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Volume 37, Issue 7
Displaying 1-18 of 18 articles from this issue
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KAZUO TAMURA, YASUHIKO ARAKI, TOSHIAKI AMAMOTO, MASASHI SEITA1984 Volume 37 Issue 7 Pages 1237-1240
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSSisomicin sulfate (SISO) was used for the treatment of infections complicated by malignant diseases in 10 cases; 4 cases with suspicious sepsis, 2 with pneumonia, 2 with urinary tract infection, 1 with renal abscess and 1 with cholecystitis.
SISO was administered by intravenous drip infusion at daily dose from 100 to 150 mg for 6 to 12 days, con-comitantly with other antibiotics.
Clinical results were as follows; Good in 2, fair in 5, poor in 3 cases.
As to the side effects of SISO, cylindruria with aggravation of microscopic hematuria and elevations of GOT, GPT and Al-P were observed each one of them, respectively. The relationship to the SISO, however, was not clear.
In view of the above results, the drip infusion of SISO may be useful for the treatment of serious infection complicated by malignant diseases.View full abstractDownload PDF (511K) -
HIDEO IKEMOTO, KAZUYOSHI WATANABE, NOZOMU KOSAKAI, JUN IGARI, TOYOKO O ...1984 Volume 37 Issue 7 Pages 1241-1262
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTwo hundred seventy-six bacterial strains were isolated as possible causative pathogens mainly from sputum in 248 patients with lower respiratory tract infections at 12 medical institutions in various parts of Japan during the period from September 1982 to March 1983. Of these, 272 isolates including 28Staphylococcus aureus strains, 38 Streptococcus pneumoniae strains, 107 Haemophilus influenzae strains, 68Pseudomonas aeruginosa strains, 17Klebsiella pneumoniae strains, 9Escherichia coli strains and 5 strains of other species were testedin vitro for MICs of various antibiotics, and their drug sensitivity distributions determined. Data were also analyzed for distribution of cases by clinical entities, age and sex, interrelations between the types of infections and the species and frequency of isolation of organisms, and relations of the antimicrobial regimens at collection of clinical specimens to the species and frequency of isolation of the organisms. It engenders great interest that there was a significant increase in frequency ofS. aureus isolation within 7 days after antibiotic therapy, compared to pretreatment isolation frequency, in the 1982 series. This seems to deserve further investigation in detail. TheH. influenzae strains isolated with the highest frequency in 1981 and those in 1982 were examined as to susceptibility to several representative antibiotics, with interdrug comparisons: ABPC vs. SBPC, CTM vs. CMZ, and CMX vs. LMOX. The isolates demonstrated high degrees of susceptibility to these drugs and there was no conspicuous change in bacterial sensitivity to the drugs.View full abstractDownload PDF (2215K) -
INTRAMUSCULAR, INTRAVENOUS OR DRIP INTRAVENOUS ADMINISTRATIONTSUKASA KURIMOTO, HIROYUKI KOBAYASHI, AKINOBU INOUE, RYO OKACHI1984 Volume 37 Issue 7 Pages 1263-1271
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAbsorption, tissue distribution and excretion of astromicin (ASTM) were studied in rats after intramuscular (i. m.), intravenous (i. v.) or drip intravenous (d. i. v.; for 15, 30min. or 60min.) administration at a dose of 20mg/kg. The pharmacokinetic studies of ASTM were carried out using one-compartment open model (i. m.) or two-compartment open model (i. v. and d. i. v.).
1. The peak values of ASTM observed in serum were 48.6μg/ml (i. m.), 255.3μg/ml (i. v.), 57.5μg/ml (15min. d. i. v.), 45.9μg/ml (30min. d. i. v.) and 39.1μg/ml (60min. d. i. v.).
2. The pharmacokinetic parameters of ASTM after 15min. d. i. v. administration were calculated as follows: Kel 0.110min-1 T1/2 21.4min., Vdβ 0.310L/kg, Tmax. 15.0min., Cmax 58.6μg/ml AUC 1,991μg·min/ml.
