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HIROMI KUMON, HIROYUKI OHMORI
1984 Volume 37 Issue 8 Pages
1445-1452
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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The clinical efficacy and safety of intravenous micronomicin (MCR) therapy were evaluated in cases with complicated urinary tract infections. MCR was administrated to 13 patients by intravenous dripinfusion over a period of 1 hour, in a dose of 120mg twice daily for 5 consecutive days. Therapeutic results were evaluated by the criteria proposed by UTI comittee and the judgement of the doctor in charge and the overall clinical efficacy rate was 69% (9/13) and 85% (11/13), respectively. Among 18 strains isolated before treatment, 15 strains were eradicated and bacteriological efficacy rate was 83%. No side effects including nephrotoxicity and ototoxicity associated with the treatment were noted, except for 1 case with transient elevation of Al-P.
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HIROSHI KAJIKAWA, SHOZO HOSOKAWA, HIROSHI KAMEOKA, NAOMITSU NISHIMOTO, ...
1984 Volume 37 Issue 8 Pages
1453-1469
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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A second part of our continuous investigation on the clinical effect of cefaclor (CCL) against urinary tract infections was reported herein. CCL, a daily dose of 0.75 g t.i.d., has been applied for the treatment of (I) 76 cases with the uncomplicated acute cystitis in the women, and (II) 55 cases with the complicated. Rates of effectiveness were obtained 98.7% in (I) and 60% in (II). Side effects were noted in 13 cases out of total 150 cases.
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(2) ITS EFFECT ON PREPARATIONS OF NEUROMUSCULAR JUNCTION, SMOOTH MUSCLE ORGANS AND GASTRO-INTESTINAL SYSTEM
YOSHIO YAMAKI, YOSHIAKI SHIBAZAKI, HIROYUKI KADOSAWA, SHINJIRO MURATA, ...
1984 Volume 37 Issue 8 Pages
1470-1487
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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The results for pharmacological experiments of MT-141 were as follows;
1. Twitch tention of gastrocnemius muscle evoked by the stimulation of sciatic nerve was slightly reduced with 400 mg/kg MT-141 i. v. and upper doses. As the change was very small, however, it seems that MT-141 has no neuromuscular junction blocking action.
2. Although MT-141 did not show any effects on most of isolated smooth muscle organs, only isolated tracheal muscle was somewhat relaxed with 10
-3g/ml MT-141.
3. The spontaneous motility of smooth muscle
in situ was temporarily increased with 800 mg/kg MT-141 i. v. and upper doses.
4. Two hundred mg/kg MT-141 showed no effect on the value of blood sugar and functions of kidney and liver.
5. Any hemolysis did not appear even in the highest dose of 200 mg/kg MT-141 used in this experiment.
From the present results and previous report (KREBE, M.
et al., Jap. J. Antibiotics, in press), it seems that MT-141 is promised to be a highly safe and useful antibiotic agent in clinical use.
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PART IV-1. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb1 IN MICE
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1488-1490
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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Miocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic3, 4) isolated from a culture broth of
Streptomyces mycarofaciens1, 2). MOM is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
5, and Mb
125).
The object of this study was to evaluate acute toxicity in male and female mice after single oral administration of Mb
1, a metabolite of MOM, at a dose level of 5,000 mg/kg as the maximum physically applicable dose.
Observations were kept for I week after administration. In conclusion, Mb
1 exhibited no acute toxicity in present study.
The LID
0 values were estimated as more than 5,000 mg/kg.
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1984 Volume 37 Issue 8 Pages
1490-
Published: 1984
Released on J-STAGE: May 17, 2013
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PART IV-2. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb1 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1491-1493
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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Acute toxicity studies on miocamycin (MOM), non-crystalline solid6), and its metabolite Mb
17) were performed in mice in the previous studies.
In the present studies, we evaluated acute toxicity of Mb
1 in male and female rats after single oral administration at the maximum physically applicable dose of 5,000 mg/kg.
Observations were continued for 1 week after treatment. It is concluded that LID
0 values of Mb
1 were estimated more than 5,000 mg/kg.
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PART IV-3. TOXICITY OF METABOLITES OF MIOCAMYCIN: SUBACUTE TOXICITY OF Mb IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...
1984 Volume 37 Issue 8 Pages
1494-1506
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1), 2). It is reported that MOM has the most interesting antibacterial properties among macrolide antibiotics3, 4) and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6 and Mb
125). It is also known that LD
0 values of Mb
1 were estimated more than 5,000 mg/kg without exhibiting any manifest toxic effects after single oral administration to male and female rats6).
