-
KUNIO INOUE, SUSUMU MITSUHASHI, MATSUHISA INOUE
1990 Volume 38 Issue Supplement1 Pages
1-11
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI) is a new oral cephalosporin ester of cefetamet (CEMT). The
in vitro and
in vivo antibacterial activity of CEMT-PI (CEMT), was investigated and compared with those of cefaclor (CCL), cephalexin (CEX) and ampicillin (ABPC). CEMT had a broad antibacterial spectrum and was more active than CCL, CEX and ABPC against
Enterobacter cloacae, Citrobacter freundii, Serratia marcescens and
Pseudomonas cepacia, which are insensitive to the three reference drugs. Moreover, it was far more active than these drugs against Streptococci,
Escherichia coli, Klebsiella, Proteus (indole+, -) and
Haemophilus influenzae. A time-kill study showed potent bactericidal activity of CEMT against
E. coli, Klebsiella pneumoniae and
Proteus vulgaris. CEMT was stable to various types of β-lactamase. The in vivo antibacterial activity of CEMT-PI against experimental infections in mice was more active than those of CCL, CEX and ABPC.
View full abstract
-
TAKESHI YOKOTA, EIKO SUZUKI, KYOKO ARAI
1990 Volume 38 Issue Supplement1 Pages
12-20
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI) is an oral cephem antibiotic of prodrug-type. We investigated the
in vitro activity of the active form, cefetamet (CEMT), its affinity to bacterial penicillin-binding proteins (PBPs), and synergy of bactericidal effect with serum complement or mouse cultured macrophages (Mφ). Minimal inhibitory concentrations of CEMT against 50% of 24-51 clinical isolates (MIC
50) of
Staphylococcus aureus, methicillin-resistant
S. aureus, coagulase-negative staphylococci,
Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Citrobacter freundii, Serratia marcescens, Pseudomonas cepacia, ampicillin-resistant
Haemophilus influenzae and
Bacteroides fragilis was 50, 100, 100, 0.25, 0.39, 0.2, 0.1, 0.2, 12.5, 0.39, 25, 0.78, 0.78, 0.2 and 25μg/ml, respectively. CEMT was inferior to other 3rd generation oral cephems in antistaphylococcal activity. The binding affinities of CEMT to the PBPs of
S. aureus was low, although they were as strong as those of cefixime against the PBPs of Gram-negative bacilli. CEMT was shown to manifest prominent synergy of bactericidal effect with serum complement and/or mouse cultured Mφ. Living cells of
E. coli NIHJ-JC 2 were well engulfed and easily digested by Mφ in the presence of higher than 1/8 MIC of CEMT.
View full abstract
-
SACHIKO GOTO, SHUICHI MIYAZAKI, AKIYOSHI TSUJI, YASUKO KANEKO
1990 Volume 38 Issue Supplement1 Pages
21-31
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied the
in vitro antibacterial activity of cefetamet (CEMT) and the
in vivo antibacterial activity of cetetamet pivoxil (CEMT-PI) and obtained the following results.
1) CEMT showed a broad antibacterial spectrum, and especially against
Streptococcus spp.,
Escherichia coli, Klebsiella spp.,
Proteus spp.,
Providencia spp.,
Haemophilus influenzae, Neisseria gonorrhoeae and
Pseudomonas cepacia, the drug was highy potent.
2) CEMT was stable to various types of β-lactamase.
3) In systemic infection, intra-nasal respiratory tract infection and urinary tract infection models in mice, the therapeutic effect of CEMT-PI was excellent.
View full abstract
-
KUNITOMO WATANABE, NAOKI KATOH, YOSHINORI MUTO, KAORI BANDOH, KAZUE UE ...
1990 Volume 38 Issue Supplement1 Pages
32-40
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet (CEMT), the active form of a newly developed cephalosporin, cefetamet pivoxil (CEMT-PI), was microbiologically evaluated using 304 strains including an array of obligate and some facultative anaerobic bacterial species, such as
Gardnerella vaginalis and
Capnocytophaga spp., and was compared with cefaclor (CCL) and cefixime (CFIX). Judging from the MICs obtained by agar dilution technique, CEMT was uniformly active against a wide range of anaerobic bacterial species, with MICs of 12.5μg/ml or less, except against six species,
Bacteroides fragilis, Bacteroides thetaiotaomicron, Eubacterium lentum, Clostridium poiringens, Clostridium septicum and
Clostridium difficile. The antibacterial spectrum of CEMT against anaerobic bacteria was similar to those of CCL and CFIX. CEMT was, however, as stable as CFIX and more so than CCL to β-lactamases from three representative strains of
B. fragilis GAI 0558, GAI 10150 and GAI7955. The activity of CEMT against 38 clinical isolates of
B. fragilis was comparable to that of CFIX and stronger than that of CCL. Against clinical isolates of
Peptostreptococcus magnus and
Peptostreptococcus asaccharolyticus it was stronger than those of either CFIX or CCL. The MICs of CEMT against
G. vaginalis and
Mobiluncus spp. were from 0.78-200μg/ml and 0.39-6.25μg/ml, respectively. The effect of CEMT-PI on the cecal flora of mice was also investigated. When mice were given 100 mg/kg of CEMT-PI for 5 days,
C. difficile was isolated from three of five cecal specimens at a concentration of 10
2-10
5 cfu/g.
View full abstract
-
TAKESHI NISHINO, KAZUO HATANO, EIJI IWAO, MASAKO OTSUKI
1990 Volume 38 Issue Supplement1 Pages
41-52
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We tested the
in vitro antibacterial activity of cefetamet (CEMT), the parent compound of cefetamet pivoxil (CEMT-PI), and the
in vivo therapeutic efficacy of CEMT-PI, a new orally active prodrug of CEMT, against experimental mouse infections and compared the results with those for amoxicillin (AMPC), cefaclor (CCL), cefuroxime (CXM), cefixime (CFIX) and cefpodoxime (CPDX).CEMT had a broad antibacterial spectrum against Gram-positive and-negative bacteria and its antibacterial activity against Gram-positive bacteria was almost equal to that of CFIX. CEMT had poor
in vitro activity against
Staphylococcus aureus, but good
in vitro activity against
Streptococcus spp. The antibacterial activity of CEMT against Gram-negative bacteria was similar to those of CFIX and CPDX and superior to those of AMPC, CCL and CXM. None of the antibiotics tested was active against
Pseudomonas aeruginosa. We got similar results in the sensitivity distribution of antibiotics to clinical isolates. CEMT showed dose-related bactericidal activity against all the bacteria tested. In a morphological investigation with
Serratia marcescens by phase-contrast microscope, CEMT induced the formation of filamentous cells at a concentration of 0.025μg/ml and spheroplast-like structures and lysis at a concentration above 0.78 μg/ml. Against intraperitoneal infections with
Streptococcus pyogenes in mice, the therapeutic efficacy of CEMT-PI was superior to that of CFIX and inferior to that of cefpodoxime proxetil (CPDX-PR), a prodrug of CPDX.On the other hand, the therapeutic efficacy of CEMT-PI against two strains of
Escherichia coli and
Klebsiella pneumoniae was almost equal to that of CFIX, inferior to that of CPDX-PR and superior to those of CCL and cefuroxime axetil (CXM-AX), a prodrug of CXM. In an experimental pulmonary infection with
K. pneumoniae in mice, CEMT-PI showed superior efficacy to CCL and CXM-AX.
View full abstract
-
YUZURU SEKINE, YURI SUDOH, CHIZUKO SAKURAI, MIKIO ARISAWA
1990 Volume 38 Issue Supplement1 Pages
53-61
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied the
in vitro antibacterial activity of cefetamet (CEMT), the active form of a new oral cephalosporin, cefetamet pivoxil (CEMT-PI), and compared it with those of cefixime (CFIX), cefteram (CFTM), cefaclor (CCL), cephalexin (CEX) and ampicillin (ABPC). CEMT had a broad spectrum and showed potent activity against Gram-positive and-negative bacteria except staphylococci,
Enterococcus faecalis, glucose non-fermentative bacteria and
Peptococcus variabilis. In comparison with the reference drugs, the antibacterial activity of CEMT was stronger than those of CCL and CEX against all species tested except staphylococci and Gram-positive anaerobes. As compared with CFIX or CFTM, the activity of CEMT against most species tested was similar to that of CFIX or CFTM. Like CFIX, the antibacterial activity of CEMT against some strains tested was affected by the pH of the medium and the inoculum size, but not by the kind of medium and the addition of serum. The effect of CEMT on the morphology of
Escherichia coli, Klebsiella pneumoniae and
Providencia rettgeri was studied by optical microscope. Filamentous cells were observed at lower concentrations, but at higher concentrations spheroplasts and lyzed cells were dominant in the population. The bactericidal activity of CEMT against Gram-positive and-negative bacteria was confirmed by comparing MICs and MBCs. The bactericidal activity was augmented by adding serum complement, showing synergy of bactericidal effect between 1/2 MIC of CEMT and complement.