3. ASTM was rapidly distributed into the kidneys and lungs. The peak values of ASTM in the kidneys were 156.8μg/g (i. m.), 185.2μg/g (i. v.), 132.9μg/g (15min. d. i. v.), 135.3μg/g (30min. d. i. v.) and 117.3μg/g (60min. d. i. v.).
4. Urinary recovery rates of ASTM amounted to 85.5% (i. m.), 99.5% (i. v.) or 87.9% (30min. d. i. v.).
5. After i. m. or 30min. d. i. v. administration of ASTM, no active metabolite was found in urine of rats.View full abstractDownload PDF (2159K) -
BACTERIA FROM BACTEREMIC PATIENTS WITH HEMATOLOGICAL DISORDERSHAJIME NAKAZAWA, SHINICHIRO OKAMOTO, TADASHI MURASE, YOHKO YOSHII, ISA ...1984 Volume 37 Issue 7 Pages 1272-1278
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAntibiotics contained in blood specimens often inhibit bacterial growth in culture media. Recently, the antimicrobial removal device (ARD) containing resins to absorb antibiotics has been made available. To evaluate the effectiveness of the ARD, we investigated how much the antibiotics were removed by the ARD. The ARD method was compared to the conventional culturing method in isolating organisms from blood specimens of patients with hematological disorders receiving antimicrobial agents.
The antibiotics, including cefotiam, cefsulodin, cefmenoxime, cefazolin and sulbenicillin, were proved to be almost completely removed by the ARD.
Bacteria were detected only by use of the ARD in the blood cultures from 2 of 21 blood specimens (11 patients) entered in the study, while all of the blood cultures were negative by the conventional method. These isolated bacteria were S. aureus and P. aeruginosa, of which septicemias were cured by intensive antibiotic therapy for these bacteria.
It is suggested that pretreatment with the ARD makes detection of bacteria easier in blood from the patients receiving antibiotics.
Literatures were reviewed concerning improvement and shortened time for isolation of organisms by using the ARD.View full abstractDownload PDF (2738K) -
TAKAFUMI BANDO, HIROSHI TOYOSHIMA1984 Volume 37 Issue 7 Pages 1279-1288
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSSerum and bile levels of fosfomycin sodium (FOM-Na) were evaluated and the pharmacokinetic parameters were estimated in 10 patients with various forms of biliary drainage (PTCD or T-tube). Clinical trials of FOM-Na were also performed in another 11 patients with bile duct infections and the clinical efficacy was estimated.
Mean serum level of FOM-Na after drip infusion of 2g fosfomycin sodium was 145.43 μg/ml at 1 hour, meanwhile bile level was 31.49μg/ml at 2 hours. Serum level of FOM-Na was interpreted by the pharmacokinetic analysis after the damping GAUSS-NEWTON method using the one-compartment open model and bile level of FOM-Na by the damping GAUSS-NEWTON method and deconvolution method. Mean Vd was 12.16L/body and half-time of serum level was 1.75 hours. Lag-time of bile level was 0.9 hour,Tmax 2.01 hours.
The clinical efficacy of FOM-Na was determined excellent without any adverse effect. FOM-Na was remarkably effective in 91% of the patients. Hence, the first choice of FOM-Na against bile duct infections could be recommended.View full abstractDownload PDF (990K) -
KIYO NISHIOKA, SHIROH IDA, TAMOTSU TAKISHIMA1984 Volume 37 Issue 7 Pages 1289-1293
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe efficacy of antibiotics including some newly developed penicillins and cephems on clinically isolated Branhamella catarrhalis was evaluated in vitro. Among 44 strains of B. catarrhalis which were isolated from expectorated sputum of patients with respiratory tract infections 36 strains were proved to produce β-lactamase.