The object of this study was to examine toxicological effects in male and female rats after repeated oral administration of Mb
1, a metabolite of MOM, for 5 weeks at daily dosages of 125, 250, 500 and 1,000 mg/kg which were selected in consideration of the maximum tolerable dosage level of 1,000 mg/kg/day for MOM, non-crystalline solid, in the rat subacute toxicity studies as previously reported7).
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PART IV-4. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb2 IN MICE
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1507-1509
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin1, 2) and is metabolized into 4 main metabolites5). At previous study, LD
0 values of Mb
1 were estimated more than 5,000 mg/kg in male and female mice7).
The object of this study was to evaluate acute toxicity in male and female mice after single oral administration of Mb
2, a metabolite of MOM, at a does level of 5,000 mg/kg as the maximum physically applicable dose. It is concluded that LD, values of Mb
2 were estimated more than 5,000 mg/kg.
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PART IV-5. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb2 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1510-1512
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin1), 2) and is metabolized into 4 main metabolites5). At previous study, LD
0 values of Mb
1, were estimated more than 5,000 mg/kg in male and female rats8).
The object of this study was to evaluate acute toxicity in male and female rats after single oral administration of Mb
2, a metabolite of MOM.
It is concluded that LD
0 values of Mb
2 were estimated more than 5,000 mg/kg.
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PART IV-6. TOXICITY OF METABOLITES OF MIOCAMYCIN: SUBACUTE TOXICITY OF Mb2 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...
1984 Volume 37 Issue 8 Pages
1513-1525
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6 and Mb
12.
At previous study, the acute and subacute toxicity of Mb
1 and acute toxicity of Mb
2 were performed that those metabolites did not exhibit any lethal toxicity even at the maximum physically applicable dose.
The object of this study was to examine subacute toxicity in male and female rats after repeated p. o. administration of Mb
2 for 5 weeks at a daily dosage of 125,250,500 and 1,000mg/kg.
It is, therefore, concluded that Mb
2, exerted no toxic effects in this subacute toxicity.
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PART IV-7. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb6 IN MICE
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1526-1528
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin and is metabolized into 4 main metabolites5).
In the present studies, we evaluated acute toxicity and estimated LD
50 values of Mb
6, one of the main metabolites of MOM, in male and female mice after single oral administration. Observations were continued for 1 week after treatment. The LD
50 values were calculated according to LITCHFIELDWILCOXON's method. It is concluded that LD
50 values of Mb
6 were 4, 150mg/kg (3,577.6-4, 814.0mg/kg) in male mice and 4,000mg/kg (3,389.8-4, 720.0mg/kg) in female mice, respectively.
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PART IV-8. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb6 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1529-1531
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin1, 2) and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6 and Mb
125).
In the previous studies, we estimated LD
50 values of Mb
6 in male and female mice7) after single oral administration. The LD
50 values were 4, 150mg/kg in male mice and 4,000mg/kg in female mice, respectively.
In the present studies, we evaluated acute toxicity and estimated LD
50 values of Mb
6 in male and female rats after single oral administration.
Observations were continued for 1 week after treatment.
It is concluded that LD
0 values of Mb
6 in male and female rats, were estimated more than 5,000mg/kg as Mb
6 did not exhibit any manifest acute toxicity even at the maximum physically applicable dose of 5,000mg/kg.
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PART IV-9. TOXICITY OF METABOLITES OF MIOCAMYCIN: SUBACUTE TOXICITY OF Mb6 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...
1984 Volume 37 Issue 8 Pages
1532-1545
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6 and Mb
12(5). It is also known that LD
50 values of Mb
6 were 4, 150mg/kg in male mice
8 and 4,000mg/kg in female mice but LD
0 values in male and female rats were estimated more than 5,000mg/kg.6) The object of this study was to examine subacute toxicological effects in male and female rats after repeated oral administration of Mb
6 for 5 weeks at a daily dosage of 125, 250, 500 and 1,000mg/kg. It is concluded that no manifest toxicity was observed in this study with Mb
6 in male and female rats after oral administration at dosage levels of 125, 250, 500 and 1,000mg/kg for 5 weeks.
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PART IV-10. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb12 IN MICE
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1546-1548
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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We evaluated acute toxicity and estimated LD
50 values of Mb
12, one of the main metabolites of MOM, in male and female mice after single oral administration. Observations were continued for 1 week after treatment. The LD
50values were calculated according to LITCHFIELD-WILCOXON'S method.
It is concluded that LD
50 values of Mb
12 were 5,750mg/kg (4,914.5-6,727.5mg/kg) in male mice and 4,950mg/kg (4, 194.9-5,841.0mg/kg) in female mice, respectively.
