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Biomedical subjects

T Motohiro

Publications and source records attributed to T Motohiro.

At least 91 records · Page 5Linked to original sources
PubMed1985

[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)

Adult↗
PubMed1985

[Experimental and clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules in the field of pediatrics].

MICs of BRL 25000, a combination of a newly developed beta-lactamase inhibitor CVA and AMPC in the ratio of 1 to 2, were determined against a number of bacterial strains and compared with those of AMPC, CVA, CEX and CCL. The 98 bacterial strains tested included 2-S. aureus, 23-H. influenzae, 25-E. coli, 22-K. pneumoniae and 26-P. mirabilis. In pharmacokinetic studies, BRL 25000 medium granules were administered to groups of 3 male subjects, aged between 7 years 8 months and 9 years 5 months, at doses of 10, 15 and 20 mg/kg, 2 hours after a meal. The resultant serum and urine concentrations and drug recoveries were measured. Furthermore, BRL 25000 was administered to a total 43 patients (2-pharyngitis, 8-tonsillitis, 3-bronchitis, 2-pneumonia and 28-urinary tract infection) whom clinically evaluable. An average daily dosage of 45.3 mg/kg was given, in 3 or 4 divided doses, for a period of 8 days on average. Clinical and bacteriological effects as well as side effects were studied. In the microbiological studies on 98 clinical strains, including beta-lactamase negative bacteria, BRL 25000 showed MICs against the Gram-positive cocci (2-S. aureus) superior to the other 4 drugs at inoculum sizes of 10(8) and 10(6) cells/ml. For the Gram-negative bacilli, against H. influenzae at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but superior in the large MIC range to AMPC, and was superior to the other 3 drugs. Against E. coli at an inoculum of 10(8) cells/ml, BRL 25000 showed antibacterial activity next to AMPC and CCL whilst at an inoculum of 10(6) cells/ml, it was inferior in the small MIC range but superior in the large MIC range to AMPC and CEX and was inferior to CCL but superior to CVA. Against K. pneumoniae at an inoculum of 10(8) cells/ml, BRL 25000 was equal to AMPC, CVA and CEX but inferior to CCL, whilst at an inoculum of 10(6) cells/ml, it was inferior to CCL but superior to the other 3 drugs. Against P. mirabilis at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but equal or superior in the large MIC range to AMPC, and was superior to CVA and CEX.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1985

[Clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules on skin and soft tissue infections in the field of pediatrics].

BRL 25000 is a combination of a newly-developed beta-lactamase inhibitor clavulanic acid (CVA) and amoxicillin (AMPC) in the ratio of 1 to 2. The drug, as medium granules, was administered to a total of 92 pediatric patients, ranging in age from 1 month to 13 years and 2 months, with cutaneous/soft tissue infections (70 impetigo, 6 furuncle, 7 phlegmon, 6 abscess and 3 cases of lymphadenitis). It was found subsequently that 2 of the 70 impetigo cases had received topical antibiotic medication and these were excluded from clinical evaluation to give a total of 90 evaluable cases. The daily dosage of BRL 25000 ranged from 23.7 to 75.0 mg/kg, given in 3 or 4 divided doses (average 48.5 mg/kg) and the duration of treatment was for 3 to 13 days (average 6 days). Clinical isolates of S. aureus from the above cases were examined for beta-lactamase production and their susceptibility determined to the 5 antibiotics BRL 25000, AMPC, CVA, cephalexin (CEX) and cefaclor (CCL). The drugs' clinical effects on the various diseases, bacteriological effects and side effects were also studied. At an inoculum of 10(8) cells/ml, major MICs of BRL 25000, AMPC, CVA, CEX and CCL against 71 strains of S. aureus, including beta-lactamase negative ones, were 3.13 mcg/ml, 12.5 mcg/ml, 50 mcg/ml, 12.5 mcg/ml and 12.5 mcg/ml, accounting for 60.6, 38.0, 49.3, 38.0 and 43.7% of the strains respectively, whilst at an inoculum of 10(6) cells/ml, major MICs were 1.56 mcg/ml, 3.13 mcg/ml, 25 mcg/ml, 6.25 mcg/ml and 3.13 mcg/ml, accounting for 57.7, 33.8, 83.1, 50.7 and 54.9%, respectively. It was noted that all drugs tended to show smaller MIC values as the inoculum size was reduced to 10(6) cells/ml and that BRL 25000 showed the most potent antibacterial activity of all 5 drugs.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1985

[Basic and clinical trials of aztreonam in the field of pediatrics].

