The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 45, Issue 2
Displaying 1-12 of 12 articles from this issue
  • YOSHIRO SAWAE, YOSHIYUKI NIHO, MINE HARADA, TSUNEFUMI SHIBUYA, TAKASHI ...
    1992 Volume 45 Issue 2 Pages 123-135
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    1. To evaluate the efficacy and tolerance of imipenem/cilastatin sodium (IPM/CS) in severe infections associated with hematopoietic disorders, IPM/CS was administered to a total of 105 patients.
    2. Out of 96 patients evaluable for efficacy, clinical responses were excellent in 23 patients, good in 30, fair in 15, poor in 19 and unknown in 9, and the overall response rate was 60.9%.
    3. The most common underlying hematopoietic disease was acute non-lymphocytic leukemia and the most common infections were sepsis and suspected sepsis.
    4. Daily dose, severity of infection and neutrophil count had effects on the clinical response.
    5. The overall eradication rate of bacteria was 83.7%.
    6. Side effects were observed in 10 patients (9.5%) and abnormal laboratory test results in 12 (11.4%).
    From the above findings, we have concluded that IPM/CS is very useful for the treatment of severe infections in compromised patients with hematopoietic diseases.
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  • KATSU SAIONJI, NORIKO MIYAKE, KAZUNORI MIYAKE, JUN IGARI, INTETSU KOBA ...
    1992 Volume 45 Issue 2 Pages 136-142
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (CTRX) was administered in dose of 1g 30 minutes intravenous drip infusion to 5 healthy volunteers. Cefpiramide (CPM) and cefotetan (CTT) were administered as control antibiotics. The serum concentrations of total and free drugs, using ultrafiltration, were assayed by bioassay and HPLC. Protein binding rates and pharmacokinetic parameters were caliculated.
    Free concentration of antibiotics were following orders in each sampling time: CTRX>CTT>CPM. Mean free concentrations of CTRX at 0 hour and at 8 hours after intravenous drip infusion was more than 20μg/ml and more than 2μg/ml. Even at 24 hours after intravenous drip infusion free concentrations of CTRX were detectable. Mean half life in beta phase by HPLC was following orders: CTRX (7.5 hours)>CPM (5.4 hours) >CTT (4.7 hours). Mean protein binding rates were following orders: CPM (98%) >CTT (94%)> CTRX (92%).
    Conclusions: Characteristic of CTRX is high free drug concentration and long half life.
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  • HARUMI SHISHIDO, HIDEAKI NAGAI, ATSUYUKI KURASHIMA, KOJI SATO, KENJI K ...
    1992 Volume 45 Issue 2 Pages 143-154
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP) is a combination drug of PAPM, a new parenteral carbapenem antibiotic and BP, an amino acid derivative at a weight ratio of 1:1.
    Its in vitro antibacterial activities against clinically isolated respiratory pathogenic bacteria were determined. It was superior to imipenem (IPM) in the in vitro antibacterial activities against Haemophilus influenzae, Haemophilus parainfluenzae, Branhamella catarrhalis, Staphylococcus aureus including MRSA, Klebsiella pneumoniae, Serratia marcescens and Escherichia coli. PAPM had antibacterial activities almost equal to those of IPM against Streptococcus pneumoniae and Enterococcus spp. Against Pseudomonas aeruginosa, however, its antibacterial activity was about 1/4 that of IPM.
    The clinical usefulness of PAPM/BP was studied by dissolving it in a solution containing lactate and administering the solution by intravenous drip infusion to 12 cases of respiratory tract infections.
    Out of 11 cases with respiratory tract infections excluding cytomegalovirus pneumonia, the efficacy rate was 90.9%, with 4 cases of excellent and 6 cases of good responses.
    In terms of its bacteriological efficacies, eradications of pathogenic bacteria including superinfection were observed in 2 out of 4 strains, but 2 strains of P. aeruginosa remained unchanged. Six strains appeared as superinfected bacteria during and after administration of this preparation substituting original pathogens.
