and blood concentrations were51ug/ml (40minutes) and55ug/ml (1hour), respectively;3were given20.0-35.7mg/kg intravenously and peak levels of18.1-76ug/ml at 30minutes gradually declined to0.93-3.95ug/ml at6hours with a half-life of0.97-1.37hours and1 was given21.6mg/kg by1-hour drip infusion, and peak level of28.8ug/ml at the end of infusion decreased with a half-life of2.11hours.Urinary concentrations of the drug were determined in2patients: urinary recovery rates up to6hours were48.9%and37.1%, respectively.
2.Cerebrospinal fluid concentrations of the drug were determined in8patients with bacterial or other meningitis following an intravenous in jention of about50mg/kg and were cosidered to be higher than3ug/ml in the acute phase and1ug/ml in the convalescent and clearly exceeded the MIC of the ordinary causative organisms.
3) Nineteen children with the following infections were treated with ceftizoxime: 5patients with purulent meningitis (causative organisms: H.influenzae3, S.pneumoniae1and unknown1), 6with pneumonia including2with complication of pleurisy (S.pneumoniae1, a mixed infection of S.aureus and P.aeruginosa, H.influenzae1, a mixed infection of S.pneumoniae and H.influenzae, K.pneumoniae 1, unknown1), 1with empyema (S.pneumoniae), 1with septic osteomyelitis associated with pneumonia (S.aureus), 2with dubious sepsis (unknown2), 1with leukemia associated with abscess of the lips and dubious sepsis (P.aeruginosa), 2 with pyelonephritis (P.mirabilis1, K.pneumoniae1) and1with gangrenous tonsillitis (H.influenzae).The daily dose for the5patients with purulent meningitis ranged from187.5to300mg/kg divided in4or6intravenous doses;and for the others49.2-120mg/kg in3 or4divided doses given intravenously or by drip infusion over30-60minutes.One patient with probably recurrent purulent meningitis (causative organism unknown) was excluded from the evaluation of clinical efficacy because of indefinite inflammatory findings but was included in the evaluation of adverse reactions.The overall efficacy rate was88.9%, i.e., excellent in3and good in13, and failure in2patients, i.e., 1with septic osteomyelitis associated with pneumonia and the other with leukemia associated with abscess of the lips and dubious sepsis.Delay in defervescence and resumption of negative CRP were recognized in patients with purulent meningitis, in spite of symptomatic improvement, sterile cerebrospinal fluid culture and a normalization of cerebrospinal fluid findings and also irrespective of recurrence, complications, sequelae or adverse reactions.The above observations remain to be clarified and need further evaluation.
4.Skin rash and paroxysmal cough after intravenous injection of the drug developed in2 patients but disappeared after the drug was withdrawn.Abnormal laboratory findings were recorded in10patients and included eosinophilia (4patients) and elevation of total bilirubin (1), GOT (5), GPT (5), alkaline phosphatase (2) and BUN (1).They were all mild and transient.
5.An intradermal skin test of the drug before the trial was negative in all22patients examined.

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Experimental and clinical trials were carried out with ceftizoxime in pediatric infections.Results were as follows.
1.The antibacterial activity of ceftizoxime against clinically isolated organisms was determined. Ceftizoxime was more active than cefazolin, cefotiam and cefmetazole against K.pneumoniae, E.coliand H.influenzae.
2.The serum concentrations of ceftizoxime following intravenous injection of10mg/kg were 16.2, 10.1, 6.2, 1.8μg/ml at30, 60,120,240 minutes after injection, respectively.Ceftizoxime was excreted with the rate of97.2%in the6-hour urine after injection.
3.Twenty-one patients comprising S with urinary tract infection, 16with respiratory tract infection were received ceftizoxime at the doses ranging from32to109mg/kg devided3or4times a day. The results were excellent in8and good in13patients. The rate of satisfactory clinical response was100%.
4.Slight and transient elevation of GPT was observed in1patient. Other side effects were not observed in any of these21patients.