View full abstract
-
MASANOBU MURAYAMA, MITSUYOSHI NAKAJIMA, TOSHIHIKO UEMATSU, ATSUHIRO MI ...
1990 Volume 38 Issue Supplement1 Pages
62-69
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
A phase I clinical study on cefetamet pivoxil (CEMT-PI) was conducted with 6 healthy male volunteers to evaluate its safety and pharmacokinetics. No abnormalities attributable to the drug were observed in subjective and objective symptoms, laboratory values and vital signs like ECG, blood pressure, pulse and respiratory rate after administration of 250mg and 500mg after a meal and 500mg in the fasting state. The plasma levels of cefetamet (CEMT) after a single dose of either 250mg or 500mg dose rapidly and peaked at 2.3h and 2.5h, with a C
max of 4.0μg/ml and 6.1μg/ml, the half-lives were 2.3h and 2.5h, the AUCs 18.9μg·h/ml and 33.1μg·h/ml and the 0-24h urinary recovery rates were 59.7% and 56.6%, respectively. The mean plasma level peaked at 2.1h with a C
max of 5.0μg/ml when 500mg of CEMT-PI was administered in the fasting state, and the half-life and AUC were 1.8h and 26.2μg·h/ml, respectively. The 0-24h urinary recovery rate was 38.5%. The plasma and urine levels of CEMT after a single dose of 500mg of CEMT-PI given after a meal were higher than in the fasting state, confirming that CEMT-PI is absorbed better when administered after meals.
View full abstract
-
MITSUYOSHI NAKASHIMA, TOSHIHIKO UEMATSU, MITSUTAKA KANAMARU, TAKAYUKI ...
1990 Volume 38 Issue Supplement1 Pages
70-81
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed a phase-1 study on cefetamet pivoxil, a new oral cephalosporin antibiotic, to evaluate its safety and pharmacokinetics in healthy adult male volunteers. A single-dose study of 1, 000mg after meals and a multiple-dose study at a daily dose of 1, 500mg (500mg t. i. d. 19 times over 7 days) were conducted. As to safety, soft stool was transiently observed in two volunteers in the multiple-dose study. No other subjective or objective symptoms, nor abnormalities in physical or laboratory tests attributable to the drug, were observed. In the single-dose study vesults were: T
max 3.58h, C
max 7.40μg/ml AUC 54.6μg·h/ml and T
1/2 2.09h. The urinary recovery amounted to 47.2% in the first 24h. No evidence of accumulation was observed after the multiple-dose study, since the pharmacokinetic parameters after the 19th dose were similar to those for the single-dose study of 500mg after a meal. The effects on intestinal bacterial flora were examined in the volunteers allocated to the multiple-dose study. The total count of anaerobes and some aerobes (for instance,
Escherichia coli, Klebsiella sp. and
Enterobacter cloacae) decreased, but the intestinal bacterial flora rapidly returned to the baseline after the final administration. From these results, we conclude that cefetamet pivoxil is well tolerated in humans and has a good pharmacokinetic profile suitable for a phase-2 clinical study.
View full abstract
-
AKIRA SAITO
1990 Volume 38 Issue Supplement1 Pages
82-88
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI), a new oral cephem antibiotics, is a prodrug of cefetamet (CEMT). We investigated the effect of food intake on the pharmacokinetics of CEMT-PI in six healthy male volunteers given 500mg CEMT-PI (equimolar to 388mg of CEMT). The pharmacokinetic parameters of CEMT-PI administered in the fasting state and after a meal to detect the serum concentration of CEMT by bioassay were: Cmax, 6.1μg/ml and 6.5μg/ml; Tmax, 2.2h and 2.8h; T
1/2, 1.8h and 1.9h; and AUC, 32.5μg·h/ml and 41.5μg·h/ml, respectively. The urinary recovery rate within 12h was 55.2% and 64.8%, respectively. These results indicate that food intake had a significant influence on the oral absorption of CEMT-PI.
View full abstract
-
TAKASHI INAMATSU, MAKIKO FUKAYAMA, TOSHIAKI NAKAJIMA, YOSHISHIGE MASUD ...
1990 Volume 38 Issue Supplement1 Pages
89-93
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated the pharmacoknetics of cefetamet pivoxil (CEMT-PI), a new oral cephem, in elderly patients with no apparent renal or hepatic deficiency. Four ambulatory patients (mean age 79.5 years, mean body weight 46.8kg), and 4 bedridden patients (mean age 83.5 years, mean body weight 37.5kg) received 500mg of CEMT-PI in the nonfasting state, and serum and urinary concentrations were determined. There was a marked delay in absorption in one patient with esophageal stenosis. Compared with 6 younger healthy volunteers, the increase and decrease in serum concentration were more delayed in the elderly patients. Urinay recovery was lower in the patients until 8 hours, but almost equal to that in the volunteers by 24 hours. These tendencies were more marked in the bedridden patients. Though there was a delay due to a protracted alimentary transfer time, absorption in the patients was good. Our data suggest that 1000mg cefetamet pivoxil b. i. d. is a recommendable dose for elderly patients.
View full abstract
-
TAKEFUMI MORIHANA, HIROYUKI NAITO
1990 Volume 38 Issue Supplement1 Pages
94-99
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated the distribution of cefetamet pivoxil (CEMT-PI) in rabbits and in humans.
1) In rabbits after oral administration of 20mg/kg, cefetamet (CEMT) was detected in blood, oral tissues (tongue, gingiva, parotid gland, submandibular gland, cervical lymphonodi, mandibular bone), liver and kidney by bioassay. When analysed pharmacokinetically, the Cmax and AUC were as follows: serum; 8.29μg/ml, 16.19μg·h/ml; tongue; 3.52μg/g, 8.80μg·h/g; gingiva; 4.84μg/g 12.54μg·h/g, parotid gland, 3.56μg/g, 6.94μg·h/g; submandibular gland, 3.76μg/g, 7.34μg·h/g; cervical lymphonodi, 3.86μg/g, 9.44μg·h/g, mandibular bone, 1.37μg/g, 4.03μg·h/g; liver, 4.70μg/g, 9.17μg·h/g; kidney, 22.42μg/g, 43.77μg·h/g.
2) In 11 healthy volunteers, the serum concentration of CEMT in a fasting state were compared with those after meal administration of 500mg by a crossover test. Cmax was 4.18±0.35μg/ml in fasting subjects and 5.68±0.60μg/ml after a meal. The Cmax after a meal administration exceeded to in fasting.
3) Blood concentration at the wound site after tooth extraction was measured in 158 patients given 500mg of CEMT-PI. 36.6 % of the cases showed levels over 3.13μg/ml which is MIC90 to clinical isolated oral strepococci, in 2-6h after administration.
