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Volume 38, Issue 1
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HIROTAKA OTA, KENJI SOGA, MAKOTO MURATA, MASAHIRO MAKI1985 Volume 38 Issue 1 Pages 1-3
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCeftriaxone (Ro 13-9904, CTRX) was administered to 3 cases with gynecological infections and following results were obtained.
1. CTRX was administered by intravenous drip infusion or intravenous injection with 2g per day for 4 to 6 days. The clinical efficacy was good in all cases (2 cases with pyometra, 1 case with adnexitis and endometritis).
2. No side effect could be determined in all cases.View full abstractDownload PDF (328K) -
KIMITOSHI INOUE, NOBUYUKI MORISAKI, TETSURO CHIMURA1985 Volume 38 Issue 1 Pages 4-7
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCeftriaxone (Ro 13-9904, CTRX), a newly developed parenteral cephalosporin antibiotic was clinically evaluated in gynecoobstetric infections and the following results were obtained.
CTRX was administered by intravenous drip infusion twice a day in a daily dose of 2 to 4 g to 10 cases with gynecoobstetric infections, consisting of 8 with intrauterine infections, 1 with adnexitis and 1 with infection of external genitalia.
The global clinical efficacy was excellent in 2 and good in 6 out of 8 cases with intrauterine infections, and in 2 others, the efficacy rate being 100%. Bacteriologically, the eradication of bacteria was observed in 5, unchange in 2 and alternation of bacteria in 2 among 9 cases where the causative strains were detected.
Neither adverse reaction nor laboratory test abnormality was observed. The above-mentioned results suggest that CTRX is a highly safe antibiotic expected to be excellent in the clinical efficacy and bacteriological effects.View full abstractDownload PDF (438K) -
MASAYA TATENO1985 Volume 38 Issue 1 Pages 8-12
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCeftriaxone (Ro 13-9904, CTRX) was administered to 13 cases with gyneco-obstetric infections and the following results were obtained.
1. The responses were excellent in 4 cases (30.8%) and good in 7 (53.8%) out of the 13 cases, the efficacy rate (good or above) being 84.6% (11/13).
2. Two cases showing a poor response were considered inappropriate for a study on the efficacy of an antibiotic, as they had received anticancer drugs concomitantly for treatment of their underlying disease of peritonitis carcinomatosa due to ovarian cancer.
3. From a bacteriological viewpoint, CTRX was effective against E. coli, S. aureus, S. faecalis, Pseudomonas, Staphylococcus, K. pneumoniae, S. epidermidis, etc.
4. No specific side effects were observed.View full abstractDownload PDF (599K) -
HARUHIKO DEGUCHI, HIDEAKI MASUZAKI, MAKOTO MURAKAMI, TOORU YAMABE1985 Volume 38 Issue 1 Pages 13-17
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSClinical studies were made on ceftriaxone (CTRX, Ro 13-9904), a new long-acting cephalosporin antibiotic, with the following results.
1. Following a single intravenous injection of 1 g, the transfer of CTRX to the internal genital organs was found to be good.
2. The transfer of CTRX to exudate of the dead space of pelvis was also good.
3. Elbow vein and uterine artery blood serum levels revealed marked increase immediately after administration, then followed by gradual reduction at very slow rate.
4. CTRX was given to 3 patients of female genital infections. Efficacy was excellent in 1 case and good in 2 cases.
5. As to side effect, 2 cases of diarrhea and 1 case of leukopenia were observed.View full abstractDownload PDF (509K) -
KOSAKU YOSHIDA, MASAMI TAKAHASHI, TOMOHIDE YONAHA, YOSHITOSHI ICHIMAN, ...1985 Volume 38 Issue 1 Pages 18-26
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSUsing strain SMK-101 of K. pneumoniae its nephelometric absorbencies, viable cell numbers and morphological changes were studied during the time course cultured in a broth medium containing cephapirin (CEPR), and following results were obtained.