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Laboratory and clinical studies were performed as follows on ceftizoxime (CZX), a new cephalosporinantibiotic.
1.Susceptibility of clinically isolated bacteria to CZX and cefotiam (CTM) or sulbenicillin (SBPC)
Antibacterial activities of CZX and CTM were compared against S.aureus, E.coli, K.pneumoniae, E.cloacae, H.influenzae and E.aerogenes;CZX was compared with SBPC against Ps.aeruginosa.CZX and CTM were nearly equal in activity against S.aureus, but CZX was found to be more active than CTM by1-10tubes against E.coli, K.pneumoniae, E.cloacae, H.influenzae and E.aerogenes. Against Ps.aeruginosa, CZX and SBPC were nealy equal in activity.
2.Serum concentration and urinary recovery
Serum concentrations of CZX were measured in6patients given CZX for prophylactic purpose during cardiac catheterization.In2patients given20mg/kg of CZX intravenously, the average serum concentration was38.9μg/ml at30minutes after intravenous bolus injection.In3patients given10mg/kg of CZX by intravenous drip infusion, the peak average serum concentration was28.1μg/ml at the end of infusion.
Urinary recovery in2patients tested was81.1%and92.5%until6-7hours after intravenous bolus injection.
3.Clinical efficacy CZX was given intravenously to24patients in doses of 30-111mg/kg (57.1mg/kg on an average) t.i.d.or q.i.d.for3-16days (5.5days on anaverage): 1with lacunar tonsillitis, 4with acute bronchitis, 12with pneumonia, 2with enterocolitis, 2with soft tissue infection, 2with lymphadenitisand1with UTI.The overall efficacy rate was 95.8%, i.e., efficacy was excellent in10 (41.7%), good in13 (54.2%), and poor in1 (4.2%).Bacteriological efficacy was excellent, i.e.21of the23strains disappeared.
One patient had mild and transient diarrhea, but no other laboratory abnormalities were observed during treatment.
The above results suggest that CZX is1of the most useful antibiotics for treating pediatric infections, especially due to Gram negative bacteria.

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Pharmacokinetics of ceftizoxime (CZX), a new cephalosporin antibiotic, was investigated in 9 children with normal renal and hepatic function. In addition, the clinical effect of CZX was evaluatedin26pediatric patients with various infections.
In4of the9children with normal renal and hepatic function, intravenous bolus injection of CZX in a dose of20mg/kg yielded a mean peak serum level of36.5μg/ml at1/2hour after infusion, and mean serum levels of12.5μg/ml at2hours and6.0μg/ml at4hours after infusion.The biological half-lives of CZX were estimated to be1.25-2.55hours.In another child, serum levels of CZX at1/2, 2and4hours after intravenous bolus injection in a dose of10mg/kg were19.60, 5.96 and2.06μg/ml, respectively.
The clear difference in dose response between 20mg/kg and10mg/kg reflected the doubled dose levels.
In the remaining4children, drip infusion of CZX in a dose of20mg/kg (1child17mg/kg) over 0.5-1.5hours yielded peak serum levels at the end of infusion.The biological half-lives of CZX were estimated to be0.95-1.50hours.
About80%of CZX was excreted in the urine within6hours after infusion in the4children tested.
Twenty-six pediatric patients with various infections were treated with CZX intravenous doses of 20mg/kg to118mg/kg b.i.d.-q.i.d for3-14days. Of the12patients with acute bronchitis and pneumonia, 5showed excellent response, 6good and 1 fair response. Of the5patients with urinary tract infection, 4showed excellent response and 1good response.One patient each with colitis, tonsillitis and facial cellulitis, pharyngitis showed excellent response and1patient each with purulent thyroiditis and gluteal abscess showed good response.The single patients with sepsis showed excellent response. One patient each with pyothorax, purulent arthritis and cerebral abscess showed poor response. Overall effectivenessrate was84.6%, although22of all26 patients treated had serious underlying diseases such as APL, AML.
A mild increase in GOT and GPT was observed in 1patient during treatment with CZX, and the values returned to normal after discontinuation of the drug.
These results suggest that ceftizoxime is1 of the most important antibiotics for treating a wide range of infections in children as well as in adults.