View full abstract
-
AKIRA SAITO, MASUMI TOMISAWA, ICHIRO NAKAYAMA, KIYOSHI SATO
1990 Volume 38 Issue Supplement1 Pages
100-105
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We tested the susceptibility to cefetamet (CEMT), the active free acid of cefetamet pivoxil (CEMT-PI), a new oral cephem antibiotic, of 172 clinical isolates of 7 species using the plate dilution method with an inoculum size of 10
6cellsiml. CEMT showed a good antimicrobial activity against
Escherichia coli and
Klebsiella pneumoniae. The MIC
90 of CEMT was 3.13μg/ml against those bacteria. The MIC
50 of CEMT was 25μg/ml against
Staphylococcus aureus. The distribution of the MIC against
Morganella morganii,
Proteus mirabilis and
Serratia marcescens ranged broadly.
Pseudomonas aeruginosa was resistant to CEMT, The antimicrobial activity of CEMT was compared with that of three reference drugs, cefaclor (CCL), cefteram (CFTM) and cefixime (CFIX); it was equal to that of CCL and CFIX and superior to CFTM against
S. aureus, and almost equal to CFIX and CFTM and superior to CCL against Gram-negative bacteria. Twenty-four patients with various infections (6 with acute bronchitis, 1 with chronic bronchitis, 4 with tonsillitis, 1 with pharyngitis and 12 with cystitis) were treated with CEMT-PI at an oral dose of 250-500mg twice daily for 1-12 days. Clinical efficacy was excellent in 11 patients, good in 12 and unevaluable in 1. The total efficacy rate was 100%. As causal bacteria, 21 strains of 7 different species were clinically isolated from 19 patients. All were eradicated after treatment with CEMT-PI. As adverse reactions, epigastralgia were observed in one case and stomach discomfort and anorexia in one case. No abnormal laboratory findings were noted.
View full abstract
-
SEIICHI AONUMA, KOTARO OIZUMI, AKIRA WATANABE, YOSHIHIRO HONDA, YUTAKA ...
1990 Volume 38 Issue Supplement1 Pages
106-109
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We examined the
in vitro antimicrobial activity of cefetamet (CEMT), a metabolite of the orally absorbed cefetamet pivoxil (CEMT-PI), a newly developed cephem antibiotic, by the broth dilution methed using the MIC-2000 system. Minimum inhibitory concentrations (MICs) of CEMT against 120 clinical isolates were compared with those of cefixime (CFIX) and cefaclor (CCL). Against
Staphylococcus aureus, CEMT was less active than CFIX and CCL, but against
Escherichia coli, Klebsiella pneumoniae and
Serratia marcescens it was much more active than CCL, though less active than CFIX. Against
Enterobacter cloacae it was as active as CFIX. Eight patients suffering from respiratory tract infections were given 500mg or 1, 000mg of CEMT-PI orally once a day for 3-8 days. Clinical response was good in seven and fair in one patient Wooziness was observed in one patient.
View full abstract
-
MASAKI YOSHIDA, ATSUSHI SAITO, JINGORO SHIMADA, KOHYA SHIBA, MASANOBU ...
1990 Volume 38 Issue Supplement1 Pages
110-115
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil (CEMT-PI), a new oral cephalosporin, for its antibacterial activity
in vitro and its clinical availability. The results obtained were as follows.
1) In a comparative study, we determined serum and urinary levels of cefetamet (CEMT), cefixime (CFIX) and concomitant therapy with probenecid in 6 healthy adult volunteers by cross-overmethod. In the comparison of CEMT with CFIX, results showed a shorter half-life in the blood (T
1/2), namely, 1.9h, a higher maximum blood concentration (Cmax) 3.0μg/ml, a shorter time until Cmax (Tmax) 3.0h and the area under the blood concentration curve (AUC) was 20.5μgμ·h/ml. Tmax was longer, Cmax was higher and T
1/2 was prolonged by concomitant therapy with probenecid. CEMT had a urinary excretion rate of 57.8±2.0% after 24 hrs, which was higher than that of CFIX, and delayed urinary excretion was observed when concomitant therapy with probenecid was given.
2) Three patients with respiratory tract infection and 4 with urinary tract infection were treated orally at a daily dose of 250-1, 000mg CEMT-PI for 2-16 days. Results were excellent in 1, good in 3, fair in 1 and unknown in 2 cases. No side effects were found. In laboratory values, elevated transaminase values were observed in a case of chronic hepatitis after administration but its relationship with the drug was unknown.
View full abstract
-
KAORU SHIMADA, KYOKO URAYAMA, YASUYUKI SANO, YASUFUMI MIYAMOTO, TAKASH ...
1990 Volume 38 Issue Supplement1 Pages
116-120
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI), a new oral cephem, was administered to 19 patients. The clinical efficacy rate in respiratory tract infections was 16/17 (94.1%), with the following breakdown: acute pharyngitis; 1/1, bacterial pneumonia; 1/1, acute bronchitis; 2/2, chronic bronchitis; 9/10 (90%), bronchiectasis; 3/3. In urinary tract infections, 2/2 patients responded satisfactorily. Eradication of causative pathogens was observed in 4 of 9 bacteriologically documented respiratory tract infections and in 1 of 2 urinary tract infections. The clinical efficacy rate according to dose in respiratory tract infections was: at 250 mg b. i. d.; 5/6, 250 mg t. i. d.; 1/1 and at 500mg b. i. d. it was 10/10. Adverse reactions were mild abdominal discomfort and moderate diarrhoea in one patient each.
View full abstract
-
YOSHIO KOBAYASHI, HIROSHI UCHIDA, TETSUHEI OGAWA, SONJI YANO
1990 Volume 38 Issue Supplement1 Pages
121-125
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
The antibacterial activity of cefetamet (CEMT), a newly developed cephem antibiotic, was superior to that of cefixime (CFIX) and of cefaclor (CCL) against
Streptococcus pyogenes, and superior to that of CCL against
Streptococcus agalactiae, Escherichia coli and
Klebsiella pneumoniae. It was, however, inferior to that of CFIX against these strains. Of 14 patients, 9 with acute pharyngitis, 2 with acute bronchitis, 1 with lymphadenitis, 1 with pneumonia and 1 with acute cystitis, were successfully treated with oral administration of cefetamet pivoxil (CEMT-PI), a prodrug of CEMT. No side effects were detected.
View full abstract
-
FUMIO MATSUMOTO, IWAO SAKURAI, TAKEO IMAI, TOSHIO HOJO, TAKAYUKI TAKAH ...
1990 Volume 38 Issue Supplement1 Pages
126-132
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied the antibacterial activity, absorption, excretion and clinical efficacy of cefetamet pivoxil (CEMT-PI), a new oral cephalosporin, and obtained the following results.
1) Antibacterial activity: the antibacterial activity of cefetamet (CEMT) against 25 clinical isolates each of 5 organisms was investigated. CEMT had broad-spectrum activity against Grampositive and-negative organisms, and the MIC
80-90s against
Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Klebsiella pneumoniae, and
Proteus mirabilis, were > 100, ≤0.1, 0.78, 0.2 and 0.2μg/ml, respectively.
2) Absorption and excretion: CEMT-PI was administered at 500mg to two elderly patients withapparent renal dysfunction. The peak plasma concentration was 5.41μg/ml, the plasma half-life was 3.90h, and the 10-h urinary recovery rate was 16.4-29.7%.
3) Clinical evaluation: CEMT-PI was administered to 14 patients with respiratory tract infections and 5 with urinary tract infections in daily doses of 500-1000mg after meals in two divided doses. The clinical response was good in 16 cases, poor in 1 and unknown in 2 cases. As to side effects, dizziness and eruption developed in one patient each, but these subsided the day after withdrawal of CEMT-PI. No abnormal laboratory findings were noted in any of the cases.
View full abstract
-
NOBUKI AOKI, YOSHIMARU USUDA, YUTAKA KODA, OSAMU SEKINE, NOBUTO WAKABA ...
1990 Volume 38 Issue Supplement1 Pages
133-142
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied a new oral cephem, cefetamet pivoxil (CEMT-PI), and obtained the following results.
