Biomedical subjects

K Sunakawa

Publications and source records attributed to K Sunakawa.

At least 73 records · Page 4Linked to original sources

PubMed1992

[Overall clinical evaluation of cefprozil against infections in pediatric fields. Pediatric Study Group for Cefprozil].

Cefprozil (CFPZ, BMY-28100) granule preparation was studied for pharmacokinetic, bacteriological and clinical aspects in the pediatric infections. The results obtained are summarized as follows: 1. Serum concentrations and urinary excretion. The pharmacokinetics of CFPZ in pediatrics was investigated by single oral administration of fine granules at doses of 4.0, 7.5 and 15.0 mg/kg. Peak blood levels of CFPZ were 3.06, 4.62 and 9.65 micrograms/ml, respectively, at 1.00-1.30 hours after each dose and AUCs were 7.44, 12.50 and 27.01 micrograms.hr/ml, respectively. These data showed that Cmax and AUC depended on dose levels. T 1/2 (beta) at these dose levels were 1.03, 0.94 and 1.01 hours, respectively. There were no differences related to dose. Urinary recovery rates in the first 6 hours after administration were 51.5-57.1%. The pharmacokinetics of CFPZ before or after meals were also investigated at a dose of 7.5 mg/kg. Peak blood levels were 4.88 micrograms/ml at 1.17 hours after administration in the fasting state, and 4.30 micrograms/ml at 1.54 hours after administration in the non-fasting state. Delay of Tmax and slight decrease of Cmax were observed in the non-fasting state, but T 1/2 and AUC were 0.91 hour and 12.96 micrograms.hr/ml, respectively, in the non-fasting state, and were similar to those in the fasting state, 0.93 hour and 12.82 micrograms.hr/ml, respectively. Urinary recovery rates in the first 6 hours after administration were 63.8% in the fasting state and 50.7% in the non-fasting state. 2. Clinical results. Clinical efficacies of CFPZ granules in various infectious diseases were studied in 804 cases. Twenty nine cases, mostly viral or mycoplasmal infections, were excluded from the statistical analysis. The clinical efficacy rate in 527 cases with causative bacteria isolated was 97.2%; and in 248 cases from whom no significant isolate had been obtained was 96.0%. The clinical efficacy rate in 475 cases with monobacterial infections (proven by culture of isolates) was 97.3%, and that in 52 case with polybacterial infections was 96.2%. Haemophilus influenzae was isolated mostly from acute respiratory infections. In 88 cases from whom H. influenzae was isolated, clinical efficacy rate was 95.5%. In cases from whom H. influenzae was found concomitant by with Staphylococcus aureus, Streptococcus pyogenes or Streptococcus pneumoniae, the clinical efficacy rates were also high. The bacteriological eradication rate in cases with 582 strains was 83.3%; the eradication rate for Gram-positive organisms was 95.8%; and for Gram-negative organisms, it was 64.2%.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1992

[Bacteriological and clinical studies on meropenem in the pediatric field].

Bacteriological and clinical studies have been performed on meropenem (MEPM, SM-7338), a newly developed carbapenem antibiotic, in the pediatric field. 1. Antibacterial activities of MEPM against 24 clinical isolates were determined. MEPM showed excellent activity against Gram-positive bacteria including Staphylococcus aureus and Gram-negative bacteria, especially Escherichia coli and Branhamella catarrhalis. Against Haemophilus influenzae, MEPM had a higher activity than imipenem and flomoxef, but had a lower activity than piperacillin and cefoperazone. 2. Clinical efficacies of MEPM were evaluated in 32 cases with bacterial infections. A poor efficacy was observed in 1 patient with phlegmon but excellent or good efficacies were obtained in other 31 patients with tonsillitis (1), pneumonia (17), UTI (12), or SSSS (1). The overall efficacy rate was 96.9%. All strains except 1 of S. aureus were eradicated by the administration of MEPM, and a high eradication rate of 95.8% (23 out of 24 strains) was obtained. 3. No side effects were observed in 35 evaluated cases. As abnormal laboratory test results, elevated GOT, elevated GPT, eosinophilia and neutropenia were noted in 4, 4, 4 and 2 patients, respectively. 4. Influences on blood coagulation parameters were studied. PIVKA II was elevated upon administration of MEPM in some cases, but no changes in ATT, TT, HPT or Fbg were observed during the treatment. Based on the above results, it has been concluded that MEPM is a safe and effective drug to use in the treatment of pediatric infections. The usual recommended dosage and administration should be 10 to 20 mg/kg of MEPM at a time, using intravenous drip infusion, 3 times a day.

