Biomedical subjects

T Motohiro

Publications and source records attributed to T Motohiro.

At least 73 records · Page 4Linked to original sources

PubMed1988

[Pharmacokinetic and clinical evaluations of ceftriaxone in neonates and premature infants].

Following a one shot injection with ceftriaxone (CTRX) 10 mg/kg or 20 mg/kg into 23 neonates (1 to 24 days old) including premature infants, plasma levels of CTRX were measured up to 12 hours post-dose in some cases and up to 72 hours post-dose in others and also urinary levels and urinary recovery rates were determined up to 12 hours post-dose. Furthermore, clinical, bacteriological and infection-prophylactic effects of CTRX were evaluated by the intravenous administration with the mean dose of CTRX of 47.7 mg/kg once daily or half the dose twice daily for 9 days on the average into 46 infants (0 to 6 months old) including neonates and premature infants; i.e., 21 cases with actual or suspected bacterial infections for the evaluation of clinical and bacteriological effects and 25 without bacterial infection for the evaluation of prophylactic effects against bacterial infection. The safety of CTRX was evaluated in 53 cases including 7 which were omitted from the efficacy evaluation due to adverse reactions and also in some cases from clinical laboratory parameters. The following is a summary of the results obtained: 1. Following the administration with CTRX 10 mg/kg into each of the neonates 6, 12, 13 and 21 days old (the 21 old one was premature), plasma levels of CTRX in these subjects reached their peaks at 5 minutes post-dose at levels of 59.38, 53.13, 37.50 and 50.00 micrograms/ml, respectively. The peak levels were similar to each other with an exception of the rather low level in the 13 day-old neonate. The plasma half-life times of CTRX in these subjects were 9.762, 7.775, 7.330 and 8.149 hours, respectively: The younger the infant the longer the half-life tended to be except the premature cases. Similarly, the younger the infant the larger the AUC was except for the premature case with the AUC values of 511.169, 324.714, 236.346 and 326.825 micrograms.hr/ml, respectively. The Vds were 0.709, 1.004, 1.316 and 0.696 liters, respectively, and the value for 13 day-old neonate was the largest. Urinary levels of CTRX reached between 42.00 and 298.30 micrograms/ml at some time within 12 hours post-dose in any cases. Urinary recovery rates in 12 hours post-dose were 79.98, 52.00, 56.82 and 60.14%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗

PubMed1987

[Pharmacokinetics and clinical studies of flomoxef in the pediatric field].

Flomoxef (FMOX, 6315-S), a new intravenous cephem antibiotics, was administered to a total of 11 cases with their ages ranging from 7 years and 4 months to 10 years and 10 months. Among them, two were administered with (FMOX at) a dose level of 10 mg/kg, three each with 20 mg/kg and 40 mg/kg using one shot intravenous injection, and the remaining 3 with 40 mg/kg by intravenous drip infusion over 30 minutes. Plasma concentrations, urine concentrations and urinary recovery rates were determined. The clinical efficacy of FMOX was evaluated in 2 cases with tonsillitis, 45 with acute pneumonia, 10 with urinary tract infections, 2 with purulent lymphadenitis, and 2 with abscess, a total of 61 cases. Of these cases, one case of pneumonia in which a side effect occurred was excluded from the evaluation because the treatment was interrupted short of the required period. In the remaining 60 cases, the mean daily dose was 79.3 mg/kg in 3 or 4 divided doses and, except one case treated by 30-minute intravenous drip infusion, all cases were treated by one shot intravenous injection for a mean period of 6 days. Bacteriological effects of FMOX, its side effects and influences on laboratory test values were also investigated. 1. Maximum plasma concentrations after one shot intravenous injections of FMOX occurred at 5 minutes after administration regardless of dose levels (10 mg/kg in 2 cases, 20 mg/kg in 3 and 40 mg/kg in 3). Mean peak values obtained upon the 3 different dose levels were 62.5, 103.1 and 244.7 micrograms/ml, respectively. Mean plasma half-lives were 0.670, 0.915 and 0.595 hour, and mean AUCs were 33.0, 65.2 and 133.1 micrograms.hr/ml, respectively. Thus, a positive dose-response relationship was found among the 3 doses. 2. Plasma concentrations after 30-minute intravenous drip infusions of FMOX at 40 mg/kg always reached a peak at 30 minutes after the initiation of infusion, i.e. at the completion of infusion, and the mean value for 3 administrations was 151.0 micrograms/ml. The mean half-life was 0.973 hour and the mean AUC was 149.1 micrograms.hr/ml. 3. Maximum concentrations in urine after one shot intravenous injections of FMOX were always obtained in 0 approximately 2 hours after administration regardless of dose levels (10 mg/kg, 2 cases, 20 mg/kg, 3 cases and at 40 mg/kg, 3 cases) and mean values for the 3 dose levels were 2,570, 4,410 and 6,290 micrograms/ml, respectively. Thus, urine concentrations were also dose-dependent.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗

PubMed1987

[Fecal and urinary excretion of norfloxacin in adults].

