Cefotetan (CTT) was administered to 97 patients of infections and laparotomies such as operation of abdominal cesarean section, abdominal hysterectomy and ovarian cancer section in the field of obstetrics and gynecology, and acute phase reactants (APR) in the patients were measured daily. The results obtained are summarized as follows:
1. Values of α₁-acid glycoprotein (α₁-AG), haptoglobin (Hp) and C-reactive protein (CRP) were measured as the factors of APR before and after the operation. Values of α₁-AG in patients before the operation were 44.04-56.62mg/dl, and rose to high values, 85.73-416.33mg/dl, after the operation determined on 7th day and then declined to values of 69.40-99.93mg/dl. Hp values showed similar tendency to those of α₁-AG values but they were usually higher than α₁-AG values. Although changes in values of CRP observed also were similar, they returned more rapidly to the level before the operation then other parameters.
2. CTT was clinically effective in all the cases examined. No side effects and no abnormal findings in laboratory examinations were observed. Based on the above results, the measurement of APR values after the operation appeared to be clinically useful to indicate degrees of recovery from the operation and the occurrence of multiple infections.

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A multi-center open study was conducted to investigate cefuzonam (CZON, L-105) regarding to its pharmacokinetic, bacteriological and clinical aspects in the field of obstetrics and gynecology with the participation of 31 medical institutions and the related facilities. The results are summarized as follows.
1. Peak MICs of CZON for Staphylococcus aureus, coagulase (-) staphylococci, Escherichia coli, Klebsiella pneumoniae, Bacteroides fragilis group, Peptostreptococcus spp. isolated from obstetrical and gynecological infections with relatively high frequencies were 0.39, 0.20, 0.024, 0.024-0.05, 12.5, 0.20μg/ml, respectively, with an inoculum size of 10⁶ CFU/ml.
2. When 1g of CZON was given through bolus injection, the maximum concentration (C_max) of CZON in pelvic dead space exudate was 18.7μg/ml at 60.9 minutes (T_max) after the injection; C_max's in all female genital tissues were observed at 0.6-27.9 minutes and ranged from 11.9-26.3μg/g. The C_max 8.3μg/ml, in the pelvic dead space exudate was noted at 97.0 minutes after the end of the intravenous drip infusion of 1g over 1 hour, and C_max's in genital tissues were 14.3-30.0μg/g at the end of infusion.
With 1 hour drip infusion of 2 g, C_max's in genital tissues were 35.0-53.9μg/g at the end of infusion.
3. The clinical efficacy of CZON was evaluated in 206 evaluable patients with obstetric and gynecologic infections. Efficacy rates classified by types of infections were 97.1% (67/69) for intrauterine infections, 81.6% (31/38) for intrapelvic infections, 91.8% (45/49) for adnexitis, 95.2% (20/21) for infections of the external genital organs and 86.2% (25/29) for other infections.
4. Side effects were observed in 7 of the 262 patients: eruption in 6 cases, itching in 2, diarrhea in 1. Abnormal laboratory test values were noted in 9 of the 256 patients. Most of them were slight elevation of hepatic function values
CZON showed satisfactory clinical efficacy and potent antibacterial activity, hence it appears that CZON will be a very useful antibiotic for obstetric and gynecologic infections.

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Cefuzonam (CZON) was given intravenously at a 1 gram dose to 24 patients prior to abdominal total hysterectomy for uterine myoma. Concentrations of CZON in the serum of cubital vein, uterine artery, and in tissues of uterus and adnexa uteri were measured by the bioassay method.
Bilateral uterine arteries were clamped at 15 and 30 minutes and 1, 2, 4 and 6 hours after the administrations of the drug. Measurements were done on 4 patients at each sampling.
Concentrations of CZON in the serum of cubital vein and uterine artery changed in a similar manner with respective half-lives of 52.0 minutes and 48.2 minutes.
Peak concentrations in oviduct, ovary, endometrium, myometrium, cervix uteri and portio vaginalis were reached at 15 minutes after drug administration. The peak concentration in the ovary was as high as 37.5μg/g, and those in other tissues varied between 17.6 and 25.5μg/g. Tissue concentrations decreased gradually after their peaks in similar manners to those in serum, and their half-lives ranged between 37.4 and 53.7 minutes.
From these results, it was found that CZON was transfered to female genital organs in high enough concentrations to inhibit growth of bacteria which were often isolated from the pelvic inflammatory diseases, and CZON seemed to be highly effective to clinical pelvic inflammatory diseases.

