The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 34, Issue 12
Displaying 1-23 of 23 articles from this issue
  • Special reference to monobactam
    KEN YOKOTA
    1981 Volume 34 Issue 12 Pages 1525-1539
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • HARUE ARATANI, SUMIKO NEGITA, HIDEKI TATEISHI, SHIGEAKI MIYAMOTO
    1981 Volume 34 Issue 12 Pages 1540-1548
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Excretion of pivmecillinam (PMPC) in bile was investigated using normal and hepatic disoder (intramuscular injection of carbon tetrachloride, 0.5g/kg twice) rabbits. Bile and blood were collected hourly (0.5-8 hours) and both concentrations and rates between both (passage), and excretion rates were investigated. Ampicillin (AMPC) was chosen as a control drug.
    1. When PMPC was given orally to the normal rabbit in a dose of 200mg/kg, a bile concentration after 0.5hour was 138.08μg/ml and a peak value was attained. The rate to plasma concentration was 22.67. An excretion rate was 0.224%.
    2. When PMPC was given orally to the hepatic disorder rabbit in a dose of 200mg/kg, a bile concentration after 0.5hour was 26.67μg/ml. A peak value of 28.87μg/ml was attained after 4 hours. Their rates to plasma concentrations were 13.27 and 8.02, respectively. An excretion rate was 0.058%. Bile and plasma concentrations, rates of bile to plasma and excretion rates of the hepatic disorder groupwere lower than those of the normal group. Disturbancesof hepatic functions were checked by biochemical tests, i.e. GOT, and so on.
    3. When ABPC as a control drug was given orally to the rabbit in a dose of 200mg/kg, plasma concentrations of hepatic disorder group were higher than those of the normal group, but rates of bile to plasma concentrations and excretion rates of the hepatic disorder group were lower than those of the normal group.
    4. Bile concentrations and excretion of PMPC were significantly higher than those of ABPC in the normal group. In the hepatic disorder group, however, no statistical difference was observed between them.
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  • COMBINED ADMINISTRATION WITH FUROSEMIDE OF TOBRAMYCIN
    YOSHIO HARADA, KUMIKO TESHIMA, TAKAO OKAMOTO
    1981 Volume 34 Issue 12 Pages 1549-1570
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    I. The nephrotoxic potential of latamoxef (LMOX, 6059-S) was evaluated in male rabbits after combined administration of 500 or 2,000 mg/kg of the compound (ear vein) with subcutaneous injection of furosemide (FUR) at 50 mg/kg. Histological examination of kidney tissues of all animals were performed after 72 hours. Three rabbits were used at each dose level, and comparative studies were performed using several cephalosporins, such as CET and CEZ.Neither LMOX nor CET produced nephrotoxic effects at 500 mg/kg when given in combination with FUR. Although slight elevation of BUN and creatinine in plasma and hyaline casts in lumen of the distal tubules were observed in animals receiving 2,000 mg/kg of LMOX or CET when dosed with FUR, no histological changes were found in renal tissues. Significantly more nephrotoxicity was observed with the treatment of CEZ alone, and this toxicity was augmented in combination with FUR.
    II. Concomitant administration of LMOX with intramuscular injection of tobramycin (TOB) was estimated in male rabbits. Rabbits received daily intramuscular injection of TOB at 50 mg/kg for 10 days in combination with single dosing of LMOX (500 or 2,000 mg/kg) on the 8th day after the start of TOB treatment. Three rabbits were used at each dose level, and comparative studies were conducted using CET or CEZ. All rabbits were killed 48 hours after the last injection of TOB and examined histopathologically. Combined administrations of LMOX or CET did not aggravate the nephrotoxicity induced by TOB. However, CEZ enhanced renal injuries produced by TOB injection.
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  • TSUTOMU HATANO, SHUNKICHI BABA, JUN HONDOH, KENJI WADA, KANETAKA MURAI ...
    1981 Volume 34 Issue 12 Pages 1571-1582
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    From the laboratory and clinical studies on ceftizoxime (CZX), the following results were obtained.