Norfloxacin (NFLX) a synthetic oral antibacterial agent of quinolone carboxylic acid, was given to 6 healthy men aged 23 to 29 years and weighing 57 to 88 kg (average 64.7 kg) at a dose of 200 mg (two 100 mg tablets) once after breakfast and its fecal and urinary recoveries were determined for 5 days after the administration. Fecal and urinary recoveries of NFLX or ciprofloxacin (CPFX) were examined under various experimental conditions where the drugs were added to the urine or feces. Effects of the drug on the clinical laboratory test parameters and side effects were also examined. The following results were obtained. 1. NFLX reached the highest level in the feces in 5 cases in 24 hours and in 1 case in 48 hours; average peak fecal level was 137.1 micrograms/g in 24 hours. Fecal recoveries were 2.32 to 36.90% in 5 days after dosing with an average of 13.83%. 2. Urinary levels of the drug reached their peaks within 24 hours (average 51.46 micrograms/ml) in all cases and then decreased. Urinary recoveries were 11.15 to 46.44% in 5 days after dosing. Both fecal and urinary levels of the drug varied greatly among the subjects. 3. The sum of the fecal and the urinary recoveries in each case varied from 13.47 to 76.88% (average 42.24%).(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗

PubMed1987

[Effects of cefotaxime on the coagulation system, especially their dependence on vitamin K-related factors].

The authors administered cefotaxime to 20 children and studied laboratory parameters concerning peripheral blood: hemoglobin count, blood platelet count, red blood cell count, and hematocrit value, and the coagulation system: protein induced by vitamin K deficiency or by the presence of a vitamin K antagonist II (PIVKA II), hepaplastin test (HPT), prothrombin time (PT) and active partial thromboplastin time (APTT). The results obtained are summarized as follows: 1. Peripheral blood No abnormal values were observed. 2. Coagulation system (1) PIVKA II: In all cases, PIVKA II was negative. (2) HPT, PT and APTT: In all cases, no significant changes of these values which would suggest the tendency for prolonged bleeding were observed.

Adolescent↗

PubMed1987

[Pharmacokinetic and clinical studies of cefuzoname in the pediatric field].

Newly developed cefuzoname (CZON) was tested in 21 children and serum and urinary concentration and urinary recovery rates were determined. To 9 cases, 3 groups of 3 cases each, CZON was given at 10, 20 or 40 mg/kg one shot intravenously, and to 12 cases, 3 groups of 5, 3, 4 cases each, 10, 20 or 40 mg/kg was drip-infused over 1 hour. To 1 case of purulent meningitis 55.6 mg/kg was given one shot intravenously and concentrations in cerebrospinal fluid (CSF) and serum were measured. In 37 pediatric patients comprising 1 with tonsillitis, 24 with pneumonia, 1 with purulent meningitis and bacteremia, 7 with urinary tract infection, and 1 each with staphylococcal scalded skin syndrome, purulent lymphadenitis, periarthritis of jaw joint, maxillary sinusitis and orbital abscess, CZON was tried at 21.6 mg/kg (mean) per dose, 3 or 4 doses daily, one shot intravenously, for 7 days (mean). The clinical efficacy and antibacterial effectiveness were investigated. Also, the side effects were investigated and clinical laboratory tests done in the 37 pediatric cases plus 6 cases in which CZON was used but which were excluded from the efficacy analysis because they did not involve infections. The following is a summary of the results: 1. To 3 groups of 3 children each, 10, 20 or 40 mg/kg of CZON was given one shot intravenously. In each case the maximum serum concentration was observed at 5 min. after injection, and mean values of 3 groups with 10, 20 and 40 mg/kg dosing were 57.1, 147.2 and 316.7 mcg/ml respectively, indicating a dose-dependent response among the 3 groups. Mean half-lives were 0.83, 1.10 and 0.79 hours for 10, 20 and 40 mg/kg groups, respectively. The 10 mg/kg and the 40 mg/kg groups showed similar half-lives but the half-life of the 20 mg/kg group was a little longer than those of the other 2. 2. CZON was drip-infused over 1 hour to a total of 12 children divided into 3 groups of 5, 3 and 4 children at dose levels of 10, 20 and 40 mg/kg, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1987

[Pharmacokinetics of amikacin in children and neonates].