Adolescent↗

PubMed1992

[Bacteriological and clinical studies of panipenem/betamipron in pediatrics].

We carried out bacteriological and clinical studies of panipenem/betamipron (PAPM/BP), a newly-developed carbapenem antibiotic, in pediatrics, and the following results were obtained: 1. When antibacterial activities of panipenem (PAPM) were determined, it was found that MICs against such Gram-positive cocci as Staphylococcus aureus and Streptococcus pneumoniae and against such Gram-negative rods as Escherichia coli, Haemophilus influenzae, Pseudomonas aeruginosa, and Branhamella catarrhalis were all sufficiently low. 2. PAPM showed better MIC-correlated antibacterial activities against 215 subcultured strains of methicillin-resistant S. aureus (MRSA) than imipenem. 3. Clinical efficacies were evaluated to be excellent in 23 of 34 patients treated with PAPM/BP, excluding 3 patients from the efficacy evaluation. In addition, good responses were obtained in 10 patients but poor response in one, showing the overall efficacy rate of 97.1%. As for bacteriological efficacies, the eradication rate was also determined to be high, 92.6%. 4. As for side effects, rash appeared in 2 patients, and soft stool and diarrhea occurred in one each. The overall incidence of side effects was calculated to be 10.8%. As for abnormal laboratory findings, increases of eosinophiles in 4 patients, thrombocytes in 2, total bilirubin in 1, and GOT in 1 were observed. From these results, PAPM/BP was thought to be a highly useful drug in pediatrics.

Adolescent↗

PubMed1992

[Overall clinical evaluation of panipenem/betamipron against infections in pediatric field].

To conduct a basic-clinical study on newly developed panipenem/betamipron (CS-533/CS-443, PAPM/BP) against various infections in pediatrics, a study group was organized and a joint research by 17 institutions and their related hospitals was undertaken. The obtained results are as follows. 1. Blood concentrations and urinary excretion Pharmacokinetics of PAPM/BP in children was studied using 30 minutes intravenous drip infusion of 10 mg/10 mg/kg, 20 mg/20 mg/kg and 30 mg/30 mg/kg, respectively. Maximum blood levels of PAPM/BP were observed at the completion of drip infusion and were 26.72 +/- 8.78 micrograms/ml/18.33 +/- 8.54 micrograms/ml (mean +/- S.D.) with administration of 10 mg/10 mg, 64.80 +/- 18.50 micrograms/ml/38.74 +/- 16.41 micrograms/ml with administration of 20 mg/20 mg and 91.70 +/- 29.42 micrograms/ml/50.08 +/- 22.41 micrograms/ml with administration of 30 mg/30 mg. Dose dependency was noted with these doses. The half-life was about 1 hour for PAPM and about 0.5 hour for BP. As for urinary excretion, PAPM was excreted about 30% and BP about 70% in the first 6 hours after the start of drip infusion. 2. Clinical results Twenty-five cases of exclusion and drop-out were deducted from a total of 391 cases and 8 cases having 2 diseases concurrently were added to the remaining 366 cases, hence 374 cases were evaluated in the study as the subjects of analysis of clinical effects. As for clinical effects in cases where pathogenic bacteria were detected, 215 out of 221 cases were rated as effective or above, hence the efficacy rate of 97.3% was obtained. In cases where pathogenic bacteria were not detected, 145 out of 153 cases were rated as effective or above, thus the efficacy rate was 94.8% which is similar to that in the cases where pathogenic bacteria were detected. The daily dose levels most commonly employed were 30 to 60 mg/kg (as PAPM) administered in 3 divided doses a day, and this regimen method accounted for 52.7% of the total cases, and the efficacy rate with this regimen was 97.0%. As for the bacteriological effect 87 (96.7%) out of 90 strains of Gram-positive bacteria (GPB) disappeared and 136 (91.3%) out of 149 strains of Gram-negative bacteria (GNB) disappeared upon the treatment. The overall bacterial eradication rate for the pathogenic bacteria was 93.4%.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗

PubMed1992

Antihypertensive effect of the new calcium antagonist (+-)-3-(benzylmethylamino)-2,2-dimethylpropyl-methyl-4-(2-fluoro-5- nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate hydrochloride in rats.

