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Volume 38, Issue 12
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IPPEI FUJIMORI1985 Volume 38 Issue 12 Pages 3437-3448
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS -
AKIHISA YOSHIMI, KEN-ICHI NISHIMURA, MASARU KITAGAWA, MEIKO KITAGAWA, ...1985 Volume 38 Issue 12 Pages 3449-3457
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSCeftizoxime suppository (CZX-S) was administered rectally to mice, rats and dogs, and the pharmacokinetics were studied in comparison with those after intravenous, intramuscular and subcutaneous administration of ceftizoxime (CZX). Absorption of CZX given rectally was rapid in all animals, similar to intramuscular or subcutaneous administration. The peak serum levels of CZX in mice, rats and dogs when administered rectally at a dose of 25 mg/kg were 23.1 μg/ml at 7.5 minutes, 23.5 μg/ml at 15 minutes and 25.2 μg/ml at 15 minutes, respectively. These values were about 76%, 68% and 42% of the values for subcutaneous or intramuscular administration in mice, rats and dogs at the same respective doses. Urinary recoveries of CZX after rectal administration of 25 mg/kg were 44.2% (0-12 hours) in rats and 27.7% (0-6 hours) in dogs, and 2.7% (0-6 hours) of the dose was excreted into bile fluid in rats. Organ distribution of CZX when administered rectally to rats was similar in distribution pattern to that of muscular administration, although its concentrations in various organs were slightly lower than those for intramuscular administration, as was the case for serum concentration. Serum concentrations of CZX were proportionately elevated with dose when dogs were rectally administered CZX-S in doses of 12.5, 25 and 50 mg/kg. In the case of multiple administrations (t. i. d. for 10 days) of CZX-S to dogs, no remarkable difference was found in serum concentrations of CZX in comparison with single doses, and no accumulation of CZX was demonstrated. Furthermore, changes in rectal absorption with aging were investigated by using 1-15-month-old dogs, and, as a result, no definite variation was observed.View full abstractDownload PDF (898K) -
TAKESHI NISHINO, TERUO TANINO, YOSHIKI OBANA1985 Volume 38 Issue 12 Pages 3458-3463
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSIn experimental infections in mice, the therapeutic efficacies of rectal administration of ceftizoxime (CZX) were compared with those of subcutaneous administration.
The efficacies of rectal administration were equivalent to those of subcutaneous administration against intraperitoneal infections due to Streptococcus pneumoniae and Escherichia coll. Against Staphylococcus aureus, Streptococcus pyogenes, Klebsiella pneumoniae, Enterobacter cloacae, Proteus mirabilis, Morganella morganii and Serratia marcescens, the efficacies of rectal administration were inferior to those of subcutaneous administration. Against urinary tract and respiratory tract infections, the efficacies of rectal administration were slightly inferior to those of subcutaneous administration. Serum concentrations of CZX for rectal administration were less than those of subcutaneous administration.View full abstractDownload PDF (729K) -
HITOHISA NIIMI, ICHIROU KAMATA, MASAHIRO TANIGAWA, SHINTAROU MIYAKE, T ...1985 Volume 38 Issue 12 Pages 3464-3470
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSLatamoxef (LMOX) at a dose of 2 g was intravenously administered to 12 cases with postoperative meningitis and the concentrations in serum and cerebrospinal fluid (CSF) were examined up to 2 hours and the results obtained were as follows;
1. The average serum and CSF concentrations of LMOX were 125.0 μg/ml, 4.33 μg/ml at 0.5 hour, 80.7 μg/ml, 4.64 μg/ml at 1 hour and 45.8 μg/ml, 3.82 μg/ml at 2 hours, respectively.
2. The clinical responses of LMOX against postoperative meningitis were revealed excellent in 4 cases and good in 8 cases.
No side effects were observed.
3. LMOX was thought to be effective agent in the treatment of the postoperative meningitis.View full abstractDownload PDF (609K) -
HIROSHI YAMAMOTO, NORITOMO SENO, SHIN MATSUMOTO1985 Volume 38 Issue 12 Pages 3471-3476
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSIn the surgery of the chest, we are often experienced pulmonary infections, so it is considered that the grasping antibiotic levels in pulmonary tissue is very important because of the decision of antibiotic dose schedule against pulmonary infections.