    1) CZX was compared with cefazolin (CEZ) for in vitro activity against 6 standard strains and clinically isolated strains of Staphylococcus aureus (19 strains), Staphylococcus epidermidis (14), Proteus sp.(17), Escherichia coli (3), Klebsiella sp.(3) and Pseudomonas aeruginosa (13). While somewhat less active against Gram-positive cocci than CEZ, CZX was far more active than CEZ against Gram-negative bacilli.
    2) The time course of mean serum CZX levels in 2 patients given a single intravenous dose of 10 mg/kg was as follows: 24.9 μg/ml at 15 minutes, 18.5μg/ml at 30 minutes, 13.2 μg/ml at 1 hour, 6.4μg/ml at 2 hours and 2.7 μg/ml at 4 hours. The mean serum half life was 1.36 hours.
    The mean tonsil concentrations of CZX 30 minutes after a single intravenous dose of 0.5g and 1.0g were 5.9 μg/g and 9.6 μg/g, respectively, with the ratio tothe serum concentration of 0.33 and 0.32.
    3) CZX was given to 28 patients with ear, nose, and throat infections, and overall rate of effectiveness was 92.3%.
    No clinical side effects were observed. Changes in laboratory test findings included slightly elevated GOT and/or GPT in 3 cases.
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  • KIYOSHI KUMANO, TOHRU FUKUBAYASHI, MASAMI AKAI, YORIYUKI KAWAI, YASUO ...
    1981 Volume 34 Issue 12 Pages 1583-1587
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    For the purpose of preventing postoperative orthopedic infections, investigation was carried out on effectiveness and safety of amikacin (AMK) after washing wound surface with its solution.
    500 ml saline solution containing 400 mg AMK was used for washing.
    As the result, no postoperative infections were observed in all the 19 patients operated in our department. Neither abnormal findings to be regarded as abnormalities in blood test nor side-effects caused by washing were also observed. The blood samples obtained after washing did not show measurable AMK in all cases.
    It is said that use of antibiotics with 1) a wide-range of spectrum, 2) a bactericidal action and 3) low cross resistance against other antibiotics is preferable in washing wound surface in order to prevent postoperative infections.Under these circumstances, administration of aminoglycoside antibiotics is used frequently.
    Concerning the use of aminoglycoside antibiotics, however, it is necessary to pay attention to auditory and renal impairment.
    The previous study has revealed that AMK is lower in auditory and renal toxicity than other aminoglycoside antibiotics.
    AMK is thought, therefore, to be free from fear of auditory and renal impairment after washing and also to be one of effective antibiotics.
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  • SUSUMU NAKAZAWA, HAJIME SATO, KENJI NIINO, YUICHI HIRAMA, AKIRA NARITA ...
    1981 Volume 34 Issue 12 Pages 1588-1594
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The clinical and pharmacokinetic studies of cefroxadine (CXD) dry syrup were conducted, and the following results were obtained.
    1. A single dose of CXD either10mg/kg or20mg/kg was given to2patients each, and serum levels were peaked in the range of about 10 to 11 μg/ml.
    2. About 30mg/kg of CXD per day was administered to 47infants and children (37;upper and lower respiratory tract infection, 3;urinary tract infection, 7; Others) aged from 6 months to 8 years and 1 month weighing 8 to 29kg, and a 97.8% (44 out of 45) of clinical response was obtained except for 2 cases whose efficacies were uncertain.
    3. As the drug-induced side effects, only transient loose stool was observed in 2 cases. This, however, allowed to continue the treatment.
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  • YUKIO IWASAKI, SATOSHI IWATA, TAKEFUMI KANEMITSU, KEIJI JOZAKI, HARUKI ...
    1981 Volume 34 Issue 12 Pages 1595-1603
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Basic and clinical evaluations of cefroxadine were carried out in children, and the following results were obtained.
    1. Cefroxadine 20mg/kg was administered to 9 children with heart disease for the prophylaxis against infections before undergoing cardiocatheterization and cardioangiography, and serum levels were determined. Peak levels reached after 30 minutes in 4 of the 9 cases, with a mean peak level of 22.5mcg/ml and after1hour in 5 cases, with a mean peak level of 16.2mcg/ml.Half life was 3.1 hours in the former group in a 6-hour blood sampling (1.04 hours in a 2-hour sampling) while in the latter group it was 1.37 hours.