To evaluate pharmacokinetics of amikacin (AMK), one of the aminoglycoside antibiotics, children with ages from 2 days to 11 years were treated with various doses by various administration routes, and both plasma and urinary levels of AMK were determined. The following is a summary of the results obtained: 1. Of 6 children, three were treated with 2.0 mg/kg of AMK by a 30-minute intravenous drip infusion, and the other 3 with 4.0 mg/kg by a 60-minute. Peaks of average plasma levels were observed at the ends of the infusions in both cases, and their levels were 9.23 and 13.67 micrograms/ml, respectively, showing a dose-dependency. Both half-lives and areas under plasma concentration-time curves (AUCs) were similar to those of adults. However, the volume of distribution (Vd) showed a lower value than that of adults. Peaks of average urine levels were 149.3 micrograms/ml with 2.0 mg/kg in 0-2 hours after the start of the infusion and 223.3 micrograms/ml with 4.0 mg/kg in 2-4 hours. Average urinary recovery rates within 6 hours after the start of the infusion were 95.4% with 2.0 mg/kg and 85.7% with 4.0 mg/kg. These recoveries were equal to or higher than that of adults. 2. When 3.0, 4.0 and 6.0 mg/kg of AMK were administered to 3 groups of mature or premature babies by intramuscular injection, average peak levels of AMK in plasma were 6.26, 8.61 and 12.60 micrograms/ml, respectively, at 30 minutes after the injection, showing dose-dependency. In these groups, the younger the day age after birth was, the longer the half-life became. The AUCs were larger as the half-life became longer. The Vd was larger than that in the intravenous drip infusion group, but, any particular was not observed. Average peak levels of AMK in urine were 78.83 micrograms/ml at 4-6 hours with a dose level of 3.0 mg/kg, 99.17 micrograms/ml at 2-4 hours with 4.0 mg/kg and 139.20 micrograms/ml at 0-2 hours with 6.0 mg/kg. Average urinary recovery rates within 6 hours were 36.57% with 3.0 mg/kg, 34.67% with 4.0 mg/kg and 43.77% with 6.0 mg/kg. These recovery rates were markedly lower than those observed in adults and children. One of the causes of this low recovery is that mature and premature babies have immature renal functions. 3. When 3.0 mg/kg of AMK was administered to three premature babies by a 30-minute intravenous drip infusion, the average peak plasma levels was 7.61 micrograms/ml at the end of the drip infusion.(ABSTRACT TRUNCATED AT 400 WORDS)

Amikacin↗

PubMed1987

[Effect of norfloxacin on bacterial flora in human feces].

Norfloxacin (NFLX), a synthetic oral antibacterial agent of quinolone carboxylic acid, was given orally for 5 full days at a dose of 200 mg, three times daily after each meal to healthy normal men with ages between 22 and 25 years weighing 53.0 to 84.0 kg (average 67.0 kg). The actual regimen followed was that the drug was administered twice after lunch and supper on the first day of dosing, and once after breakfast on the last day of dosing. On the 5th day before the start of dosing, on the first, 3rd and 5th days (last dosing day) of dosing, and on the 3rd, 5th, 10th and 20th days after the end of dosing, effects of the drug on the fecal flora were examined and its fecal levels were determined. Susceptibilities against NFLX and nalidixic acid (NA) of various fecal isolates from 7 men were determined. Adverse effects and influences on clinical laboratory tests were also examined. The results obtained are summarized below. 1. Following the drug administration, a transient decrease or disappearance of Escherichia coli, Klebsiella sp., Citrobacter sp. and Enterobacter sp. of Enterobacteriaceae was noted. The 3 strains other than E. coli were isolated from increasing number of cases after the end of dosing. No constant trend was observed in the isolation of Proteus sp. Organisms belong to Enterobacteriaceae were isolated only in 4 and 2 cases after 3 and 5 days of the start of dosing, respectively, but then gradually increased to the predose level. Among other Gram-negative bacteria, no constant trend was noted in the isolation frequency of Plesiomonas sp. Pseudomonas sp. was isolated from 6 and 5 cases on the 3rd day after dosing and on the 3rd day after the end of dosing, respectively; the frequency of isolation increased after dosing. Gram-positive bacteria such as Staphylococcus sp. were isolated with a reduced frequency on the 3rd day of dosing. However, the number of isolates increased in all cases both on the 5th day of dosing and on the 3rd day after the end of dosing, and then decreased. No change was noticed in the number of isolates of Enterococcus sp., and no constant trend was observed for Micrococcus sp. and YLO. The average count of the whole aerobic bacteria did not change. Some strains decreased significantly after the start of dosing. 2. Among anaerobes, Bacteroides fragilis and other Bacteroides were isolated on every test day.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗

PubMed1986

[Pharmacokinetic and clinical studies of imipenem/cilastatin sodium in the pediatric field].

