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Volume 23 (1970)
- Issue 5-6 Pages 451-
- Issue 4 Pages 353-
- Issue 3 Pages 217-
- Issue 2 Pages 99-
- Issue 1 Pages 1-
Predecessor
Volume 23, Issue 1
Displaying 1-12 of 12 articles from this issue
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KIYOSHI KONNO, KOTARO OIZUMI, IZUMI HAYASHI1970 Volume 23 Issue 1 Pages 1-25
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS -
KANJI SEIKA, MASAAKI KANEO, JIRO OKUMURA1970 Volume 23 Issue 1 Pages 26-29
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
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KANJI TSUCHIYA, TOKIKO OISHI, CHIKA IWAGISHI1970 Volume 23 Issue 1 Pages 30-36
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAC-PC, 6-(1-aminocyclohexanecarboxamido) penicillanic acid, exhibits antibacterial activity in vitro against Gram-positive and Gram-negative bacteria. Minimal inhibitory concentrations against Gram-positive bacteria range from 0.195 to 3.125mcg/ml and against Gram-negative bateria range from 12.5 to 100mcg/ml. Mild penicillin G resistant staphylococci are inhibited in the range of 3.125-50mcg/ml. The antibacterial activity of this penicillin is not greatly influenced by the pH of medium, the inoculum size and presence of horse serum. Susceptibility to AC-PC decreases rapidly in vitro by serial transfer, but resistant degree in terms of concentration become stationary after the 6 th passages through the 15th. AC-PC demonstrates bactericidal and bacteriolytic actions against Staph. aureus and E. coli. The solution of AC-PC at pH 2 is stable at 37°C at least for a period of 5 hours.View full abstractDownload PDF (1012K) -
TOSHIYUKI YAMAZAKI, KANJI TSUCHIYA1970 Volume 23 Issue 1 Pages 37-41
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe therapeutic effectiveness of AC-PC, 6-(1-aminocyclohexanecarboxamide) penicillanic acid, in CF-1/H mice intraperitoneally challenged by penicillin G sensitive as well as resistant strains of Staph. aureus, Strept. pyogenes, E. coli, Pr. vulgaris and K. pneumoniae is determined by single oral, subcutaneous, intravenous or intraperitoneal administration of the antibiotic, immediately after the challenge. The effective dose (ED50) is calculated on the basis of numbers of deaths for 7 days. AC-PC is very effective against Gram-positive bacterial infection. The antibiotic is also effective against Gram-negative bacterial infection.View full abstractDownload PDF (849K) -
KEIMEI MASHIMO, YASUMICHI KATO, AKIRA SAITO, YOSHITAKA MATSUMOTO, TAKA ...1970 Volume 23 Issue 1 Pages 42-47
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe results of our studies on aminocyclohexylpenicillin (AC-PC) are summarized as follows:
1. The antimicrobial activity against Staphylococcus aureus, Escherichia coli and Pseudotnonas tested by plate-dilution method was poor.
2. The protein binding was very low by cellophane bag dialysis.
3. Urinary and biliary excretions were studied following intravenous administration in a dog. The half-life was 1.05 hour, Cr and Cb 38.4 and 0.37 ml/min, Kr and Kb 0.55 and 0.005, respectively.
4. The tissue distribution was studied following oral administration in rats. The concentrations in the kidneys and the liver were three or four times higher than those in plasma and lungs. The concentrations in the spleen and muscle were low.
5. The mean peak level of serum was 18.7mcg/ml one hour after 500mg oral administration in adults, and the mean urinary recovery was 50.3% of the dose in 6 hours.
6. The immunological cross-reactivity was found by agar diffusion (OUCHTERLONY'S method) and quantitative precipitin reaction.
7. Twenty two cases of infectious diseases were treated with oral administration of 1-1.5g daily. Sixteen cases were cured. The gastrointestinal disturbance was observed in 4 cases.View full abstractDownload PDF (793K) -
YASUSHI UEDA, FUMIO MATSUMOTO, NOBORU NAKAMURA, ATSUSHI SAITO, KAZUO N ...1970 Volume 23 Issue 1 Pages 48-52
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThis paper describes some experimental results of cyclacillin (aminocyclohexyl penicillin) as to its sensitivity, absorption, excretion, organ distribution, nephrotoxicity and clinical data.
