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Volume 34, Issue 11
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FUSANOSUKE YAMASAKU, HIDEO YAMADA1981 Volume 34 Issue 11 Pages 1429-1435
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTobramycin (TOB) was administered to 4 healthy adult volunteers (mean body weight 63.5 kg, surface area 1.71 m2) as one time 90 mg dose by intramuscular injection or by intravenous infusion (30 or 60 minutes) in a crossover study. Serum and urinary concentrations were assayed by bioassay and radioimmunoassay (RIA).Pharmacokinetic analysis was done with a one-compartment open model in the case of intramuscular injection and a two-compartment open model in the case of intravenous infusion.The correlation constant was 0.92, and the relation formula was y=0.81x+0.13 between bioassay and RIA.
In the case of intramuscular injection, the peak serum concentration was 5.1-6.3 mcg/ml (mean 5.3 mcg/ml), and values calculated with pharmacokinetic parameters from the mean serum concentration were Tmax=0.745 hour, Cmax=5.34 mcg/ml and half life (T1/2) =89.6 minutes.With 60 minutes intravenous infusion, the peak serum concentration was 6.7-9.1 mcg/ml (mean 7.5 mcg/ml), and the calculated value was 7.63 mcg/ml.The value after 2 hours was nearly equal to those for intramuscular injection.T 1/2 of /3-phase was 95.8 minutes.With 30 minutes intravenous infusion, the peak serum concentration was 8.4-11.8 mcg/ml (mean 10.2 mcg/ml), and the calculated value was 9.81 mcg/ml. T 1/2 of β-phase was 105.3 minutes and the serum concentration of the β-phase was same as that for intramuscular injection administration after 6 hours.
We concluded that 60 minutes intravenous infusion of TOB 90 mg is more effective and safe than the 30 minutes method from the standpoint of toxicity, and the serum concentration of the β-phase is similar to that with intramuscular injection. With each administration method, urinary recovery was 70-80% for 8 hours.View full abstractDownload PDF (882K) -
YOSHIKIYO TOYONAGA, YOSHIIE KUROSU, MAKOTO HORI1981 Volume 34 Issue 11 Pages 1436-1446
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSFundamental and clinical studies on tobramycin (TOB) by intravenous drip infusion were carried out, and following results were observed.
1) Serum concentration of TOB
TOB was administered1.5mg/kg or 3.0 mg/kg by intramuscular or intravenous drip infusion method to16pediatric patients.
In 1.5mg/kg dose, the mean peak serum concentration were 3.9 mcg/ml at the 1/4-1/2 hour after administration by intramuscular method, 4.9 mcg/ml at the 1/2 hour after adininistration by 30 minutes intravenous drip infusion, 6.4mcg/ml at 1hour by 60 minutes intravenous drip infusion method.The half lives (T 1/2) of TOB in those methods, were 1.48, 1.42, 1.26 hours, respectively.
In 3.0 mg/kg dose schedule by 30 or 60 minutes intravenous drip infusion method, the mean peak serum concentrations were 11.5 mcg/ml, 8.0 mcg/ml at the end of infusion, respectively.Those of the T1/2 were 1.54, 1.24 hours.
Pharmacokinetic parameters of TOB were following results.
The ranges of Vd (apparent volume of distribution), K10 (elimination constant (hr-1)), T 1/2 were 0.20-0.34L, 0.63-1.37 hr-1, 1.20-2.07 hrs., respectively and there was no significant difference in the serum concentrations and in the pharmacokinetic parameters.
2) Clinical results
Eight patients including 1 purulent cervical lymphadenitis, 4acute pyelonephritis, 2 broncho-pneumonia, 1-septicemia were treated with TOB 1.5 mg/kg or 3.0 mg/kg twice a day, by intravenous drip infusion for 6-15 days.
Clinical effects were excellent in 3 cases, good in 4 cases and poor in 1 case.
Efficacy rate was 87.5%.
No side effects were observed.View full abstractDownload PDF (1319K) -
HIDEAKI SUZUKI, TSUNEYUKI KUROSE, JIRO NAGAO, YOSHINOBU SUMIYAMA, MASA ...1981 Volume 34 Issue 11 Pages 1447-1450
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCefoxitin (CFX)was administered to the total of 21 hospitalized patients at a daily dose of 1 to 6 g for the duration of 6 to 23 days and the following results were obtained.