    2. Clinical responses were evaluated in 56 children comprising 23 cases of pharyngitis, 8 of tonsillitis, 13 of scarlet fever, 10 of urinary tract infections and 2 of impetigo. Fifty of these cases had excellent and good responses showing a efficacy rate of 89.3%.
    3. From 42 of the cases, 43 strains were isolated as causative organisms.Major organisms included 27 strains of S.pyogenes, 9 of E.coli a 3 of S. aureus. As for bacteriological responses, all strains were eradicated.
    4. No severe side effects were observed except for diarrhea of 1 case and eosinophilia of 2 cases. Furthermore, no children refused to take cefroxadine dry syrup.
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  • TATSUHIKO SHINOZAKI, SHINTARO HASHIRA, YORIKO KOIKE, RYOCHI FUJII
    1981 Volume 34 Issue 12 Pages 1604-1607
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefroxadine dry syrup was administered to 57 children with acute febrile respiratory tract infections and 2 children with scarlet fever in the dose of 40mg/kg/day q. i. d. for 2-7 days.
    65 strains of organism were isolated as pathogen from the 59 patients, and 50 of the 65 strains (76.9%) showed bacteriologically good response. Clinically, 55 children (93.2%) had good response.
    Out of 63 strains isolated from the 57 cases with respiratory infections, 48 strains (76.2%) showed good bacteriological response.As for the type of pathogen, all strains of Staphylococcus aureus, 86.4% of Streptococcus haemolyticus and 90.0% of Streptococcus pneumoniae had good response, but as for Haemophilus influenzae it was only 47.6%.
    In one child, Streptococcus pneumoniae appeared during cefroxadine treatment in addition to the preexisting Haemophilus influenzae. From the 4 children having no response for their respiratory infections, H. influenzae were isolated in 3 cases and Streptococcus haemolyticus was isolated in 1 case, before starting the treatment.
    As for side effects, mild diarrhea developed in only 3 children.
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  • YOSHIKIYO TOYONAGA, YOSHIIE KUROSU, MAKOTO HORI, SABURO KOHNO
    1981 Volume 34 Issue 12 Pages 1608-1625
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental and clinical studies on cefroxadine (CXD) were carried out, and we have obtained the following results.
    (1) Sensitivity distribution:
    As for the sensitivity distribution in S. aureus, the peak was within the ranges from 3.13 to 6.25μg/ml in the inoculum size of 108 CFU/ml, the distribution was _??_0.1 to 50μg/ml in the inoculum size of 106 CFU/ml, with the peak at 1.56 to 6.25μg/ml. In S. pyogenes, the sensitivity distribution ranged between _??_0.1 and 1.56μg/ml, with the peak at _??_0.1μg/ml in the inoculum size of 106 CFU/ml, In the inoculum size of 106CFU/ml, however, the all strains were distributed within the ranges of 0.1 to 0.78μg/ml, and the growth of 49 out of 54 strains (91%) was inhibited at _??_0.1μg/ml. In, E. coli, the sensitivity peak was at 25 to 50μg/ml in the inoculum size of 106CFU/ml, and 5 strains (9.3%) were detected with _??_100μg/ml. Of the 5 strains, 1 strain showed cross tolerance with CEX, the remaining 4 strains was at 50μg/ml and at 25μg/ml in 2 strains each. In the case of inoculum size of 106CFU/ml, the sensitivity distribution was all within the ranges from 0.78 to 12.5μg/ml, except for 1 strain at 100μg/ml, with the peak being within the ranges from 3.13 to 12.5μg/ml. As for the above 100μg/ml-strain, it was showing cross tolerance with CEX.
    (2) Serum concentration:
    CXD was administered at a dose level of 10mg/kg and 20mg/kg between meals to 5 children, and CXD concentration in their serum was measured. In the group of the 10mg/kg administration: average 30 minutes value; 8.7μg/ml, 1 hour value; 9.15μg/ml, 2 hours value; 7.4μg/ml, 3 hours value; 2.85μg/ml, 4 hours value; 1.0μg/ml and 6 hours value; 0.32μg/ml, with half-life of 0.88 hours. In the group of the 20mg/kg administration: average 30 minutes value; 11.7μg/ml, 1 hour value; 16.8μg/ml, 2 hours value; 10.7μg/ml, 3 hours value; 8.15μg/ml, 4 hours value; 3.33μg/ml, 6 hours value; 1.22μg/ml, with half-life of 1.03 hours. A significant interrelation in dose response was observed between the 2 groups.