Pharmacokinetic and clinical studies of imipenem/cilastatin sodium (MK-0787/MK-0791), a newly developed combined antibiotic in a 1:1 ratio, were performed in the field of pediatrics. The MK-0787/MK-0791 was administered to 15 children. Ten and 20 mg/kg doses of MK-0787 were administered by a intravenous drip infusion for 30 minutes to 3 children each. In the remaining 9 cases, MK-0787 doses of 10, 20 and 30 mg/kg were administered to 3 children each by a 1 hour intravenous drip infusion. Levels of MK-0787 and MK-0791 in plasma, urine and urinary recovery rate of the drugs were also determined. In addition, MK-0787/MK-0791 was administered to a total of 29 children; 2 children with bronchitis, 16 with pneumonia, 4 with UTI, 2 with purulent lymphadenitis and 1 child each with tonsillitis, septicemia suspected disease, peritonitis, staphylococcal scalded skin syndrome and osteomyelitis/bacteremia. The average single dose was 15.3 mg/kg of MK-0787 and administrations were performed by 20-60 minutes intravenous drip infusion 3-4 times daily for an average period of 6 days. The clinical and bacteriological effects of this drug were evaluated in these cases and adverse reactions and unusual laboratory findings were also studied in a total of 33 cases including 4 other drop-out cases. Results of these studies were summarized as follows. In 6 children, 3 each who were given doses of 10 or 20 mg/kg, the mean peak plasma concentrations of the drugs were found at the end of the 30 minutes-infusion with values of 35.20 and 74.90 micrograms/ml for MK-0787 and 44.85 and 93.32 micrograms/ml for MK-0791 after the dose of 10 and 20 mg/kg, respectively. The peak plasma levels of MK-0791 were approximately 1.3 times higher than those of MK-0787 and higher peak levels were observed in the groups with larger doses of either drugs. In the 10 mg/kg group, the mean half-lives of MK-0787 and MK-0791 were 0.97 and 0.71 hour, respectively and those values were 0.89 and 0.63 hour, respectively in the 20 mg/kg group. In both group, MK-0787 tended to have longer half-lives than MK-0791. In 9 children, 3 each who were administered doses of 10, 20 and 30 mg/kg by a 1 hour intravenous drip infusion had the highest plasma levels for both MK-0787 and MK-0791 at the end of the infusion.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1986

[Fundamental and clinical studies of cefotiam in neonates and premature infants].

Single doses of cefotiam (CTM) by bolus injection of 20 mg/kg of CTM were given to 17 neonates and premature babies (11 prematures) and plasma and urine CTM levels as well as urinary recovery rates of CTM were determined. The CTM was also evaluated clinically with regard to therapeutic and protective effects, bacteriological efficacy as well as safety. A mean daily dose of 56.6 mg/kg of CTM was given intravenously in 2 to 4 divided doses for an average of 8 days to 11 neonates and prematures consisting of 1 case with pneumonia, 2 suspected septicemia, 3 urinary tract infections and 5 for prophylaxis against infections. (In the 6 babies evaluated for clinical effects, a mean dose of 59.8 mg/kg/day of CTM was given for an average 9 days). The findings of these studies are summarized below: The mean peak plasma level of 2 cases of 4-7 day-old neonates was 32.3 mcg/ml 5 minutes after injection. The mean AUC was 96.6 mcg X hr/ml, and the mean half-life was 2.12 hours. In 3 of the 4 neonates of 8-14 day-old group, the mean peak plasma level of 55.6 mcg/ml was obtained after 5 minutes. The mean AUC was 63.0 mcg X hr/ml and the mean half-life was 0.82 hour. Compared to the 4-7 day-old group, AUC was smaller and half-life was shorter in this group. In premature infants, plasma CTM levels were determined in 2, 1, 1, 5 and 2 cases of the 0-3, 4-7, 8-14, 15-21 and 22-28 day-old infants, respectively. In the 8-14 day-old group and one of 15-21 day-old group, peak plasma levels were obtained after 15 minutes. Peak plasma levels in the remaining groups, were attained after 5 minutes. Peak plasma levels in the 5 groups were 40.7, 48.4, 33.9, 38.1 and 45.3 mcg/ml, respectively. Mean or individual AUC's obtained after excluding markedly varying values from the respective groups were 122.0, 96.2, 65.2, 72.8 and 60.4 mcg X hr/ml, respectively. With the increasing age, the AUC tended to decrease. Mean or individual half-lives were 2.31, 1.47, 1.28, 1.41 and 0.96 hours, respectively, showing a tendency to decrease with increasing age. In 6 neonates, high urinary levels continued up to 6 hours after administration. Mean 6-hour urine recoveries in the 4-7 and 8-14 day-old groups were 16.6% and 43.0%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Cefotaxime↗

PubMed1986

[Fundamental and clinical evaluations of ceftazidime in neonates and premature infants].