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Cefuzonam (CZON, L-105) was used clinically for the treatment of obstetrical and gynecological infections at a dosage of 1g once or twice daily by intravenous drip infusion. The results obtained are summarized as follows.
1. Clinical effects of CZON were analyzed in 10 patients, including 5 patients with intrapelvic infections, 3 with intrauterine infections, and 1 each with adnexitis and an external genital infection. Excellent responses were observed in 1 patient (11.1%), good responses in 7 (77.8%), poor responses in 1 (11.1%), and one remaining case was unevaluable. The efficacy ratio was 88.9%.
2. Upon the treatment, eradications of causative bacteria were observed in all 4 cases tested. Staphylococcus sp.(2 strains), Staphylococcus epidermidis (1 strain), Klebsiella oxytoca (1 strain) and Pseudomonas putida (1 strain) were all eradicated by the CZON treatment.
3. The safety of the drug was analyzed in the 10 patients and rash occurred in 1 patient as a side effect.
4. One patient showed eosinophilia after the CZON treatment. It appeared that CZON would be useful for the treatment of obstetrical and gynecological infections.

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Cefuzonam (L-105, CZON), a new β-lactam antibiotic, was studied for its transfer into intrapelvic tissues and for clinical efficacy in the treatment of obsterical and gynecological infection.
1. Following an intravenous 1 hour drip infusion of 1g, the transferred CZON into uterine tissues reached and was maintained at effective concentrations which were defined as levels exceeding MICs against clinical isolates frequently obtained from patients in the field of obstetrics and gynecology. The peak concentration of CZON in the pelvic dead space exudate was estimated to be 20μg/ml at 0.5-1 hour after infusion.
2. Subjects studied were 5 patients with the following infections: pyometra (3 cases), puerperal intrauterine infection (1 case), vaginal cuff infection (1 case). Clinical efficacies were good in 4 cases and poor in 1 case. No notable side effects or abnormal laboratory test results were noted.

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Cefuzonam (CZON, L-105), an antibiotic injectable of cephalosporin family, was studied pharmacokinetically, clinically and bacteriologically to examine its distribution to female genital tissues and the activity on infections in the field of obstetrics and gynecology. Maximum concentrations in serum and genital tissues achieved 19-46 minutes after intravenous injection of CZON 1g were 69.6μg/ml for serum, 63.1μg/g for oviduct, 34.2μg/g for ovary, 22.5μg/g for endometrium, 33.4μg/g for myometrium, 30.7μg/g for cervix uteri, and 37.1μg/g for portio vaginalis.
Clinical efficacies on 15 cases of intrauterine infection and adnexitis were proved with 4 cases of ‘marked improvement’ and 11 cases of ‘improvement’, thus the efficacy rate was 100%.
Of 21 strains of aerobes and anaerobes isolated from infectious lesions, 19 strains were eliminated after administration of the drug. No side effects were observed.
From these results of fundamental and clinical studies CZON appeared to be a highly useful drug for the obstetric and gynecological infections.