MICs of penicillins for β-lactamase positive strains ranged from 6.0.05 to 3.13μg/ml, while those for β-lac-tamase negative strains were all less than 0.05μg/ml. MICs of cephems, on the other hand, ranged more variably, especially among β-lactamase positive strains. The most effective cephem we tested was LMOX which could inhibit all the strains of B. catarrhalis at the concentration of 0.05μg/nal or less. Aminoglycosides as well as macrolides also showed sufficiently low MIC values. We therefore concluded that the confirmation of β-lac-tamase production by B. catarrhalis seems to be indispensable for the determination of an antibacterial activity of β-lactam antibiotics.View full abstractDownload PDF (625K) -
KAZUHIRO KASAI, AKIYOSHI TSUJI, SHUICHI MIYAZAKI, SACHIKO GOTO, KAZUMI ...1984 Volume 37 Issue 7 Pages 1294-1305
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe in vitro activity and β-lactamase stability of cefodizime (HR 221), a new cephalosporin, were compared with those of other cephem antibiotics.
HR 221 was highly active against Gram-negative bacteria. The compound inhibited growth of all tested Haemophilus influenzae strains at 0.10μg/ml and showed strong activity even against penicillin-resistant Neisseria gonorrhoeae strains, but it was less effective against Pseudomonas aeruginosa than the other antibiotics tested. Against Gram-positive bacteria, HR 221 showed 100% inhibition of growth of Streptococcus pneumoniae at 0.39μg/ml, and it was slightly less active against Staphylococcus aureus (MIC90: 12.5,μg/ml) than other antibiotics such as cefotaxime (CTX).
The bactericidal activity of HR 221 against E. coil was dose-related and comparable to that of CTX, cefoperazone and latamoxef. The bactericidal activity of the compound at medium concentrations simulating human serum levels was higher than that of CTX and cefmetazole, and no cell regrowth was noted after β-lactamase-induced inactivation of the compound.
HR 221 was stable to most drug-inactivating enzyme preparations from various bacterial species.View full abstractDownload PDF (1283K) -
KAZUHIRO KASAI, AKIYOSHI TSUJI, SHUICHI MIYAZAKI, SACHIKO GOTO, KAZUMI ...1984 Volume 37 Issue 7 Pages 1306-1312
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe in vivo activity of cefodizime (HR 221) was compared with that of cefotaxime (CTX), cefmen-oxime, latamoxef, cefazolin and cefmetazole (CMZ).
The protective effects of HR 221 on experimental infections in mice caused by Staphylococcus aureus SMITH, Escherichia coli C-11, Proteus vulgaris GN-76 and Serratia marcescens No.2 were directly related to its in vitro activity against these strains. In contrast, the compound showed the smallest ED50 values, among the 5 antibiotics tested (not including CMZ), for Klebsiella pneumoniae 3K-25 and Pseudomonas aeruginosa PI 67 against which it had relatively low in vitro activity, and its ED50 for Citrobacter freundii GN-346 was as small as 1.821mg/mouse in spite of its MIC of>100μg/ml.
HR 221 exerted potent bactericidal activity against Streptococcus pneumoniae Sp-1 inoculated into the mouse lung; the duration of action was prolonged. When tested against the E. coli Ec-89 infection induced in the rat uterus, the activity of HR 221 given to rats once daily was equal to that of CTX or CMZ given at the same dose twice daily.View full abstractDownload PDF (910K) -
PART I-1. ACUTE TOXICITY IN MICEMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...1984 Volume 37 Issue 7 Pages 1313-1316
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2).
The objective of this study was to determine the acute toxicity of MOM, non-crystalline solid, in male and female mice (Jcl-ICR, SPF, 5-week-old) after single i. p., s. c. and p. o. administration of this material at a dose level of 5,000mg/kg as the maximum physically applicable dose.
MOM, non-crystalline solid, exhibited no acute toxicity in the present study. LD0 values were estimated as more than 5,000mg/kg in each route of administration.View full abstractDownload PDF (2048K) -
PART I-2. ACUTE TOXICITY IN RATSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...1984 Volume 37 Issue 7 Pages 1317-1320
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a cul-ture broth of Streptomyces mycarofaciens1, 2). The object of this study was to determine the acute toxicity in male and female rats (Wistar, 5-week-old) after single i. p., s. c. and p. o. administration of MOM, non-crystalline solid, at a dose level of 5,000mg/kg as the maximum physically applicable dose.