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A clinical trial with a special emphasis on anaerobic infections was designed for evaluation of the efficacy, safety, and patient tolerance of cefoxitin.
Of the 35 patients who clinically evaluated, 19 had intrareproductive organ infections, 8 had extrareproductive organ infections and 8 had urinary tract infections.Twenty-nine out of the 35 (82.9%) responded satisfactorily to therapy with cefoxitin.The daily dose of cefoxitin for the 35 adult patients (ages ranged from 17 to 62 years) were 1-6g.There were no adverse systemic reactions, nor was any renal or hematologic toxicity noted.
Antibacterial activity tests demonstrated that cefoxitin was active against anaerobic bacteria, especially Bacteroides fragilis.
Cefoxitin is thought to be the drug of choice in the treatment of obstetric and gynecologic infections.

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We conducted a therapeutic trial with cefmenoxime in the field of otorhinolaryngology on a total of 14 subjects including 7 cases of otitis media, 5 cases of peritonsillar abscess, 1 case of chronic sinusitis and 1 case of congenital aural fistula.
1.The effective rate for peritonsillar abscess was extremely high being judged ‘markedly effective’ in 3 cases and ‘effective’ in 2 cases.
2.The effective rate for otitis media was also remarkably high;it was judged effective in 85.7% of the cases.It is thought that this is probably due to the fact that therapy and supervision were carried out on inhospital patients.
3.The 1 case of chronic sinusitis and the 1 case of congenital aural fistula were each judged ‘effective’ and ‘markedly effective’.The only side effect observed was a slight case of skin eruption in 1 of the patients.

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In order to examine the venous blood and bone marrow blood concentrations of cefmenoxime (CMX) and cefotiam (CTM) in man, 1g of CMX or CTM was administered by one shot intravenous injection prior to surgery of the hip joint. At 30, 60,120 and 180 minutes after the administration, venous blood and bone marrow blood were collected from each of 3 patients and the concentrationassayed by the agar well method.
Both CMX and CTM showed excellent distribution to bone marrow blood with peak levels of 50.1 /ml and 50.9μg/ml on the average 30 minutes after administration.
The levels of CMX in bone marrow blood exceeded those in the venous blood at 60 minutes and thereafter and CTM at 30 minutes of administration and thereafter.
It is therefore considered that both CMX and CTM appear to be useful drugs for the prophylaxis and treatment of bone marrow infection, e.g.osteomyelitis.

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Serum and urinary levels of PIPC (sodium piperacillin) in patients with liver disease were investigated.
Serum and urinary levels of PIPC are affected by the degree of liver disease which is estimated most exactly by KICG, and it is available for determination of dose and administration interval.
When PIPC was administered intravenously at a dose of 2g, serum level in patients with liver disease was showed high and prolonged.Therefore this is convenient for PIPC of which biological half life is comparatively short.
In patients with serious liver cirrhosis, PIPC is probably cumulated by continuous administration and in this case, dose and administration interval will be needed to regulate.

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Chronic toxicity study of latamoxef (LMOX, 6059-S) by intravenous administration at dose levels of 100,200 and 400mg/kg daily for 6 months was carried out in adult Beagle dogs.
All dogs of the 6059-S treated groups survived throughout the experimental period without showing any toxic signs other than occasional vomiting. Slight decrease of RBC, Ht, Hb and platelet, and increase of reticulocytes were noted in the 400mg/kg group. Blood chemistry revealed decreased activity of GPT in the 6059-S treated groups, and increased contents of total protein and lipids in the 400mg/kg group. These clinical changes were slight and transient in most instances.
Liver and kidneys weights increased slightly without accompaning any pathological alterations. Inflammatory changes, probably due to mechanical irritation, were found in the subcutis and around the vein at the injection sites in all groups including the mannitol control group.
From these results it is concluded that the maximum nontoxic dose in dogs is in the range of 200 to 400mg/kg when the 6059-S was intravenously administered daily for 6 months.