Ceftazidime (CAZ) was administered to 24 neonates and premature infants aged 0-31 days in a dose of 10 mg/kg or 20 mg/kg by an intravenous bolus injection, and plasma concentration, urinary concentration and urinary recovery rate during the first 6 hours after the administration were determined. The CAZ was also administered to a total of 43 patients consisting of neonates, premature infants and infants at ages ranging from 0 day to 1 year 9 months (21 suffering or suspectedly suffering with various bacterial infections, and 22 treated for prophylaxis of infections), by intravenous bolus injections in a mean daily dose of 59.6 mg/kg in 2 to 4 divided doses for 9 days on the average. The clinical efficacy, prophylactic effects and bacteriological response were evaluated. Adverse effects of the drug were examined in 65 cases including 22 drop-out cases, and in some of them, abnormal laboratory findings were also examined. The results obtained are summarized as follows: Patients given 10 mg/kg of CAZ were divided into 5 groups on the basis of age: 0-3 days, 4-7 days, 8-14 days, 15-21 days, and 29 days and older, and mean peak plasma concentrations of CAZ were 40.7, 43.1, 37.1, 38.0 and 35.6 micrograms/ml, respectively, at 5 minutes after administration, with no significant difference. Mean AUC values were higher in younger-age groups, i.e. 189.9, 170.8, 159.1, 135.3 and 134.4 micrograms X hr/ml for the 5 different day-age groups, respectively, and mean half-lives of CAZ in plasma tended to be longer in younger-age groups, i.e. 3.16, 3.05, 2.84, 2.44 and 2.43 hours for the 5 groups, respectively. Patients given 20 mg/kg of CAZ were divided into 4 groups also on the basis of age: 0-3 days, 4-7 days, 8-14 days, and 15-21 days, and mean peak plasma concentrations for the 4 day-age groups were 72.9, 73.3, 70.0 and 78.4 micrograms/ml, respectively, at 5 minutes after administration, without any difference among these groups. Mean AUC values were 429.9, 327.3, 279.3 and 302.1 micrograms X hr/ml for the 4 groups, respectively, with the highest AUC in the youngest-age group. Dose response was observed in mean peak plasma concentrations and mean AUCs when 10 mg/kg and 20 mg/kg dose groups were compared for similar day-age patients. Mean half-lives of CAZ in plasma were 4.01, 3.51, 3.00 and 3.07 hours, the longest being in the youngest-age group.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacterial Infections↗

PubMed1986

[Effect of S6472 and cefaclor on bacterial flora in adult human feces].

S6472 is a mixture of cefaclor (CCL) granules with gastric-soluble coating and those with enteric-soluble coating at the ratio (in potency) of 4 to 6. With administration of this formulation, a prolonged blood level of CCL is obtained. S6472 and CCL were administered orally to 19 healthy male volunteers between 20 and 27 years of age (mean: 23 years) weighing between 51 and 80 kg (mean: 64.7 kg). Four subjects were given 2 capsules and 5 subjects were given 4 capsules each containing 187.5 mg of S6472, 30 minutes after breakfast and supper for 5 days. Five subjects were given 1 capsule and 5 subjects were given 2 capsules each containing 250 mg of CCL 30 minutes after breakfast, lunch and supper for 5 days. The number of fecal bacteria was examined 5 days before the start of administration, the day of the start of administration, 3 and 5 days after the start of administration, and 3, 5 and 10 days after the end of administration. Concentration of CCL in feces and susceptibility of isolated fecal bacteria (at the inoculum size of 10(6) cells/ml) to CCL were examined. Adverse reactions and the effects on laboratory test values were also checked. In 4 subjects receiving 375 mg of S6472 twice a day, the mean population of E. coli was 10(7)-10(9) cells/g feces on all days of observation. There was no effect on the population of Klebsiella sp., Citrobacter sp. Enterobacter sp. and other Enterobacteriaceae. The mean population of all Enterobacteriaceae was 10(8)-10(9) cells/g feces on all days of observation. The population of other Gram-negative bacilli did not show a consistent change, either. There was no effect on the population of Gram-positive bacteria such as Staphylococcus sp., Enterococcus, sp., Micrococcus sp., and of Candida sp. Among anaerobic bacteria, Bacteroides sp. showed the mean population of 10(10) cells/g feces on all days of examination. C. difficile was isolated from 2 subjects out of 4 at the level of 10(2)-10(3) cells/g feces 5 days after the start of administration and 3 days after the end of administration. However, there was no production of toxin in either of the 2 subjects. In another subject, C. difficile was isolated at 10(2)-10(4) cells/g feces with a toxin titre of 10(-3)-10(-4) 3 and 5 days after the start of administration and 10 days after the end of administration. The total population of anaerobic bacteria was 10(10)-10(11) cells/g feces on all days of examination.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗

PubMed1986

[Pharmacokinetics and clinical effects of cefixime in pediatrics].

