Fundamental and clinical studies of ceftizoxime suppositories in pediatrics

Fundamental and clinical studies were carried out on ceftizoxime suppository (CZX-S), and the following results were obtained in pediatrics. In 4 patients of the CZX-S 125 mg-administered group (9.4-9.9 mg/kg), the serum concentration of CZX reached a peak of 5.55 micrograms/ml on the average, 30 minutes after dosing, i.e. at the time of initial blood collection, and decreased gradually to 0.20 microgram/ml 6 hours after dosing. The half-life was 1.09 hours. In 5 patients of the CZX-S 250 mg-administered group (8.4-18.1 mg/kg), the serum concentration of CZX peaked at 7.07 micrograms/ml on the average and then gradually declined to 0.16 microgram/ml 6 hours after dosing. The half-life was 1.00 hour. The urinary recovery rate varied as widely as 6.5-38.0% in all the patients of both groups. CZX-S was given to total 19 patients; 8 patients with urinary tract infection (UTI), 3 with pharyngitis or tonsillitis, 4 with bronchitis, 2 with pneumonia, 1 with otitis media and 1 with staphylococcal scalding skin syndrome. The overall effect of CZX-S in 15 patients was "effective" or better response, with an effectiveness rate of 83.3%, except one who discontinued the drug because of side effects. CZX-S was given to most of the patients weighing 15 kg or higher in a dose of 250 mg 3-4 times a day and frequently to patients weighing less than 15 kg in a dose of 125 mg 3-4 times a day. As to side effects, slight diarrhea was encountered in 1 patient. Laboratory examinations disclosed an increase in GOT in 1 patient, which returned to normal after continual insertion of the suppository.     

Fundamental and clinical studies of ceftizoxime suppositories in the pediatric field

The fundamental and clinical studies of ceftizoxime suppository (CZX-S) in the field of pediatrics were made, with the following results. The serum concentration of CZX in the CZX-S 250 mg-administered group peaked 6.00-22.5 micrograms/ml during the period of 15 minutes to 1-hour after dosing, and gradually declined thereafter. The half-life was 1.37-3.81 hours. In the CZX-S 125 mg-administered group, the serum concentration peaked 2.25-21.0 micrograms/ml at 15-30 minutes after dosing and decreased with time. The half-life was 0.95--1.84 hours. The 6-hour urinary recovery rate of CZX in the CZX-S 250 mg group was 22.0-47.5%. The 6-hour urinary recovery rate in the CZX-S 125 mg group was 17.2-25.3%. CZX-S was given 12-73 mg/kg/day (divided into 1-3 times) to 7 children with respiratory tract infection etc. who were considered to respond well to the drug. The clinical effectiveness rate was 100% inclusive of "excellent" and "good". The side effect of pain on insertion was encountered in 1 child.     

Fundamental and clinical studies on ceftizoxime suppositories in children

The peak levels of serum ceftizoxime (CZX) after a single rectal administration of CZX-S at doses of 125 and 250 mg in 157 pediatric patients were occurred at 21 approximately 25 minutes in pediatric patients aged less than 1 year and over than 7 years, at 16-20 minutes in 1-3 years patients, at more than 26 minutes in 4-6 years patients. They were 9.45, 9.58, 11.71, 12.43 mcg/ml, respectively. The mean highest levels of serum CZX were 8.56, 10.66, 12.50 mcg/ml after the administration of CZX-S as less than 10.0, 10.1-15.0, 15.1-20.0 mg/kg dose respectively, all of which were occurred at 21-25 25 minutes. A close dose response was observed. The pain of insertion was not observed in any cases. The discharge of melted suppository or defecation after administration was observed in 15.2% of total 184 cases, which was noticed more frequently in the lower aged children. There was no influence by dose. Clinical effects of CZX-S were studied in 72 pediatric patients with various infections. CZX-S was administered rectally at the mean daily dose of 41.0 mg/kg divided into 3 or 4 times for 6 days. Clinical responses were excellent in 46 cases, good in 24 cases, fair in 2 cases. The efficacy rate was 97.2%. Regarding side effects, the pain of insertion was noted in 2 cases (2.8%), diarrhea in 6 cases (8.3%), the elevation of eosinophil in 1 case (1.7%). Bacteriologically, 23 strains (92.0%) out of 25 strains isolated from the patients were eradicated.     