1. After 1 to 3 hours culture in the presence of varying concentration of the antibiotic, the absorbency increased in spite of without change in the viable cell number. Morphologically, elongation and swelling of central portion of the cells were observed though differences of the degree of these findings varied depending upon the concentration of the antibiotic. At the concentration higher than 1/4 MIC, indistinct structure was shown in cytoplasm.
2. After 6 hours culture, 3 directions of absorbence curves, ascending, descending and no change, and 2 directions of viable cell numbers, decreasing and increasing were shown. As the morphological changes of the cells, filamentation, leaking of intracellular components were shown in rather upper concentration of the antibiotic. Fission was demonstrated around the end of cells cultured in rather lower concentration of the antibiotic.
3. After 9 hours culture, absorbency and viable cell number were parallel. In this period, structural findings of cytoplasm became clear and fission was also demonstrated by light microscope except for the cells cultured in more than 1 MIC of the antibiotic.
4. After 24 hours culture, both absorbency and viable cell number increased again and fission was observed in the cell which showed filamentation in 1 MIC of the antibiotic.View full abstractDownload PDF (11693K) -
COMPARATIVE STUDYCHOICHIRO TAKAHASHI, KOZUI MIYAZAWA1985 Volume 38 Issue 1 Pages 27-30
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAntibacterial activity of cefmenoxime (CMX) against clinically isolated organisms was examined in com-parison with that of 4 other antibiotics and concluded as follows:
1. Antibacterial activity of CMX was markedly stronger than those of cefazolin (CEZ), cefmetazole, latamoxef and ampicillin against E. coli, K. pneumoniae, S. marcescens, H. influenzae, P. mirabilis and indolepositive Proteus.
2. But the MIC level of CMX against S. aureus was higher than that of CEZ.View full abstractDownload PDF (544K) -
HIROSHI TSUBURAYA, IWAO WATANABE, MIKIO OIKAWA, SHINICHIRO ENDO1985 Volume 38 Issue 1 Pages 31-40
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSBasic and clinical studies in 37 patients with biliary tract disease on comparison between cefmenoxime (CMX) and cefotiam (CTM) were studied and the following results were obtained.
1. In vitro antibacterial activities of CMX and CTM against 25 strains (15 organisms) isolated from bile of patients with biliary tract disease were stronger than that of cefazolin (CEZ).
2. In cholecystectomized patients, CMX (2g) or CTM (2g) was injected intravenously, followed by determination of concentration in bile and gallbladder tissue about 2 hours after administration.
In CMX administration, the mean concentration in gallbladder bile was 812.13μg/ml, and the mean concentration in duct bile was 1,050.6μg/ml, and the mean concentration in gallbladder tissue was 100.7μg/g.
In CTM administration, the mean values were, 1,092.5μg/ml, 1,287.8μg/ml, 28.5μg/g, respectively. The concentration of CMX and CTM were almost similarly.
3. The bile concentration of CMX (i.v.) was compared with CTM (i.v.) by cross-over method in cases of T-tube drainage.
The peak bile concentrations of CMX and CTM were as high as 172.4μg/ml and 182.2μg/ml, respectively, 1-2 hours after 2g intravenous administrations. Furthermore, the concentration of them were highly gained, 16.1μg/ml of CMX and 33.8μg/ml of CTM, even at 5-6 hours.
4. In choledochostomized patients, CMX (4g/day) was injected intravenously, followed by determination of concentration in intraperitoneal exudate. The mean concentration of CMX was 15.3μg/ml on the first day after the operation, and 6.0μg/ml even on the third day after the operation.
5. Those results suggest that the high antibacterial activity of CMX against organism in bile and, the high penetration of CMX to bile, gallbladder tissue and intraperitoneal exudate will promise its important role in treatment of biliary tract infections.View full abstractDownload PDF (868K) -
MASAHIKO WASHIO, MINORU KOBAYASHI, NOBUAKI NAGAE1985 Volume 38 Issue 1 Pages 41-44
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTen patients who were performed pulmonary resection for the disease of the lung, were administered 2g of cefmenoxime (CMX) by intravenous injection before their operation.