The antihypertensive effect of TC-81 ((+-)-3-(benzylmethylamino)-2,2-dimethylpropyl-methyl-4-(2-f luoro-5- nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate hydrochloride), a new calcium antagonist, was investigated in normotensive and hypertensive rats. By oral administration, the antihypertensive activity of TC-81 (ED20% in spontaneous hypertensive rats (SHR), DOCA-salt hypertensive rats and renal hypertensive rats were 0.37, 0.32, and 0.38 mg/kg p.o., respectively) was 7-14 times more potent in conscious hypertensive rats in comparison with nicardipine. Duration of the antihypertensive effect of TC-81 was about 2 times longer than that of nicardipine, and the response was elicited more slowly than that of nicardipine at an equipotent dose. Similar results were observed by intravenous injection, but the potency of TC-81 was only 3 times higher than that of nicardipine in anesthetized rats. Tolerance of the antihypertensive effect of TC-81 in long-term daily dosing and the rebound phenomenon after discontinuance of the treatment were not observed in hypertensive rats. TC-81, at a concentration of 10(-10)-3 x 10(-9) mol/l, inhibited the KCl-induced contraction of isolated rat vascular preparations. Moreover, TC-81 inhibited the norepinephrine-induced contraction of isolated SHR aorta preparation, but in isolated normotensive rat aorta, TC-81 inhibited the norepinephrine-induced contraction very little. From these observations, TC-81 can be characterized as having a strong, long-lasting, and slow-onset antihypertensive activity, especially by oral administration. Therefore, this new calcium antagonist may be useful for long-term antihypertensive therapy.

Animals↗

PubMed1992

Antihypertensive effect of the new dihydropyridine calcium antagonist (+-)-3-(benzylmethylamino)-2,2-dimethylpropyl methyl 4-(2-fluoro-5-nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedica rbo xylate hydrochloride in dogs.

The antihypertensive effect of TC-81 ((+-)-3-(benzylmethylamino)-2,2-dimethylpropyl methyl 4-(2-fluoro-5-nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridine dicarboxylate hydrochloride, CAS 96515-74-1), a new calcium antagonist, was investigated in normotensive dogs (NTD) and renal hypertensive dogs (RHD). By oral administration, the antihypertensive activity of TC-81 (ED20% was 0.09 mg/kg p.o.) was about 18 times more potent in conscious RHD in comparison with nicardipine (ED20% was 1.65 mg/kg p.o.). Duration of the antihypertensive effect of TC-81 was about 2 times longer than that of nicardipine, and the response was elicited more slowly than that of nicardipine at equipotent dose. Similar results were observed more clearly by intravenous injection, but the potency of TC-81 was only 3 times higher than that of nicardipine in anesthetized dogs. Tolerance of the antihypertensive effect of TC-81 in daily dosing for 2 weeks and the rebound phenomena after discontinuance of the treatment were not observed in RHD. TC-81 at a concentration of 10(10)-3 x 10(-9) mol/l inhibited the KCl- or norepinephrine-induced contraction of isolated dog femoral artery. From these observations, TC-81 can be characterized as having a strong, long-lasting, and slow-onset antihypertensive activity, especially by oral administration. Therefore, this new calcium antagonist may be useful for long-term antihypertensive therapy.

Anesthesia↗

PubMed1991

[A clinical study on cefdinir 10% granule in pediatrics].

Clinical evaluations of cefdinir (CFDN) 10% granule were carried out. The obtained results are summarized as follows. 1. Clinical responses to CFDN of 23 patients with pediatric infections were excellent in 11 and good in 8. The overall efficacy rate was 82.6%. 2. Bacteriologically, the eradication rate for 23 strains of bacteria identified to be pathogens was evaluated and was 82.6%. 3. Side effects observed were diarrhea in 2 of 25 patients. The incidence was 8.0%. Abnormal laboratory test results observed included 2 cases with elevation of GOT and 1 case with elevation of GPT. These results suggest that CFDN 10% granule, as well as 5% granule, may be a very useful and safe drug for the treatment of pediatric infections.

Administration, Oral↗

PubMed1991

[Pharmacokinetic and clinical studies on flomoxef in neonates and premature infants].