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A pharmacokinetic and clinical study of ceftizoxime (CZX), a newly developed cephem antibiotic intended for parenteral use, was conducted in premature and newborn infants, and resulted in the following findings.
1. Pharmacokinetics
(1) Average serum half-lives (T 1/2) following a one shot intravenous dose of 20mg/kg of CZX to mature and premature newborn infants in age groups of 0-3, 4-7, 8-44, and 15-30 days were: 4.14, 3.01, 2.57, and 1.98 hours (for mature infants) and 5.26, 4.59, 3.71, and 2.64 hours (for premature infants), respectively, decreasing with ages in days of the infants.
(2) Average T 1/2's after a one shot 10mg/kg dose was similar to that after a 20mg/kg dose. Serum concentrations of CZX were dose-dependent.
(3) T 1/2 after 1-hour intravenous drip infusion revealed a same trend after one shot injection.
(4) Urinary in the first approximately 6 hours recoveries following a 20mg/kg one shot dose to mature and premature newborn infants were as follows: 35% (0-3 days old) and 45-55% (4 days old and older) in mature infants and 30% (0-3 days old) and 45% (4 days old and older) in premature infants.
2. Therapeutic effectiveness
(1) The subjects examined were 112 newborn infants consisting of 83 with infections and 29 who received CZX for prophylaxis. The 83 infants had 86 cases of infections, which were classified as A, when the causative organisms were identified and as B, when the causative organisms were not identified. Rates of therapeutic effectiveness were 95.0% for group A and 95.7% for group B. Bacteriological effectivenesses were studied on 41 strains isolated from group A, and were as high as 89.5% for Gram-positive organisms and 95.5% for Gram-negative organisms.
The rate of successful prophylaxis for the 29 infants was 96.6%.
(2) Side effects did not occur among the 120 newborn infants. Laboratory tests with abnormalities included leukopenia, neutropenia, eosinophilia, thrombocytosis and increased GOT or GPT.
These pharmacodynamic and clinical findings have fully substantiated the satisfactory therapeutic usefulness of CZX in both the treatment and prevention of neonatal infections in the usual dose of 20mg/kg, which is to be given b.i.d. for infants up to 3 days old; b.i.d. or t.i.d. for infants 4 to 7 days old, and t.i.d. or q.i.d. for infants 8 days old and older. The drug can be given in a daily dose as high as 120mg/kg when infection is severe.

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Thirteen neonates and young infants, including 5 infants with very low birth weight, were treated with ceftizoxime (CZX) and its clinical efficacy and side effects were evaluated. The ages of the patients ranged from 0 to 96 days, and their body weights ranged from 580 to 5,050g. Doses given were 20-54mg/kg every 6 to 12 hours for 2.5 to 7.5 days. Two infants with sepsis, one with urinary tract infection, one with sepsis and urinary tract infection, and 1 with fetal infection were considered to have responded satisfactorily to the CZX treatment. The drug was well tolerated and side effects was not apparent.
Pharmacokinetic studies were done on CZX in 8 patients including 4 infants with very low birth weight. Their ages ranged from 2 to 91 days, and body weights from 545 to 5,050g. Serum concentrations at 2 hours after single 20mg/kg intravenous bolus injections were 19.2 to 44.2μg/ml and the levels were 2.11 to 26.3μg/ml at 8 hours. Elimination half-lives of CZX ranged 1.90 to 9.57 hours in these patients. In 2 infants with very low birth weights with ages 7 and 91 days, half-lives were as long as 9.57 and 8.24 hours, respectively. Urinary recovery in 6 hours was 31.9-66.9% in 5 patients. Urine concentrations of the drug in 24 samples collected at various time from the 7 patients ranged from 130 to 3,219μg/ml.
Influence of CZX on the fecal flora was studied in 1 patient given 20mg/kg×4/day of the drug. The characteristics observed during the drug administration were suppressions of Enterobacteriaceae and anaerobic bacteria, and the preservation of Streptococcus and Staphylococcus. The antibiotic concentration was 93.6μg per gram of wet feces. On the fifth day after the cessation of the drug administration, considerable numbers of Bifidobacterium and Enterobacteriaceae appeared in the stool, and antibiotic activity was not detectable.