(1) Sensitivity: The sensitivity of this drug to coagulase-positive Staphylococci was distributed in the range of 0.8 to 100mcg/ml which was not significantly different from that of ampicillin. The sensitivity of E. coli was found to be 50 mcg/ml or above.
(2) Blood level: With oral administration of cyclacillin at a dose of 500mg to normal subjects, its blood concentration reached the maximum of 11.0mcg/ml after an hour and decreased to trace level after 6 hours. The half life was found to be 0.78 hours. In chronic renal failure higher blood concentration was apt to be maintained for a longer period of time as compared with the normal cases.
(3) Urinary excretion: The urinary concentration of cyclacillin was remarkably high with a recovery rate of 48% at 6 hours.
(4) The mechanism of renal excretion: The possible mechanism of renal excretion was evaluated by the stop flow method. The result disclosed that the drug was filtered through glomerular apparatus and excreted at both proximal and distal tubules.
(5) Tissue concentration: The study of tissue assy in rats revealed that the highest activity of cyclacillin was obtained in the kidneys followed by the order of serum, liver, lungs, and spleen.
(6) Nephrotoxicity: The nephrotoxicity of cyclacillin was evaluated in rats with oral administration of the drug with doses of 200mg/kg and 400mg/kg daily for 21 days. No significant side effects were noted as to urinary protein, osmolarity, BUN, serum creatinine and renal histology.
(7) Clinical data: Cyclacillin was administered into 10 cases with urinary tract infections. In 8 of cases the drug was proved to be effective. No noticeable side effects were observed in the study.View full abstractDownload PDF (680K) -
FUMIO MIKI, TOMOTSUGU HIGASHI, TAKASHI IWASAKI, MITSURU AKAO, TATSUO O ...1970 Volume 23 Issue 1 Pages 53-59
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSLaboratory and clinical investigations were made on aminocyclohexyl-penicillin (AC-PC), and the following results were obtained.
1. The antibacterial activity of AC-PC against Staphylococcus aureus, growth of which were inhibited by 0.78 to 25 mcg/ml of AC-PC, was far inferior to that of isoxazolylpenicillins, while it is superior over aminobenzyl-penicillin (AB-PC).In vitro activity of this penicillin against E. coli, showing MIC of 100mcg/ml or more, was much weake rthan that of AB-PC. As in the case of AB-PC, all the strains of Klebsiella pneumoniae was resistant to more than 100mcg/ml of AC-PC.
2. The maximum serum levels of 10.45mcg/ml and 10.2mcg/ml in an average were obtained 30-60 minutes after a single oral administration of 500mg and 250mg of AC-PC, respectively, and the level goes down rapidly thereafter, being trace amount 4 hours after the administration. About 55% of the administered dose in an average were recovered in urine over a six-hour period.
3. Of 18 infectious diseases, treated with oral administration of AC-PC, ten excellent and five good amelioration were obtained. while the rest of three was not improved. No side effects were observed, except that there were two cases who complained of mild gastro-intestinal disturbances.View full abstractDownload PDF (3479K) -
HIROSHI OKUBO, YASUO FUJIMOTO, YURUKO OKAMOTO, JIRO TSUKADA, JUNKO MAK ...1970 Volume 23 Issue 1 Pages 60-68
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSStudies have been made on the absorption, excretion and distribution of aminocyclohexyl penicillin (AC-PC) in the human and animal body, as well as on its anti-bacterial activity. Some clinical trialshave also been made.
(1) The blood level of AC-PC reached its peak (14.4mcg/ml on average) 30minutes after singleoral dose of 500mg in adult humans. The peak level of AC-PC was much higher and came earlierthan that of aminobenzyl penicillin (AB-PC)(5.2mcg/ml on average; 2 hours after administration).