Basic and clinical studies of ceftizoxime suppositories in the pediatric field

A bacteriological and clinical study of ceftizoxime suppositories (CZX-S) let to the following results. The CZX serum concentration 10 minutes after insertion of one 250 mg suppository (i.e. 5.7-15.2 mg CZX per kg body weight) ranged from 1.64 to 6.53 micrograms/ml (average: 4.41 micrograms/ml). In one child the concentration 7 minutes after insertion was 4.13 micrograms/ml. Therapeutic responsiveness was recorded as "effective" in 8 (88.9%) of the 9 children who were broken down into 6 with tonsillitis, 1 with pharyngitis, and 2 with UTI. Bacteriological studies conducted in 5 children have confirmed eradication in 4 children, one of whom showing appearance of another strain. The rate of discharge of the suppository within 10 minutes after insertion was 20.4%. Reddening and erosion of the anus were observed in 1 child.     

Clinical investigation of ceftizoxime sodium suppositories in the field of pediatrics

The clinical study of CZX-S in the field of pediatrics was performed and the following results were obtained. The overall effect of CZX-S was "markedly improved" in 2 and "moderately improved" in 4 of the 6 patients with bacterial infection. Bacteriological findings show that causative organisms were eradicated in all the 5 patients observed. The breakdown of the organisms was S. aureus, S. pyogenes, S. pneumoniae, H. influenzae and E. coli. The serum concentration of CZX was 3.3 approximately 15.4 micrograms/ml (mean +/- S.E. 8.9 +/- 2.0 micrograms/ml) at 15-37 minutes after initial rectal administration with CZX-S 125 (dose: 7.7-11.9 mg/kg). While, in the CZX-S 250 administratered group, the serum concentration was 3.1 micrograms/ml and 10.5 micrograms/ml at 20 minutes after initial rectal administration (dose: 5.6 mg/kg and 14.7 mg/kg). The urinary recovery rate up to 6 hours after initial rectal administration was 68.6% in 1 patient given CZX-S 125 and 28.3-52.5% (mean +/- S.E. 38.7 +/- 7.2%) in 3 patients given CZX-S 250. Side effects and abnormalities in laboratory test values were not observed in any cases.     

Clinical studies of ceftizoxime suppositories in the pediatric field

Ceftizoxime suppository (CZX-S) was given to 19 children with infections, including upper and lower respiratory tract infections, urinary tract infections and otitis media at dose level of 18-83 mg/kg/day divided into 2-3 times. Clinical response was excellent in 12 patients, good in 6 patients and poor in 1 patient. Bacteriological response was eradicated in 11 strains, decreased in 3 strains and unchanged in 4 strains. No severe side effects were observed with this drug. These results obtained suggest that CZX-S should be a useful antibiotic in treatment of infections in pediatric field.     

Fundamental and clinical studies of ceftizoxime in obstetrical and gynecological field

This paper, is concerned with fundamental and clinical studies of ceftizoxime, a newly developed cephalosporin derivative, in the field of obstetrics and gynecology. 1. Concentrations of ceftizoxime after administration 1 g of ceftizoxime by 1 hour drip infusion were determined in genital organs in 17 patients and the exudate of pelvic dead space in 6 patients. Simulated maximal concentrations with the ratios to the simulated peak serum levels were as follows: 27.9 micrograms/g for fundal myometrium with the ratio of 48%, 36.0 micrograms/g for portio vaginalis with 62%, 17.1 micrograms/g for ovary with 29%, 15.0 micrograms/g for oviduct with 26% and 16.2 micrograms/ml for the exudate of pelvic dead space with 30%. 2. Minimal inhibitory concentrations of ceftizoxime were determined against clinically isolated organisms from female genital infectious diseases. Ceftizoxime was found to have a potent in vitro activity against Gram negative bacilli; for example, 0.1 microgram/mg or low against E. coli and K. pneumoniae. Against P. aeruginosa, P. cepacia and b. fragilis, ceftizoxime had an activity which expected to be effective in the clinical use. 3. We gave ceftizoxime to 6 patients comprising 4 patients with puerperal fever, 1 with septic abortion and 1 with tubo-ovarian abscess in daily doses of 2 to 3 g by b.i.d or t.i.d intravenous drip infusion for 4--12 days. The results of the treatment were 'excellent' in 3 patients, 'good' in 2, and 'unevaluatable' in 1. 4. Adverse reactions occurred in 2 patients who showed eruption during the medication with ceftizoxime. These patients had allergic histories due to penicillin derivatives. From the above results it is concluded that ceftizoxime is a useful drug for infections in obstetrical and gynecological field.     