    Side-effects were not observed in the 12 cases, and in laboratory tests, slight transient increases of S-GOT and S-GPT were found in 1 case.
    In conclusion, PAPM/BP is a very useful parenteral antibiotic against respiratory tract infections and can be one of the drugs of the first choice.
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  • KAZUO KURATA
    1992 Volume 45 Issue 2 Pages 155-159
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP), a new parenteral carbapenem antibiotic, was investigated with regard to their levels in sera and various tissues collected from patients under orthopedic surgery.
    The subjects were 17 patients, complaining low back pain and hospitalized for surgical operations. PAPM/BP was administered by intravenous drip infusion for 30 minutes of a dose of 500mg/500mg.
    Serum and cerebrospinal fluid (CSF) specimens were taken from 8 patients at 15-70 minutes after administration and assayed for PAPM and BP levels. Serum, bone, and joint capsule samples where taken from the other 9 cases at 25-127 minutes after administration and assayed.
    PAPM levels in CSF were considerably lower than those in serum. They were 23.74-1.11μg/ml in sera, 0.31-0.05μg/ml in CSF's during 15 to 70 minutes after administration.
    PAPM levels were 27.85-2.97μg/ml in sera, 2.54-0.20μg/g in bones, 5.63 and 1.67μg/g in joint capsules during 25 to 127 minutes after administration.
    BP levels in sera and various tissues were low compared to those of PAPM.
    These results showed that PAPM was detected at higher levels than 0.2μg/g in various tissues, except CSF during 20 to 120 minutes after drip infusion of PAPM/BP 500mg/500mg for 30 minutes.
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  • SHIGEKI ODAGIRI, MASANORI MATSUMURA, KANEO SUZUKI, KOU MUROHASHI, KENI ...
    1992 Volume 45 Issue 2 Pages 160-171
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (CS-976, PAPM/BP), a new carbapenem antibiotic, was administered a single dose of 500mg or 750mg via intravenous drip infusion twice a day for teatment of chronic respiratory infection to study its clinical efficacy, bacteriological efficacy and safety. Twenty nine cases were studied for the efficacy evaluation. Only the safety evaluation was made in 6 cases which were judged to be unsuitable, because in some of them pneumonia and other diseases were not specified as the subject diseases, of serious illness in some the conditions were too serious, and in the other cases the duration of administration was insufficient since administration had to be discontinued due to side-effects. The duration of administration was 6 to 18 days with 1g divided into 2 doses daily or 4 to 15 days with 1.5g in 2 divided doses daily.
    When clinical efficacies were classified according to different diseases, this preparation was effective in 11 cases and slightly effective in 1 case of 12 cases of chronic bronchitis with an efficacy rate of 91.7%. It was effective in 10 cases, slightly effective in 1 case and ineffective in 1 case of 12 cases of bronchiectasis with an efficacy rate of 83.3%. It was slightly effective in 2 and ineffective in 1 out of 3 cases of diffuse panbronchiolitis, and was effective in 2 cases of pulmonary emphysema with infections. PAPM/BP was given at a dose level of 1g in 2 divided doses daily to 17 cases and that of 1.5 g in 2 divided doses daily to 10 cases. For the remaining 2 cases, changes in the dose level were made in middle course of treatment. The efficacy rate in the 1g regimen was 76.5% and that with the 1.5g regimen was 90%. The overall results in the 29 cases included 23 effective, 4 slightly effective and 2 ineffective cases, thus the overall efficacy rate was 79.3%. As pathogens, 11 species including 24 strains were isolated and identified from 19 cases. They were Gram-positive cocci including 2 strains each of Staphylococcus aureus and Streptococcus pneumoniae, 1 strain each of Staphylococcus epidermidis, Streptococcus sanguis, and Streptococcus viridans and a strain of Streptococcus spp., and Gram-negative rods including 9 strains of Psudomonas aeruginosa, 4 strains of Haemophilus influenzae and 1 strain each of Klebsiella pneumoniae, Enterobacter cloacae and Pseudomonas spp. Bacteriological efficacies against these 24 strains of pathogens were: disappearance, 8; decreased, 2; substituted, 8; unchanged, 3; and unassessed, 3 strains, hence the eradication rate was 76.2% (16/21). Three of the unchanged strains and the 2 decreased strains were P. aeruginosa. Side effects were noted in 2 cases in which the dose level was 1g daily administered in 2 divided doses. They included 1 cases each of rash and palpitation/sleeplessness/ itching. All these symptoms were mild and disappeared rapidly upon discontinuance of the regimen. Abnormal laboratory test results were observed in 8 cases including 2 cases of elevation of LDH, 1 case of eosinophilia, 1 case of increased basophilic leukocytes and 1 case each of elevation of GOT, bilirubin, BUN and NAG. They were all mild and transient, and posed no clinical problems at all.