Serum and urinary concentrations and recovery rates of aztreonam (SQ26,776, AZT), a newly developed antibiotic, were studied for a total of 20 pediatric cases by one-shot intravenous injections of 10, 20 and 40 mg/kg to 3, 4 and 3 cases, respectively, and by intravenous drip infusion of 10, 20 and 40 mg/kg to 3, 4 and 3 cases for 1 hour, respectively. Clinical and bacterial effects of AZT were studied by administering 76.7 mg/kg per day on average for a total of 36 cases of tonsillitis (6), pneumonia (13), otitis media and pneumonia complication (1), pleurisy (1), sinusitis (1) and UTI (14). The above daily dose was given t.i.d. (9 cases) or q.i.d. (27 cases), by intravenous drip infusion for 30 minutes for one t.i.d. case and by one-shot intravenous injection for 7 days for the remaining 35 cases. Also, side effect and laboratory values were examined for 43 cases including 7 dropouts. Serum concentration of AZT in 10 pediatric cases were measured by dosing 10, 20 and 40 mg/kg by one-shot intravenous injection to 3, 4 and 3 cases, respectively. In every dosage group, the serum concentrations were highest 5 minutes after the intravenous injection with average values of 91.0, 174.0 and 175.3 mcg/ml, respectively. Dose response was observed between 10 mg/kg dose group and 20, 40 mg/kg dose groups, but it was not between 20 mg/kg group and 40 mg/kg group. This was considered to be attributable to the individual case-fluctuations in the 2 groups and to a high concentration case of 240.0 mcg/ml in the 20 mg/kg group. Half-life of each dosage group was 1.55, 1.65 and 1.93 hours. Serum concentrations of AZT in 10 pediatric cases at the dosage level of 10, 20 and 40 mg/kg for 3, 4 and 3 cases, respectively, by 1 hour intravenous drip infusion were highest at the end of the administration with average values of 95.7, 126.0 and 170.7 mcg/ml, respectively. There was a dose response among the 3 groups and the half-life of them were 1.02, 1.41 and 2.48 hours, respectively. A longer half-life of the 3rd group with 40 mg/kg administration than the other 2 groups was due to 1 particular case of 4.44 hours with unknown cause of such an exceptional extension.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1985

[Fundamental and clinical studies of aspoxicillin in the pediatric field].

Aspoxicillin (ASPC), a new semisynthesized penicillin, was administered to 20 children; by one shot intravenous injection in the doses of 10, 20 and 40 mg/kg to each of 3 children, and by intravenous drip infusion in the doses of 20 and 40 mg/kg over a period of 1 hour to 8 and 3 children, respectively, and the serum levels, urinary levels and recovery rates were determined. ASPC was administered to 1 patient with tuberculous pleurisy in the dose of 20 mg/kg by one shot intravenous injection, then the thoracic fluid level and serum level were determined. In addition, ASPC was administered to 3 children with tonsillitis, 3 with bronchitis, 40 with pneumonia, one each for pleuropneumonia, pleurisy, lung abscess, scarlet fever, staphylococcal scalded skin syndrome and purulent lymphadenitis and 2 with UTI (total 54 children), in the mean dose of 81.4 mg/kg/day t.i.d. (12 children) or q.i.d. (42 children) by one shot intravenous injection for 6 days on the average, and clinical effectiveness and bacteriological response were evaluated in these cases, and adverse reactions and abnormal laboratory findings were examined in the 60 cases which included 6 drop-out cases. After the administration of ASPC to 9 children; 10, 20 and 40 mg/kg to each of 3 children, by one shot intravenous injection, the mean serum levels reached to the peak of 58.4, 147.0 and 221.0 mcg/ml, respectively, in 5 minutes. The mean half-lives were 1.03, 1.01 and 1.23 hours, and the mean areas under the curve (AUCs) were 44.9, 94.1 and 192.9 mcg X hr/ml, respectively. A dose response was seen among the 3 dosage levels. After the administration of ASPC to 11 children; 20 and 40 mg/kg to 8 and 3 children, respectively, by intravenous drip infusion over a period of 1 hour, the mean serum levels reached to the peak of 58.2 and 114.0 mcg/ml, respectively, on completion of the administration. The mean half-lives were 1.22 and 1.09 hours, and the mean AUCs were 109.4 and 181.7 mcg X hr/ml, respectively. A dose response was observed between the 2 dosage levels. In the above mentioned each 3 cases receiving one shot intravenous injection in the dose of 10, 20 and 40 mg/kg, the mean urinary levels of ASPC reached to the peak of 1,000.0, 2,300.0 and 4,350.0 mcg/ml, respectively, at 0 approximately 2 hours after the administration, and the urinary recovery rates during the first 6 hours were 66.1, 66.5 and 56.9%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Amoxicillin↗
PubMed1985