1) Serum and urine levels of cefetamet (CEMT) were determined after oral administration of CEMT-PI 250mg to 7 patients with various degrees of renal function. In the patients with severely impaired renal function, serum concentration decreased more slowly than in those with moderately impaired renal function, and high serum levels were maintained over a long period. Urinary excretion of CEMT diminished in relation to the degree of renal failure.
2) CEMT-PI was used to treat 23 patients with respiratory tract infections. Clinical response was good in 20, fair in 1 and poor in 2 patients. Laboratory tests revealed neutropenia in one case, although this finding was alleviated rapidly following cessation of the therapy.
View full abstract
-
YOSHIMITSU HAYASHI, MASAHITO KATO, TORU MATSUURA, TOSHIHIKO TAKEUCHI, ...
1990 Volume 38 Issue Supplement1 Pages
143-148
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We carried out bacteriological and clinical studies of cefetamet pivoxil (CEMT-PI)
1) Antibacterial activity. The MIC of cefetamet (CEMT) against clinical isolates were measured and compared with those of cefixime (CFIX). The MIC of CEMT was equal to that of CFIX against
Escherichia coli, inferior to that of CFIX against
Staphylococcus aureus and
Klebsiella pneumoniae by one or two steps,
Serratia marcescens by three or four steps,
Proteus vulgaris by about four steps, and
Morganella morganii and
Proteus mirabilis by four or five steps, but the MIC distribution ranged broadly. Neither CEMT nor CFIX were active against
Pseudomonas aeruginosa.
2) Clinical study. CEMT-PI was used in the treatment of 15 patients: 1 with acute bronchitis, 6 with acute exacerbation of chronic respiratory tract infections and 8 with pneumonia. The patients, aged 33-78 years, were given a daily does of 0.75-1.0g for 3-18 days. Clinical efficacy was excellent in 2, good in 9, fair in 1 and poor in 3. The efficacy rate was 73.3%. Bacteriologically, 2 strains of
Haemophilus influenzae were eradicated, 1 of
Streptococcus pneumoniae decreased and one each of
P. aeruginosa decreased and persisted. No adverse effects were observed. As clinical abnormalities, elevated GOT, GPT and eosinophilia were observed in one case each. These normalized after the end of medication. One positive result in an indirect Coombs' test during the treatment was considered to be related to the drug.
View full abstract
-
NIRO OKIMOTO, RINZO SOEJIMA, YOSHIHITO NIKI, JIRO HINO, MASARU SUMI, Y ...
1990 Volume 38 Issue Supplement1 Pages
149-153
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed bacteriological and clinical studies on cefetamet pivoxil (CEMT-PI), a new oral cephem antibiotic, in respiratory tract infections and obtained the following results.
1) The MICs of cefetamet (CEMT) against
Escherichia coli, Klebsiella sp.,
Enterobacter cloacae, Serratia marcescens, Proteus mirabilis and
Proteus vulgaris were 0.025-3.13μg/ml, which were superior to those of cefaclor. They were, however, weak against
Staphylococcus aureus and
Pseudomonas aeruginosa.
2) Seventeen patients with respiratory infection were treated with CEMT-PI. The overall efficacy rate was 58.8%(excellent 1, good 9, fair 4, poor 3). One patient experienced nausea. No remarkable abnormal laboratory findings were observed in any of the patients after treatment.
View full abstract
-
OSAMU KURIMURA, HIDEO SASAKI, HIROFUMI FUKUHARA, TETSUZO KOUDA, KIMITO ...
1990 Volume 38 Issue Supplement1 Pages
154-162
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We carried out bacteriological studies on cefetamet (CEMT) and clinical studies on cefetamet pivoxil (CEMT-PI) against respiratory tract infections. The MICs of CEMT against 445 clinicallyisolated strains of 30 species were measured and compared with those of cephalexin (CEX), cefteram (CFTM), cefixime (CFIX), cefazolin (CEZ) and cefotaxime (CTX). Gram-positive cocci: The MICs of CEMT against
Staphylococcus sp. were higher than those of the reference drugs, and against
Streptococcus sp. its MICs were also higher with the exception of CEX. Gram-negative rods: CEMT showed potent antimicrobial activity against strains subject to
Enterobacteriaceae except for
Morganella morganii and
Proteus vulgaris.
Against Haemophilus influenzae the peak MIC of CEMT was only 0.2μg/ml, but CFTM, CFIX and CTX proved even more effective. Against
Pseudomonas cepacia CEMT was the most potent of the drugs tested, with a peak MIC of 3.13μg/ml. CEMT and the reference drugs were scarcely active against
Acinetobacter calcoaceticus, Flavobacterium sp.,
Pseudomonas aeruginosa and Xanthomonasmaltophilia. Six cases of pneumonia, 3 of chronic bronchitis and 2 of acute upper respiratory tract infection were treated with CEMT-PI at a dose of 250-500mg b. i. d for 7-14 days. The clinical response was excellent in 1 case of acute upper respiratory tract infection and good in 4 cases of pneumonia, 2 of chronic bronchitis and 1 of acute upper respiratory tract infection. One of two isolated strains of
S. pneumoniae, and one of
H. influenzae were eradicated. As to adverse reactions, elevated GOT, GPT and γ-GTP values were observed in one case.
View full abstract
-
YOSHIRO SAWAE, KAORU OKADA, YUKIO KUMAGAI, TOSHIYUKI ISHIMARU, KOJI TA ...
1990 Volume 38 Issue Supplement1 Pages
163-169
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed basic and clinical studies on cefetamet pivoxil (CEMT-PI), a new oral cephalosporin antibiotic, with the following results.
1) Antimicrobial activity
The MICs of cefetamet (CEMT), the active substance of CEMT-PI, against various clinical isolates were determined with an inoculum size of 10
6cells/ml. The MIC
50 was 50, μg/ml for
Staphylococcus aureus, >100
for Enterococcus faecalis, 0.78 for
Escherichia coli, 0.39 for
Klebsiella pneumoniae, 6.25 for
Enterobacter cloacae, 0.78 for
Enterobacter aerogenes, 1.56 for
Serratia marcescens, 0.20 for
Proteus mirabilis, 1.56 for
Proteus vulgaris, 3.13 for
Citrobacter spp. and >100 for
Pseudomonas aeruginosa. Its activity against Gram-negative rods except
P. aeruginosa was much more potent than those of cephalexin and cefaclor, but a little less so than those of cefixime and cefteram.
2) Clinical efficacy
Four patients with pneumonia, 3 with bronchitis, 3 with tonsillitis, 3 with pharyngitis, 1 with gingival abscess, and 1 with cystitis were treated with CEMT-PI at a daily dose of 0.5-1.0g for 3-26 days. Clinical response was excellent in 4, good in 6, fair in 1, poor in 2 and unknown in 2 patients. The clinical efficacy rate was 76.9%. Five out of 9 cases which causative strains were isolated were eradicated by CEMT-PI. Heartburn, epigastralgia and abdominal fullness were observed in 3 patients. Eosinophilia was observed in 2 patients and elevated GOT, GPT, AL-P and γ-GTP in one patient.
View full abstract
-
AKIRA YASUOKA
1990 Volume 38 Issue Supplement1 Pages
170-178
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil (CEMT-PI), a new oral cephem, basically and clinically with the following results.
1. Antimicrobial activity: the
in vitro antimicrobial activity of cefetamet (CEMT) was tested by the MIC-2000 system.The minimum inhibitory concentrations (MICs) of CEMT against 567 clinical strains isolated from the respiratory tract were compared with those of cephalexin (CEX), cefixime (CFIX), cefteram (CFTM) and amoxicillin (AMPC). CEMT had no activity against
Staphylococcus aureus, but showed the same or lower MICs against
Streptococcus spp.than the compared drugs did.Against Gram-negative bacilli, except
Pseudomonas, CEMT showed the same antimicrobial activity as CFTM and CFIX.