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The authors have carried out some studies on MOM dry syrup in the field of pediatrics and the results were as follows.
1. After oral administration of MOM at20mg/kg, the serum level peaked at30minutes and MOM could still be detected in the serum at up to 4 hours.The half-life was0.67hour. The urinary recovery rate of MOM was1.43%up to6hours after this oral administration.
2. The clinical efficacy rates with MOM continuous treatment at a daily dose of19.4to50.0mg/kg (almost about30mg/kg) were85.7%for upper respiratory tract infections, 66.7%for lower respiratory tract infections and95.7%for Mycoplasma pneumonia.
3. It was easy to administer MOM orally even to the younger children. Although MOM was administered for4to21days, no side effects were observed locally or systemically except for transient slight diarrhea.
These results confirmed the usefulness of MOM in the treatment of acute respiratory tract infections in children.

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MOM was administered at a daily dose of20to40mg/kg q.i.d.orally to65pediatric patients, These consisted of 37 cases of acute feverish respiratory tract infection, 13 cases of Mycoplasma infection, 1case of scarlet fever and14cases of whooping cough.
Forty pathogenic bacteria were isolated from the37patients with acute feverish respiratory tract infection and1pathogenic bacteria was isolated from the patient with scarlet fever. Thirty-five of these clinical isolates disappeared as a result of MOM administration.
For these65cases, the clinical efficacy was good in51cases (78.5%), fair in5cases (all whoopingcough) and poor in9cases.
Twelve strains of St. pyogenes were isolated from12cases and3of these isolates persisted (25%). Ten strains of S.aureus were isolated from10cases and1of these isolates persisted.Superinfection was observed in3cases, 2of which were the same species.
Although the clinical effect in the40mg/kg/day treatment group was superior to the effects in the 20mg/kg/day and30mg/kg/day treatment groups, the difference was not statistically significant.

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Fundamental and clinical studies were carried out to objectively evaluate the effectiveness and safety of cefmetazole (CMZ) in the treatment of S.aureus infections of the skin, and the following results were obtained.
1. Blisters are induced with cantharis ointment to determine transfer of CMZ and cefazolin (CEZ) into the serosity and skin.The sensitivity of clinically isolated S.aureus was measured to these drugs.
2. In case of CMZ, antibacterial activity, exudate and tissue transfer were favorable, and the serosity and skin concentration of the drug was such that it covered the major portion of MIC distribution of the clinically isolated S.aureus.
3. In the crossover test following one shot intravenous injection of CMZ and CEZ at the doses of1g, drug concentrations in the serosity and skin were higher after CMZ as compared with those after CEZ.
4. Clinical effect of this drug in the treatment of S.aureus infections of the skin in10cases was such that it was markedly effective in4cases, moderately effective in4and slightly effective in2cases. Bacteriological, effect of CMZ was eradication of the bacteria in9cases and change of bacterial flora in1case. In addition, the clinical effect of the drug in2cases in which cephalexin had been ineffective was that it was markedly effective in1and slightly effective in the other.
5.Side effect was not observed in any of the treated cases.
From the above, it was concluded that CMZ is highly useful drug in the treatment of S.aureus infections of the skin.

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Ten patients with postoperative infections were treated intramuscularly with netilmicin, a new aminoglycoside.
Netilinicin was administered either with or without antibiotics. The overall cure rate was60%.
No adverse reaction was appeared in10patients during the course of the treatment.

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Daily150mg or200mg dose of netilmicin (NTL) were administered to26patients with chronic complicated urinary tract infections for5days, and the following results were obtained.
1) Out of26cases excellent response was seen in5cases, good response in 4, and poor response in11. Effectiveness rate was45%. Six cases were excluded from the evaluation.
2) Effective result was not seen in the catheterized group, whereas5excellent and4good cases were observed in the noncatheterized group, resulting60%in effectiveness rate.
3) MICs of NTL against various bacteria were comparative to GM against P.aeruginosa, to AMK against Serratia, and to both GM and AMK against other bacteria.
4) Except a slight local irritation, no subjective side effect was observed.One case showed a slight elevation in hepatic function tests but it was not definitely judged as the side effect due to NTL.

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