[Influence of ceftriaxone on bacterial flora in human feces].

Ceftriaxone (CTRX), a newly developed antibiotic agent, was administered at 1,000 mg intravenously twice a day for 5 days to 7 healthy volunteers aged 21 to 26, weighing 61 to 79 kg (mean: 67.7 kg). The fecal bacterial flora was examined and the fecal level of CTRX was determined before, on 3 and 5 days after starting the administration, and on 3, 5 and 10 days after terminating the administration. At the same time, various bacteria isolated from the collected fecal specimens were studied for the sensitivity to CTRX, CEZ, CMZ and CTX. Adverse reactions and influence on various clinical laboratory parameters of CTRX were also examined. The results were as follows. Fecal bacterial flora: Enterobacteriaceae was at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) before starting the administration. The bacteria were detected from none of the 7 subjects on 5 days after starting the administration and on 3 days after terminating the administration. On 10 days after terminating the administration, the bacteria were detected in 6 out of 7 subjects at the level of 10(3) to 10(7) cells/g (mean: 10(7) cells/g). The level was the same as before starting the administration as a whole, but it had not been recovered to the initial level in any individual subject. With regard to other Gram-negative bacilli, P. aeruginosa which was isolated from none of the 7 subjects before starting the administration was detected at the level of 10(2) to 10(6) cells/g in 1 or 2 subjects on 3 days after starting, and on 3, 5 and 10 days after terminating the administration. Concerning Gram-positive bacteria, Staphylococcus sp. was isolated at the level of 10(3) to 10(4) cells/g in 3 subjects before starting the administration. The detection rate was decreased after starting the administration; it was detected in 2 and 1 subjects on 3 and 5 days after starting the administration, respectively, and in 1 subject on 3 days after terminating the administration. Then the detection rate was gradually increased; i.e., in 3 and 5 subjects on 5 and 10 days after terminating the administration, respectively. The level became gradually higher from on 5 days after terminating the administration than before starting the administration. Enterococcus sp. was isolated at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) in all of the 7 subjects before starting the administration. It was was detected in 1 and 4 subjects on 3 and 5 days, respectively, after starting the administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗
PubMed1985

[Fundamental and clinical studies on intravenous drip infusion of dibekacin in the pediatric field].