Clinical experience with ceftizoxime suppositories in pediatrics

Ceftizoxime suppositories (CZX-S), containing 250 mg or 125 mg of CZX, were given to 6 children, 4 with acute bronchopneumonia and 2 with acute pharyngobronchitis, who were not suited to treatment with injectable or oral form of the drug. The clinical response was "good" in all the children and the causative organisms were eradicated in 2 children (H. influenzae or S. aureus). Adverse reactions consisted of 1 case each of diarrhea and transiently increased GPT. In conclusion, CZX-S proved to be highly effective in the treatment of bacterial infections in children.     

Fundamental and clinical studies of ceftazidime in the field of pediatrics

We have studied ceftazidime (CAZ), a cephem antibiotic of the new generation, for its antibacterial activity against H. influenzae and clinical effects. Antibacterial activity: MICs of CAZ for 142 strains of H. influenzae including 11 ABPC-resistant strains which were clinically isolated, were determined, and the results were good for all the strains. Clinical effects: CAZ was administered to 9 children with infections. Suspected causative organisms were H. influenzae, E. coli, P. aeruginosa, group B Streptococcus and S. pneumoniae. Eradication of these organisms was confirmed in all the strains except for one in which the antibacterial effect of CAZ was unknown. Clinical efficacy was excellent or good in all the cases. No side effect was observed except for eosinophilia noted in 1 case.     

The clinical evaluation of ceftizoxime suppositories in the pediatric field

Clinical evaluation of ceftizoxime suppository (CZX-S), a new antibiotic rectal suppository, was performed in 5 cases with bacterial infections in pediatric field (2 with acute bronchitis, 1 with acute tonsillitis, UTI and pertussis, respectively) and the following results were obtained; Blood levels of CZX at 10-20 minutes after administration of CZX-S at a dose of 10.0-26.3 mg/kg in 5 cases were 3.26-23.3 micrograms/ml and the urinary excretion rates within 6 hours were 15.2, 60.1, 60.2% in 3 of 5 cases measured respectively. Clinical effects were excellent in 3 and good in 2 cases. Slight elevation of GOT and GPT was observed in 1 case. No other side effects were observed. The patients' tolerability against rectal suppository was good. From the above results, we concluded that CZX-S is useful for treating the pediatric patients with various infections.     

Fundamental and clinical studies on cefuzonam in the field of pediatrics

Fundamental and clinical studies on cefuzonam (L-105, CZON), a newly semisynthesized cephem antibiotic, were carried out in the field of pediatrics and the following results were obtained. Antibacterial activities of CZON against clinically isolated strains of Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, S. pyogenes, Escherichia coli, Klebsiella pneumoniae, Haemophilus parainfluenzae and H. influenzae were compared with those of cefmenoxime (CMX), latamoxef (LMOX), cefoperazone (CPZ), cefmetazole (CMZ), cefotiam (CTM) and cefazolin (CEZ). CZON was nearly as active as CEZ against S. aureus and S. epidermidis and superior to other antibiotics against other Gram-positive cocci. Against Gram-negative rods, CZON was as active as CMX and superior to other 5 antibiotics compared. Serum concentrations and urinary excretion rates after intravenous bolus injection of CZON at doses of 10 mg/kg, 20 mg/kg and 40 mg/kg for 5 minutes in 1, 5 and 4 cases, respectively, were determined. Mean serum concentrations of CZON at these dose levels were 11.0, 43.8 and 111.5 micrograms/ml at 15 minutes, 2.4, 10.3 and 30.3 micrograms/ml at 1 hour and 0.17, 0.72 and 1.28 micrograms/ml at 4 hours, with serum half-lives of 1.79, 0.88 and 1.19 hours, respectively. Mean cumulative urinary excretion rates within 6 hours after administration were 47.9, 56.3 and 40.3%, respectively. Thirty-four pediatric patients with various bacterial infections (tonsillitis 2, acute bronchitis 1, pneumonia 14, pyothorax 1, sepsis 1, suppurative lymphadenitis 1, UTI 13 and enteritis 1) were treated with CZON at a daily dose of 40-94 mg/kg t.i.d. or q.i.d.. The overall clinical efficacy rate was 94.1%. No adverse reactions were observed except 2 cases with mild diarrhea. Abnormal laboratory findings were also mild; slight elevation of GOT and GPT in 2, eosinophilia in 1 and thrombocytosis in 1. These results clearly indicate the usefulness of CZON in the treatment of bacterial infections in children.     