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PART IV-11. TOXICITY OF METABOLITES OF MIOCAMYCIN: ACUTE TOXICITY OF Mb12IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, HARUO KAWA ...
1984 Volume 37 Issue 8 Pages
1549-1551
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (MOM) is a derivative of midecamycin and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6 and Mb
125). In the previous studies, LD
50 values of Mb
127) were 5,750mg/kg in male mice and 4,950mg/kg in female mice, respectively.
The object of this study was to evaluate acute toxicity in male and female rats after single oral administration of Mb
12. Observations were continued for 1 week after treatment. It is concluded that LD
0 values of Mb
12were estimated more than 5,000mg/kg.
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PART IV-12. TOXICITY OF METABOLITES OF MIOCAMYCIN: SUBACUTE TOXICITY OF Mb12 IN RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, HITOSHI SASAKI, TETSUTARO ...
1984 Volume 37 Issue 8 Pages
1552-1564
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
FREE ACCESS
Miocamycin (MOM) is a derivative of midecamycin, a macrolide antibiotic isolated from a culture broth of Streptomyces mycarofaciens1, 2). It is reported that MOM has the most interesting antibacterial properties among macrolide antibiotics3, 4) and is metabolized into 4 main metabolites of Mb
1, Mb
2, Mb
6, and Mb
125). It is also known that LD
0 values of Mb
12 were estimated more than 5,000mg/kg without exhibiting any manifest toxic effects after single oral administration to male and female rats6).
The object of this study was to examine toxicological effects in male and female rats after repeated oral administration of Mb
12, a metabolite of MOM, for 5 weeks at a daily dosage of 125, 250, 500 and 1,000mg/kg which were selected in consideration of the maximum tolerable dosage level of 1,000mg/kg/day in MOM rat subacute toxicity studies as previously reported7).
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PART VI-1. ACUTE TOXICITY IN INFANT MICE IN COMPARISON WITH YOUNG ADULT MICE
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, MASAHIDE MORIGUCHI, TAKASH ...
1984 Volume 37 Issue 8 Pages
1565-1568
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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SUTHERLAND1) and WEISS et al.7) reported cases of newborn human deaths or GRAY syndrome after overdosage of chloramphenicol. In general, it has been reported that the acute toxicities of drugs are enhanced in immature animals compared with adult animals.
The objective of this study was to determine the LD
50 values in infant (5-day-old) and young adult (5-week-old) male and female mice after single subcutaneous and oral administration of MOM, noncrystalline solid and to estimate the toxicity ratio of those LD
50 values.
LD50 values of MOM, non-crystalline solid, were more than 5,000mg/kg and the lethal toxicity was the same in infant and adult mice. Toxicity ratios were not obtained.
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PART VI-2. ACUTE TOXICITY IN INFANT RATS IN COMPARISON WITH YOUNG ADULT RATS
MASAYUKI YOKOTA, UETO TAKEDA, MASUZO ODAKI, MASAHIDE MORIGUCHI, HIROSH ...
1984 Volume 37 Issue 8 Pages
1569-1571
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
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In the present acute toxicity studies on MOM, non-crystalline solid, with infant male and female rats (5-day-old) and young adult male and female rats (5-week-old), it is confirmed as follows:
1. LD
50 values were estimated more than 5,000mg/kg in both cases of subcutaneous and oral administrations.
2. MOM, non-crystalline solid, did not exhibit any toxic effects similarly as previously reported with infant male and female mice and young adult male and female mice.
3. There might be no definite age difference in toxicity between young and adult rats as LD
50 values were estimated more than 5,000mg/kg in independence upon the age.
4. There might be no definite species difference in toxicity between mice1) and rats.
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MASAHIDE MORIGUCHI, UETO TAKEDA, TOSHIAKI HATA, ATSUKO YAMAMOTO, TAKEM ...
1984 Volume 37 Issue 8 Pages
1572-1595
Published: August 25, 1984
Released on J-STAGE: May 17, 2013
JOURNAL
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Miocamycin (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 effect of MOM on reproductive performance in rats and rabbits. MOM, non-crystalline solid, was suspended in 0.1% CMC solution immediately before use.
In this study, reproductive performance was studied according to the following designs:
1. Fertility test (Segment I) in Wistar rats
2. Teratogenicity test (Segment II) in Wistar rats
3. Peri-and post-natal tests (Segment III) in Wistar rats
4. Behavioral test in rat newborns in Segments II and III
5. Teratogenicity test (Segment II) in New Zealand white rabbits
In conclusion, MOM, non-crystalline solid, might have no teratogenesis and little influence on dams and their fetuses and offsprings.
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