Dibekacin (DKB), an antibiotic of aminoglycoside group, was administered at 4 different dosages of 0.5, 1.0, 1.5 and 2.0 mg/kg as intravenous drip infusion taking 30 minutes or 1 hour. For each dose level, 3 cases each were used out of 24 boys from 1 year and 1 month to 14 years and 7 months of age, and serum concentrations as well as urinary concentrations and recovery rate were determined. After removed of 4 cases unassessable of therapeutic efficacy, 7 cases consisting of 1 case of chronic bronchitis, 1 case of lung abscess and 5 cases of urinary tract infections were treated with DKB at a mean daily dosage of 3.3 mg/kg in 2 or 3 divided doses as intravenous drip infusion taking 30 minutes or 1 hour. The mean treatment period was 7 days. The clinical and bacteriological results were analyzed in these cases and for analysis of side effects drop out cases were also included. The following results were obtained. Following 30 minutes intravenous drip infusion of DKB at 0.5, 1.0, 1.5 and 2.0 mg/kg, the serum concentration peaked at the end of infusion for all dose levels. The highest peak concentration of 9.17 mcg/ml was obtained for the dose level of 2.0 mg/kg. The highest dosage with which serum concentration does not exceed concentrations of 10 to 12 mcg/ml was found to be 2.0 mg/kg. The mean highest serum concentrations obtained were 1.65, 3.49, 5.40 and 8.67 mcg/ml for the dosages of 0.5, 1.0, 1.5 and 2.0 mg/kg, respectively, and the mean AUCs determined by the two-compartment model were 2.99, 6.04, 10.5 and 14.2 mcg X hr/ml, respectively, showing dose response relation in terms of peak concentration and AUC among groups. The mean T1/2 values for each dosage were 1.55, 1.54, 1.77 and 2.03 hours, respectively, with a longer tendency in T1/2 for the dose level of 2.0 mg/kg with unknown cause. When 0.5, 1.0, 1.5 and 2.0 mg/kg of DKB were infused taking 1 hour, the peak of serum concentration appeared also at the end of the infusion. The highest concentration was obtained with 2.0 mg/kg and it was 7.02 mcg/ml. Considering from the concentrations obtained for 0.5 mg/kg and 1.0 mg/kg groups the highest dosage at which the serum concentration does not exceed 10 to 12 mcg/ml was estimated to be 2.5 mg/kg.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1985

[Clinical trial of SM-4300 in the pediatric field].

SM-4300, a newly developed human immunoglobulin for intravenous use, was administered to 6 patients in the pediatric field. Two cases out of 3 cases with immunodeficiency syndrome were studied in terms of absorption and excretion of SM-4300 and all of them were observed effect of preventive bacterial infection. Three cases were administered combination therapy with SM-4300 and antibiotics. Two cases were pneumonia and 1 case was pleurisy. The following results were obtained. Two cases with immunodeficiency syndrome were observed serum levels of immuno gammaglobulin before and after administration of SM-4300. At 2-3 hours after the administration of SM-4300, the serum levels got to peak and the half-lives were 22.1 days and 22.6 days, respectively. The half-lives of SM-4300 were similar to plasmin or polyethylene glycol treated and sulfonated human immunoglobulin. The clinical effects of substitution therapy against 3 patients with immunodeficiency syndrome were observed. Through the administration of SM-4300 every 18 to 21 days for 6 months, 1 case was doing well. One case with chronic bronchitis and otitis media was hanging in the balance as well as she has been administered other immunoglobulin preparations. The last case didn't control the serum levels of immunoglobulin because he did not visit a hospital until incidence of infectious disease.

Adolescent↗
PubMed1985

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

Aztreonam (AZT), a new injectable monobactam antibiotic, was administered to 7 healthy male volunteers, aged 21-28 years (23 years, on average) and weighing 60.5-87.0 kg, (69.5 kg, on average) by one shot intravenous injection of 1,000 mg twice a day for 5 days. The effect of AZT on the fecal flora was studied 3 days before administration, on the day of the initiation, 3 and 5 days (end of the administration course) after the initiation, and 3, 5 and 10 days after the end of the administration. Fecal concentration of AZT was also studied. Also, fecal concentration and recovery rate of AZT in 4 healthy male volunteers aged 23-31 years (26 years, on average), weighing 59.5-70.5 kg (65.6 kg, on average) were measured by injecting 1,000 mg of AZT by intravenous injection only one time. Susceptibility of the bacteria isolated from the 7 cases receiving consecutive dosage to AZT, cefmetazole (CMZ), latamoxef (LMOX), cefoperazone (CPZ) and ceftazidime (CAZ) as well as side effect and laboratory values were examined with the following results. In the fecal flora, the population of Enterobacteriaceae on average was 10(7) cells/g feces on the day of the initiation and decreased by 2 logarithms to 10(5) cells/g 3 days after the initiation, 10(5) cells/g feces 5 days after the initiation with no bacterial isolation in 2 cases, 10(7) cells/g feces on 3 and 5 days after the end of administration respectively with recovery of the population to the average population on the day of the initiation. However, it increased 10 days after the end of administration with the population of 10(9) cells/g feces due to the isolation of one 10(10) cells/g feces, which was an increase by 2 logarithms as compared with average population before the administration. It was also higher than the average population 3 days before the initiation of administration. Temporal decrease or disappearance of the bacteria were noted by the administration of AZT. As to other cases of Gram-negative bacilli, Pseudomonas sp. was detected from only 2 cases 3 days before the initiation of administration and on the day of the initiation, but there was an increase to 4 and 5 cases 3 and 5 days after the initiation respectively. Number of isolation returned to 2 cases, 3, 5 and 10 days after the end of administration respectively and it was same as the number before the initiation of administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗
PubMed1984