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Pharmacokinetic and clinical studies of ceftizoxime (CZX) were performed in infants given intravenously. The obtained results are summarized as follows.
1. Serum concentrations of CZX in 2 and 3 day-old mature infants given 20mg/kg by one shot intravenous injection peaked at 49.0 and 57.9μg/ml in 1 hour and decreased to 14.4 and 24.9μg/ml in 8 hours after dosing, respectively. Half-lives were 3.9 and 5.6 hours, respectively. In 5 day-old or older mature infants, peak serum levels ranged from 20.9 to 38.0μg/ml at 1 hour after the injection. Levels of CZX at 8 hours after injection were 1.31 to 7.32μg/ml. Half-lives were 1.6-3.0 hours in all the infants except one.
2. In a 3 day-old premature infant given the same dose by a bolus intravenous injection, the serum level peaked at 45.7μg/ml in 1 hour after the injection. The level at 8 hours after injection was 15.7μg/ml. The half-life was 4.2 hours. In 5-15 day-old premature infants, half-lives were 2.3-3.1 hours in all the infants except one.
3. Serum concentrations of CZX in 1 and 2 day-old infants given 20mg/kg by intravenous drip infusion peaked at 49.4 to 115.0μg/ml in 1 hour after dosing. Half-lives were rather long, 4.0 and 5.1 hours, in the 2 infants.
4. Peak serum levels and half-lives tended to be lower and shorter in 5 day-old or older ones than in the 3 day-old or younger infants.
5. No changes in the serum concentration were observed even after dosing with 20mg/kg of continuous one shot intravenous injection.
6. Urinary recovery rates during the first 8 hours (one is 6 hours, two is 9 hours) after 20mg/kg intravenous bolus injection of CZX tended to be lower in 3 day-old or younger infants than in 5 day-old or older infants.
7. Eleven infants with various bacterial infections were given CZX by intravenous bolus injection or drip infusion. Dosage of CZX used in the present study were 36-148mg/kg/day in 2-3 divided doses. Duration of treatment ranged from 3 to 12 days. Clinical efficacy of CZX was excellent or good in all the infants with acute bronchitis, acute pneumonia, suspected sepsis infected in uterine, acute otitis media, cellulitis, meningitis caused by Klebsiella pneumoniae and Escherichia coli, acute urinary tract infection and periproctic abscess except 1 case of acute bronchitis. 5 species of organisms identified from various cultures of 11 patients were all eradicated after treatment of CZX.
8. Neither systemic nor local adverse effect ascribed to CZX was encountered in any of the infants. Laboratory tests revealed an increase in blood platelet in 3 infants and an elevation of GOT in 1.