Studies were made on pharmacokinetics, clinical effects and influence on intestinal bacterial flora in neonates upon administration of flomoxef (FMOX), and the results obtained are summarized as follows: 1. Serum concentrations of FMOX after intravenous administration of 20 mg/kg/dose were 48.5 micrograms/ml in 30 minutes, 33.0 micrograms/ml in 1 hour and 7.3 micrograms/ml in 6 hours. The T 1/2 was 2.7 hours. FMOX at a dose of 40 mg/kg was given to only one new born baby on the 1st day after birth, and serum concentrations were 73.6 micrograms/ml in 30 minutes, 55.9 micrograms/ml in 1 hour and 16.9 micrograms/ml in 6 hours. The T 1/2 was 4.60 hours. 2. FMOX was administered to 21 neonates between 0 and 32 days of age. Clinical effects were evaluable in 8 of 21 cases. The results were excellent in 2 cases, good in 5 cases and poor in 1 case. Of the 21 cases, diarrhea in 1 case, elevation of eosinophile in 2 cases (9.5%), elevation of platelet count in 3 cases (14.3%), and elevation of GOT in 2 cases (9.5%) were recognized during treatment. 3. FMOX was detected in feces at levels of 0.84-44.4 micrograms/g. Except for a slight decrease in numbers of anaerobes, little fluctuations of intestinal flora were observed during treatment.

Bacterial Infections↗

PubMed1991

[Bacteriological and clinical studies of cefodizime in pediatrics].

Bacteriological and clinical studies on cefodizime (CDZM, THR-221), a new cephem developed by Hoechst AG and Roussel Uclaf, were carried out and the results are summarized below: 1. Against Gram-positive bacteria, Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae, antibacterial activities of CDZM were similar to those of cefotaxime (CTX), cefazolin, cefotiam and piperacillin. Against Escherichia coli, Klebsiella pneumoniae and Serratia sp., antibacterial activities of CDZM were similar to that of CTX, and superior to those of other tested antibiotics. Especially against Haemophilus influenzae and Branhamella catarrhalis, it showed an excellent antibacterial activity. 2. Although the clinical efficacy was poor in 1 patient with sepsis caused by Salmonella marcescens and in another with cervical lymphadenitis, in 5 patients with upper respiratory tract infection, 4 patients with bronchitis, 6 patients with bronchopneumonia, 18 patients with pneumonia, 5 patients with urinary tract infection and 1 patient with enteritis, the clinical efficacy was excellent or good and the efficacy rate was 95.1% (39/41) including excellent efficacies in 25 cases. 3. Bacteriologically, all identified causative bacteria were eradicated except for 1 case of Salmonella sp., thus the eradication rate was 97.4% (38/39). Especially S. pneumoniae in 10 cases, H. influenzae in 12 cases and B. catarrhalis in 3 cases were eradicated totally. 4. Adverse reactions were studied in 46 cases, and digestive symptoms were observed in 9 cases (diarrhea 5 cases, loose stools 4 cases). Eruption and vascular pain were observed in 1 case each. As digestive symptoms in 9 cases were mild, the treatment were not suspended. In laboratory test values, elevation of GOT, elevation of GPT, elevation of bilirubin, and eosinophilia were observed in 1 case each. Influences on blood coagulation parameters were studied. No change was observed between the beginning and the end of the treatment. From above results, we have concluded that CDZM is a useful and safe antibiotic in pediatrics, administered at a daily dose of 20 mg/kg divided into 3 or 4 doses and administered intravenously.

Adolescent↗

PubMed1991

[Influence of cefodizime on intestinal bacterial flora].

Effects of cefodizime (CDZM), a new injectable cephem antibiotic, on the intestinal bacterial flora were studied in tetra-contaminated mice and in pediatric patients. CDZM was intramuscularly administered at a dose of 100 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of organisms: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. For 3 species except E. faecalis, bacterial populations in feces were markedly reduced after the start of the treatment. Subjects in the pediatric study were 5 children with bacterial infections (4 boys and 1 girl) at ages from 7 months to 9 years 6 months and with their body weights ranging from 7.6 kg to 51.1 kg. CDZM was intravenously administered at a dose of 9.7 mg/kg to 23.0 mg/kg 4 times a day for 5 to 15 days. Although some variations in the fecal bacterial flora were noticed among these subjects during the treatment, populations of main aerobes and anaerobes such as Enterobacteriaceae, Enterococcus, Bacteroides, Bifidobacterium and Eubacterium decreased markedly in most cases. Glucose non-fermenting Gram-negative rods and fungi tended to increase during or after the administration of CDZM, and they were the most predominant species in some cases. Although these changes tended to return to predosing states after the cessation of the treatment with CDZM, attention must be paid to possible occurrences of diarrhea, superinfection or bleeding tendency when treatment with the drug is continued for long periods of time. Fecal concentrations of CDZM considered to be closely related to the changes of the intestinal bacterial flora showed pretty high values in all cases.