[Fundamental and clinical studies of sulbactam/cefoperazone in the pediatric field].

To 6 cases of children in 2 groups of 3 each, newly developed sulbactam/cefoperazone (SBT/CPZ) was given at 20 and 40 mg/kg by intravenous bolus injection, respectively, and the serum and urinary concentrations and recoveries of SBT and CPZ were determined. To 1 case of purulent meningitis, this drug was given at 40 mg/kg by intravenous bolus injection, and the cerebrospinal fluid and serum concentrations of SBT and CPZ were determined. Susceptibility tests to SBT/CPZ and CPZ of total 289 strains were conducted; Gram-positive cocci tested consisted of 26 S. aureus strains, 20 S. pyogenes strains and 21 S. pneumoniae strains, and Gram-negative bacilli consisted of 24 H. influenzae strains, 22 E. coli strains, 26 K. pneumoniae strains, 24 E. cloacae strains, 21 E. aerogenes strains, 19 Citrobacter sp. strains, 20 S. marcescens strains, 23 P. mirabilis strains, 23 indole-positive Proteus sp. strains and 20 P. aeruginosa strains. SBT/CPZ was given to total 43 cases at a mean daily dosage of 80.4 mg/kg, in 3 or 4 divided doses (6 cases in 3 and 37 cases in 4), 1 case receiving the drug by drip infusion over 30 minutes (in 3 divided doses) and all the other 42 cases by intravenous bolus injection, for 7 days on an average. They consisted of 2 cases of tonsillitis, 1 case of otitis media, 1 case of otitis media associated with mastoiditis, 30 cases of pneumonia, 1 case of suspected septicemia, 1 case of purulent meningitis, 5 cases of urinary tract infection, 1 case of purulent lymphadenitis and 1 case of submaxillaritis. And the clinical and bacteriological effects were evaluated. Also, side reactions and laboratory examinations for abnormal values due to administration of this drug were made on 47 cases including 4 drop-outs. The following results were obtained: After administration of this drug to 2 groups of 3 children each at 20 and 40 mg/kg by intravenous bolus injection, mean serum concentrations of both SBT and CPZ reached the peaks in 5 minutes; SBT levels were 60.9 and 124.7 micrograms/ml for the 2 groups and CPZ levels were 105.0 and 214.1 micrograms/ml, respectively. In either group, CPZ levels were 1.7 times as high as SBT levels, and there was observed a dose-response in both. In the 20 mg/kg group, mean half-lives of SBT and CPZ were 0.96 and 1.24 hours, respectively, and in the 40 mg/kg group, they were 1.01 and 1.32 hours, CPZ values tending to be longer.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

[Fundamental and clinical evaluation of ceftriaxone in the pediatric field].

Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX), a newly-developed injectable cephem antibiotic was performed as follows. The serum and urine concentrations of CTRX as well as the urinary recovery rate were determined in 7 children at 3 different dose levels; 3 cases administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg by one shot intravenous injection. The concentration in the cerebrospinal fluid was determined in 1 case of purulent meningitis associated with bacteremia, administered by one shot intravenous injection with 47.6 mg/kg. CTRX was also examined in its clinical and bacteriological efficacies by one shot intravenous injection for 8 days on average in a mean daily dose of 46.5 mg/kg, divided into twice a day in 31 cases, 3 times in 1 case, and 4 times changed from twice in 1 case; in a total of 33 children consisting of 3 with tonsillitis, 1 with chronic bronchitis, 20 with pneumonia, 2 with purulent meningitis associated with bacteremia, 3 with urinary tract infections, 1 with osteomyelitis associated with phlegmon, 3 with purulent lymphadenitis. The adverse reactions and laboratory test values were examined in a total of 40 cases, i.e., the above-mentioned 33 cases plus the 7 drop-out cases in which the clinical efficacy could not be evaluated. The results were as follows. The serum levels of CTRX in 7 cases consisting of 3 administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg reached their peaks 5 minutes after one shot intravenous injection and the mean values of them were 93.6 mcg/ml, 143.0 mcg/ml and 558.0 mcg/ml, respectively, indicating the existence of a dose-response among these groups, while the half-life times were 4.41, 5.86 and 4.09 hours. Among the 7 cases examined in the urinary levels as well as the serum levels, the 3 cases administered with 10 mg/kg reached the mean peak of 334.0 mcg/ml 2 to 4 hours after administration, while another 3 cases administered with 20 mg/kg showed peaks of 793.0, 522.0 and 536.0 mcg/ml, respectively, 2 to 4 hours, 4 to 6 hours and 6 to 12 hours after injection; this dispersion being partly because of that the urine specimen was unable to be collected regularly every hour in this dose group. In the case administered with 48 mg/kg, urinary level reached the highest value of 6,100.0 mcg/ml from 0 to 2 hours.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗
PubMed1984

[Fundamental and clinical studies of ceftazidime in the pediatric field].

Ceftazidime ( CAZ ), a newly-developed parenteral cephem antibiotic, was administered to 8 children; by one shot intravenous (i.v.) injection in the doses of 20 and 40 mg/kg each to 2 children, and by 30 minutes' i.v. drip infusion in the doses of 10 and 20 mg/kg each to 2 children, and the serum levels, urinary levels and recovery rates were determined. CAZ was also administered to 2 patients with purulent meningitis, one complicated with subdural abscess and the other with bacteremia, in the doses of 19.2 and 50.7 mg/kg, respectively, by one shot i.v. injection, and the CSF level of CAZ was determined. In addition, CAZ was administered to 2 children with acute bronchitis, 1 with chronic bronchitis, 37 with pneumonia, 3 with pleuropneumonia, 1 each for purulent meningitis, purulent meningitis accompanied with subdural abscess and purulent meningitis with bacteremia, 5 with urinary tract infections and 3 with purulent lymphadenitis (total 54 children), in the mean dose of 85.8 mg/kg/day mostly in 4 divided doses by one shot i.v. injection for 9 days on the average, and clinical effectiveness and bacteriological response were evaluated in these cases, and adverse events and abnormal laboratory findings were examined in the 66 cases which included 12 drop-out cases. 1. After the administration of CAZ to 4 children; 20 and 40 mg/kg each to 2 children, by one shot i.v. injection, the mean serum levels got to the peak of 115.8 and 199.5 mcg/ml, respectively, at 5 minutes. The results were good, showing dose response. The mean half-lives were 1.48 and 1.37 hours, respectively. After the administration of 10 and 20 mg/kg of CAZ each to 2 children by 30 minutes' i.v. drip infusion, the mean serum levels got to the peak of 58.5 and 80.0 mcg/ml, respectively, on completion of the administration, showing dose response. The mean half-lives were 1.06 hours in the former 2 cases, and 1.38 and 3.26 hours, respectively, in the latter 2 cases. The reason for the prolongation observed in 1 case was not clear. 2. In the above mentioned each 2 cases receiving one i.v. injection, the mean urinary levels got to the peak of 4,240 and 4,445 mcg/ml, respectively, at 0-2 hours after the administration , and the urinary recovery rates during the first 6 hours were high, 95.7% and 99.5%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

[A pharmacokinetic investigation of sisomicin administered intramuscularly to children].