1)Clinical results of the 10 patients with surgical infections were excellent in 3 patients,good in 5,fair in 1 and poor in 1,with the efficacy rate of 90%.
2)CFX was also administered to 11 cases for prophylaxis of postoperative infections and the clinical efficacy rate was 100%.
3)Susceptibility tests showed all clinical isolates such as E. coil, Klebsiella and Gram-negative anaerobes were highly susceptibility to CFX except for Pseudomonas.
4)There were no subjective nor objective side effects related to CFX.
The above results indicate that CFX is exceedingly useful for the treatment of infections in the field of gastro-surgery.View full abstractDownload PDF (537K) -
Hanshin Infection Study GroupTADAHIRO TSUBAKIO, TERUO KITANI, KIYOYASU NAGAI, AKIHISA KANAMARU, ATS ...1981 Volume 34 Issue 11 Pages 1451-1456
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSSeventy patients with severe infection accompanying hematologic disorders including leukemia and lymphoma were treated with ticarcillin in combination with aminoglycosides and/or cephem derivatives.
Of the 58 patients in whom the efficacy could be evaluated, 17 (29%) responded markedly and 22 (38%) moderately, the effective rate being 67%.
Side effects attributable to the treatment were noted: rash in 2, fever and rash in 1, vascular pain in 2 (5 and 7 years of age). Renal and hepatic functions were abnormal in 4 each.However, these abnormal findings were not attributed to ticarcillin.
These results indicate that ticarcillin is an effective and safe antibiotic for the treatment of severe infection accompanying hematologic malignancy when used in combination with aminoglycosides and/or cephem derivatives.View full abstractDownload PDF (854K) -
TOMOMITSU HOTTA, NORIYUKI HIRABAYASHI, KAZUYUKI SHIMIZU, MAKOTO UTSUMI ...1981 Volume 34 Issue 11 Pages 1457-1464
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSInvestigation was made on absorption, excretion and clinical responses following intravenous drip infusion of amikacin (AMK) and the following results were obtained.
1) Serum concentrations of AMK were determined after completion of a 1 hour-course of its intravenous drip infusion at a dose of 200 mg, involving 2 patients with normal renal function and 1 patient with impaired renal function.In the patients with normal renal function, a mean peak serum concentration of 15.9μg/ml was reached at the termination of the intravenous drip infusion and, then, gradually declined to 0.97μg/ml at 6 hours after completion of the intravenous drip infusion.The halflives were 1.64 and 1.41 hours, respectively.In the patients with impaired renal function, the elimination of AMK from blood flow was markedly delayed and the serum concentration was 5.52μg/ml even at 6 hours after completion of the intravenous drip infusion. The half-life was prolonged, its value being 5.98 hours.
2) The mean urinary excretion rate for the patients with normal renal function was 67.7% within 7 hours, while the patient with impaired renal function had a lower rate of 14.0%.
3) Ten infectious patients with hematological malignant diseases were treated with AMK intravenous drip infusion.Clinical responses were excellent in 6, good in 2, fair in 1 and poor in 1.Thus, 80% of the patients responded to AMK.
4) In order to check the side effects of AMK, investigation was made on the results of various clinical laboratory tests and the subjective and objective findings.But, no side effects attributed to AMK were observed.
Therefore, it is thought that the intravenous drip infusion of AMK will be very useful when attention is paid to infusion time, dose and interval.View full abstractDownload PDF (1305K) -
TADAHIKO MATSUMOTO1981 Volume 34 Issue 11 Pages 1465-1469
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCefmetazole (CMZ) was applied to the subjects with infectious skin disease of more than middle severe cases in the present study, and the following results were obtained.
1. The clinical effects were as follows: among 15 clinical cases, 1 remarkably effective and 14 effective cases were observed, with 100% of effectiveness.
2. Bacteriological effects were as follows: 11 strains of S. aureus and 4 strains of S. epidermidis were isolated and all of them disappeared by the administration of CMZ.
3. Sensitivity test using a disc method showed that good sensitivity of better than (++) was obtained by CMZ and CEZ for all tested bacteria.
4. CMZ showed excellent clinical effects on the subjects to which oral cephalosporins and penicillins were not effective.