    (3) Clinical results:
    Clinical investigations were held in 79 cases (47 boys and 32 girls). Their diseases comprised of 2 acute pharyngitis, 28 acute purulent tonsillitis, 11 scarlet fever, 3 carvical purulent lymphadenitis, 14 acute bronchitis, 7 acute pneumonia, 11 urinary tract infection and 3 skin soft tissue infection. The drug was effective in 74 out of the 79 cases (93.7%).
    Causative organism was proved in 60 out of the 79 cases. Fifty-five cases (91.7%) were observed bacterial disapPearance or reduction in the 60 cases. Side effects were observed in atotal of 3 cases (3.8%), i.e. 2 cases of abnormal values in the laboratory findings (an eosinophilia and/or an elevation of the GPT readings) and 1 case of manifestation of exanthema.
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  • MIKIO MINAMITANI, KEI HACHIMORI, MASATOSHI SUZUKI, ITSUO MINAMIKAWA
    1981 Volume 34 Issue 12 Pages 1626-1633
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical evaluation was carried out on cefroxadine dry syrup (containing 100mg of cefroxadine per 1g) for child use, and the following results were obtained.
    1. Serum levels:
    Peak serum levels at 1 hour after single administration of CXD 100mg (9.1mg/kg) to a 4-year old child (11kg) and 300mg (12.8mg/kg) to a 8-year old child (23.5kg) were 20.32μg/ml and 18.75 μg/ml, respectively.They declined to 0.78μg/ml and 0.88μg/ml respectively after 6hours and to undetectable levels after8hours.Half-life was1hour and 1.2 hours, respectively. CXD has shown the same concentration pattern as CEX, except for the fact that serum levels were peaked after 30 minutes and not detectable after 6 hours.
    2. Clinical responses:
    CXD was administered, for 7 days, to 33 children with scarlet fever in the dosage of _??_20-<60mg/kg/day (7childrenin _??_20-<30mg/kg/day, 21in _??_30-<40mg/kg/day and 5 in _??_40-<60mg/kg/day). Clinical responses were excellent in19cases and good in 14 cases, with an efficacy rate of 100%. All strains of group A Streptococcus is lated from the pharynx of 22 children were eradicated withln 24 hours. In 1 case each of acute pharyngitis, acute tonsillitis, acute laryngotracheitis and staphylococcal scalded skin syndrome, the dosage of _??_30-<45mg/kg/day produced a 100% good clinical response and eliminated the causative pathogens.
    3. side effect:
    Only 2 cases of eosinophilia were observed in hematologlc study as well as in hepatic and renal function tests before and after administration.
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  • TADAFUMI NISHIMURA, KAZUO TABUKI, KENJI HIROMATSU, TOSHLO TAKASHIMA, Y ...
    1981 Volume 34 Issue 12 Pages 1634-1646
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The authors have carried out the laboratory and clinical studies of cefroxadine (CXD), and obtained the fbllowing results.
    The antibacterial activities of CXD were measured by plate dilution method on 26clinical isolates of S. aureus, E.coliand K.pneumoniae.
    CXD inhibited the growth of all strains of S.aureus at concentrations less than 6.25 μg/ml, and the peak of activity distribution was obtained at 3.13μg/ml with an inoculum size of 106cells/ml. And the peak sensitivity distribution of, E.coli was obtained at 6.25μg/ml. The growth of all strains of K. pneumoniae was inhibited at concentrations of less than 25μg/ml.
    Phagocytosis was determined by QulE's method. In the presence of CXD, phagocytosis of human PMNs was not enhanced to E.coli and K. pneumoniae.
    For pharmacokinetic study, CXD was given orally at a single dose of 10mg/kg to 3 children befbre and after meals. The serum levels of CXD on fasting were 14.2μg/ml, 11.0μg/ml, 4.0μg/ml and 0.57 μg/ml at 0.5, 1, 2, 4 hours after administration respectively, and the level at6hours was not detectable. Half-1ife was 0.65hours.