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Serum concentrations and urinary recovery rates of ceftizoxime (CZX) were investigated in 13 mature newborns and 16 premature newborns (with ages 1-17 days) after one shot intravenous injection of 10 and 20mg/kg, respectively, for treatment and prophylaxis of various infections. Obtained data were studied comparatively among the 3 groups, i. e. the 1st group (age: 0-3 days), 2nd group (age: 4-7 days) and 3rd group (age: 8 days or older). The clinical investigation was made in 9 male and 6 female newborns aged 3-34 days including 4 pediatrics patients with septicemia (1 with purulent miningitis, 1 with urinary tract infection, 1 with Staphylococcal pneumonia and 1 without complication), 1 with maxillary sinusitis, 5 with bron-chopneumonia and 5 with urinary tract infections.
1. Serum concentrations and urinary recovery rates
(1) Mature newborns given one shot intravenous injection of 10mg/kg
Serum concentrations of the drug in the 1st, 2nd and 3rd groups in 30 minutes after one shot intravenous injection of 10mg/kg peaked at 18.9-23.3μg/ml, without any significant differences, and thereafter gradually declined to 2.10-4.99μg/ml at 8 hours. Serum half-lives were shorter in older subjects and values in the 3 groups were 3.89, 2.99 and 2.35 hours, respectively. Urinary recovery rates ranged from 55.5% to 70.0% at 8-6 hours in the 3 patients.
(2) Mature newborns given one shot intravenous injection of 20mg/kg
Serum concentrations of the drug in the 3 groups peaked in 30 minutes after one shot intravenous injection of 20mg/kg at, respectively, 36.9, 41.4 and 38.4μg/ml, and thereafter they gradually declined to 9.0, 7.3 and 4.5μg/ml at 8 hours, respectively. Serum half-lives were shorter in older subjects and values in the 3 groups were 3.59, 2.93 and 2.49 hours, respectively. Urinary recovery rates ranged from 43.5 to 78.2% within 12 hours in 2 patients, within 8 hours in 2 patients and within 6 hours in 1 patient.
(3) Premature newborns given one shot intravenous injection of 10mg/kg
Serum concentrations of the drug in the 3 groups peaked in 30 minutes after one shot intravenous injection of 10mg/kg at, respectively, 27.9, 21.5 and 23.0μg/ml, and they gradually declined thereafter to 10.8, 6.2 and 6.5μg/ml at 8 hours, respectively. Serum half-lives were shorter in older subjects and values in the 3 groups were 5.28, 4.43 and 4.24 hours, respectively. Urinary recovery rates were 98.5% within 24 hours in 1 patient; 72.1 and 81.5% within 12 hours in 2 patients; and 59.0-79.4% within 8 hours in 3 patients.
(4) Premature newborns given one shot intravenous injection of 20mg/kg
Serum concentrations of the drug in the 3 groups peaked in 30 minutes after one shot intravenous injection of 20mg/kg at, respectively, 49.8, 37.0 and 42.2μg/ml, they gradually declined thereafter to 14.1, 6.6 and 4.9μg/ml at 8 hours, respectively. Serum half-lives were shorter in older subjects and values in the 3 groups were 4.27, 3.02 and 2.06 hours, respectively. Urinary recovery rates were 75.1% within 24 hours in 1 patient; 60.0 and 56.9% within 8 hours in 2 patients; and 53.8-70.6% within 6 hours in 5 patients.
2. Clinical results
CZX was given at dose levels between 21.1 and 175.4mg/kg in 2-4 times in divided portions to 15 patients (18 diseases). The drug was ineffective in only 1 patient with septicemia+Staphylococcal pneumonia. The effectiveness rate was 94%. Pathogens were detected in 13 patients (16 diseases) including 7 diseases caused by Escherichia coli, 2 diseases caused by Klebsiella pneumoniae, 3 diseases caused by Staphylococcus aureus, 1 disease caused by Staphylococcus epidermidis, 2 diseases caused by GBS and 1 disease caused by Streptococcus pneumoniae. All the pathogens were eradicated during the clinical treatment, except S. aureus in 1 patient which did not respond to the drug.