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  • TAKUYA KISHIDA, YUICHI SANNOMIYA, YOSHITAKA NAKAO, YOSHINORI YASUI, KE ...
    1992 Volume 45 Issue 2 Pages 172-180
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Forty-three patients with severe infections which were complicating hematological disorders were treated with panipenem/betamipron, and the efficacy and the safety of the drug were evaluated. The results obtained are summarized below.
    1. Out of 40 patients in whom efficacies are evaluable, the clinical responses were excellent in 17 patients, good in 4, fair in 7 and poor in 12, and the total clinical efficacy rate was 52.5%.
    2. The efficacy rate in 7 patients who had failed to respond to prior treatment with other antibiotics was 57.1%. Thus, no significant difference was observed in efficacy rates between the patients who had failed to respond to prior treatment with other antibiotics and the patients who received no preceding antibiotics therapy.
    3. Out of the 43 patients in whom the safety was evaluable, no side effects nor abnormal laboratory findings were found.
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  • TETSUNORI YOSHIDA, EIJI NARUMI, MASAHIKO MURAZUMI, RIEI KAMO, TAKEHIKO ...
    1992 Volume 45 Issue 2 Pages 181-187
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The effectiveness and the safety of panipenem/betamipron, new antibiotics of the carbapenems for burn infections, were studied and the following results were obtained:
    1. The preparation, 0.5g/0.5g, was administered by intravenous drip infusion twice a day to 11 cases of patients with burn infections. In 10 cases for which clinical effects were evaluable, results were rated as “excellent” in 2 cases, “good” in 2 cases and “fair” in 6 cases, with an efficacy rate of 40%.
    2. Penetration to the affected tissue was studied in 2 cases. The tissue level of panipenem was 0.20μg/g immediately after the end of drip infusion and 6.86μg/g 60 minutes thereafter.
    3. As for the safety, a slight increase in GOT, GPT and Al-P was noted in 1 case; a slight increase in GPT, NAG and β2MG was found in 1 case; and a slight increase in GOT, GPT, Al-P and LAP was noted in 1 case, as abnormal variations in laboratory test results.
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  • KEN TSUYUKI, YOSHITO ARISAWA, ISAO YOKOYAMA, KANJI MATSUMOTO, TOMONOBU ...
    1992 Volume 45 Issue 2 Pages 188-196
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Studies were done on the effectiveness and safety of panipenem/betamipron, a new carbapenem antibiotic, in infections in the surgical domain and its safety when dissolved in infusions containing lactate. The obtained results are summarized as follows.
    The preparation, 0.5g/0.5g or 1.0g/1.0g, was administered by intravenous drip infusion 2 to 3 times a day to 31 cases of patients with infections in the surgical domain. A physiological saline solution was used as the solvent in 21 cases (group A) of them and Solita T3®, an infusion containing lactate, was used as the solvent in the 10 remaining cases (group B).
    As for its clinical effects, results were rated as “excellent” in 20, “good” in 7, “fair” in 3 and “no response” in 1 out of the 31 cases, and the efficacy rate was 87.1%. Regarding its bacteriological effects, results were rated as “disappeared” in 22, “decreased” in 2, “unchanged” in 1 and “unknown” in 1 out of 26 cases from which bacteria were isolated, hence the bacteriaclearance rate was 88.0%.