    The serum levels of CXD after meals were 3.9μg/ml, 5.3μg/ml, 5.3μg/ml, 2.4μg/ml and 0.42 μg/ml at 0.5, 1, 2, 4, 6hours after administration respectively, but at 8 hours it was not detectable. Half-1ife was 0.95hours.
    The 8-hour urinary excretion rates on fasting and non fasting were 89.4%, 89.0% respectively.
    CXD was given to 31 cases with tonsillitis, 4 with bronchitis, 1with impetigo, 3 with cervicallymphadenitis, 7 with U. T. I, totalling 46. A daily dose of CXD 400-1, 500mg was given for 4-14 days.
    Clinical results obtained were good and excellent responses in 43/46 (93.5%) cases.
    No side effects were observed except for lcase with elevation of GOT, 2 cascs with elevation of GOT and GPT and 1case with eosinophilia.
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  • KAZUO NISHIKAWA, KOZABURO ASO, YUKINORI MIYACHI, AKIMASA OGAWA, MASAMI ...
    1981 Volume 34 Issue 12 Pages 1647-1654
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefroxadine (CXD) was applied to infectious diseases in children and the following results were obtained.
    1. Serum concentration and urinary excretion:
    CXD was given orally in dose of 10mg/kg in dry syrup from 30 minutes after meals. The peak serum concentration was at 1 hour after administration in 3 cases and at 2 hours in 1 case, and the average peak serum concentration was 16.41 & mu;g/ml in these 4 cases. The average urinary excretion rate of the antibiotic during 6 hours after administration was 93.9% in another 4cases.
    2. Antibacterial activity:
    The MIC of CXD against E. coli was slightly superior to that of CEX, butagainst S. aureus, S. epidermidis, str. pyogenes, str. faecalis, str. pneumoniae, Kleb. pneumoniae, Kleb. oxytoca, Pro. mirabilis, pro. yulgaris, H. influenzae, H. parainfluenzae, H. parahaemolyticus the MICs of CXD were almost equal to those of CEX.
    3. Clinical study:
    Thirty seven patients with bacterial infections (7 cases of urinary tract infection, 2 of cystitis, 10 of tonsillitis, 9 of scarlet fever, 7of bronchitis and 2 of bronchopneumonia) were orally treated with CXD dry syrup, 15-48mg/kg/day divided into 3 doses. The overall efficacy rate was 91.7%, and side efrects inclusive of abnormal laboratory findings were not observed.
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  • YOSHIAKI KAWAMURA, TOYOKI NOMURA, TOSHIAKI IHARA, SHIN SHIMIZU, HITOSH ...
    1981 Volume 34 Issue 12 Pages 1655-1662
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefroxadine (CGP-9000, CXD) is an orally active cephalosporin which has been newly developed by Ciba-Geigy.
    Its antibacterial activity against clinically isolated organisms, absorption and excretion after oral administration and clinical responses of patients with infections were studied. Its antibacterial activity against S. aureus and K. pneumoniae was comparable to that of CEX. Against E. coli, it showed slightly stronger activity than CEX.
    The serum concentrations of CXD was measured in 6 patients given orally 10mg/kg of it after meals. The peak mean serum level attained1hour after administration was 11.66mcg/ml.
    Forty-three children with various infections (upper respiratory infections, lower respiratory infections, urinary tract infections, etc.) were given 17-46mg/kg (average 28.7mg/kg) of CXD daily. The result was excellent in 26 cases, good in 12 cases, fair in 3 cases and poor in 2 cases, showing an effective rate of 88.4%.
    Side effect of transient leukopenia and elevation of S-GOT were noticed in 2 cases.
    However, there were no serious adversed reactions in our study. It is concluded that CXD might be effective in rather mild cases of respiratory or urinary tract infections.
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  • NAOICHI IWAI, AKIRA SASAKI, YOICHI TANEDA, KAZUYO INOKUMA, HARUHI NAKA ...
    1981 Volume 34 Issue 12 Pages 1663-1679
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Basic and clinical evaluations of a new oral cephalosporin cefroxadine (CXD) in pediatric fields were investigated, and the following results were obtained.