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Pharmacokinetic, bacteriological and clinical studies of ceftizoxime (CZX) were performed in neonates.
1. Serum concentrations and urinary excretion of CZX were investigated in 12 neonates ranging ages from 1 to 27 days (gestational age, 35-41 weeks; birth weight, 2,150-4,030 g) and 2 infants ranging ages from 55 to 57 days (gestational age, 39-40 weeks; birth weight, 2,320-2,650g). Each of the subjects was given a single intravenous dose of 20 mg/kg by one shot.
Serum concentrations of CZX in the neonates were 24.9-53.7 μg/ml at 1/4 hour after intravenous injection, with an average of 40.6±7.6 μg/ml. Serum half-lives of CZX were 1.32-4.75 hours and averaged 2.60±1.06 hours. Serum concentrations ranged from 2.01 to 14.6 μg/ml at 6 hours after injection with an average of 7.70±3.89 μg/ml. In the 2 infants, serum concentrations were 42.0 and 46.2 μg/ml at 1/4 hour (average: 44.1± 3.0 μg/ml), and 2.91 and 5.04 μg/ml at 6 hours after injection (average: 3.98± 1.51 μg/ml). Half-lives were 1.54 hours in 1 infant and 1.93 hours in the other (average: 1.74±0.28 hours). Furthermore, 6-hour urinary recovery rates were 28.5-71.7% (average: 49.3±12.8%) in the neonates and 42.1-55.5% (average: 48.8±9.5%) in the infants.
The above results suggest that the following 3 points are accepted; 1) peak serum concentrations (at 1/4 hour) in neonates were similar to those in infants and older children irrespective of age (days after birth). 2) Serum half-lives of CZX in neonates shortly after birth were 4 or 5 times longer than those in older children, but decreased rapidly with the advance of dayages. The half-life in neonates of 2 weeks of age or so became shorter to about twice the normal value in infants. Furthermore, half-lives of the drug in those at an age of the first half of infancy were similar to those in older children. 3) The urinary excretion rates tended to be somewhat low with neonates soon after birth, but became very similar to those in infants and older children at a relatively early stage.
2. CZX was administered to 3 patients with suspected sepsis, 14 with acute penumonia, 2 with acute bronchitis, 3 with upper respiratory tract infection, 4 with acute urinary tract infection, 1 with acute purulent otitis media, 7 with perinatal infection and 11 for prophylaxis of infection.
The clinical efficacy and the safety of CZX in neonates were investigated. Overall effects of the drug in 29 patients of the above excluding 1 with non-bacterial acute pneumonia, 1 with acute bronchitis, 3 with upper respiratory tract infection and 11 for prophylaxis of infection were “excellent” in 15 patients, “good” in 13 and “fair” in 1, with an effectiveness rate of 96.6%.
Bacteriological responses observed are as follows: 2 of 3 strains of Staphylococcus aureus, 2 strains of Streptococcus agalactiae, 1 strain of Streptococcus pneumoniae and 4 strains of Escherichia coli were eradicated, and 1 strain of S. aureus and 1 strain of Pseudomonas aeruginosa persisted. Thus, the eradication rate was 81.8%.
No side effects were encountered in any of the patients but one who had an episode of diarrhea. The diarrhea subsided with an additional treatment with an antidiarrheic. As abnormal laboratory test values, thrombocytosis was noted in 1 case, elevation of GOT and GPT in 1 and eosinophilia in 2, though these changes were slight.
In conclusion, CZX appeared to be a safe and highly effective antibiotic in neonatal infections.

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Ceftizoxime (CZX) was evaluated for absorption and excretion as well as for therapeutic effectiveness in neonates and premature infants. The following results were obtained.
1. Serum CZX concentrations were determined in 8 neonates or premature infants who were not more than 6 days old.
Serum concentrations of the drug were examined in 6 neonates and/or premature infants after intravenous administration of about 20 mg/kg body weight. Average concentration at 1/2, 2, 4 and 6 hours after administration were 52.3, 36.4, 26.7 and 16.7 μg/ml, respectively. Serum concentrations in the other 2 infants who were given 29.7 and 25.1 mg/kg, were as high as 71 and 94 μg/ml at 1/2 hour and 22.1 and 39 μg/ml at 6 hours, respectively.
Serum half-lives in 5 of the 6 mature neonates ranged from 2.36 to 3.34 hours, with averaged 2.75 hours, but was exceptionally long, 7.92 hours, in the other one. Half-lives in the 2 premature infants were 4.14 and 4.90 hours.
2. The therapeutic effectiveness on bacterial infection was evaluated for 10 newborn infants. Intravenous doses of 16.9 to 24.6 mg/kg were given in b.i.d. or t.i.d. regimen to 4 cases with pneumonia and 2 with septicemia, urinary tract infection and fetal infection each. To 1 infant with septicemia complicated with cephalhematoma, higher doses ranged from 21.8 to 49.8 mg/kg were given t.i.d. or q.i.d. Therapeutic efficacies were assessed as “Excellent” in 3, “Good” in 6, and “Poor” in 1, with an efficacy rate of 90.0%. Eradication of bacteria was complete in 2 infants each with Escherichia coli-induced septicemia or urinary tractinfection.
3. For prophylactic use, the drug was given to 8 newborn infants in intravenous doses of 17.5 to 29.1 mg/kg b.i.d. or t.i.d. and no infection occurred in 7 cases.
4. No adverse reactions were obtained. Slight and transient increases in platelet count, GOT and GPT in 1 case and eosinophilia in another were observed.
5. These results suggested that CZX in an intravenous dose of 20 mg/kg b.i.d. or t.i.d. regimen in newborn infants up to 7 days of age would be effective and safe for the treatment of neonatal bacterial infections.