    As for side effects, skin rash was seen in 1 case and slight increases of GOT and GPT were noted as abnormal changes in laboratory data in 2 cases. These side effects were all observed among the cases in group A but not at all in group B where a lactate containing infusion was used as the solvent.
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  • JIRO ARATA, HISANORI AKIYAMA, HIROKO KANZAKI, HISASHI TAKAHASHI, YUI T ...
    1992 Volume 45 Issue 2 Pages 197-207
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP), a new carbapenem, was studied in dermatology.
    PAPM/BP was used clinically in the treatment of skin and skin structure infections in a multicenter trial. Fifty three patients were enrolled in the trial. Clinical evaluations were made in 50 patients. Most patients received intravenous infusion of PAPM/BP in a dose of 500 mg twice daily. Other dosages were used in some patients.
    The overall clinical efficacy rate was 78%. When 15 cases of secondary infections were excluded, the rate was 85.7%. Adverse responses were nausea and/or vomiting in 3 patients, redness with itching in 1 patient, headache or head heaviness in 2 patients and diarrhea in I patient. The patient with redness and itching had also nausea and vomiting. This occurred 1 hour after the start of the first infusion of this drug. After the discontinuation of the treatment the symptoms went away on the next day.
    Abnormalities in laboratory test results were observed in 7 out of 53 patients. One patient with liver cirrhosis and hepatocellular carcinoma developed anemia (RBC 372×104/mm3→275×104/mm3, Hb 11.9g/dl→8.8g/dl, 35.1%→26.0%). Other abnormalities were all mild.
    Penetration of the drug into skin tissues after intravenous infusion of 500mg of this drug in skin surgery patients was studied. Skin/serum concentration ratios ranged from 0.20 to 0.97. Skin concentrations were higher than the concentration of PAPM inhibiting 80% of clinical isolates over a period of 6 hours. In rats, skin concentrations were much lower than serum concentrations probably due to the difference in in vivo metabolism of PAPM.
    A few resistant strains of Staphylococcus aureus against PAPM and imipenem (IPM) were isolated. However, PAPM and IPM showed good antibacterial activities compared to other drugs tested.
    In conclusion, PAPM/BP is considered to be a useful drug in the treatment of skin and skin structure infections.
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  • RYOCHI FUJII, TOSHIAKI ABE, TAKESHI TAJIMA, ITARU TERASHIMA, HIDENORI ...
    1992 Volume 45 Issue 2 Pages 208-227
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    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 10mg/10mg/kg, 20mg/20mg/kg and 30mg/30mg/kg, respectively. Maximum blood levels of PAPM/BP were observed at the completion of drip infusion and were 26.72±8.78μg/ml/18.33±18.54μg/ml (mean±S. D.) with administration of 10mg/10mg, 64.80±18.50μg/ml/38.74±16.41μg/ml with administration of 20mg/20mg and 91.70±29.42μg/ml/50.08±22.41μg/ml with administration of 30mg/30mg. 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 60mg/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%. The efficacy rate of this drug preparation in cases in which other antibacterial drugs administered for more than 3 days proved to be ineffective was 95.9% (71/74). The bacterial eradication rate for Gram-positive bacteria was 100% (17/17) and that for GNB was 86.2% (25/29).
    3. Side effects and abnormal laboratory data
    A study on the safety was conducted in 380 cases excluding 11 cases. Side effects were noted in 9 cases (2.4%), consisting of skin rash in 3, urticaria in 1, soft stool in 2 and diarrhea in 3.
    Abnormal laboratory data were found in 64 cases, consisting mainly of elevations in platelet count, increases in eosinophils and elevations of trans-aminase. Side effects and abnormalities in laboratory data were not particularly serious and disappeared or returned to normal with discontinuation or completion of the medication with this preparation.
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  • 1992 Volume 45 Issue 2 Pages 228-230
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • 1992 Volume 45 Issue 2 Pages 231-232
    Published: February 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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