Pharmacokinetics and clinical effects of cefixime (CFIX), a new oral cephalosporin antibiotic, in pediatric field were investigated. The result obtained were summarized as follows. CFIX (5% granules) was given to each of 5 children twice in a single dose of 1.5 or 3.0 mg/kg in a cross-over trial. The mean peak serum concentration of CFIX was 0.64 micrograms/ml at 4 hours after given the dose of 1.5 mg/kg and 1.15 micrograms/ml at 4 hours after the dose of 3.0 mg/kg. The mean half-life and the mean AUC values were 2.72 hours and 4.10 micrograms X hr/ml, respectively after the dose of 1.5 mg/kg, and 2.77 hours and 8.26 micrograms X hr/ml after the dose of 3.0 mg/kg. The urinary recovery was investigated in 5 children after the dose of CFIX of 1.5 mg/kg and in 4 children after the dose of 3.0 mg/kg. The mean peak urinary concentrations of CFIX and the mean 12-hour urinary recovery rates were 10.6-67.9 micrograms/ml at 2-10 hours and 15.7% after the dose of 1.5 mg/kg, and were and were 6.16-230 micrograms/ml at 2-8 hours and 18.9% after the dose of 3.0 mg/kg, respectively. CFIX was given to 6 children twice in a single dose of 50 mg either in the form of 5% granules or in capsules in a cross-over trial. The mean peak serum concentrations, half-life and AUC values were 1.26 micrograms/ml at 4 hours, 3.09 hours and 9.63 micrograms X hr/ml, respectively after the dose of 50 mg CFIX in 5% granules, and were 1.16 micrograms/ml at 4 hours, 2.87 hours, and 7.82 micrograms X hr/ml, respectively after the dose of 50 mg in capsules. The urinary recovery was investigated in 5 children. The mean peak urinary concentrations and the mean 12-hour urinary recovery rates were 19.1-114 micrograms/ml at 4-10 hours and 15.7%, respectively after the dose of 50 mg in 5% granules, and were 8.16-89.0 micrograms/ml at 4-10 hours and 11.3%, respectively after the dose of 50 mg in capsules. Clinical efficacy of CFIX was investigated in a total of 26 children including 2 with tonsillitis, 2 with acute bronchitis, 2 with scarlet fever and 20 with urinary tract infection. Each of children were given orally a dose of 2.6 mg/kg CFIX 2-3 times a day for 11 days in average.(ABSTRACT TRUNCATED AT 400 WORDS)

Acute Disease↗

PubMed1986

[Effect of cefminox on bacterial flora in human adult feces].

Cefminox (CMNX), a new cephamycin, was administered by one shot intravenous injection twice daily with a dose of 1,000 mg each time for 5 days to seven healthy male volunteers whose ages ranged from 21 to 28 years (mean: 25 years) and body weights were from 60 to 92 kg mean: 72 kg). The effect of the drug on fecal bacterial flora was investigated and the concentrations of the drug in feces were measured on 5th day before the treatment, on 0, 3rd, and 5th day (the final day of the treatment) during the treatment, and on 3rd, 5th, and 10th day after the treatment. Antibiotic susceptibility tests of CMNX, cefmetazole (CMZ) and cefotaxime (CTX) against several strains of organisms isolated from feces of the seven volunteers were performed. Clinical adverse reactions and effect on laboratory examinations were also investigated. The results of the study are described as follows. Among Enterobacteriaceae, populations of E. coli, Klebsiella sp. and Citrobacter sp. temporarily disappeared during the treatment of CMNX. After 5-day-treatment, that of Citrobacter sp. transiently increased and the isolation of Enterobacter sp. increased during treatment and up to 5 days after treatment, while those of Proteus sp., H. alvei, or Serratia sp. did not show a definite change. The mean Enterobacteriaceae population in general was 10(8) to 10(9) cells/g feces, showing almost no variation, on all examination days except 5th day during treatment when these organisms were not isolated from only one subject. No remarkable change was not found in populations of other isolated organisms including Gram-negative bacilli; Aeromonas sp., Pseudomonas sp. and Acinetobacter sp., and Gram-positive bacteria; Staphylococcus sp., Enterococcus sp., Micrococcus sp. and Candida sp. Among anaerobes, the mean population of Bacteroides sp. was 10(10) to 10(11) cells/g feces, showing almost no variation, and C. difficile was not isolated from any subject, however the toxin was detected in samples from 5 of 7 subjects; one subject showed always positive for toxin on all examination days; 1 on 5th day during treatment to 10th day after treatment; 2 on 5th and 10th day after treatment, and 1 only on 10th day after treatment.(ABSTRACT TRUNCATED AT 400 WORDS)