For this purpose, latamoxef (LMOX) at a dose of 2 g was intravenously administered to 14 cases with pulmonary cancer, 3 cases with pulmonary tuberculosis, 2 cases with pulmonary abscess and 1 case with bronchiectasis, totally 20 cases and the concentrations in serum, pulmonary tissue, bronchia and sputum were measured up to 6 hours and the results obtained were as follows;
1. The average serum concentration of LMOX was 137.2 μg/ml at 1/2 hour and decreased gradually, fell to 20.3 μg/ml at 6 hours.
2. The average levels of LMOX in normal alveolus of pulmonary tissue and in bronchia were 63% and 48% of the serum level, respectively.
3. The average level of LMOX in inflammatory alveolus of pulmonary tissue was approximately 20% lower than the normal alveolus.
4. The average level of LMOX in sputum increased gradually and appeared 4.6 μg/ml at 6 hours.
5. LMOX was shown a good results on the penetration into the pulmonary tissue and its level almost exceeded the minimal inhibitory concentration against clinical isolates from sputum of respiratory tract infections.View full abstractDownload PDF (781K) -
KOJI KIKUCHI, TADAAKI SAKAI, TAKAAKI IKEDA, TETSUSHI SUITO1985 Volume 38 Issue 12 Pages 3477-3480
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThere are few reports on concentrations of antibiotics in human lung tissues. The concentrations of clindamycin (CLDM) in human lung tissues were determined in 11 patients with lung tumor who were treated with the antibiotic.
In the case of 600 mg drip infusion for 1 hour, the concentrations of CLDM in lung tissues were 24 μg/g and 23 μg/g, 2 and 3 hours after the start of drip infusion, respectively.
In the case of 1,200 mg drip infusion, the value reached 47 μg/g in 2 hours and 39 μg/ g in 3 hours. The concentrations in lung tissues were about 4-5 times higher than in blood.View full abstractDownload PDF (453K) -
FUMIKO KOBAYASHI, KYOICHI SAKAMOTO, MASARU KUREBE, MASAYUKI YOKOTA, MI ...1985 Volume 38 Issue 12 Pages 3481-3486
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMale guinea pigs were given 0.1 ml of 2, 3 or 5% fosfomycin (FOM) ototopical solution once a day for 5 days into a middle ear cavity through artificially perforated ear drum Kanamycin A (KM) was used at 2% ototopical solution as control drug Four animals of each group were sacrificed under pentobarbital anesthesia to isolate the cochlea 10 days after the final application The cochlea was washed with 0.1 M phosphate buffer (pH 7.0), followed by fixing with 2.5% glutaraldehyde and 1% osmic acid Cochlear specimens were prepared by standard method for scanning electron microscopic observation The scanning electron microscopic observations revealed some damages in outer and inner hair cells, such as partial deformation or loss of auditory hair in hair cells, but these damages were not correlated to drug treatments.
In order to determine the transfer of FOM and KM from middle ear cavity to cochlear lymph in male guinea pigs, the cochlear lymph was collected 0.5, 1, 2 and 4 hours after an application of 0.1 ml of 3 or 5% FOM and 2% KM ototopical solution into a middle ear cavity, followed by estimating content of these antibiotics in the lymph The results showed the peak concentration in lymph at 1 to 2 hours after an application of 3% FOM was lower than that after 2% KM, but the AUC of 3% FOM was higher than that of 2% KM The AUC value of FOM was dependent on the applied concentration of FOM The value of half-life time was about 4.8 hours at FOM and about 2.3 hours at KM.
These results suggest that FOM is freely diffused from applied middle ear cavity into cochlear lymph and distributed for longer time than KM, but FOM exerts no toxic effect on the cochlear hair cells in guinea pigs.View full abstractDownload PDF (3217K) -
MAYURI KUBO, YOSHIAKI KATO, YOSHIHIKO INAMORI1985 Volume 38 Issue 12 Pages 3487-3496
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe combined actions of sisomicin (SISO), gentamicin (GM) and cefmenoxime (CMX), ceftizoxime (CZX), cefoperazone (CPZ), cefotetan (CTT) against S. marcescens IFO-3735 and P. aeruginosa IFO-12689 were investigated. The results were summarized as follows.
1. The synergistic effect of the combinations of SISO-CMX, SISO-CZX, SISO-CPZ, SISO-CTT, GM-CMX, GM-CZX, GM-CPZ and GM-CTT using the checker board dilution method on S. marcescens IFO-3735 and P. aeruginosa IFO-12689 were found. Especially the minimum FIC index value of combination of SISO-CTT and GM-CTT were rather low as 0.14 and 0.13, respectively and these synergistic effect was remarkably strong on S. marcescens IFO-3735.