Animals↗

PubMed1991

[The influence of cefpirome on intestinal bacterial flora].

Cefpirome (CPR, HR810), a new parenteral cephalosporin antibiotic, was studied for its effect on the intestinal bacterial flora in pediatric patients. The subjects were children admitted for infections (6 males and 3 females, 1 month to 5 years 1 month old, weighted 3.94 to 21.0 kg). CPR was intravenously administered at a dose between 19.0 to 40.0 mg/kg, 3 to 4 doses daily over 6 to 12 days. The feces from these children were collected before, during, and after administration, and bacteria were identified and counted. CPR concentration, beta-lactamase activity, and Clostridium difficile D-1 antigen were also assayed. Bacterial flora changes in feces during CPR administration showed some variance, but generally 5 cases out of the 9 showed a significant decrease in Enterobacteriaceae and Enterococcus faecalis among aerobic bacteria. The other 4 cases showed some transient decrease, but no significant change was observed. No significant changes were recognized for Enterococcus avium and Enterococcus faecium, and the total aerobic bacterial count decreased in a transient manner in only one patient. Regarding anaerobic bacteria, Bifidobacterium and Eubactrium revealed a significant decrease, a transient decrease or no change from case to case. Bacteroides showed little change in count. Consequently, the total anaerobic bacteria count did not reveal a large change aside from 1 case in which Bacteroides was not detected before administration and a significant decrease of other bacteria was noted. In no case, glucose nonfermentative Gram-negative bacilli or fungi were found dominant. Although C. difficile and C. difficile D-1 antigen were detected in 3 and 4 cases, respectively, there was no exact relationship between the number of C. difficile and the characteristics of the feces. CPR was detected in fecal samples from 6 cases during administration with concentrations ranging between 1.20 to 22.4 micrograms/g. High values of CPR tended to be found in specimens with low beta-lactamase activity in the feces. When drug sensitivities of the bacteria isolated from feces before and after administration were compared, higher levels of resistance were found in some bacteria such as Enterococci and Bacteroides during or after administration than before administration. The above results suggest that CPR is a drug with a relatively small influence on the intestinal bacterial flora in children, but a particular attention is required for diarrhea and microbial replacement during a continuous, long-term administration of the drug.

Bacteria↗

PubMed1991

[Pharmacokinetic and clinical studies on cefpirome in pediatrics].

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

Adolescent↗

PubMed1990

[A clinical study on cefdinir in pediatrics].

Clinical evaluations of cefdinir (CFDN, FK482) were carried out. The obtained results are summarized as follows. 1. Clinical responses to CFDN of 43 patients with pediatric infections were excellent in 23, good in 15, fair in 4 and poor in 1. The overall efficacy rate was 88%. 2. Bacteriologically, the eradication rate for 34 isolates presumed to be pathogens was evaluated and the eradication rate was 85.3%. 3. Side effects observed were diarrhea in 4 of 48 patients. The incidence was 8.3%. Abnormal laboratory findings were an elevation of GOT, an elevation of eosinophils and an increase in platelet counts. The results suggested that CFDN might be a very useful and safe drug for the treatment of pediatric infections.

Administration, Oral↗

PubMed1990

[Pharmacokinetic and clinical studies on aztreonam in neonates and premature infants].