2. Serum and sputum levels of CEMT: the maximum concentrations of CEMT after a single oral administration of 500mg in 2 patients with chronic respiratory infection were 6.67μg/ml and 9.31μg/ml in serum, and 0.29μg/ml and 0.62μg/ml in sputum.
3. Clinical results: 15 patients of respiratory tract infections (chronic bronchitis 1, diffuse panbronchiolitis 3, bronchiectasis 2, infectious bulla 1, pneumonia 7, and acute tonsillitis 1) were administered CEMT-PI.The overall efficacy rate was 73.3%. Three adverse reactions (one of oral dryness and two of skin eruption) and two abnormal laboratory findings (eosinophilia and GPT elevation) were observed.
View full abstract
-
HIROFUMI TANAKA, KEIZO MATSUMOTO, MISAO TAO, KIWAO WATANABE
1990 Volume 38 Issue Supplement1 Pages
179-184
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed basic and clinical studies on cefetamet pivoxil (CEMT-PI) to evaluate its usefulness in respiratory tract infections. Minimal inhibitory concentrations (MICs) of cefetamet (CEMT) and other antibiotics against pathogenic
Streptococcus pneumoniae, Haemophilus influenzae, Branhamella catarrhalis, Staphylococcus aureus and
Pseudomonas aeruginosa were determined. The MIC
90 of CEMT against 50 strains of
S. pneumoniae was 0.78μg/ml, against 43 strains of
H. influenzae 0.39μg/ml, and against 49 strains of
B. catarrhalis 1.56μg/ml, but the MIC
50 values against 47 strains of
S. aureus and 42 of
P. aeruginosa were above 100μg/ml. In one patient given, 500mg concentrations of CEMT in serum and sputum were measured. The peak serum level was 3.68μg/ml, but the drug was not detectable in sputum. Thirteen patients with respiratory infection (chronic bronchitis 12, pneumonia 1) were treated with CEMT PI in a daily dose of 1, 000mg. Clinical efficacy was assessed in 10 of the 13 patients (76.9%), and 12 of 14 causative organisms (3/4 S.
pneumoniae, 7/7
H. influenzae, 2/2
B. catarrhalis, 0/1
P. aeruginosa) were eradicated.
View full abstract
-
JUN GOTO, MASUMI IKUTA, HIDEAKI SHIGENO, TAKAYOSHI TASHIRO, MASARU NAS ...
1990 Volume 38 Issue Supplement1 Pages
185-192
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We evaluated cefetamet pivoxil (CEMT-PI), a newly developed cephem antibiotic of the ester type, for its antimicrobial activity
in vitro and for its serum and sputum levels and clinical efficacy in patients with respiratory infections. The results were as follows.
1) Antimicrobial activity: the MICs of cefetamet (CEMT) against 918 strains (26 organisms) isolated from clinical specimens were measured and compared with those of cefaclor (CCL), cefixime (CFIX) and cefteram (CFTM). Against Gram-positive cocci, CEMT showed similar or slightly lower activity than other competitive antibiotics. Against Gram-negative rods, it showed almost the same activity as did CFIX and CFTM against intestinal bacteria, and superior activity to other competitive antibiotics against a glucose non-fermenting Gram-negative rod,
Pseudomonas cepacia.
2) Serum and sputum levels: the time course of changes in serum and sputum levels of CEMT were measured in two patients with chronic bronchitis and one with bronchiectasis after a single oral administration of 500mg of CEMT-PI. The maximum serum levels were 5.4-6.2μg/ml at 2-3h after administration, and even at 8h they were 2.1-2.6μg/ml. The maximum sputum levels were 0.36-0.68, μg/ml at 4 7h after administration. The rate of the maximum sputum to the maximum serum level was 5.9-10.8%.
3) Clinical efficacy in respiratory infections.: we administered 500mg or 1000mg/day b.i.d. for 7-1 0 days to 9 patients: 2 with acute bronchitis, 1 with diffuse panbronchiolitis, and 6 with chronic bronchitis. The clinical response was excellent in 1, good in 4, fair in 3 and poor in 1.patient.No adverse reactions or abnormal laboratory findings were observed.
View full abstract
-
YUEI IRABU, HIROSHI FUKUHARA, HIROAKI NAKAMURA, HIROSHI KANESHIMA, KAT ...
1990 Volume 38 Issue Supplement1 Pages
193-197
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed basic and clinical studies on cefetamet pivoxil (CEMT-PI), a new oral cephalosporin, with the following results.
1) Antimicrobial activity: the minimum inhibitory concentrations (MICs) of cefetamet (CEMT) against 338 clinically isolated strains were determined and compared with those of cefteram, cefixime, cefa. clor, cefotiam, ampicillin, using a Dynatech MIC-2000 system. CEMT had wide-spectrum antimicrobial activity against these isolated strains, except
Pseudomonas aeruginosa, methicillin sensitive
Staphylococcus aureus and methicillin resistant
S. aureus.
2) Clinical efficacy: CEMT-PI at 500 or 1, 000mg/day was given to 2 patients with bacterial pneumonia, 2 with bacterial pneumonia complicated with chronic bronchitis, 5 with chronic bronchitis and 1 with diffuse panbronchiolitis for 4-14 days. Clinical response was excellent in 2 patients, good in 6, fair in 1 and poor in 1, and the overall clinical efficacy was 80%.
3) Bacteriological efficacy: one strain of Haemophilus influenzae was eradicated, one strain of
Klebsiella pneumoniae changed to
Proteus vulgaris, and one strain of
Streptococcus pneumoniae persisted.
4) Safety: no side effects and altered laboratory findings were observed.
View full abstract
-
FUMIO MATSUMOTO
1990 Volume 38 Issue Supplement1 Pages
198-209
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed a dose-finding study on cefetamet pivoxil (CEMT-PI), a new oral cephem, in the treatment of acute exacerbation of chronic bronchitis, by a multicenter well-controlled comparative study. CEMT-PI was orally administered at 500 mg b. i. d., 750mg t. i. d. or 1, 000mg b. i. d. The clinical efficacy rate assessed by committee was 61.8%(21/34) in the 500mg group, 67.6%(23/34) in the 750mg group and 72.7%(24/33) in the 1, 000mg group. There were no significant differences among the three groups. The bacteriological eradication rate was 81.3%(%) in the 500mg group, 78.6%(11/14) in the 750mg group and 66.7%(8/12) in the 1, 000mg group. There were no significant differences among the three groups. Except for the cases infected with
Staphylococcus aureus and
Pseudomonas aeruginosa, bacteriological eradication was 11/13 in the 500mg group, 10/12 in the 750mg group and.7/8 in the 1, 000mg group. There were no significant differences among the three groups. The incidence of side effects was 11.1%(4/36) in the 500mg group, 2.8%(1/36) in the 750mg group and 2.7%(1/37) in the 1, 000mg group. There were no significant differences among the three groups. We conclude from our results that 1, 000mg b. i. d. is the optimal dose of CEMT-PI in the treatment of acute exacerbation of chronic bronchitis.
View full abstract
-
YASUHIRO YAMAGUCHI, YOSHIAKI KUMAMOTO, TAKAOKI HIROSE, NAOTO MIKUMA
1990 Volume 38 Issue Supplement1 Pages
210-221
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We carried out basic and clinical studies on cefetamet pivoxil (CEMT-PI), a new oral cephem antibiotic.
1) Antibacterial activity: The MIC
90 of cefetamet (CEMT) against clinical isolates of
Escherichia coli, Klebsiella pneumoniae and
Proteus mirabilis-0.78μg/ml, 0.2μg/ml and 0.2μg/ml, respectively-were almost equal to those of cefixime and cefteram and superior to those of cefaclor, cefuroxime and ampicillin.