2. With the killing kinetic method, all combinations tested showed the synergistic effect in both bacteria.View full abstractDownload PDF (1047K) -
MASAMI TAKAHASHI, TOSHICHIKA OHTOMO, YOSHITOSHI ICHIMAN, YUKIO OHSHIMA ...1985 Volume 38 Issue 12 Pages 3497-3504
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSSub-MIC range of 8 kinds of β-lactam antibiotics and 3 kinds of aminoglycoside antibiotics against strain of Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa isolated from clinical source were determined by nephlometic method, and following results were obtained.
1. When 10 strains of S. aureus tested to ampicillin (ABPC), hetacillin (IPABPC), mecillinam (MPC), cephalexin (CEX), cefotaxime (CTX), latamoxef (LMOX), cefatrizine (CFT), cephapirin (CEPR), gentamicin (GM), dibekacin (DKB) and amikacin (AMK), ratio of MIC to MAC were 36.8, 53.6, 156.8, 29.6, 61.6, 34.4, 50.0, 111.2, 9.2, 20.0 and 13.6, respectively.
2. When 10 strains of K. pneumoniae tested to MPC, CEX, CTX, LMOX, CFT, CEPR, GM, DKB and AMK, ratio of MIC to MAC were 409.6, 10.4, 34.4, 123.2, 39.2, 167.2, 5.2, 5.6 and 13.2, respectively.
3. When 10 strains of P. aeruginosa tested against CTX, LMOX, GM, DKB and AMK, ratio of MIC to MAC were 16.8, 38.4, 6.8, 3.2 and 10.4, respectively.View full abstractDownload PDF (912K) -
AKIRA SOUMA, HIROMITSU HAGA, HISATOMI MIZOGUCHI, KAZUHIDE MURE, KAZUO ...1985 Volume 38 Issue 12 Pages 3505-3512
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a monobactam antibiotic, is known to have a high activity against Gram-negative bacteria. Fundamental and clinical studies were carried out on AZT with the following results.
1. Following 1g of bolus intravenous injection, the transfer of AZT to uterine artery and internal genital organs was found to be satisfactory. The levels of the drug in uterine artery showed 34.28, 4.50μg/ml at approximately 2, 6 hours, and those in internal genital organs showed 3-34μg/g at 2 hours.
2. Clinical efficacy was; excellent in 4 cases, good in 13 cases and poor in 1 case, with the very high overall efficacy rate of 94.4%.
3. Abnormal laboratory findings and side effects due to the drug were not noted.View full abstractDownload PDF (673K) -
KIHYOE ICHINOHE, SATORU MAKINODA, SEIICHIRO FUJIMOTO, TOSHINOBU TANAKA1985 Volume 38 Issue 12 Pages 3513-3519
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSClinical effect in obstetrics and gynecology was studied on aztreonam (AZT), a potent monobactam antibiotic for Gram-negative bacteria. AZT was tested for 7 cases and effective for all of them with quite a high effective rate of 100%. Neither side effect nor abnormal laboratory findings were noted and it sufficiently proves the property of AZT, a totally chemical-synthesized product with lower incidence of allergic reaction. The above results suggest that AZT is useful for obstetrics and gynecologic infections in view of its high stability to β-lactamase and dehydropeptidase and high potency against Gram-negative bacteria.View full abstractDownload PDF (552K) -
HARUO SEKI, MASAHIRO MAKI1985 Volume 38 Issue 12 Pages 3520-3526
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monobactam antibiotic, was studied in obstetrics and gynecology with the following results.
1. The tissue concentration of AZT in the female genital organs was relatively high at the portio vaginalis and the cervix uteri followed by at the ovary and the myometrium, but the distribution to the endometrium and the oviduct was a little poor.
2. The concentration of AZT in the pelvic dead space exudate was highest at 2 hours after intravenous injection whereas it was highest at 5 hours after intravenous drip infusion. However, there was no significant difference in the concentration between intravenous injection and intravenous drip infusion and the distribution to the pelvic dead space exudate was relatively good.
3. AZT was clinically administered to pyometra (3 cases), puerperal endometritis (3), adnexitis and endometritis (3), pelvioperitonitis (1), BARTHOLIN'S abscess (4) and purulent vulvitis (1), a total of 15 cases with an overall effective rate of 93.3%.
4. AZT was microbiologically effective for Gram-negative bacteria such as E. coli and K. pneumontae, but also effective for anaerobes and some Gram-positive bacteria, etc., for which MIC of AZT is high.