Fundamental and clinical studies on aspoxicillin in the field of pediatrics

Fundamental and clinical studies were performed with aspoxicillin (ASPC), a new developed injectable broad penicillin, in pediatric infectious diseases, and the following results were obtained. Pharmacokinetics ASPC was administered to 2 cases at a dose of 20 mg/kg by one shot intravenous injection. The mean half-life (T 1/2) was 1.17 hours. The mean urinary excretion rate was 58.4% during 6 hours after ASPC treatment. In 3 cases of intravenous drip infusion with a period of 1 hour at a dose of 10 mg/kg (2 cases) and 20 mg/kg (1 case), the half-lives (T 1/2) were 1.7 hours, 3.5 hours and 1.0 hour, respectively. The urinary recovery rate during 6 hours after administration was 57.7%, 32.6% and 42.7%, respectively. At only one case treated with 10 mg/kg intravenous drip infusion, the half-life was prolonged and urinary excretion rate was lower than other 2 cases. Clinical study ASPC was administered 50-80 mg/kg/day for 4-8 days to 22 children comprising 6 tonsillitis, 2 bronchitis, 6 pneumonia and 8 urinary tract infections. Clinical efficacy was excellent in 13 cases, good in 8 cases and fair in 1 case, the total cure rate was 95%. As for the clinical response classified by diagnosis, the each efficacy rate of tonsillitis, bronchitis and pneumonia was 100%, and that of urinary tract infection was 87.5%. Clinical side effect and abnormal laboratory findings were not observed in any cases. From the above results, it was concluded that ASPC was one of the useful secure drug for treatment of infections in pediatric field.     

Fundamental and clinical studies on cefminox in the field of pediatrics

Cefminox (CMNX, MT-141) is a new injectable cephamycin antibiotic, which was studied for its antibacterial activity, absorption and excretion after administration and clinical efficacy of patients with infections. The following results were obtained. Antibacterial activity The antibacterial activity of CMNX against 19 clinical isolates consisting of 11 species made the results that its activity against E. coli, P. vulgaris and C. jejuni was superior to CMZ and CEZ. Concentration in serum and urine CMNX was given intravenously to 3 groups at 20 mg/kg by one shot (2 cases), 40 mg/kg by one shot (2 cases) and 40 mg/kg by 1 hour drip infusion (1 case). The half-lives were between 1.15 to 1.80 hours. We obtained over 70% of its excretion to urine within 6 hours after injection. Clinical efficacy Clinical evaluation was made on a total of 18 patients with various infections, 11 of whom had underlying diseases. The result was excellent in 1 case, good in 11 cases, fair in 2 cases and poor in 4 cases, and the effective rate was 66.7%. Side effect Clinical and laboratory abnormal findings related to CMNX were not found. It is concluded that CMNX seems to be effective and safetive antibiotic in the field of pediatrics.     