Aztreonam (AZT) was studied for its pharmacokinetics, clinical effect and effect on intestinal bacterial flora in neonates, and the results obtained are summarized as follows: 1. Serum concentrations of AZT upon intravenous administration of 20 mg/kg were 38.6 micrograms/ml in 30 minutes, 30.6 micrograms/ml in 1 hour and 13.6 micrograms/ml in 6 hours. The T 1/2 was 3.73 hours. Ampicillin (ABPC) 25 mg/kg was concurrently used with AZT in 2 cases and serum concentrations of AZT in these 2 cases were 40.3 and 36.9 micrograms/ml in 30 minutes, 35.7 and 32.6 micrograms/ml in 1 hour, and 13.1 and 10.2 micrograms/ml in 6 hours, respectively. T 1/2's were 3.32 and 2.91 hours, respectively, and no interaction between the 2 drugs was observed. 2. AZT was administered to 21 neonates between 0 and 83 days of age and ABPC was concurrently administered to 18 of the cases. Clinical evaluation was made in 14 cases, where AZT was remarkably effective in 7 cases, effective in 6 cases and not effective in 1 case. Of the 21 cases, 1 case of diarrhea, 1 case each of eosinophilia, an increase in platelets, an increase in platelets and an elevation of GOT and a decrease in platelets were recorded. 3. With respect to effects of AZT on intestinal bacterial flora, fecal concentrations of AZT upon its single administration to 2 cases were low suggesting, there was little effect on the intestinal flora. Some effect on anaerobes, however, was recognized in 4 cases in which ABPC was concurrently used.

Ampicillin↗

PubMed1990

[Laboratory and clinical studies on norfloxacin in pediatrics].

Norfloxacin (NFLX, AM-715) is a new quinolone antibacterial agent. In the present study, we carried out laboratory and clinical investigations on NFLX in the field of pediatrics. The obtained results are summarized as follows. 1. NFLX was very active against Escherichia coli, Salmonella sp., Klebsiella sp., Enterobacter sp. and Pseudomonas aeruginosa among Gram-negative rods. Antibacterial activities of NFLX against Gram-positive cocci were lower than those against Gram-negative rods but superior to activities of usual quinolone agents. MIC values of NFLX against Campylobacter jejuni were distributed in a range of less than or equal to 0.05-0.78 micrograms/ml. 2. A peak serum level of 0.49 micrograms/ml was observed in 2 subjects and its urinary recoveries were 13.7%, 21.5%, respectively. 3. Clinical efficacies to NFLX were excellent in 25 patients and good in 9 patients with a efficacy rate of 92%. In a bacteriological examination, causative organisms were eradicated with an eradication rate of 87%. 4. No side effects were observed except eosinophilia in 1 patient. These findings indicate that NFLX will be useful and safe drug against bacterial infections in pediatrics.

Adolescent↗

PubMed1989

[Laboratory and clinical studies on clarithromycin in pediatrics].

Clarithromycin (TE-031, A-56268) is a new 14-membered ring macrolide antibiotic developed by Taisho Pharmaceutical Co., Ltd. TE-031 has a methoxy group at position 6 in its structure. In the present study, we carried out laboratory and clinical investigations on TE-031 in the field of pediatrics. The obtained results are summarized as follows. The antibacterial activity of TE-031 was investigated against 16 clinically isolated strains of Streptococcus pyogenes, Staphylococcus aureus, Haemophilus influenzae, Bordetella pertussis and Campylobacter jejuni. TE-031 showed antibacterial activity comparable to erythromycin. The pattern of changes in TE-031 concentrations in the blood after administration was investigated. In subjects administered the granular preparation of TE-031, Cmax values were 0.64 micrograms/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 micrograms/ml in 2 subjects administered with 10 mg/kg. The tablet form of TE-031 was administered to 3 subjects at 5 mg/kg, and Cmax values were 2.09-3.92 micrograms/ml, while T 1/2 values were in a range of 2.9-3.8 hours. When drug concentrations in the urine were investigated, it was found that 6-hour recovery rates were 9.9% (dose: 5 mg/kg) and 53.4% (dose: 10 mg/kg) in the subjects administered the granular form, whereas recovery rates averaged 36.8% in the tablet-administered subjects. In the clinical trial, TE-031 was administered in 2-3 doses/day for 2-18 days. In cases given the granular form, dosages were 12-38 mg/kg/day, while tablets were administered at 12-29 mg/kg/day. The overall clinical efficacy rate was 92.8%, i.e., the drug was effective in 64 of 69 patients. TE-031 was ineffective in 1 case of otitis media, but efficacious in 10 of 10 (100%) cases of upper respiratory infection, 15 of 18 (83.3%) cases of bronchitis and pneumonia, 5 of 6 (83.3%) cases of pertussis, 13 of 13 (100%) cases of mycoplasmal pneumonia, 4 of 4 (100%) cases of Chlamydia psittaci pneumonia, 16 of 16 (100%) cases of gastroenteritis (including 15 cases of Campylobacter gastroenteritis), and 1 (100%) case of impetigo. In bacteriological studies conducted on the patients, the overall elimination rate was 93.1%, i.e., bacterial elimination was obtained in 27 of 29 cases. TE-031 showed especially good bacteriological efficacy (100%) against C. jejuni and B. pertussis, which were eliminated from all of 15 and 2 cases examined, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1989

[Clinical studies on sulbactam/ampicillin in the field of pediatrics].