5. With regard to safety of AZT, neither side effects nor abnormal laboratory findings were reported.View full abstractDownload PDF (663K) -
KIMITOSHI INOUE, NOBUYUKI MORISAKI, TETSURO CHIMURA1985 Volume 38 Issue 12 Pages 3527-3530
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (SQ 26,776, AZT), a new monobactam antibiotic, was studied in obstetrics and gynecology with the following results.
1. For the study of tissue penetration, 1g AZT was administered by intravenous drip infusion for 1 hour. The concentration was high in elbow venous blood and uterine arterial blood 60 minutes after the administration. Each uterine tissue concentration other than the endometrium was as high as 26.7-31.7% of the blood level and salpinx and ovary concentration were 25.9% and 5.2%, respectively. Each tissue concentration decreased to <0.6μg/g in the uterine, the ovary and the salpinx 280 minutes thereafter.
2. In the review of obstetric and gynecologic genital infections, clinical efficacy of AZT was “poor” for 1-endometritis, “poor” for 1-pyometra, “excellent” for 1-puerperal fever, “excellent” (1) and “good” (2) for 3-pelvioperitonitis, “excellent” for 1-parametritis and “good” for 2-infectious lymphocele with overall effective rate of 77.8% (7/9).
3. AZT was microbiologically effective for Gram-negative bacteria, such as E. coli, K. pneumoniae, etc.
4. As for safety, neither side effects nor abnormal laboratory findings in the examination of blood, hepatic function, renal function and urine due to AZT were reported.View full abstractDownload PDF (448K) -
KAZUNORI YAMADA, KENICHI FUNAKI, KUNIHIRO OKAMURA, MASAAKI NAKAKUKI, Y ...1985 Volume 38 Issue 12 Pages 3531-3534
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT) was evaluated for its clinical efficacy in 6 patients with pelvic peritonitis. In all the cases, AZT was administered by intravenous injection, and the duration of treatment ranged from 4 to 12 days. Daily dose was 2g in 4 cases, and 4g in the remaining 2 cases. Surgical treatment was necessary in 2 cases, whereas in another 2 cases, either LMOX or ABPC was administered in addition to AZT. The clinical results was excellent or good in 5 out of 6 cases.
Side effects possibly attributed to AZT were diarrhea in 2 cases and slight increase of GOT and GPT in 1 case, although they disappeared promptly afterward.View full abstractDownload PDF (380K) -
ATSUSHI KAWAGOE, HAJIME TSUNODA, KEIKO OGASAWARA, MASAHIRO SAITO, SATO ...1985 Volume 38 Issue 12 Pages 3535-3541
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT) was administered to 10 patients with obstetric and gynecologic infections to evaluate its clinical effect. Two-four grams of AZT per day (b. i. d.) were administered for the treatment for 4-15 days by intravenous drip infusion or intravenous injection. AZT was effective for 3 cases of pelvic peritonitis, 1 case of pyoovarium and 2 cases of BARTHOLIN'S abscess. For 2 cases of intrauterine infection, AZT was effective for 1 case, and the other case could not be judged. For 2 cases of local infection, AZT was effective for 1 case and ineffective for 1 case. Efficacy rate was 89% for the 9 cases excluding the 1 unevaluable case. Microbiological effect was determined for 4 out of 10 cases. Two strains of Haemophilus influenzae and one each of Escherichia coli, Bacteroides fragilis and Streptococcus intermedius were isolated, but all of them were eliminated for a elimination rate of 100%. Neither abnormal laboratory findings in hepatic or renal functions, etc. nor side effects were recognized.View full abstractDownload PDF (2793K) -
FUKUSHO HAYASHI, ISAO OBATA, KAZUHIKO OCHIAI, KIYOHIKO KOIKE, NOBUYUKI ...1985 Volume 38 Issue 12 Pages 3542-3560
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSPenetration of aztreonam (AZT) into the uterus and the adnexal tissues and usefulness and safety of AZT for obstetric and gynecologic infections were studied with the following results.
1. By one shot intravenous injection of AZT 1g, the uterus and the adnexal tissues showed favorable penetration with Cmax27.0-48.5μg/g, AUC 29.4-84.9μg·hr/g and Tmax0.10-0.44 hours.
2. MIC50, MIC80 and MIC90 of AZT for Gram-negative bacteria measured prior to administration were very low being 0.10μg/ml, 0.20μg/ml and 1.56μg/ml, respectively.