Fundamental and clinical studies on ceftazidime in the field of pediatrics

Fundamental and clinical studies were carried out on ceftazidime ( CAZ ), a new cephalosporin, in the field of pediatrics. 1. Antimicrobial activity MICs of CAZ were determined for clinical isolates of 24 strains of S. aureus, 15 of S. pyogenes, 8 of H. influenzae, 22 of E. coli, 20 of K. pneumoniae, 18 of P. mirabilis, 3 of P. morganii, and 21 of P. aeruginosa, and compared with those of the control drugs, i.e. CEZ, CXM, CMZ, CTX, LMOX and CMX. For P. aeruginosa, CPM, CFS and GM were also employed as the control drugs. CAZ was as active as CTX, LMOX and CMX, its MICs distributing in the range not higher than 0.10 microgram/ml for H. influenzae, 0.78 microgram/ml for E. coli, 0.39 microgram/ml for K. pneumoniae, 0.10 microgram/ml for P. mirabilis, and 0.10 microgram/ml for P. morganii in all the strains. Against P. aeruginosa, CAZ showed MICs in the range between 0.39 and 3.13 micrograms /ml, which showed activity higher than that of CTX, LMOX , CPM, CMX and GM, and comparable to that of CFS. Against S. pyogenes, CAZ was as active as all the control drugs except for LMOX , its MICs for all strains tested being 0.20 microgram/ml or below. Against S. aureus, CAZ was slightly more active than LMOX , but less active than the other control drugs, its MICs being relatively high ranging from 6.25 to 50 micrograms/ml. 2. Pharmacokinetics After a one-shot intravenous injection of CAZ 20 mg/kg, serum levels and urinary excretion were studied in 3 children aged 6 to 9 years, and CSF levels were determined in 2 children aged 6 to 7 years with aseptic meningitis. The mean serum levels of CAZ were 85.3 micrograms/ml at 1/4 hour, 53.3 micrograms/ml at 1/2 hour, 32.0 micrograms/ml at 1 hour, 16.1 micrograms/ml at 2 hours, 5.3 micrograms/ml at 4 hours, and 2.0 micrograms/ml at 6 hours, with the mean half-life of 1.18 hours. The mean urinary levels were 9,700 micrograms/ml at 0 to 2 hours, 803 micrograms/ml at 2 to 4 hours, 540 micrograms at 4 to 6 hours, and the mean urinary recovery rate during the first 6 hours was 83.9%. The CSF levels at 1 hour after intravenous injection were 0.44 microgram/ml in acute stage and 0.10 to 0.22 microgram/ml in convalescent stage. 3. Clinical study Thirty-one pediatric patients with bacterial infections were treated with CAZ , and the clinical efficacy, bacteriological response, and side effects were evaluated.(ABSTRACT TRUNCATED AT 400 WORDS)     

Laboratory and clinical studies on ceftizoxime in the field of pediatrics (author's transl)

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 10(8) 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 10(8) cells/ml and 10(6) cells/ml. A dose of ceftizoxime 10 mg/kg or 20 mg/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 (T 1/2) were estimated to be 1.17 hours in dose of 10 mg/kg and 1.31 hours in dose of 20 mg/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 79.4 mcg/ml) at the end of infusion. The levels, thereafter, tapered to mean levels of 45.3 mcg/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 64.2 mcg/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 of 0.97 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.     

Fundamental and clinical studies in pediatric field on ceftizoxime (author's transl)

Fundamental and clinical studies in the pediatric field on ceftizoxime were carried out, and the following results were obtained. 1. In 4 children age from 3 years to 5 years, the serum concentrations and urinary excretion of ceftizoxime 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 microgram/ml (mean 45.0 microgram/ml) at the end of infusion. The mean serum levels after the end of infusion were 16.9 microgram/ml at 30 minutes, 12.1 microgram/ml at 1 hour, 6.2 microgram/ml at 2 hours, 1.6 microgram/ml at 4 hours and 0.6 microgram/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 microgram/ml, which were 8 to 60 times higher than the MICs of the causative organisms. 3. Ceftizoxime was administered to 38 children with pneumonia, bronchitis, Salmonella enteritis, purulent meningitis, etc. in the daily dose of 44--200 mg/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.     

Fundamental and clinical studies on ceftizoxime in pediatric field (author's transl)

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), Klebsiella 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. coli and K. pneumoniae, 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--10 years old given a single intravenous dose of 20 mg/kg was as follows: 45.4 micrograms/ml at 15 minutes, 40.4 micrograms/ml at 30 minutes, 22.1 micrograms/ml at 1 hour, 10.4 micrograms/ml at 2 hours, 2.9 micrograms/ml at 4 hours and 0.9 microgram/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: 2,477 micrograms/ml for 1--2 hours, 1,235 micrograms/ml for 2--4 hours and 462 micrograms/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, 'good' 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.     