    1. MICs of CXD against various bacteria were compared with those of cephalexin (CEX).
    MIC peaks of CXD against clinically isolated S. aureus (22 strains), S. pyogenes (25), S. pneumoniae (8), H. influenzae (23), and E. coli (23) in pediatric fields, were 1.56, 0.2, 1.56, 25-50 and 6.25μg/ml, respectively in the inoculum size of 108 cells/ml, and they were 1.56, _??_0.1, 0.78, 25 and 6.25μg/ml respectively in the inoculum size of 106 cells/ml. In comparison with CEX, MIC peaks of CXD against S. aureus, S. pyogenes, H. influenzae and E. coli were almost the same with those of the former, it was, however, better by 1-2 tubes than that of CEX against S. pneumoniae.
    2. CXD in the form of dry syrup was administered orally at a dose of either 10 mg/kg or 20mg/kg to 5 children, and the serum levels and the urinary excreation were evaluated.
    In the case of 3 children who were administered a dose of 10 mg/kg the mean serum levels were 11.9μg/ml after 30 minutes, 13.7μg/ml after 1 hour, 4.7μg/ml after 2 hours, 0.7μg/ml after 4 hours, and 0.3μg/ml after 6 hours, while those 2 children who were administered a dose of 20 mg/kg, they were 15.1, 28.5, 12.5, 2.0 and 0.9μg/ml respectively. The mean periods of half-life in serum were 0.87 hour in the case of 10 mg/kg and 0.94 hour in the case of 20 mg/kg.
    The mean excretion rates were 83.8%in the case of 10mg/kg and 59.8% in the case of 20mg/kg.
    3. CXD dry syrup was administered to 31 children with various bacterial infections i. e. acute pharyngitis (15 cases), acute purulent tonsillitis (10 cases), acute bronchitis (4 cases) and 1 case each of acute pyelonephritis and acute purulent cervical lymphadenitis, and the clinical and bacteriological responses and side effect were investigated.
    The clinical response was either excellent or good in all of the cases. Out of the S. pyogenes (20 strains), S. aureus (1), S. pneumoniae (2), E. coli (1) and H. influenzae (1), bacteriological eradication was observed in all strains with the exception of 1 strain each in S. pyogenes and H. influenzae in which reduction was observed.
    No side effects and abnormal laboratory findings were observed.
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  • YUTAKA KOBAYASHI, TSUNEKAZU HARUTA, SHIGEKAZU KUROKI, KAN-ETSU OKURA, ...
    1981 Volume 34 Issue 12 Pages 1680-1690
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical efficacy of cefroxadine dry syrup, a new oral cephalosporin antibiotic, was evaluated in children, and the following results were obtained.
    1. Three children were given a single oral dose of about 10 mg/kg of the drug when fasting, and its blood concentrations were determined. Blood concentrations were maximum at 30-60 minutes, i.e., 16.9-18.2 μg/ml, and markedly low at 4 hours.
    2. Thirty-six patients with the following diseases were treated with 23.1-44.4 mg/kg/day of the drug in 3 to 4 divided doses; 21 patients with lacunar tonsillitis, 2 with tonsillitis, 1 with scarlet fever, 4 with bronchitis and tonsillitis, 2 with cystitis, 4 with pyelonephritis, 1 with impetigo and 1 with probable Mycoplasma pneumonia. An overall efficacy rate in 35 patients excluding the last mentioned case was 91.4%, i.e., excellent in 20, good in 12 and poor in 3, and an eradication rate of the causative organisms was 88.9%.
    3. Adverse reactions noted were diarrhea in 1 patient, eruption and diarrhea in 1, transient neutropenia in 1, eosinophilia in 3 and an elevation of GOT and GPT in 1. None were significant.
    4. Taste and flavor of the drug was considered to be well palatable to children.
    5. Taking into consideration of the results of fundamental evaluation of the drug, cefroxadine dry syrup is considered to be a potent new antibiotic in children, and the recommended dose will be 10mg/kg 3 to 4 times a day.
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  • TAKANORI SEKIGUCHI, TEIZO HOSODA, TAKAO ICHIOKA, MASUHIDE MIYAO, TAMIO ...
    1981 Volume 34 Issue 12 Pages 1691-1696
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In order to evaluate effectiveness of cefroxadine (CXD) in the treatment of bacterial infections of children, the clinical studies were carried out.
    CXD was orally administered to 30 patients at daily dose of 27.5-50.0mg/kg (average 32.3mg/kg) in 3-4 divided dose for 3-10 days (average 4.9 days).