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Ceftizoxime (CZX), one of the fifth group in cephem-antibiotics classified by FUJII, was administrated intravenously with a one shot dose of 20 mg/kg to neonates and low birth weight infants with ages ranged 4-21 day old and plasma and urinary concentrations and urinary recovery rates of the drug were determined. Clinical, prophylactic and bacteriological effects of CZX were evaluated and adverse reactions and effects on laboratory test values due to this drug were studied in 22 neonates and low birth weight infants (0-76 day old) consisting of 16 cases with various bacterial infections including presumptive cases of bacterial infections and 6 cases with prophylactic administration against infectious diseases. An average CZX daily dose of 55.3 mg/kg was given once or divided into 2-4 times daily (twice: 16 cases, 3 times: 3 cases, 4 times: 2 cases) through intravenous one shot administration for 6 days on the average. The results obtained are summarized as follows.
1. Neonates and low birth weight infants were classified into 3 groups by age: 4-7, 8-14, 15-21 day old. Plasma peak levels of CZX were observed at an average of 5 minutes after administration in all 3 groups with mean values of 58.3, 74.9 and 76.9 μg/ml, respectively, and the 4-7 day old-group showed a lower value than with other 2 groups. Mean values of AUC were 218.9, 221.0 and 197.0 μg·hr/ml, respectively, and no notable difference was observed within each group. Mean values of half-lives of CZX were 3.61, 2.72 and 2.37 hours, respectively, and the younger group tended to have the longer value.
2. Urinary concentrations of CZX ranged 10.9-1,190 μg/ml in all of the 3 groups during 0-2, 2-4, 4-6, 6-8 hours after administration. Mean values of urinary recovery rates during 8 hours of the 3 age-groups were 60.1, 68.7, 56.7%, respectively. The oldest group showed the lowest mean value bacause one of the cases had the lowest value of 34.5% for an unknown reason.
3. Clinical effect of CZX in 16 cases with various bacterial infections and presumptive bacterial infections was evaluated with an efficacy rate of 87.5%. The prophylactic effect was recognized in all 6 cases that were given CZX to prevent infectious diseases.
4. The bacteriological effect was evaluated in only one case with an infection due to Escherichia coli, which was eradicated by the treatment.
5. No adverse reactions were observed in any cases and eosinophilia was seen in 1 case (5.3%) as an abnormal laboratory test value, probably due to this drug.

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Pharmacokinetic and clinical studies of ceftizoxime (CZX) in the perinatal period gave the following results:
1. Peak concentrations of CZX in the maternal serum, umbilical cord serum and amniotic fluid in mothers after one intravenous injection of 1g were, respectively, 70.2 μg/ml at 0 hour; 15.7 μg/ml at 0.5 hour; and 10-30 μg/ml at 3-6 hours. Concentrations of CZX in the neonatal serum were 0.87-13.5 μg/ml during 6-14 hours after parturition. The mean concentration of CZX in the milk in 1-8 hours after injection was 0.32-0.52 μg/ml.
2. Good or excellent clinical efficacy was obtained in 28 of the 29 patients with perinatal infections, with an efficacy rate of 96.6%. Prophylactic effectiveness was obtained in 14 of the 15 patients, with an efficacy rate of 93.3%.
3. No side effects were observed in 44 cases. GOT and GPT values increased slightly in 1 patient. No abnormal values in total serum bilirubin or other parameters were found in any neonates after parturition.
4. The above results suggest that CZX is safe and effective for the treatment and prophylaxis of infection in the perinatal period.