2) Clinical efficacy: Of 29 patients with urinary tract infections, 8 with acute uncomplicated cystitis (AUC) were given CEMT-PI orally at 250mg once or twice daily for 7 days, and 21 with chronic complicated urinary tract infections (UTI) at 500mg twice daily for 10 days. Twenty-four patients (6 with AUC and 18 with complicated UTI) were evaluated by the criteria of Japanese UTI Committee (3 rd ed.) On day 3, overall clinical efficacy was excellent in all 6 evaluable cases of AUC. On day 5, in the 18 evaluable cases of complicated UTI, it was excellent in 10, good in 7 and poor in 1, with an overall efficacy of 94.4%. Bacteriologically, all 6 strains clinically isolated from the 6 cases of AUC were eradicated; 20 of 24 (83.3%) strains from the 18 cases of complicated UTI were eradicated, and 11 new strains appeared in 8 cases of complicated UTI after 5 days' treatment.
3) Side effects: As side effects, stomach discomfort, headache and vomiting were observed in one case each. As abnormal laboratory findings, slight elevation of GPT and slight decrease in WBC were found in one case, and a slight elevation of GOT, GPT in two cases.
View full abstract
-
HIROKAZU GOTO, SHOICHI ONODERA, HIROSHI KIYOTA, GEN KAWAHARA, KATSUHIS ...
1990 Volume 38 Issue Supplement1 Pages
222-227
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied the antibacterial activity and clinical efficacy of cefetamet pivoxil (CEMT-PI), a new oral cephalosporin.
1) Antibacterial activity: the in vitro activity of cefetamet (CEMT) was tested against Clinical isolates of
Enterococcus faecalis, Klebsiella pneumoniae, Escherichia coli, Serratia marcescens and
Pseudomonas aeruginosa and compared with that of cefpodoxime, cefteram and cefaclor. Against
E. coli and
K. pneumoniae, the MICs of CEMT were 0.1->200μg/ml, it's MIC
50's being 0.39 μg/ml and 0.2μg/ml respectively. But its activity againt
E. faecalis, S. marcescens and
P. aeruginosa was poor.
2) Clinical efficacy: the clinical efficacy of CEMT-PI was found to be excellent in 4 cases and moderate in 5 of acute uncomplicated cystitis. In 3 patients with complicated urinary tract infection, efficacy was excellent in one case, moderate in one and poor in one. The bacteriological efficacy rate was 92.3%. Laboratory abnormalities were shown in one case, namely elevation of GOT and GPT.
View full abstract
-
MINORU KANEMATSU, MASAYOSHI YAMAHA, KENICHI OGUCHI, HARU KATOH, HIDEJI ...
1990 Volume 38 Issue Supplement1 Pages
228-239
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI) is a new orally absorbed pro-drug of cefetamet (CEMT). We basically studied the antimicrobial activity of CEMT and used CEMT-PI to treat patients with uncomplicated and complicated urinary tract infections (UTIs) with the following results.
1) The antimicrobial activity of CEMT was excellent against Gram negative bacilli but less effective against Gram positive cocci than that of cefaclor or ampicillin.
2) Thirteen patients with acute uncomplicated UTIs and forty-two patients with chronic complicated UTIs were treated with CEMT-PI at a daily dose of 500, 750 or 1, 000mg for 3, 4, 5 or 7days, and the therapeutic results were evaluated in accordance with the criteria proposed by the Japanese UTI Committee. In acute uncomplicated cystitis the overall efficacy rate was 100%, while in chronic complicated UTI, it was 58%. In the latter cases,
Pseudomonas aeruginosa was detected in nine patients and
Citrobacter freundii in three, and these organisms persisted after treatment. Slight elevations of serum transaminase and serum bilirubin were noted in three patients during treatment.
View full abstract
-
ZHAO-REN KO, MASAYUKI KUWAYAMA, MASUO YAMASHITA, SOICHI ARAKAWA, OSAMU ...
1990 Volume 38 Issue Supplement1 Pages
240-249
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We basically and clinically evaluated cefetamet pivoxil, a new oral cephalosporin, in the urological field.
1) The
in vitro antimicrobial activity of cefetamet (CEMT) was compared with those of cefaclor (CCL), cefteram (CFTM) and cefixime (CFIX) against 2 Gram-positive cocci and 8 Gram-negative bacilli of a total 357 clinical isolates.Its activity against
Proteus mirabilis and
Klebsiella pneumoniae was similar to that of CFTM but slightly inferior to that of CFIX. It showed no activity against
Enterococcus faecalis and
Pseudomonas aeruginosa.
2) The diffusion of CEMT into the prostatic fluid (PF) was studied in six healthy male volunteers by means of expressed prostatic secretion 2, 3 and 4 hours after oral administration of 0.5g in a single dose. The drug concentrations in PF were<0.1-3.9μg/ml, <0.1-0.67μg/ml, <0.1-0.88μg/ml, respectively, and the PF serum ratio ranged from 0.06 to 0.07.
3) The clinical efficacy in 50 patients with various types of genito-urinary tract infection was evaluated by oral administration of 0.25g or 0.5g two times daily for 3-14 days. The 50 cases comprised 21 cases of with acute uncomplicated cystitis (AUC), 1 of acute epididymitis and 28 of complicated urinary tract infection (UTI). According to the criteria of the Japanese UTI Committee, the overall clinical efficacy rate was 100%(10/10) in AUC and 67%(12/18) in complicated UTI. The bacteriological eradication rate was 100%(10/10) in AUC and 81%(17/21) in complicated UTI. The side effect was stomach discomfort in one patient, and slight elevation of GOT and GPT in one patient.
View full abstract
-
MASANOBU TANIMURA, SHINICHI KATAOKA, KEIJI INOUE, YUKITOSHI FUJITA
1990 Volume 38 Issue Supplement1 Pages
250-258
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil (CEMT-PI), a new oral antimicrobial agent, for its antibacterial activity, absorption and excretion, clinical efficacy and side effects.
1) The antibacterial activity of cefetamet (CEMT) against
Escherichia coli, Serratia marcescens, Klebsiella pneurnoniae, Proteus mirabilis and
Proteus vulgaris was clearly superior to that of cefaclor but slightly inferior to that of cefixime.
2) CEMT-PI (500mg) was administered to three healthy volunteers. Serum levels reached a maximum of 5.82±1.40μg/ml at 2h fasting and 7.77±1.28μg/ml at 2h after a meal. The urinary recovery rates within 8h were 44.43±9.06% fasting and 70.25±2.32% after a meal.
3) Nine patients with acute simple cystitis and 7 with complicated urinary tract infection were treated with CEMT-PI. All 5 cases with acute cystitis and 4 in 5 cases with complicated urinary tract infection were effective by the criteria of the Japanese UTI Committee.
4) Side effects were observed in only two cases: one of redness and edema of the feet and another of fever with slight increase in transaminase.
View full abstract
-
TETSURO MATSUMOTO
1990 Volume 38 Issue Supplement1 Pages
259-268
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI), a novel oral prodrug of cephalosporin type, was administered to 87 patients with uncomplicated or complicated urinary tract infection (UTI) and the following results were obtained.
1) After 2 days' treatment, of 8 patients with acute uncomplicated cystitis, excellent response was observed in 6 and moderate in 2, and after 5 days' treatment, excellent in 3, moderate in 2 and poor in one case.
2) In one case of acute uncomplicated pyelonephritis, moderate response was observed.
3) In complicated UTI cases without indwelling catheter, excellent response was observed in 12, moderate in 12 and poor in 19. The overall efficacy rate in complicated UTI was 56%. Bacteriologically, 45% of gram positive cocci were eliminated from urine after 5 days' treatment and 72% of gram negative rods. But 4 patients with indwelling catheter showed poor results.
4) Side effects were observed in 3 cases, namely, sleepiness, chill and abdominal fulness. There were six instances of abnormal laboratory findings related to liver function and blood cell counts.
View full abstract
-
SHINICHI MAKINOSE, TAKESHI SHIMADA, MOTOSHI KAWAHARA, KAZUYA KAWAHARA, ...