During 8 months from October 1986 to May 1987, the clinical efficacy of sulbactam/ampicillin (SBT/ABPC) was evaluated in 63 pediatric inpatients with various infections. Clinical efficacies were evaluable in 58 patients among them (consisting of 2 patients with sepsis, 3 with tonsillitis, 12 with bronchitis, 6 with bronchopneumonia, 24 with pneumonia, 1 with phlegmon, 2 with lymphadenitis, 1 with impetigo and 7 with urinary tract infection) and were excellent in 40 patients and good in 17 with an overall efficacy rate of 98.3%. Bacteriological efficacies were assessed in 25 patients and 27 strains of organisms (consisting of 3 strains of Staphylococcus aureus, 2 Streptococcus pneumoniae, 1 Streptococcus pyogenes, 2 beta-Streptococcus, 1 Gram-positive cocci, 5 Escherichia coli, 1 Enterobacter aerogenes, 7 Haemophilus influenzae, 2 Haemophilus parainfluenzae, 1 Branhamella catarrhalis, 1 Proteus mirabilis and 1 Salmonella subgenus I). Bacteriological eradication rates were 88.9% for Gram-positive organisms, 66.7% for Gram-negative organisms and 74.1% overall. No superinfection was observed in any of patients treated. Side effects and clinical laboratory parameter abnormalities observed consisted of diarrhea in 7 (11.1%) of the 63 patients, eosinophilia in 2 (3.3%) of 61 tested, thrombocytosis in 3 (5.5%) of 55, elevation of direct bilirubin in 1 (3.3%) of 30, elevation of total bilirubin in 1 (3.1%) of 32, elevation of GOT in 4 (6.8%) of 59 and elevation of GPT in 1 (1.7%) of 59 patients tested. As an effect on the hemostatic mechanism of this drug, PIVKA II was detected in 1 patient (4.2%) of 24 tested, but findings of other coagulation tests were normal and none of patients showed bleeding tendency or inhibition of platelet aggregation. From the above results, it appears that SBT/ABPC is an efficacious and safe drug in the treatment of bacterial infections of pediatric patients.

Adolescent↗

PubMed1989

[The influence of cefpodoxime proxetil on the intestinal bacterial flora].

The influence of cefpodoxime proxetil (CPDX-PR, CS-807), a new oral cephalosporin, on the intestinal bacterial flora was studied in tetra-contaminated mice and in pediatric patients. CPDX-PR dry syrup was administered at a dose of 10 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of bacteria: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. No notable changes were observed in fecal viable cell counts except that slight decreases of E. coli counts were observed on the days 3 to 5 after starting administration. The subjects in the pediatric study were 5 children with infections, 3 boys and 2 girls at ages from 1 year 1 month to 6 years 10 months, with their body weights ranging from 9.3 to 23.8 kg. CPDX-PR dry syrup was administered at a dose between 3.0 to 3.7 mg/kg, 3 times a day for 4 to 7 days. Although some variations of the fecal bacterial flora were noticed between subjects during the administration of CPDX-PR, no notable changes were observed in major aerobic and anaerobic bacteria such as Enterobacteriaceae, Enterococcus, Bacteroides and Bifidobacterium in 4 of the 5 cases. Large decreases in Streptococcus, Enterobacteriaceae, Bifidobacterium, Eubacterium and anaerobic cocci and an increase in Enterococcus were observed in the other case. There was no case in which glucose non-fermenting Gram-negative rods and fungi became predominant. Regarding Enterobacteriaceae, transitory bacterial replacement was observed within the genus. Fecal concentration of CPDX during the administration of CPDX-PR was extremely low or below the detectable limit except one specimen from a case in which intestinal bacterial flora showed remarkable changes. From the above, CPDX-PR appears to be a drug with a relatively small influence on the intestinal bacterial flora.

Animals↗