5. No undesirable side effects ascribable to the CMZ administration were observed.View full abstractDownload PDF (484K) -
TSUYOSHI KOCHI, TADAO HONDA, NOBUHIRO ITOH, MASAHIRO YOGO, HISAO YAMAG ...1981 Volume 34 Issue 11 Pages 1470-1476
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThis study was performed to develop a prolonged acting preparation on the bases of our in vitro study of AMPC that the bactericidal effects of AMPC were not proportional to the concentration on and above MIC but to the exposing time.
A desirable serum level was obtained in the AMPC preparation containing 30% of non-coated granules and 70% of enteric-coated granules dissolvable on and above pH 6.
The duration time of the serum concentration on and above 2.5μg/ml in the administration of this preparation (500mg (Potency)) was 5.3 hours and it was 2.4 times that of the conventional capsule (250mg (Potency)).
The prolonged activity of this preparation was also observed in the urinary concentration.
These results suggest that this prolonged action granules of AMPC could reduce the administration frequency and also might be more useful in increasing therapeutic effects than conventional capsule.View full abstractDownload PDF (753K) -
KEIU NINOMIYA, YUKIO HASEGAWA, KEIKO HAMAYA, KAORUKO MASUDA, TAKEHITO ...1981 Volume 34 Issue 11 Pages 1477-1484
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSA fundamental and clinical study of ceftizoxime (CZX), a new cephalosporin antibiotic, has brought about the following results.
1. The antibacterial activity of CZX against Bacteroides fragilis and B. thetaiotaomicron was superior to that of CEZ, but inferior to that of CFX.CZX was the most active of the 3 drugs against B. distasonis, and was as active as CFX against B. vulgatus.The MICs of CZX against Peptococcus, Peptostreptococcus and anaerobic Streptococcus were 1.56μg/ml or lower. CEZ was more active than CZX against these anaerobic cocci.
2. The concentrations of CZX in female genital organs and retroperitoneal dead space exudate after drip infusion of 1g were high enough to fulfill the MICs of many bacterial isolates.
3. CZX administered intravenously to 9 patients in daily doses of 1-8g for 4-11 days was 100% effective. Pathogenic bacteria in 6 of the patients were eradicated in 4 and partially eradicated in 1. The other patient had no bacteriological examination ter therapy.
4. No adverse reaction was observed.
From above results it is concluded that CZX must be one of the most effective antibiotics for the treatment of gynecological infections.View full abstractDownload PDF (1007K) -
KOKI YAGISHITA, HIDEAKI JINNOUCHI, HARUO YAMAMOTO1981 Volume 34 Issue 11 Pages 1485-1495
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe investigation of mechanism of synergistic action with SYN and ECZ was performed using C. albicans SC5314 so that SYN was confirmed to show strong synergistic effects against Candida sp.in particular with addition of extremely small quantities under the MICs of imidazole antimycotics such as ECZ, MCZ and CTZ.
The synergistic effect of antifungal activity against C. albicans SC5314 with a combination of SYN and ECZ (SYN+ECZ) showed fungistatic action. Effect of SYN+ECZ on osmotic resistance was not recognized and protoplast was not observed under a microscope. Accordingly, SYN+ECZ was considered not to take part in cell wall synthesis directly. For effect of SYN+ECZ on release of intracellular components, slow release of 260 nm-absorbing substances was occurred, so that SYN+ECZ was seemed not to affect cytoplasmic membrane damage directly. Also, it was suggested clearly that SYN+ECZ affected lipid metabolism and glycolysis including TCA cycle from the investigation on antagonism by growth recovery of C. albicans SC5314 by 106 kinds of substances such as fatty acids, isoprenoids, phospholipids, vitamins, amino acids, nucleic acid-related substances and TCA cycle-related substances. From the above results, it was suggested that the mechanism of synergistic action with SYN and ECZ against C. albicans SC5314 was due to affect the different reactions in lipid metabolism and the similar reactions in glycolysis including TCA cycle, respectively, in consideration of respective mechanism of actions of SYN alone and ECZ alone.
A part of this work was presented at the Annual Meeting of the Agricultural Chemical Society of Japan, 1981 (Kyoto).View full abstractDownload PDF (1365K) -
1981 Volume 34 Issue 11 Pages 1497-1513
Published: November 25, 1981
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSDownload PDF (2349K)
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