1990 Volume 38 Issue Supplement1 Pages
269-277
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI), a new oral cephem, has been developed at Nippon Roche K.K. We investigated the antimicrobial activity and clinical efficacy of the drug in urinary tract infections (UTIs). The antimicrobial activity of cefetamet (CEMT) against 295 strains isolated from patients with UTIs were measured by the agar dilution method with an inoculum size of 106 cfu/ml, and compared with that of cefaclor (CCL). Bacterial strains consisted of 30 strains each of
Staphylococcus spp.,
Enterococcus faecalis, Escherichia coli, Citrobacter freundii, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Proteus vulgaris and
Pseudomonas aeruginosa and 25 strains of
Proteus mirabilis. The antibacterial activity of CEMT against these bacteria was definitely superior to that of CCL. CEMT-PI was given to 17 patients with acute uncomplicated cystitis at daily doses of 250mg for 3-7 days, and to 25 with complicated UTI at 250-500mg for 3-14 days. According to the criteria proposed by the UTI Committee in Japan, the clinical efficacy in 8 cases of acute uncomplicated cystitis was excellent in all of the cases. The clinical response in 14 cases of complicated UTI was excellent in 6, moderate in 3 and poor in 5 cases, with an overall efficacy rate of 64%. As to side effects, stomach discomfort, abdominal pain with constipation and skin itch were noticed in one case each. Abnormal laboratory findings induced by the drug were observed in two cases of elevated bilirubin and GOT.
View full abstract
-
MASAHIKO ABE, KAZUO SENGOKU, TETSUYA SHIMIZU, TENSHU HASEGAWA, HIROMIT ...
1990 Volume 38 Issue Supplement1 Pages
278-283
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil (CEMT-PI), a new cephalosporin, for its clinical efficacy and transfer into serum and tissues, and obtained the following results.
1) After oral administration of 500mg CEMT-PI, the serum concentration in the uterine artery was almost equal to that in the cubital vein, showing good transfer of the drug. Favorable results were also obtained for concentrations in all adnexal tissues studied.
2) The clinical response in 16 patients with gynecological infections was: excellent 2, good 12, and poor 2, the efficacy rate being 87.5%.
3) As to side effects, diarrhoea was observed in only one patient, who also had elevated GOT, GPT and LDH. But these side effects recovered without treatment. This drug showed excellent efficacy and high safety in the treatment of gynecological infections.
View full abstract
-
NANKUN CHO, KANGO FUKUNAGA, KATSUAKI KUNII
1990 Volume 38 Issue Supplement1 Pages
284-294
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated a newly developed oral cephem antibiotic agent, cefetamet pivoxil (CEMT-PI), for its tissue penetration and clinical efficacy in obstetric and gynecological infections, and obtained the following results.
1) Tissue penetration: tissue penetration of the drug into the intrapelvic genital organs was good. The peak serum level in uterine arterial blood was 2.42μg/ml after oral administration of 250mg and 5.16μg/ml after 500mg, The peak tissue levels were 0.66-15μg/g after 250mg and 1.47-3.35μg/g after 500mg.
2) Clinical results: CEMT-PI was given to 64 patients with obstetric and gynecological infections or UTI at a daily dose of 500mg or 1000mg. Clinical efficacy was 92.2% and bacteriological response 87.3%. Few side effects were observed.
From these findings, we consider CEMT-PI to be an effective antibacterial agent in obstetric and gynecological infections.
View full abstract
-
KUNIHIKO ITO, TERUHIKO TAMAYA, TOSHIYA ITO, YOSHITAKA YAMADA, TOYOHIRO ...
1990 Volume 38 Issue Supplement1 Pages
295-303
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated cefetamet pivoxil (CEMT-PI), a new oral cephalosporin antibiotic, for its tissue penetration and clinical efficacy in various obstetric and gynecological infections, and obtained the following results. After a 500 mg single oral administration, the peak serum concentrations in the antecubital vein and uterine artery were both about 5μg/ml, while genital tissue concentrations were more than 3μg/g. CEMT-PI was given orally to 35 patients with obstetric and gynecological infection, at a daily dose of 500mg or 1, 000mg b. i. d. for 3-10 days. Clinical efficacy was excellent in 1, good in 31, poor in 1 and unknown in 2, with overall clinical efficacy was 97.0%. Bacteriologically, 18 organisms (of 11 species) were isolated from 18 patients, and 17 (94.4%) of these were eradicated. Side effects, sleepiness was observed in one case. But there were no clinical abnormalities.
View full abstract
-
ISSEI NAKAYAMA, EMIKO YAMAJI, HIROSHI KAWAMURA, HIROSHI KAWAGUCHI, YOZ ...
1990 Volume 38 Issue Supplement1 Pages
304-313
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil (CEMT-PI), a new oral cephalosporin antibiotic, for its clinical efficacy and safety in skin and soft-tissue infections. CEMT-PI was administered at 500-1000 mg twice a day for 3-10 days to 81 cases with periproctal abscess, subcutaneous abscess, infected atheroma, furuncle, wound infection, phlegmon, felon, lymphangitis, etc. Clinical efficacy judged by physicians in charge was: excellent 11, good 52, fair 13, and poor 5, out of the 81 cases, the efficacy rate being 77.8%. On the other hand, clinical efficacy according to the standard criteria excellent 23, good 44, fair 2, poor 8, and unknown 4 cases. The efficacy rate was 87.0%. In bacteriological evaluation, the eradication rate in 49 cases of monomicrobial infection was 75.5%, and in 23 cases of polymicrobial infection, 78.3%. When CEMT-PI was administered to 4 cases who had previously failed to respond to other antibiotic treatment, clinical efficacy was good 3 cases. There were no adverse reactions among the 81 cases but abnormal laboratory findings was noted in one case. Against 97 clinically isolated strains of 33 species, the MICs of cefetamet (CEMT) determined, those for 46 (47.2%) of the 97 strains being 3.13μg/ml or less.
View full abstract
-
KEN MORIMOTO, HIROAKI KINOSHITA, SHUICHI NAKATANI, KATSUJI SAKAI, MIKI ...
1990 Volume 38 Issue Supplement1 Pages
314-321
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We clinically investigated a new oral cephalosporin, cefetamet pivoxil, with the following results.
1) Thirty-three patients with surgical infections were enrolled in this study, and 31 were eligible for evaluation.
2) Of the 31 assessable patients, clinical response was excellent in 13, good in 8, fair in 6 and poor in 4 cases, and the efficacy rate was 67.7%.
3) This drug is best prescribed against infections caused by Gram-negative aerobic rods, not by Gram-positive cocci.
4) The recommended dose is 1, 000mg daily.
View full abstract
-
SHINJI KATO, SATOAKI HOJO, TAKEHIRO KOBAYASHI, SHUNKICHI BABA, TAKESHI ...
1990 Volume 38 Issue Supplement1 Pages
322-330
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
From our laboratory and clinical studies on cefetamet pivoxil (CEMT-PI) the following results were obtained.
1) Antibacterial activity: the MIC level was greater than 12.5, ugiml against 14 strains of
Staphylococcus aureus. The peak MIC were at 0.1μg/ml against 13 strains of
Proteus mirabilis and greater than 100 geml against 16 strains of
Pseudomonas aeruginosa.
2) Tissue concentration: palatine tonsil and serum levels were 1.09-2.76 μg/g, 5.09-6.25μg/ml at 3°16'-4°00' after 500mg p.o. fasting. The rate of tissue/serum was 19.9-45.5%. The mucosal levels of maxillary sinus and serum levels were 1.13-2.76 μg and 1.46-4.69μg/ml at 2°46'-4°38' after 500mg p.o. fasting. The rate of tissue/serum was 48.1-106.9%. Otorrhea and serum levels were <0.2-1.46μg/ml and 1.96-7.82μg/ml at 1°15'-4°00' after 500mg p.o. non-fasting. The rate of otorrhea/serum was 10.0-37.5%. Palatine tonsil and serum levels were 0.75μg/g and 1.96 μg/ml at 2°43' after 250mg p.o. fasting. The rate of tissue/serum was 38.3%.