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Bacteriological studies and clinical evaluations of ceftizoxime (CZX) in perinatal period were carried out, and results are summarised as follows:
Antibacterial activities of CZX in amniotic fluid were determined using the broth dilution method, and bactericidal effect on Streptococcus agalactiae, Staphylococcus aureus and Escherichia coli were demonstrated. The bactericidal effect of CZX increased in amniotic fluid and remarkable increases of activities against resistant strains were demonstrated.
The penetration of CZX into mother's milk was low, and it was speculated that the drug transfer to the newborn through breast feeding was very little.
Clinically, CZX was effective in the treatment of perinatal infections without any side effect.
The above results has demonstrated that CZX is a clinically useful antibiotic for the prophylaxis and the treatment of perinatal infections.

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Pharmacokinetic and clinical evaluations of ceftizoxime (CZX) in 3 obstetrical and gynecological clinics have substantiated the therapeutic usefulness of this drug in the relevant specialty. The results are summarized below.
1. The peak serum CZX concentration after drip infusion of 2 g given over 60 minutes was 115.3 μg/ml. The peak CZX concentration in the pelvic dead space exudate was 34.10 μg/ml which was attained 2.02 hours after beginning infusion. Half-lives of CZX in the serum and in the pelvic dead space exudate were 1.64 hours and 3.65 hours, respectively.
2. The passage of infused CZX to the umbilical cord serum was satisfactorily rapid, as evidenced by figures reaching 10 μg/ml or higher at 1 hour and 15 minutes and still as high as 3 μg/ml or higher at 6 hours after administration.
3. The passage of CZX to the milk of mothers receiving this drug was low, and no untoward effect on the infant was likely.
4. CZX would effectively prevent infections due to premature ruptures of membrane.

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Pharmacokinetic and clinical studies were carried out on the use of ceftizoxime (CZX) in the perinatal period. The results obtained are summarized below.
1. Mean maternal serum concentrations of CZX reached 57.3 μg/ml at about 15 minutes after a single intravenous injection of CZX 1 g and then gradually decreased to 13.1 μg/ml in 1 hour and 55 minutes, 3.59 μg/ml in 4 hours and 20 minutes and 0.11 μg/ml in 17 hours and 51 minutes.
CZX in umbilical cord serum was at detectable concentrations soon after administration and peaked to 23.5 μg/ml in 32 minutes. Although the concentrations in umbilical cord serum gradually decreased thereafter, they were higher than those in maternal serum at 3 hours and more after an injection and was 0.41 μg/ml at 17 hours and 51 minutes. The CZX in amniotic fluid became detectable a little later than CZX in umbilical cord serum. The concentration of CZX in amniotic fluid was below 1.00 μg/ml at 30 minutes after administration. Concentrations then gradually increased to 21.3 μg/ml in 1 hour and 55 minutes and, even in 17 hours and 51 minutes, they were as high as 9.44 μg/ml.
2. In the clinical evaluation, CZX was given to a total of 7 cases, i.e., 1 of amnionitis, 2 of puerperal endometritis, 1 of puerperal fever, and 3 of pyelonephritis. The treatment showed satisfactory results, i.e. excellent result was obtained in 1 case, good in 5 and poor in 1 with an clinical efficacy rate of 85.7%.
Microbiological examinations resulted in the isolation of 5 bacterial strains of 4 species and 1 fungal strain from 5 cases. After CZX administration, all bacterial strains were eradicated, but the fungal strain was replaced with a strain of coagulase-negative Staphylococcus.
Neither side effects nor abnormal laboratory test data were observed in any of the cases (mothers and babies) treated with CZX.

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