Fundamental study on ceftizoxime suppositories in adults and children

The pharmacokinetics of newly developed ceftizoxime suppository (CZX-S) was studied in healthy volunteers and in children, compared with that of intramuscular CZX and intravenous CZX: In 8 volunteers (aged 19 to 24 years), each of 500 mg (potency) CZX-S containing 3%, 4% and 5% sodium caprate was compared with 500 mg intramuscular CZX and 500 mg intravenous CZX as a single administration in the cross-over method. In addition each of 500 mg CZX-S containing 4% and 5% sodium caprate was studied in 2 groups of 8 volunteers (aged 22 to 24 years) and of 8 volunteers (aged 19 to 27 years); each CZX-S was given 3 times a day successively for 5 days. The pharmacokinetics of 125 mg and 250 mg CZX-S, which contained 3% sodium caprate, were also evaluated as a single administration in 9 children (aged 6 years 4 months to 12 years 0 month) and in 11 children (aged 7 years 8 months to 12 years 4 months), respectively. The irritabilities of CZX-S were studied in all subjects who participated in this trial. The feeling of foreign body, the feeling of defecation, the burning sensation and the pain were evaluated in volunteers; the feeling of defecation and the pain were evaluated in children. The results were as follows: I. Pharmacokinetics in healthy volunteers 1. Given as a single administration The mean peak concentrations of serum CZX were occurred 30 minutes after 500 mg CZX-S containing 3%, 4% and 5% sodium caprate, which were 10.5 mcg/ml, 12.3 mcg/ml and 12.4 mcg/ml, respectively. These values were 1.35 mcg/ml, 1.60 mcg/ml and 1.69 mcg/ml at the conversion unit of 1 mg dose per 1 kg body weight. The mean peak serum CZX concentration of CZX-S containing 3% sodium caprate was slightly lower than that of CZX-S containing 4% or 5% sodium caprate, but was 1.9 times higher than that of the ABPC suppository. There was no marked difference among 3 preparations of CZX-S in mean Tmax and T1/2. Cmax of CZX-S containing 3% sodium caprate was 1.40 mcg/ml at the conversion unit of 1 mg/kg. AUC of CZX-S containing 3% sodium caprate was slightly smaller than that of CZX-S containing 4% or 5% sodium caprate, but 3.1 times that of the ABPC suppository in healthy volunteers. When 500 mg CZX was intramuscularly administered by one shot to 8 volunteers, Tmax was same as that of CZX-S or was slightly later.(ABSTRACT TRUNCATED AT 400 WORDS)     

Fundamental and clinical studies of sulbactam/cefoperazone in the field of pediatrics

Sulbactam/cefoperazone (SBT/CPZ) was evaluated in the treatment of pediatric patients to have the following results: Peak serum concentrations which occurred just after the drip infusion of 20 mg/kg SBT/CPZ were 36.4 micrograms/ml and 8.6 micrograms/ml for CPZ and SBT, respectively. The half-life of CPZ was 1.91 hours, and that of SBT, 0.97 hour. Following the 40 mg/kg drip infusion, the peak serum concentration of CPZ was 79.1 micrograms/ml, and that of SBT, 27.0 micrograms/ml. The half-lives were 1.99 hours for CPZ, and 1.07 hours for SBT, respectively. In 6 hours after drip infusion of 20 mg/kg and 40 mg/kg 21.7, 37.0% of CPZ and 41.6, 85.6% of SBT were excreted in urine. Daily doses of about 50-90 mg/kg SBT/CPZ were administered by intravenous or drip infusion to 26 pediatric patients with acute infections such as lacunar tonsillitis, bronchitis, bronchopneumonia, suppurative diseases caused by Staphylococcus (staphylococcal scalded skin syndrome), purulent parotitis, cervical lymphadenitis, phlegmon and acute UTI related with ABPC/CPZ resistant beta lactamase producing E. coli. SBT/CPZ demonstrated the bacteriological effect on all the causative organisms. The clinical efficacy was also confirmed with the efficacy rate of 88.5%. No side effects were observed in all the cases though transient eosinophilia developed in 2 patients.