3) Clinical results: CEMT-PI was used clinically in 56 cases of various infections in otorhinolaryngological infection. The clinical result was excellent in 20, good in 24, fair in 6, poor in 4 cases and unknown in 2 cases. The efficacy rate was 81.5%.
4) Adverse reaction: no adverse reactions were observed.
View full abstract
-
JIRO SASAKI, TAKEFUMI MORIHANA, AKIHIRO KANEKO, JUN GOTO, MASATAKA UEM ...
1990 Volume 38 Issue Supplement1 Pages
331-339
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI) was administered at 250 mg b. i. d. or 500 mg b. i. d. to 97 patients with acute odontogenic infections and evaluated in 92 cases. The clinical efficacy rate, evaluated by the point method of the Japanese Society of Oral and Maxillofacial Surgeons, was 89.1%, and evaluated by the doctor in charge was 83.7%. Sixty-one strains were isolated from closed abscesses in 39 of 92 caces. Against 38 strains of aerobes and 23 strains of anaerobes, the antibacterial activity of cefetamet (CEMT) was compared with those of cefaclor (CCL), cefixime (CFIX), cefteram (CFTM) and ampicillin (ABPC). The MIC
50 and MIC
90 against oral streptococci were as follows, CEMT 0.39 μg/ml, 3.13μg/ml, CFIX 0.39μg/ml, 6.25μg/ml, CFTM 0.05μg/ml, 0.39μg/ml, CCL 0.78μg/ml, 1.56μg/ml, ABPC 0.025μg/ml, 0.05 μg/ml. No side effects were observed, but in the laboratory investigation, slightly elevated GPT was noted in one patient.
View full abstract
-
KAZUO SHIIKI, HIDEYUKI HARA, KAZUYUKI KANNO
1990 Volume 38 Issue Supplement1 Pages
340-343
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated the effect of food intake on the pharmacokinetics of cefetamet pivoxil (CEMT-PI) from the serum concentration in 5 healthy male volunteers given 250 mg of CEMT-PI in a fasting state and after a meal. Serum concentrations were determined by HPLC and bioassay. The results are summerized as follows;
These results show that food intake had no significant influence on the absorption of CEMT-PI
View full abstract
-
MITSUHIDE OHMICHI, YOHMEI HIRAGA, YASUSHI ITOH
1990 Volume 38 Issue Supplement1 Pages
344-346
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
Cefetamet pivoxil (CEMT-PI), a new oral cephem antibiotic, was given to 7 patients with respiratory tract infections in a daily dose of 500 mg, to evaluate its clinical efficacy, safety and usefulness. Of 7 patients (1 with acute bronchitis and 6 with chronic bronchitis), clinical efficacy was good in 5 patients (1 with acute bronchitis and 4 with chronic bronchitis) and fair in 1 patient with chronic bronchitis. No adverse events or abnormal laboratory findings were noted. These results indicate that CEMT-PI is a reliable antibiotic agent with interesting features.
View full abstract
-
KAZUO TAKEBE, MITSUO MASUDA, SEIICHI MURAKAMI, MORIO SAGARA, KATSUHIRO ...
1990 Volume 38 Issue Supplement1 Pages
347-349
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We evaluated the clinical efficacy and safety of cefetamet pivoxil (CEMT-PI), a new oral cephalosporin antibiotic, at a dose of 250-500 mg twice a day for 3-12 days in 13 patients with respiratory tract infections. The overall clinical efficacy was 83.3%(10/12). Eruption in one and slight increase of GPT in two cases were observed.
View full abstract
-
FUMITOSHI YAMAUCHI, NORIMI MAIYA, KAZUKI KONISHI, MASAO TAMURA, TAKASH ...
1990 Volume 38 Issue Supplement1 Pages
350-353
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated the clinical efficacy of cefetamet pivoxil (CEMT-PI), a new oral cephalosporin, in 13 patients with respiratory tract infections. CEMT-PI was given in a daily dose of 500mg, or 1, 000mg in 2 divided doses, for 7-15 days. Clinical efficacy was excellent in 7, good in 5 and fair in 1 patient. Slight elevations of GPT or GOT-EGPT were observed in 3 patients during the treatment, but no side effects were noted.
View full abstract
-
IZUMI HAYASHI, KIKUO ONUMA, MIKI HASUIKE
1990 Volume 38 Issue Supplement1 Pages
354-357
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We performed a clinical evaluation of cefetamet pivoxil (CEMT-PI) in eight patients with respiratory tract infection. CEMT-PI was given orally in a dose of 500mg or 1, 000mg in two divided portions for 4-9 days. Two strains of
Staphylococcus aureus, two of
Streptococcus pneumoniae and one of
Haemophilus influenzae were isolated from sputum before administration. One strain each of
S. aureus, S. pneumoniae and
H. influenzae were eradicated. The clinical efficacy was evaluated as excellent in two cases, good in five, and poor in one case. There were no side effects or laboratory findings after the therapy. From the above results, we conclude that CEMT-PI is an effective, safe and useful new oral cephem in respiratory tract infections.
View full abstract
-
JUNICHI KATAHIRA, KOHSUKE HARUKI, YUSUKE SHIBATA, KEN KIKUCHI, HIROMI ...
1990 Volume 38 Issue Supplement1 Pages
358-360
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We investigated cefetamet pivoxil (CEMT-PI) by orally administering the drug to 16 patients with various respiratory tract infections. Clinical efficacy was excellent or good in 6 of 7 cases of both chronic bronchitis and acute bronchitis, poor in one case of bronchiectasis, and good in one case of pneumonia. Bacteriologically, the drug showed bactericidal activity in 4 of 8 pathogen-identified cases. Diarrhea, as a side effect, was observed in one case. In laboratory data, slight elevation of Al-P was noted in 2 cases.
View full abstract
-
TOSHIAKI HAGA, NORIO NOZUE, MASUMI BABA, ATSUKO GUUJI, YASUO ONO, HAJI ...
1990 Volume 38 Issue Supplement1 Pages
361-363
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We evaluated cefetamet pivoxil (CEMT-PI), a new oral cephalosporin, for its clinical efficacy and safety in 8 patients with respiratory tract infections (acute bronchitis 2, pneumonia 4, pulmonary abscess 1 and mycoplasmal pneumonia 1). CEMT-PI was administered orally at a daily dose of 1, 000 mg in two divided doses for 6-13 days. The overall efficacy was excellent in 2, and good in 5 patients. As to side effects, eruption with pruritus developed in one patient and vomiting with stomach discomfort in another. In laboratory findings, an elevation of eosinophils was noted in two patients.
View full abstract
-
HIROAKI TAKEDA, HIROSHI OSHITANI, HIDEHIRO WATANABE, HIROYUKI KOBAYASH ...
1990 Volume 38 Issue Supplement1 Pages
364-365
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied cefetamet pivoxil, a new cephalosporin, to determine its clinical efficacy and safety at a dose of 250-500 mg twice a day in 4 patients with respiratory tract infections. Clinical response was good in 3 and fair in one patient. The only side effect was transient constipation in one patient.
View full abstract
-
MASAYUKI NOGUCHI, EIYASU TSUBOI, AKIHIKO YAMAGUCHI, KOUJI NARUI, TATSU ...
1990 Volume 38 Issue Supplement1 Pages
366-370
Published: November 30, 1990
Released on J-STAGE: August 04, 2011
JOURNAL
FREE ACCESS
We studied the clinical effects and adverse effects of cefetamet pivoxil (CEMT-PI), a new cephem antibiotic, in 11 patients with acute exacerbation of chronic respiratory tract infections. The efficacy rate was 36.4%. As to adverse effects, only 1 patient had mild anorexia during the treatment. One case showed transient and slight abnormality in the liver function test. Though its efficacy rate was not so high, cefetamet (CEMT) is stable to β-lactamases, which are thought to characterize the major pathogens involved in acute exacerbation of chronic respiratory diseases, abd hence maybe efficacious in these kinds of complaint.
View full abstract