For the purpose of studying the pharmacokinetic profile of sisomicin (SISO) and the proper conditions for its administration to children, SISO was administered intramuscularly to 10 infants aged less than 1 year, 16 young children and 18 school children at doses of 1.0, 1.5 and 2.0 mg/kg and its serum and urine levels were determined by bioassay. The mean peak levels of SISO in serum appeared at 1/4 hour in the infants, irrespective of the dose; the mean peak levels were 2.27, 3.05 and 4.83 micrograms/ml after the 1.0, 1.5 and 2.0 mg/kg doses, respectively. In the young children, the mean peak levels appeared at 1/4 hour after the 1.0 mg/kg dose and at 1/2 hour after both the 1.5 mg/kg and 2.0 mg/kg doses. The mean peak levels were 2.82, 3.80 and 6.43 micrograms/ml, respectively. In the school children, the mean peak levels appeared at 1/2 hour after all the doses and were 4.34, 5.31 and 6.87 micrograms/ml, respectively. The mean peak levels were in the order of school children greater than young children greater than infants and were dose-dependent. In the infants, the mean urinary recovery was 43.7% for the 1.0 mg/kg dose and 31.2% for the 1.5 mg/kg dose; in the young children, 50.5, 35.9 and 65.6% for the 1.0, 1.5 and 2.0 mg/kg doses, respectively; and in the school children, 54.2, 50.2 and 56.7%. Using the observed serum levels, the pharmacokinetic parameters were calculated according to the one-compartment open model theory. (1) The mean elimination rate constants (K) were calculated at 0.60, 0.67 and 0.56 hr-1 for the infants, young children and school children, respectively. There were found no great differences among the above 3 age groups. The mean absorption rate constants (ka) were 18.5, 7.6 and 5.9 hr-1 and the apparent volumes of distribution per kg body weight, Vd (L/kg), 0.44, 0.26 and 0.22 L/kg, respectively. These 2 parameters were significantly greater in the infants than in the young children and school children. The maximum serum concentration (Cmax) and the time when the concentration reaches a maximum (Tmax) were substantially in agreement with the observed values. The half-lives (T1/2) were 1.16, 1.03 and 1.23 hours for infants, young children and school children, respectively, and did not differ significantly among the 3 groups. A serum level simulation curve constructed by plotting the mean values for K, ka and Vd did not reveal any substantial deviation from the observed values.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

[Clinical trials of cefmetazole for pneumonia and pyothorax caused by Staphylococcus aureus resistant to cefazolin].

Cefmetazole (CMZ), an antibiotic agent of the cephamycin group, is resistant to beta-lactamase and has a broad antibacterial spectrum covering Gram-positive cocci and Gram-negative bacilli. However, it has not been indicated for Gram-positive cocci. We examined its clinical, bacteriological and side effects in 2 infants with pneumonia and 2 with pyothorax, which had been suggested to be caused by CEZ-resistant and CMZ-sensitive Staphylococcus aureus or other inflammatory organisms by a disc sensitivity test, for 2 years and 3 months from January, 1981 to March, 1983. The patients aged 1 to 22 months, and a mean daily dose of 108 to 115 mg/kg was divided into 2 to 4 equal doses and injected into the vein at one shot for a mean fo 19 days. The following results were obtained: The clinical effect of CMZ was evaluated to be good in 1 and fair in 1 of 2 infants with pneumonia, and excellent in 1 and good in 1 of 2 with pyothorax. Bacteriologically, S. aureus was removed in an infant with pneumonia and in 2 with pyothorax. Bacteriological test was not conducted in the remaining 1 with pneumonia. No side effects were found in any cases. Eosinophilia appeared as an abnormal clinical test value in a case, but the number of eosinophils became normal after termination of the medication. As mentioned above, CMZ manifested an excellent clinical effect in infants with pneumonia or pyothorax caused by S. aureus although the number of the patients was small. From the results the antibiotic agent can be expected to be effective in these disease.

Age Factors↗
PubMed1983

[Pharmacological evaluation of an ampicillin suppository (KS-R1) in acute pneumonia in children--a comparison with a parenteral preparation of ampicillin].