Abdomen↗

PubMed1986

[Effect of orally administered lenampicillin and ampicillin on bacterial flora in human adult feces].

Newly developed lenampicillin (LAPC) which is a prodrug of ampicillin (ABPC), and ampicillin (as the control) were each administered to 6 healthy male volunteers, aged from 21 to 25 years (mean 22.4 years) and weighing 57-78 kg (mean 67.0 kg) to study the effect of LAPC and ABPC on fecal bacterial flora. Each drug was given orally 3 times daily (after meals) with each dose of 250 mg for five days. Changes of the fecal bacterial flora caused by the antibiotic were investigated by determining fecal bacterial counts on the 3rd day before the treatment, 0 (the start of treatment), 3rd and 5th days (the final day of treatment) during treatment, and 3rd, 5th and 10th days after the treatment. Fecal concentrations of LAPC and the metabolites (ABPC, 2-aminobenzyl penicilloic acid (ABPA) and 5S-ABPA) for the LAPC group and ABPC for the ABPC group were assayed. A single dose of 500 mg of LAPC was administered orally after breakfast to additional 6 healthy male volunteers and concentrations of LAPC, metabolites (ABPC, ABPA and 5S-ABPA) in the entire stool were determined daily for 5 successive days after the administration. Clinical adverse reactions and abnormal laboratory-findings caused by either drug were studied in the 18 volunteers. The results obtained are summarized as follows. In the bacterial flora of the 6 volunteers to whom LAPC was administered (the LAPC group), the number of isolated E. coli showed no tend of decrease. Mean bacterial counts obtained 3 days before the treatment and at the day of the treatment were 10(9) and 10(8) cells/g, respectively. These values were compared to the counts obtained on the 3rd and the 5th days during the treatment and were found to be about 10(2)-folds as high as the latter. The decreased counts observed on the 3rd and the 5th days did not last and counts increased again to similar levels observed before the treatment. Klebsiella sp. was isolated from 1 or 2 samples before the treatment. It was isolated from as many as 5-6 cases with mean bacterial counts of 10(7)-10(11) cells/g during and up to 5 days after the treatment. The frequency of isolation then decreased to 4 cases on the 10th day after the treatment.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

PubMed1985

[Fundamental and clinical studies of cefminox in children].

Cefminox (CMNX, MT-141), a newly developed injectable cephem antibiotic, was administered intravenously as one shot injection at 3 different dosages of 10, 20 and 40 mg/kg to 9 children; for each dose level 3 children were used. In these children serum and urinary concentrations as well as recovery rates were determined. In addition, in order to determine clinical and bacteriological efficacies of CMNX, it was used in the treatment of 37 cases of various infections consisting of 2 cases of acute tonsillitis, 1 case of acute tonsillitis associated with otitis media, 1 case of acute bronchitis, 1 case of chronic bronchitis, 20 cases of pneumonia, 1 case of pneumonia associated with otitis media, 8 cases of urinary tract infections, 2 cases of purulent lymphadenitis and 1 case of gluteal abscess. The drug was administered intravenously as one shot injection at a mean daily dosage of 76.6 mg/kg, in 4 divided doses in most cases, for a mean period of 6 days. Finally, in 43 cases added of 6 drop out cases which were included in analysis of efficacy side effects and abnormal laboratory findings were examined. The following results were obtained. In 9 cases, which received CMNX at 3 different dosages of 10, 20 and 40 mg/kg for 3 cases each intravenously as one shot injection, mean serum concentrations reached the peaks of 109.4, 218.1 and 357.1 mcg/ml at 5 minutes after injection, respectively, showing dose response relation. The mean half-lives were 1.74, 1.62 and 1.84 hours, respectively. The mean concentrations of CMNX in urine in the same cases as used for determinations of serum concentrations were highest during the 0 approximately 2 hours period, reaching 1,582, 3,304 and 4,618 mcg/ml at the respective doses. The mean recoveries within the first 6 hours were 82.8, 69.8 and 81.3%, the rate for 20 mg/kg group being lower than those obtained for the other groups. This is possibly due to 1 case which showed unusually low recovery rate of 44.4%. When this case is excluded, the recovery rates became similar for all groups. As to clinical results, responses rated as good or higher were obtained for 91.9% of the cases (34 cases/37 cases), with high efficacy rate. No side effects were seen in 43 cases included of drop out cases.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

PubMed1985

[Effect of BRL 25000 (clavulanic acid-amoxicillin) on bacterial flora in human feces].