The concentrations of CMX in serum and lung tissue were determined.
The CMX concentrations in lung tissue were observed to be higher than the MIC of CMX for Klebsiella pneumoniae, Haemophilus influenzae and Serratia.
These results suggested that CMX will be useful agent for the prevention and treatment of pulmonary infection.View full abstractDownload PDF (373K) -
HIDEKAZU NOGAKI, KAZUHIKO ISHIDA, TETSURO KAWAGUCHI, TOMONORI NAGAO, Y ...1985 Volume 38 Issue 1 Pages 45-48
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTwo grams of cefmenoxime (CMX) was administered by one-shot intravenous injection to the patients in normal pressure hydrocephalus without meningitis, and the transference of CMX into the cerebrospinal fluid (CSF) from blood was investigated. After the injection of CMX, CSF and serum were serially taken, and the concentrations of CMX were measured by agar-well method using E. coli.
The conclusions drawn from this study are summarized as follows:
1. The concentrations of CMX in CSF were more slowly decreased than those in serum. The mean ratio of transference of CMX into CSF from the serum was 1.4%.
2. After the intravenous injection of 2g CMX, the mean maximum concentration of CMX in CSF was 0.36μg/ml, which exceeded 80% MIC (minimal inhibitory concentration) against several Gram-positive cocci and Gram-negative rods, and higher concentrations than the 80% MIC were kept over 4 hours in CSF.
3. The efficacy of CMX may be kept by its injections less than 4 times a day.View full abstractDownload PDF (533K) -
ATSUO ASHIKI, ATSUSHI TSUKUI, KENJI YAMATO, TADASHI SUZUKI, WAICHIRO H ...1985 Volume 38 Issue 1 Pages 49-61
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe efficacy of cefmenoxime (CMX), which is a third generation, β-lactamase-resistant cephem with a broad antibacterial spectrum, was examined in 43 patients with chronic complicated urinary tract infections.
The usual dosage regimen was given 2-4g/day of CMX by intravenous drip infusion over 1 hour. The duration of treatment was 5 days. Fifteen patients were cured and 21 improved, and the effective rate was 83.7%. Bacterial eradication rate in these cases was 88.2%, especially eradication of the original pathogens such as Serratia marcescens, Proteus species and Klebsiella species, occurred in high frequency.
Laboratory abnormalities were slight elevation of serum GOT and GPT in 2 cases.
From these findings, CMX was considered to be very effective in complicated urinary tract infections.View full abstractDownload PDF (956K) -
HIROYASU HAYASAKA, HITOSHI SASAKI, MASARU KUREBE, MICHIKO SANDA, TETSU ...1985 Volume 38 Issue 1 Pages 62-68
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCisplatin caused toxic effects in adult male rats, such as renal disturbance, decrease of platelet and WBC, increase of RBC, elevation of GPT and GOT activity, decrease of plasma protein and albumin, loss of body weight gain and lethal effect when treated intravenously with 1mg/kg/day of cisplatin for 12 days. Fosfomycin (FOM) exerted preventive effects on the renal disturbance, the changes in blood cells and plasma protein and the lethal effect induced by cisplatin when treated with a combination of FOM and cisplatin.
However, FOM did not prevent the cisplatin-induced effects on GPT and GOT activity and body weight gain.
These results suggest that FOM prevents the cisplatin-induced disturbance of renal and hematopoietic function but does not the cisplatin-induced hepatic disturbance.View full abstractDownload PDF (3413K) -
NOBUYUKI MORISAKI, TETSURO CHIMURA1985 Volume 38 Issue 1 Pages 69-73
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. The endocervical flora was examined in 20 with rupture of membranes, 20 pregnant women served as control. The isolated organisms were aerobic and anaerobic in both groups, whereas P. cepacia was common in group of rupture of membranes, but another microorganisms were not statistically significant.