(2) Percent recovery of AC-PC from urine in human adults was larger than that of AB-PC;i. e. 71% of AC-PC and 42% of AB-PC in 6 hours on average.
(3) AC-PC was excreted into bire in a lower concentration than AC-PC or carbenicillin. Percent recoveryof AC-PC from bile was similar to that of PC-G.
(4) Concentration of AC-PC in organs of rats after oral administration was found to be several times higher than that of AB-PC. The order of organs according to their concentration of AC-PC was kidney>liver>lung>spleen>blood (brain, muscle≅0), while that of AB-PC was liver>kidney>lung>blood>spleen (brain, muscle≅0).
(5) Forty-nine strains of Staphylococcus aureus isolated from patients were tested for their sensitivityto AC-PC. The MIC of AC-PC was generally higher than that of AB-PC; while MIC of some strainswere lower than those of PC-G.
All of 24 strains of Eschericia coli isolated from patients were resistant against AC-PC (>100mcg/ml); while the MIC of AB-PC was lower than 25 mcg/ml in 14 strains.
(6) Thirteen patients with various infections (1 acute bronchitis, 2 chronic bronchitis, 3 cholecystitis, 1 cystits, 5 pyelonephritis, and 1 salpingitis) have been treated with AC-PC. The daily dose was 1.5g orally in most cases. The total dosages varied from 6 to 94g (21g on average). Twelve patients out of the thirteen showed fair response to the therapy.View full abstractDownload PDF (1141K) -
TADAFUMI NISHIMURA, YASUSHI KOTANI, YASUNORI ASATANI1970 Volume 23 Issue 1 Pages 69-75
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe fundamental and clinical studies, in the pediatric field, of a broad spectrum semi-synthetic penicillin, aminocyclohexyl penicillin (AC-PC), have been conducted.
(1)In vitro antibacterial activities: The sensitivity of coagulase-positive Staph. aureus isolated from clinical materials was distributed widely, giving a peak at 12.5mcg/ml of AC-PC. In comparison with aminobenzyl penicillin (AB-PC), the in vitro activity of AC-PC against penicillin G-resistant Staph. aureuswas superior to AB-PC, while against the sensitive strains their relation was reversed. Against E. coli and Proteus vulgaris AC-PC exhibited growth inhibition, but was inferior to AB-PC.
(2) Absorption and excretion: The maximum serum levels, when AC-PC was orally given in asingle of 500 or 250mg, reached 9.1 and 4.3mcg/ml in average, respectively. In the fasted subject the peak level was attained at an hour after administration, while it tended to lag somewhat when antibiotic was given after meal. The antibiotic was excreted rapidly, and therefore, persistance in blood was considerably of short duration and it was not detected at six hours after the administration, during which 80% of AC-PC was recovered in urine.
(3) Clinical effects: Of the total of 33 patients (acute tonsillitis 8, acute pharyngitis 4, acute bronchitis 3, acute dyspepsia 9, acute enteritis 6, acute cystitis 2 and pyelonephritis 1), 5 cases showed excellent results, 20 cases good and 8 cases poor. From the results, AC-PC may be more effective against respiratory diseases than the intestinal. As for the dosage in children 50-100mg/kg/day of AC-PC is recommendable.View full abstractDownload PDF (977K) -
SHUNJI ISHIYAMA, TAKASHI SAKABE, MASAKAZU FURUHASHI, UICHI TAKAHASHI, ...1970 Volume 23 Issue 1 Pages 76-81
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSSome experiments on aminocyclohexyl-penicillin (AC-PC) were undertaken with the purpose of its clinical evaluation in the field of surgery, and the following results were obtained.
1)In vitro activity of AC-PC, antibacterial spectrum of which being similar with ampicillin (AB-PC), was weak and inferior to AB-PC.
2) The cross resistance with AB-PC and PC-G was proved to exist.