Observations were kept for 1 week after administration.
In conculusion, no animal died during an observation period for 1 week so that the LD0 values were estimated to be more than 5,000mg/kg in all routes of administration.View full abstractDownload PDF (2604K) -
SUBACUTE TOXICITY IN RATSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1321-1332
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin (MDM), a macrohde antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2). Its chemical stmcture is shown in Fig. 1. It is reported that MOM has the most interesting antibacterial properties among the known macrohde antibiotics3, 4).
As previously reported on the acute toxicity of MOM in mice and rats5, 6), LD50 values in male and fbmale mice and rats after single intraperitoneal, subcutaneous and oral administration of MOM, non-crystalline solid, were estimated more than 5, 000mg/kg in all routes of administration without markedly toxic effects.
The oblective of this study was to examine toxicological effects of MOM, non-crystalline solid, in male and female rats after repeated oral administration for 5 weeks at selected dosage levels of 1, 000, 2, 000 and 4, 000mg/kg.View full abstractDownload PDF (1278K) -
SUBACUTE TOXICITY IN RABBITSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1333-1354
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin (MDM), a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2). Its chemical structure is shown in Fig. 1. It is reported that MOM has the most interesting antibacterial properties among macrolide antibiotics3, 4).
It has been known that MOM, non-crystalline solid, did not exhibit any noticeable toxic effects in male rabbits when it was orally administered once daily for 5 weeks at daily dosage levels of 100, 200 and 400mg/kg as previously studied in dose-finding studies. The objective of this study was to examine toxicological effects in male rabbits after repeated oral administration of MOM, non-crystalline solid, for 5 weeks at daily dosages of 400, 800, 1, 600 and 3, 200 mg/kg, which were selected for the studies in consideration of the results obtained from the dose-finding subacute toxicity studies in rabbits. The lowest dosage level of 400 mg/kg/day is corresponding to the highest dosage level of the dose-finding studies.View full abstractDownload PDF (5511K) -
CHRONIC TOXICITY IN RATSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1355-1375
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin (MDM), a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2). Its chemical structure is shown in Fig. 1. It is reported that MOM has the most interesting antibacterial properties among the known macrolide antibiotics3, 4). It has been known that the maximum tolerable dosage level of MOM, non-crystalline solid, was 1, 000 mg/kg in male and female rats when it was orally administered once daily for 5 weeks at daily dosage levels of 1, 000, 2, 000 and 4, 000 mg/kg as previously reported5).
The objective of this study was to examine toxicological effects in male and female rats after repeated oral administration of MOM, non-crystalline solid, for 26 weeks at daily dosage levels of 62. 5, 125, 250, 500 and 1, 000mg/kg.View full abstractDownload PDF (5314K) -
PART III-2. CHRONIC TOXICITY IN BEAGLE DOGS: 13-WEEK-TREATMENT IN MALE DOGSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1377-1382
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2).
The objective of this study was to determine the chronic toxicity of MOM in male Beagle dogs after once daily repeated p. o. administration of MOM, non-crystalline solid, for 13 weeks at daily dosage of 200 and 400mg/kg.
It is concluded that no toxic effects of MOM, non-crystalline solid, were shown in the present studies.
Therefore, the maximum non-toxic dose is presumed to be 400mg/kg or more in male Beagle dogs administered p. o. once daily for 13 weeks.View full abstractDownload PDF (722K) -
PART III-3. CHRONIC TOXICITY IN BEAGLE DOGS: 26-WEEK-TREATMENT IN FEMALE DOGSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1383-1397
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic1, 2) isolated from a culture broth of Streptomyces mycarofaciens3, 4).
The objective of this study was to determine the chronic toxicity of MOM in female Beagle dogs after once daily repeated p. o. administration of MOM, non-crystalline solid, for 26 weeks at daily dosages of 100, 200 and 400mg/kg.