Culture specimens taken from the vagina in nonpregnant women showed a higher presence of total bacteria than did those in pregnant women.
2. The MICs of ampicillin (ABPC) were measured against isolated aerobic organisms from rupture of membranes. The distribution of sensitivity of Bacillus sp. was 0.20μg/ml, but another organisms were inhibited in concentration of higher than 3.13μg/ml.
3. The antibacterial effect of amniotic fluid during 24 weeks of gestation on S. aureus and S. pyogenes, but during 34 to 39 weeks of gestation the amniotic fluid has inhibitory effect only on the growth of K. pneumoniae. In contrast, the growth of E. coli was not inhibited by amniotic fluid during 24 to 39 weeks of gestation.View full abstractDownload PDF (542K) -
HIDEKI SAKAI, SUNAO MAE, TETSUYA IRIE1985 Volume 38 Issue 1 Pages 74-82
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCefoxitin (CFX) was administrated to a total of 12 hospitalized patients with digestive diseases, in combination with aminoglycosides.
The following results were obtained:
1. Clinical effects of CFX on 12 cases were “excellent” in 4 cases, “good” in 5, “fair” in 1 and “unknown” in 2, with the efficacy rate of 75%.
2. All 4 cases who developed septicemia with underlying severe diseases showed “excellent” effect to CFX.
3. Clinical results of 8 cases with hepatic biliary tract infections were “good” in 5, “fair” in 1 and “unknown” in 2, with the efficacy rate in 62.5%.
4. As for side effects, an allergic reaction was observed in 1 case, and it is suggested renal function should be monitored carefully in a case of combination use with aminoglycosides.View full abstractDownload PDF (892K) -
CLINICAL EXPERIENCE WITH CEFOXITINHIROTSUGU ODA, KAZUTERU DOI, KOZO SUNAGO, MINORU SAIKA, SHIGEKI OKA, S ...1985 Volume 38 Issue 1 Pages 83-94
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. The clinical effects of cefoxitin (CFX) were evaluated in the prophylaxis of postoperative infections in the field of orthopaedics. The clinical response was good in 46 out of 50 patients; an efficacy rate of 92%.
2. Four patients (8%) who did not respond to CFX were suffering from infections due to Mycobacterium tuberculosis (1), suspected Pseudomonas aeruginosa (1), and infection of unknown organism (2).
3. A review was also made of recent trends among clinically isolated bacterial strains and their susceptibility to antibiotics in the field of orthopaedics.
4. CFX is recommended as an antibiotic of first choice for the prophylaxis of postoperative infections in the field of orthopaedics.View full abstractDownload PDF (1226K) -
KATSUMI NODA, KAZUTOSHI MATSUNAMI, KUNIHIKO ITO, MOTOKI HAYASAKI1985 Volume 38 Issue 1 Pages 95-101
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe concentration of cefoxitin (CFX, Merxin®) in dead space exudate was studied in 14 patients following total extirpation of diffuse uterine cervical cancer. A two-compartment model was used for the analysis.The results obtained were as follows:
Calculated maximum concentrations of CFX in the pelvic dead space exudate were 26.55μg/ml at 2.11 hours, 31.07μg/mg at 2.01 hours and 51.51μg/ml at 2.10 hours after 1 hour intravenous drip infusions of CFX 2, 3 and 4 g, respectively. These concentrations were higher than the MIC80 of 12.5μg/ml against E. coli and B. fragilis and were maintained for a sufficient period of time.
Based on the results of this study, CFX is considered to be an important and valuable drug in the field of obstetrics and gynecology.View full abstractDownload PDF (625K) -
AKIO SAKAI, AKIRA KAWASHIMA, GOU UEDA, HIKARU YAGI, KAZUHIKO YOSHIMURA ...1985 Volume 38 Issue 1 Pages 102-106
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe levels of cefotaxime (CTX) in serum and lung lymph were compared in awake sheep which were prepared for collection of lung lymph. A single dose of 50 mg/kg of CTX was administered intravenously to sheep. The CTX level in serum or lung lymph reached a peak within 15 minutes after administration and decreased rapidly. The measurable concentration persisted for 240 minutes after administration. Ratios of lung lymph to serum concentration of CTX ranged from 1.0 to 1.2.