    The overall efficacy rate in30cases was 93.3%, i.e., excellent in 22 (73.3%), good in 6 (20.0%), fair in 1 (3.3%) and poor in 1 case (3.3%).
    Drug eruption and transient eosinophilia were observed in 1 case each out of 30 cases (6.7%), but any other abnormality was not observed throughout this series.
    Based on the above results, CXD was thus considered to be a useful antibiotic in treatment of pediatric infections.
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  • SEIKYO FURUKAWA, TAKASHIGE OKADA, FUMIO HIRAO
    1981 Volume 34 Issue 12 Pages 1697-1702
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefroxadine dry syrup was studied clinically and the following results were obtained.
    The drug was administered to 19 cases of bacterial infections: acute tonsillitis (6), acute bronchitis (6), scarlet fever (2), acute pyelonephritis (4) and acute cystitis (1).
    The daily dose was about 30-50mg/kg except for 1 patient.The drug was given orally, 3 times a day and the duration of administration was from 4 to 11 days.
    The overall efficacy rate was 100%, i.e., excellent in 17 cases, good in 2 cases.
    One patient experienced a mild S-GOT elevation and another patient a mild vomiting.
    From the results obtained in this study, cefroxadine dry syrup seems to be useful in the treatment of infectious diseases of children.
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  • TAKASHI MOTOHIRO, YASUTAKA SAKATA, TAMOTSU FUJIMOTO, TOHRU NISHIYAMA, ...
    1981 Volume 34 Issue 12 Pages 1703-1731
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A study was made with the newly developed cefroxadine (CXD) dry syrup by measuring the serum level, urine excretion and recovery rate in10child ren who were orally administered 5, l0and 20mg/kg at 1hour after meals and the following results were gained. Also, its clinical efncacies and side efrects were investigated in the following cases who were treated with amean dose of 33mg/day divided into3to4portions for a period ofg days on the average; viz. a total of 151cases consiting of 9 cases of pharyngitis, 39of tonsillitis, 11of streptococcal infection, i.e. scarlet fever, 7 of bronchitis, 6 of pneumonia, 1of otitis media, 6 of purulent Iymphadenitis, 1of purulent parotitis, 1 of subcutaneous abscess and3of impetigo.
    1. The serum level tends to reach its maximum level within 1hour after administration. The mean concentrations of5, 10and20mg/kgdose in the foregoing time were6. 35, 9. 12 and 21. 62 mcg/ml respectively and dose response was observed. CXD showed higher concentration than CEX, CED and CFT. The mean half-1ife periods of the 3 dose were 72, 84 and 66 minutes respectively and variations were observed, but the drugs maintains a satisfactory serum level.
    2. The time which showed highest urine excretion was mainly in the 0to2hours bracket and th eaverage concentrations of5, 10and20mg/kg dose in the foregoing time were381. 2,771. 7 and 1,577. 7mcg/ml respectively. The dose response was more evident than in the serum concentrations. The average recovery rates within6hours were93. 6, 88. 3and94. 3%respectively and they were similar to those of CEX, CED and CFT.
    3. The clinical effects were evaluated were in148cases out of the total of151and136cases, or 91.9%showed good or excellent efficacy response.
    4. The daily dose groups of less than30mg/kg and31to40mg/kg formed the majority and there was no difference in the comparison of the clinical effectiveness in these2groups. Administration of a daily dose of20to40mg/kg is sufficient for the treatment of the aforementioned mild diseases except for pneumonia.
    5. The clinical effects were compared between the3and4times a day treatment groups, but there was no difference between these two groups with regard to the foregoing daily dose. The3times a day treatment is acceptable, but the4times a day treatment is preferable when pharmacokinetics is taken into account.
    6. The bacteriological effects in41cases, or97. 6%out of the42cases were above the efficacy base line and a high efficacy rate was achieved.
    7. With regard to side effects, diarrhea developed in4cases and eosinophilia in6cases, abnormal simultaneous increases in GOT and GPT in1case and1case each for abnormal values in LDH and BUN were seen in the clinical test values.
    The foregoing results show that CXD has high efficacy and safety and it can be said that it is adrug required in the pediatric field.