BRL 25000 (187.5 and 375 mg tablets), a formulation of CVA-K and AMPC in the ratio of 1:2, and AMPC (as control drug) were administered to healthy volunteers, aged 20 approximately 28 years and weighing 60 approximately 85 kg (68.8 kg, on average). Each drug was administered 3 times a day (after meals) for 5 days and the volunteers were separated into 3 groups of 4 subjects each. The effect on the fecal flora was studied before dosage, during administration (day 3 and 5) and day 3 and 5 after the administration course was completed. Studies were undertaken to isolate C. difficile on the last day of administration and 3 and 5 days after administration had ceased. Fecal concentrations and the susceptibility of the isolates to AMPC, CVA-K and BRL 25000 were measured. Side effects and laboratory findings were studied. The results obtained were as follows: 1. In BRL 25000 (187.5 mg X 3/day) group, the population of E. coli was on average, 1 X 10(6) approximately 9 X 10(6) cells/g feces before initiation of administration and it increased by 2 logarithms 3 and 5 days after initiation of administration. By 3 and 5 days after end of administration, the E. coli population was similar to the initial population. The population of Klebsiella sp. was 1 X 10(6) approximately 9 X 10(6) cells/g feces on average before commencement of dosage and it increased by 2 logarithms 3 days after initiation of administration but there was no consistent change in the Klebsiella sp. population thereafter. The Enterobacter sp., population was not consistent neither was the population of other Enterobacteriaceae. In total, the mean Enterobacteriaceae population was 1 X 10(7) approximately 9 X 10(7) cells/g feces before initiation of administration and increased by 2 logarithms 3 days after initiation of administration, and then returned to the initial level 5 days after end of administration. No consistent changes in population were noted for the other Gram-negative bacilli. The Staphylococcus sp. population was 1 X 10(6) approximately 9 X 10(6) cells/g feces on average before initiation of administration. This organism was detected in only 1 case 3 days after initiation of administration and in another 5 days after initiation of administration, thereafter, the population was similar to the initial population.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

PubMed1985

[Effects of KS-R1 (ampicillin suppository) and ampicillin oral dosing on fecal flora of children].

A newly developed product, KS-R1 (a suppository containing 250 mg potency of ampicillin (ABPC)), was given to 7 children (5 boys and 2 girls) ranging from 4 years and 5 months to 8 years and 10 months in age, 3 times a day (average daily dose, 62.4 mg/kg) for 5 days. As a control, the same amount of ABPC dry syrup was given orally to 7 children (4 boys and 3 girls) ranging from 2 years and 8 months to 7 years and 7 months in age, 3 times a day (average daily dose, 55.3 mg/kg) for 5 days. The effects of these 2 preparations on the bacterial flora of the feces were investigated, and concentrations of ABPC in the feces and sensitivities of the isolated strains to ABPC were determined. The results were as follows. As for Gram-negative bacilli in the feces from children given KS-R1, there was no change in Escherichia coli, Klebsiella sp., Citrobacter sp. and Enterobacter sp. which were isolated from many children 3 days after the end of treatment, but they did not show any constant pattern of change in mean number. Other species did not show any pattern of increase in the number of children from whom they were isolated, or in the number of bacteria during the course after the beginning of treatment. The total number of bacteria identified as Enterobacteriaceae was at the level of 10(8) cells/g on any day of examination. Of Gram-negative bacilli other than Enterobacteriaceae, Pseudomonas sp. showed no constant pattern of change in number. On the other hand, of Gram-positive bacteria, there was no constant pattern of change in the number of Staphylococcus aureus, Coagulase-negative Staphylococci began to be isolated from many children 5 days after the beginning of treatment and were isolated from all children 5 days after the end of treatment, but there was no tendency for the mean number to increase. Enterococcus sp. was not isolated from 3 children 3 days after the beginning of treatment, and was decreased in number by one order in 3 out of other 4 children as compared with before-treatment. However, this species was isolated from all children 3 days after the end of treatment, and the mean number of bacteria was similar to that before-treatment although the number of bacteria was different in individual children.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

PubMed1985

[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.

Bacteria↗