In addition, the CTX levels in serum, lung lymph and tissue of right lower lobe were compared in anesthetized sheep to which CTX 50 mg/kg were given. Ratios of lung lymph and tissue in right lower lobe to serum concentration of CTX were 0.81 ±0.14, 0.06 ±0.02, respectively.
From above results, CTX was well distributed in lung lymph. The levels of CTX in tissue of right lower lobe were markedly lower than those of lung lymph.View full abstractDownload PDF (570K) -
AKIRA TSUCHIDA, AZUMA HIRAMOTO, HAJIME YOSHIOKA, KEN-ICHI IZEKI, MASAT ...1985 Volume 38 Issue 1 Pages 107-113
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCefotaxime (CTX) was administered to 117 pediatric patients. Although 26 of these patients were excluded from the clinical evaluation of the study because other antimicrobial agents were given concomitantly with CTX or because no infectious diseases were proved, these cases were evaluated for adverse effects of the drug.
The remaining 91 cases were evaluated for clinical effect; pneumonia in 56 cases, septicemia in 5, suspected septicemia in 5, meningitis (aseptic cases included) in 3, urinary tract infection in 5 and other diseases in 17.
No pathogenic organisms were identified in any of the pneumonia cases, even either by bacterial culture or other laboratory test methods.
Pathogens of septicemia were E. coli in 3 cases, K. pneumoniae in 1 and E. agglomerans in 1.
Those of urinary tract infections were E. coli in 3 cases, a mixed infection of S. aureus and an unidentified species of Gram-negative rods in 1, and unknown in 1. Clinical effectiveness rates of CTX were 78.6% in pneumonia and 100% in septicemia, suspected septicemia and urinary tract infections.
One patient with purulent meningitis caused by H. influenzae was also treated with CTX successfully.
Adverse reactions and abnormal laboratory findings were observed in 12 cases (12/117=10.3%); rash in 2 cases, vomiting in 1, abdominal pain in 1, diarrhea in 5, granulocytopenia and thrombocytopenia in 1, eosinophilia in 3 and elevation of liver enzymes (GOT and LDH) in 1.View full abstractDownload PDF (718K) -
AKIO URABE, FUMIMARO TAKAKU, HIDEAKI MIZOGUCHI, KAZUO DAN, KEISUKE TOY ...1985 Volume 38 Issue 1 Pages 114-120
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSA new antibiotic cefminox (CMNX, MT-141) was administered to 54 patients with severe infections accompanying various hematological diseases. The rate of effectiveness was 55.3% on the whole. Mild liver dysfunction was observed in 3 cases, which recovered quickly following the stop of the administration.View full abstractDownload PDF (578K) -
FLUID OF PATIENTS WITH HYDROCEPHALUSMIZUO KAGAWA, NOBUHIKO MORI, SHIGEKI ASAHI, YASUHIKO TAJIKA1985 Volume 38 Issue 1 Pages 121-127
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSEleven neurosurgical patients without intracranial infection were given 4g cefoperazone (CPZ) intravenously for 30 minutes. Ventricular drainage was performed in 10 cases, and 1 case with cisternal drainage. Eight of 11 cases showed moderate to severe ventricular dilatation. Serum and ventricular cerebrospinal fluid (CSF) concentrations of CPZ were measured for 8 hours after injection.
1. Average peak serum concentration of CPZ was 476μg/ml and the half-life was 150 minutes.
2. Patients with obstructive hydrocephalus showed relative good penetration of CPZ in CSF (2.74-5.29 μg/ml). Especially, those who had severe dilatation of ventricles demonstrated sequential increased concentration (5.48-6.25 μg/ml at 8 hours).