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  • TAKASHI MOTOHIRO, KOUICHI TANAKA, TATSUHIKO KOGA, YASUSHI SHIMADA, NAO ...
    1981 Volume 34 Issue 12 Pages 1732-1747
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    CXD was administered orally at an average dose of 28.6mg/kg (18.3-42.3mg/kg) for an average 6 days (3-12days) to a total of99pediatric cases with skin and soft tissue infections (impetigo 89, abscess7 and furuncle 3) ranging from 3 months to 9 years old. The drug was given twice to4times per day after meals.The clinical and bacteriological effects and adverse reactions of CXD as well asthe susceptibility of the causative organisms against CXD and CEX were studied, and the results obtained are as described below:
    1. According to judgement of the attending doctors, CXD had a high global efficacy rate of90.9%.
    2. Analysis of the attending physicians' evaluations of the clinical effects on impetigo revealed that a dose of CXD 20.5-30.4mg/kg t.i.d. can produce satisfactory responses.
    3. According to the assessments by Evaluation Committee, the global clinical effects after 3, 5 and 7 days were 81.4, 91.2 and 94.6%, respectively. This indicates that clinical responses increased with prolongation of the treatment period, viz. better responses obtained after 5 and 7 days. This suggests that a minimum of 5 days administration is required for treating these infections.
    4. As for impetigo having the largest number of patients in this study, a dose of CXD 20.5-30.4 mg/kg per day seemed to produce satisfactory clinical effects.
    5. As for dose per day, the t.i.d.regimen of CXD 20.5-30.4mg/kg seemed to exhibit satisfactory clinical responses, as already mentioned. Because of quite a small number of patients on the q i.d. egimen of higher doses, however, the question of whether the t.i.d. treatment with 20.5-30.4mg is adequate or not should be determined by a comparative study between the q.i.d. and t.i.d. treatments.
    6. As for bacteriological responses, a high global effect of 87.1% was obtained with CXD against S. aureus and S. pyogenes isolated from 74 and 1cases, respectively.
    7. As for impetigo with predominant number of cases, CXD was highly effective bacteriologically at a daily dose of 20.5-30.4mg/kg t.i.d. As an appropriate comparative evidence with the q.i.d. treatment was lacking, however, therapeutic validity of the t.i.d. treatment could not be determined definitely.
    8. Utility was evaluted by the attending physicians on the total 99 cases, and CXD showed as high as 88.9%.
    9. There were neither non-compliances nor adverse reactions to this treatment.
    10. CXD showed a distribution of antimicrobial activity similar to that of CEX, against 74 isolates of S. aureus with the MICs of CXD ranging from 1.56 to 25mcg/ml and those of CEX ranging from.78 to 25mcg/ml, with peak MIC being 3.13mcg/ml for both drugs. As for S. pyogenes, only one isolate from the same species, CXD was antimicrobial activity at 0.2mcg/ml and CEX was antimicrobial at 0.39mcg/ml.
    The above findings suggest that CXD is highly effective against acute skin and soft tissue infections in pediatrics.
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  • JIRO ARATA, YASUO YAMAMOTO, MASAHARU HAGIYAMA, NOZOMI NOHARA, MASAO SU ...
    1981 Volume 34 Issue 12 Pages 1748-1764
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    1. Cefroxadine dry syrup was in principle administered at the dosage of 10 mg per kilogram of body weight 3 times a day.
    2. Evaluation was done in 4 grades, i.e. excellent, good, fair and poor.
    3. According to subjective judgement by attending doctors, ‘excellent’ or ‘good’ was marked in 87.7% of total 163 cases. If impetigo cases (108) were picked out, ‘excellent’ or ‘good’ was recorded in 90.7%.
    4. If the evaluation was partially standardized, ‘excellent’ or ‘good’ was obtained in 74.8% of total 163 cases and in 78.7% of 108 impetigo cases.
    5. Side effects were observed in 3 cases (diarrhea 1, fever 2) No direct correlation of these complaints with the administration of the present drug was confirmed.
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  • 1981 Volume 34 Issue 12 Pages 1765-1769
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • 1981 Volume 34 Issue 12 Pages 1770-1774
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Download PDF (830K)
  • 1981 Volume 34 Issue 12 Pages 1775
    Published: December 25, 1981
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Download PDF (133K)
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