3) In the sensitivity distribution of Staphylococcus aureus isolated from infectious lesions, high resistant strains against AC-PC were somewhat less than against AB-PC and PC-G. According to the inactivation test by penicillinase, the stability of AC-PC to such enzyme, however, was only comparable with that of phenoxyethyl-penicillin, being stronger than AB-PC but weaker than PC-G. Such being the case, it is doubtful if this synthetic penicillin is of value as penicillinase resistant one.
4) Effective serum and urine concentrations of AC-PC, when it was administered orally in 500 mg as single dose, persisted four and six hours, respectively.
5) Though the excretion was mainly taken place renally, it also migrated into bile, concentration of which reaching 4 to 7 times higher than that of serum, and consequently its good distribution into organs such as kidneys and liver was observed.
6) Of twenty-two cases of minor surgical infection, to which AC-PC was given, 77 % was successfully treated.
7) Side effects complained of and noticed were mild and transient.View full abstractDownload PDF (809K) -
KIYOHITO SHIBATA, TAKEMI KATO, MICHITERU FUJII, YASUO OKUDA1970 Volume 23 Issue 1 Pages 82-86
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. The antibacterial activity of AC-PC against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Proteus vulgaris, isolated from surgical infectious lesions at our department, were as follows:
Eighty percent of staphylococcal strains tested was sensitive to the concentration of 1.6-50mcg/ml. The minmium inhibitory concentration for E. coli and Kl. pneumoniae was 100mcg/ml or higher in the case of Proteus vulgaris, 40% of the strains was sensitive to 12.5 mcg/ml and 20% was inhibited at 25-50 mcg/ml, while the rest showed resistance to 100mcg/ml of AC-PC.
2. The serum levels of AC-PC after a single oral dose of 250 mg exhibited peak, 15.94 mcg/ml in average, after 1 hour. The antibiotic was scarcely detected at 6 hours, during which 40.30% of the administered dosis recovered in urine.
3. Pus levels of AC-PC in abscess induced in animals reached their peak, being 13-15% of the serum level, appearing later than those in serum and persisting longer than the serum. Similar tendency was observed in clinical trials, but peak level of the drug in pus reached as high as 1/2 of serum level and persisted longer.
4. AC-PC was found effective in 19 of 23 cases of surgical infection and ineffective in three, uncertain in one, taht is 86. 4% of effective rate. As to the side effect, single case of nausea, diarrhea and skin rash, which disappeared upon discontinuation of the administration, were noted.
5. AC-PC, being inferior to AB-PC in in vitro antibacterial activity, gives high serum as well as urine concentrations and considerably high persistent pus levels and is regarded as the effective agent in the treatment of stphylococcal as well as gram-negative bacilli infection.View full abstractDownload PDF (694K) -
SHINICHI FUZITA, JIRO ARATA, NOBUYUKI TOKUMARU, KAORU MIYOSHI, HAJIME ...1970 Volume 23 Issue 1 Pages 87-89
Published: February 25, 1970
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSLaboratory and clinical studies were conducted on a new semi-synthetic penicillin, aminocyclohexyl penicillin (Cyclacillin ‘Takeda’), and the followings were observed.
1. Serum levels after the oral administration of 500mg to 3 healthy volunteers were studied. Peak concentration, 9.5mcg/ml in average, were obtained at 30 minutes to 1 hour after the administration.
2. The sensitivity of 31 strains of coagulase-positive staphylococci to aminocyclohexyl penicillin was studied with plate dilution method. The distribution of minimum inhibitory concentration was as follows: 16% at 0.8 mcg/ml, 6% at 1.56mcg/ml, 3% at 3.13 mcg/ml, 32% at 6.25mcg/ml, 23% at 12.5mcg/ml and 19% at 25mcg/ml. Thus, 58% was inhibited by the concentration lower than attainable peak blood level. No complete cross resistance with ampicillin was observed.
3. The clinical effect of the antibiotic was examined in 7 cases, and good effect was obtained in 4. Four staphylococci isolated from the patients showed resistance to ampicillin.
4. No remarkable side effects were seen except headache in a case, but it is uncertain that the complaint was due to the drug.View full abstractDownload PDF (427K)
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