3. In poor risk patient and intracerebral hemorrhage with ventricular hemorrhage cases, who had normal range of CSF cell counts and protein, CPZ level was low, less than 2 μg/ml.
4. In cases with severe subarachnoid hemorrhage, sufficient concentration (11 μg/ml) of CPZ was observed in cisternal CSF.
5. The CPZ concentrations in CSF after 4g administration did not seem to exceed comparing to 2g dosing.View full abstractDownload PDF (760K) -
KAORU ITOSE, MASATO FURUKAWA, MITSUJI OHTSUBO, RYUHEI YAMADA, SHIGERU ...1985 Volume 38 Issue 1 Pages 128-132
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. The concentration of cefoperazone (CPZ) in serum and bile was estimated after intravenous drip infusion of 1g of the drug in 11 patients, who have performed cholecystectomy, choledocholithotomy and T-tube drainage for gallstone diseases. Administration of cefazolin (CEZ) 1g was compared by the cross over method.
2. After 1g intravenous drip infusion of CPZ, the mean serum concentration was 88.3±24μg/ml at 1 hour, 52±11.7μg/ml at 2 hours and 36.5±10μg/ml at 4 hours. The maintenance period of serum concentration was inclined to be longer in CPZ than in CEZ.
3. After 1g intravenous drip infusion of CPZ, the mean bile concentration reached to810±459μg/ml in 2 hours and it was maintained as high as 562±319μg/ml even after 4 hours. On the other hand, after 1g intravenous drip infusion of CEZ, the mean bile concentration was only 28.7±26ug/ml in 1 hour and was low level in the progress.
4. As compared with the highest concentration of CPZ and CEZ in same patient, the mean bile concentration of CPZ (942±525μg/ml) was about 30 times higher than that of CEZ (28.6±26.3μg/ml).
5. There was no difference in the group of Gram-positive cocci between minimum inhibitory concentration (MIC) of CPZ and that of CEZ. While MIC of CEZ in the group of Gram-negative bacilli was from 0.78 to over 400μg/ml, MIC of CPZ in that group was from 0.10 to 50μg/ml. The value in CPZ was lower than that in CEZ at all strains. No side effects was seen in all patients.View full abstractDownload PDF (604K) -
A STUDY ON ADMINISTRATION OF ANTIBIOTICS DURING OPERATION FOR PREVENTION OF POSTOPERATIVE INFECTIONSHIDEKI WATANABE, HIROSHI SAKAGAMI, KAZUO OHTAGURO, KOSUKE UEDA1985 Volume 38 Issue 1 Pages 133-136
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTwo antibiotics, piperacillin (PIPC) and cefoperazone (CPZ) were administered during operation and determined of efficacy for prevention of postoperative infections.
1. Following administration of PIPC and CPZ during operation, high serum concentrations were obtained.
2. In exudates not so high concentrations were achieved with either PIPC or CPZ. This was considered to be probably due to the period and methods of collection of specimens used in this study.
3. Bacteriological studies of washings of wounds obtained during operation gave negative results in all cases.
4. It was considered that administration of antibiotics during operation may suffice for prevention of postoperative infections for all cases with relatively short operation time excepting for cases operated for malignant tumors or urinary tract lithiasis.View full abstractDownload PDF (449K) -
INHIBITORY EFFECTS OF VARIOUS DRUGS ON THE TOXICITY OF NEOCARZINOSTATIN IN VITRO AND IN VIVOAKIRA ITO, ISOKO HANEDA, KAZUYOSHI TORIYAMA, MASARU OUCHI, TOMONORI MA ...1985 Volume 38 Issue 1 Pages 137-144
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSNeocarzinostatin (NCS) used for the chemotherapy of leukemia and cancers such as stomach, pancreas and bladder, has been pointed out to have the side effects mainly causing leukopenia.
In order to prevent these side effects of NCS by systemic administration, we have attempted to inject NCS directly into the tumor tissues and to inactivate NCS leaked from the tissues by the treatment of antidotes for NCS.