A comparative well-controlled study was performed to evaluate the efficacy and tolerability of KS-R1 (ampicillin (ABPC) rectal suppository) compared with those of intravenous injection of ABPC against acute bacterial pneumonia caused by ABPC-sensitive bacteria, such as Streptococcus pyogenes, Streptococcus pneumoniae and Haemophilus influenzae in pediatric field. KS-R1 at the dose of 250 mg X 4/day of ABPC in potency, or the intravenous injection at the dose of 125 mg X 4/day of ABPC in potency, was given to 68 cases of patients with bacterial pneumonia, aged between 10 months and 8 years and 2 months, for 7 days, as a rule. The clinical efficacy rates evaluated in 61 cases (KS-R1 group in 31 cases, intravenous group in 30 cases) on standard criteria of committee members were 93.5% for the KS-R1 group and 83.3% for the intravenous group, respectively. There was no significant difference between 2 groups. Evaluation by stratification according to the age showed that KS-R1 was significantly superior, the rate being 90.5% among the children from 1 year to 3 years in the KS-R1 group and 61.5% in the intravenous group. The bacteriological effect was evaluated in 16 cases (KS-R1 group in 7 cases, intravenous group in 9 cases), the disappearance rate was 100% for the KS-R1 group and 88.9% for the intravenous group, without significant difference. With regard to side effects, 66 cases (KS-R1 group in 35 cases, intravenous group in 31 cases) were strictly evaluated in relation to subjective and objective symptoms. As a result, no significant difference was noted between 2 groups in the incidence rate which was 17.1% for the KS-R1 group and 9.7% for the intravenous group. The above results indicate that against acute bacterial pneumonia in pediatric field, the KS-R1 at the dose of 250 mg X 4/day of ABPC in potency possesses clinical efficacy and safety similar to the intravenous injection at the dose of 125 mg X 4/day of ABPC in potency, and that it is a useful suppository.

Acute Disease↗
PubMed1983

[Clinical evaluation of josamycin for the treatment of Mycoplasma pneumonia in children].

Thirty-one strains of Mycoplasma pneumoniae were tested for drug sensitivity to both josamycin (JM) and erythromycin (EM), to evaluate the efficacy of JM for mycoplasmal pneumonia in children. In addition to the sensitivity tests of 31 M. pneumoniae strains against JM and EM, 50 patients, between the ages of 3 years 1 month and 13 years 3 months, suspected of suffering from mycoplasmal pneumonia were treated with 50 or 200 mg JM tablets at an average daily dose of 43.1 mg/kg t.i.d. or b.i.d. for an average period of 14 days; an additional 31 patients between the ages of 2 years 9 months and 11 years, suspected of suffering from this disease were treated with tablet or dry syrup of EM, with the exception of EM estolate, t.i.d. or b.i.d. at an average daily dose of 72.5 mg/kg for an average period of 15 days. Patients were selected in 37 and 22 mycoplasmal pneumonic patients respectively for JM and EM. Clinical and bacteriological effects, efficacy and side effects of the drugs on this disease were studied and the following results were obtained. Drug sensitivity test Of all 31 strains tested for JM sensitivity the populations which exhibited 0.125 mcg/ml were most abundant (18/31, 58.1%) and MIC pattern of all strains were distributed from 0.0313 to 0.125 mcg/ml. In the EM group, 61.3% (19/31) of the populations were sensitive at 0.015 mcg/ml, exhibiting the dominant distribution pattern and MIC range of all organism varied from 0.0078 to 0.0313 mcg/ml. Resistant strains were found to neither JM nor EM. EM was approximately 2 to 10 times more active than JM in MIC evaluation. Clinical effects of JM by daily doses Clinical effects relative to the daily dose were evaluated in 3, 7, 10 days after administration of drugs. The response was favorable, according to assessments of the attending doctors, in 96.7, 100% and 95.8% of the patient group given JM in a daily dose of 40-49 mg/kg, the group to which the largest number of patients belonged. Similar favorable results were obtained by the assessments of Evaluation Committee, showing 86.7, 96.7% and 100% of favorable response. Upon comparison, in the same interval, of these results with those of the groups given EM in a daily dose of 50 mg/kg, the group in which the largest number of patients were seen, there was no significant difference in the assessments either of the attending doctors or of the Evaluation Committee.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