It is concluded that MOM, non-crystalline solid, did not show any toxic effects in this study and the maximum non-toxic dose is presumed to be 400mg/kg or more in female Beagle dogs administered once daily for 26 weeks.View full abstractDownload PDF (3525K) -
PART III-4. CHRONIC TOXICITY IN BEAGLE DOGS: 26-WEEK-TREATMENT IN MALE DOGSMASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...1984 Volume 37 Issue 7 Pages 1399-1416
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMiocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens.
The objective of this study was to determine the chronic toxicity of MOM in male Beagle dogs after repeated oral administration of MOM, non-crystalline solid, for 26 weeks at b.i.d. dosage of 200, 400, 800 and 1,200mg/kg/day.
It is concluded that MOM, non-crystalline solid, did not show any toxic effects in this chronic toxicity study.
Therefore, the maximum non-toxic dose is presumed to be 1,200mg/kg/day or more in male Beagle dogs administered orally at b.i.d. for 26 weeks.View full abstractDownload PDF (5595K) -
XI. IMMUNOLOGICAL PROPERTIES OF ITMASARU KUREBE, HIROYASU ASAOKA, MASANORI IZAWA, SHUKO NAGAI, CHIHO HIR ...1984 Volume 37 Issue 7 Pages 1417-1427
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSImmunogenicity, eliciting antigenicity of MT-141 and its cross-reactivity with other β-lactam antibiotics were studied in mice, guinea pigs and rabbits. The results were as follows.
1. Injections of MT-141 failed to produce IgE-type antibody in mice but injections of the MT-141 conjugated to rabbit serum albumin produced a trace of IgE-type antibody.
2. No antibody was produced in the guinea pigs immunized with the MT-141 conjugated to rabbit serum albumin in alum or FREUND'S complete adjuvant. The conjugated MT-141 also failed to elicit anaphylactic shock in the immunized guinea pigs.
3. The subcutaneous treatments with MT-141 in FREUND'S complete adjuvant produced an amount of hemagglutination antibody in rabbits. The intravenous treatments with MT-141 produced no antibody in rabbits.
4. When rabbits were subcutaneously immunized with the MT-141 conjugated to rabbit serum albumin in FREUND'S complete adjuvant, production of specific antibody in the rabbits was demonstrated by observations of passive cutaneous anaphylaxis and hemagglutination.
5. The results of hapten-induced inhibition of passive hemagglutination, passive cutaneous anaphylaxis, anaphylactic shock and hemagglutination by using conjugates of antibiotics and rabbit serum albumin as immunogens and conjugates of antibiotics and bovine γ-globulin as eliciting antigen showed that MT-141 did not cross-react with other antibiotics.
6. MT-141 did not cause the in vitro direct COOMBS' reaction in the human blood even at a high concentration of 160mg/ml.
7. It is concluded from these results that immunological activity of MT-141 preparation is weak.View full abstractDownload PDF (1264K) -
(1) ITS EFFECT ON CENTRAL NERVOUS SYSTEM, RESPIRATION AND CARDIOVASCULAR SYSTEMMASARU KUREBE, HIROYASU ASAOKA, YOSHIO YAMAKI, SHIRO SUGIYAMA, YOSHIAK ...1984 Volume 37 Issue 7 Pages 1428-1439
Published: July 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe results on pharmacological effects of MT-141 were as follows.
1. MT-141 did not exert effect on central nervous system in mice and rabbits but potentiated the anesthetic effect of thiopental at doses above 800mg/kg i. v.
2. MT-141 slightly raised a level of blood pressure in dogs and also caused a slight increase in the blood flow and heart rate when intravenously given more than 400mg/kg.
3. This compound did not affect the spontaneous contraction of isolated guinea pig atria and the blood vessels in perfused rabbit ears.
4. MT-141 did not significantly affect the spontaneous contraction and coronary flow in isolated hearts of guinea pig.
5. The body temperature was raised slightly by an injection of more than 400mg/kg of MT-141.
6. These results suggest that MT-141 does not possess specific effect on central nervous system but at a high dose slightly affects the autonomic nervous system such as blood pressure, body temperature, heart rate and blood flow in experimental animals.View full abstractDownload PDF (5828K)
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