The present report deals with the influence of some antidotes on the toxicity of NCS in vitro and in vivo.
The results demonstrated that;
1. Four SH-compounds, such as thiopronin, glutathione (reduced form), sodium thioglycolate and L-cysteine monohydrochloride monohydrate were effective to inactivate antibacterial activity of NCS against M. luteus ATCC 9341 in vitro.
2. It was recognized that acute toxicity of NCS was reduced by pretreatment of these SH-compounds and its action was dose related. The LD50 values of NCS intravenous administration in mice increased 5.8-to 24-fold when 150, 300, 500 and 1,000 mg/kg of thiopronin were administered intravenously 2 minutes prior to NCS. And 2.3-to 4.2-fold by 500 and 1,000 mg/kg of glutathione (reduced form), 1.6-to 4.2-fold by 50,100 and 200 mg/kg of sodium thioglycolate, 1.9-to 4.2-fold by 100, 200 and 400 mg/kg of L-cysteine monohydrochloride monohydrate respectively.
3. On the other hand, pretreatment of NCS didn't affect the acute toxicity of thiopronin.View full abstractDownload PDF (1078K) -
AKIRA OKADA, KENZO OKUMURA, MASATO OZEKI, TETSUYA HIGASHIJIMA, YOSHIKA ...1985 Volume 38 Issue 1 Pages 145-154
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCefsulodin (CFS), a cephem antibiotic, was administered to 26 children aged from 11 months to 11 years by intravenous injection or intravenous 1-hour drip infusion in doses of 15 and 50 mg/kg body weight to investigate serum and urinary concentrations. The following results were obtained. 1. Serum concentration
The serum concentrations of CFS at 5 minutes after intravenous injection of 15 and 50 mg/kg were 57.1 and 224.2 μg/ml, respectively. The biological half-lives (T 1/2β) were 1.28 and 1.12 hours.
The serum concentration of CFS after intravenous 1-hour drip infusion reached a peak at the end of infusion, i.e. 29.9μ/ml for 15 mg/kg and 121.9μg/ml for 50mg/kg, and T 1/2β were 1.22 hours for 15mg/kg and 1.27 hours for 50mg/kg. The AUC was proportional to the doses for both intravenous injection and intravenous drip infusion. The serum clearance was about twice the value in adults and the distribution volume was about 1.5 times as large.
2. Urinary excretion
The urinary excretion up to 6 hours after administration was: 69.0% for 15mg/kg and 61.9% for 50mg/kg in cases of intravenous injection, and 62.4% for 15 mg/kg and 71.1% for 50mg/kg in cases of intravenous 1-hour drip infusion. The percent urinary excretion was similar to that in adults.View full abstractDownload PDF (958K) -
THE BLOODLESS LUNGHAJIME MAEDA, JUNPEI HASHIMOTO, KAZUYA NAKAHARA, KIYOSHI OHNO, MASAHIT ...1985 Volume 38 Issue 1 Pages 155-159
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe concentration of cefotiam (CTM) in the serum and the bloodless lung with time is discussed.
Five patients who were undergone pneumonectomy or lobectomy, were given 1 g of CTM intravenously during the operation. Blood samples and lung samples were collected 15, 30, 60, 90, 120, and 300 minutes after the administration.
The CTM levels in the blood and the lung samples were measured by the agar well bioassay.
The CTM levels in the lung samples were modified as the CTM levels in the bloodless lung by calculating the contained blood volume, as lung samples were proven to have a mean value of 34.2% of blood in weight.
The serum CTM level was 73.3μg/ml at 15 minutes after injection and then decreased gradually.
The CTM level in bloodless lung was elevated during the first 60 minutes, became equal to that of the blood during next 30 minutes and then exceeded the serum levels thereafter.
These results indicate that the distribution of CTM to the bloodless lung was excellent and a satisfactory preventative effect against postsurgical infection could be expected.View full abstractDownload PDF (472K) -
HIROKI KIMATA, MASAHIRO YAMAMOTO, SEISHI NAKAYA, YOICHI SAITOH1985 Volume 38 Issue 1 Pages 160-165
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSComparative study of prophylaxis with cefotiam (CTM) was carried out in 47 patients undergoing surgery for gastric cancer. The patients were randomized in 2 treatment groups. The first group A received a single intravenous drip dose of 0.5 g CTM, given 4 times daily for 5 days after surgery. The second group B received a single intravenous drip dose of 1 g CTM, given twice daily for 5 days.
Postoperative infections occurred in 8.7% (2/23) of the patients receiving CTM in group A, and in group B 8.3% (2/24). The number of infections was similar in both groups of patients.
Prophylactic efficacy of CTM has also been evaluated in fever index of A and B groups. Fever index was 16.36±4.00 degree hours in A group, and in B group 7.91±2.30 degree hours, respectively. The difference between the 2 groups are statistically significant tendency. A single dose of 1 g CTM, given twice daily for 5 days, provide effective prophylaxis against infections in patients undergoing surgery for gastric cancer. CTM can be recommended for surgical prophylaxis.View full abstractDownload PDF (735K) -
ISAO HIROKAWA, TOKUJI ICHIKAWA, YASUSHI ISHIHARA1985 Volume 38 Issue 1 Pages 166-178
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. Bestatin was administered to 20 patients with urogenital tumors. The therapeutic results showed 12 surviving patients and 8 dead patients (including 7 due to cancer and 1 due to a cerebrovascular disorder).
2. One patient has survived for 5 years since bestatin treatment of pulmonary metastasis of renal cancer, and one other patient achieved 5-year survival in spite of systemic metastases of testicular tumor. It is noteworthy that in earlier times these patients could have been expected to experience sudden relapse and aggravation, instead of the long-term survival recorded in this bestatin trial.
3. Studies were conducted on the immunological parameters of the patients before and after the use of bestatin, and it was found that these parameters showed improvement as a result of the treatment.
4. Even though bestatin was ingested for long periods of time by these patients, there was almost no development of adverse reactions to the treatment.View full abstractDownload PDF (7379K) -
AKIRA FUJII, JOJI ISHIGAMI, NOBUMASA KATAOKA, SADAO KAMIDONO, SOICHI A ...1985 Volume 38 Issue 1 Pages 179-189
Published: January 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSIn vitro antibacterial activity of several cephems (CEZ as the first generation (group A); CTM and CMZ as the second generation (group B); CMX, CPZ, LMOX, CTX and CZX as the third generation (group C)) against 8 species, each of 54 strains, of Gram-negative clinical isolates from complicated urinary tract infection was compared by determination of the MICs.
The following results were obtained:
1. The most sensitive drugs against each species in MIC80; CTX (MIC80, 0.20μg/ml) against E. coli, CMX (1.56μg/ml) against K. pneumoniae, LMOX (0.39μg/ml) against P. mirabilis, LMOX (0.78μg/ml) against Indole (+) Proteus, CMX and CPZ (50μg/ml) against E. cloacae, CMX and LMOX (50μg/ml) against C. freundii, CMX (3.13μg/ml) against S. marcescens and CPZ (25μg/ml) against P. aeruginosa
2. The most sensitive drugs against each species in MICs100; CMX (MIC100 3.13μg/ml) against E. coli, CMX (6.25μg/ml) against K. pneumoniae, CTX (0.78μg/ml) against P. mirabilis, LMOX (1.56μg/ml) against Indole (+) Proteus, CPZ (100μg/ml) against E. cloacae, CMX (100μg/ml) against C. freundii, CMX (12.5μg/ml) against S. marcescens and CPZ(50μg/ml)against P. aeruginosa.
3. In each species, the group C were most sensitive followed by those of the group B. Many isolates were highly resistant to the group A (especially in C. freundii, S. marcescens and P. aeruginosa).View full abstractDownload PDF (870K)
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