3. Clinical effect of AZT for 30 infection cases in obstetrics and gynecology was evaluated according to an overall efficacy criteria resulting in “good” for all the cases.
4. With regard to microbiological effect, 90.9% of theμathogens isolated prior to the administration were eliminated by AZT.
5. During and after the administration of AZT, side effect due seemingly to AZT was not observed in subjective and objective symptoms and laboratory values.View full abstractDownload PDF (1632K) -
KANGO FUKUNAGA, KATSUAKI KUNII, NANKUN CHO1985 Volume 38 Issue 12 Pages 3561-3572
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monobactam antibiotic was evaluated on clinical efficacy and bacteriological response in gynecological and obstetrical infections, and the following results were obtained.
AZT was given to 22 cases with obstetrical and gynecological infections at a dose of 1g ×2 times daily and 86.4% of clinical efficacy, 45.5% of eradicated rate on diagnosis, 52.5% of bacteriological response on isolated organisms and 83.3% of bacteriological effect on cases isolated Gram-negative bacteria were assessed.
Side effect incidence was very low.View full abstractDownload PDF (1028K) -
MASAKAZU NODA, SHINICHI HIRAI, SHINYA IIDA, TATSUYA KOHARA, YUKIO MATS ...1985 Volume 38 Issue 12 Pages 3573-3577
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTissue penetration and clinical efficacy were studied on aztreonam (SQ 26, 776, AZT) in obstetrics and gynecology with the following results.
1. Number of cases was too small to sufficiently review the penetration into each uterine tissue, the ovary and the tube after the intravenous injection of AZT 1g.
2. Overall clinical effect for all the 6 cases reviewed was more than “ good ”. Also, neither side effect nor abnormal laboratory findings were reported.
3. From the above results, AZT was considered to be a highly useful antibiotic in obstetrics and gynecology.View full abstractDownload PDF (498K) -
KIYOSHI ARAI, MASANOBU HOGAKI, YUTAKA YOSHIDA1985 Volume 38 Issue 12 Pages 3579-3584
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monobactam antibiotic, was basically and clinically applied to the field of obstetrics and gynecology, obtaining the following results.
1. The pelvic dead space exudate level of AZT after 30 minutes-intravenous drip infusion of 1g attained the peak of 22. 66ug/ml at 1 hour from initiation of infusion and thereafter declined gradually, contrasting the peak of 34. 38ug/ml of the cubital vein at 30 minutes.
2. Total of 13 cases comprising 4 with intrauterine infection, 5 with adnexitis and 4 with pelveoperito-nitis were intravenously treated with AZT at a dose of 1g twice daily.
The overall clinical results were excellent in 3 cases and good in 10 cases.
3. No side effects were observed in any of the cases treated with AZT.View full abstractDownload PDF (627K) -
HIDEYO NAKAMURA, KENICHI SEKI, SHIGERU HAYASHI, YOSHIYUKI IWATA1985 Volume 38 Issue 12 Pages 3585-3590
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monobactam antibiotic, was studied for clinical efficacy in the field of gynecologic infection.
1. AZT was administered at a daily dose of 2g in 2 divided doses by single shot intravenous injection. The subjects were patients with the following infections: adnexitis (6), pelvic peritonitis (5), endometritis (1) and wound abscess (1).
2. Good response was seen in 10 patients out of 13. The overall efficacy rate of 76.9% was obtained.
3. Slight increase in GOT, GPT and Al-P was seen in 1 case. It was normalized on 6th day after completion of the therapy.
4. No notable side effects were observed.View full abstractDownload PDF (560K) -
HIKARU KAMIISHI, HIROSHI MINAGUCHI, TAKENDO YANAGIHASHI, TSUGUO UEMURA ...1985 Volume 38 Issue 12 Pages 3591-3598
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe following results were obtained through the fundamental and clinical studies of aztreonam (AZT), a new monobactam antibiotic, in obstetrics and gynecology.
1. Satisfactory tissue penetration was not recognized in 3-5 hours after intravenous injection of 1g. However, the concentration was more than MIC for the majority of aerobic Gram-negative bacteria in intravenous drip infusion of AZT 1g and in intravenous injection and intravenous drip infusion of 2g.
2. There was no difference of serum concentration of AZT between uterine arterial blood and cubital venous blood.
3. AZT was administered by intravenous drip infusion to 2 cases of puerperal endometritis, 2 cases (the same patient) of vaginal wall abscess, 1 case of postoperative lymphocele infection and 1 case of infected ovarian cyst suspected, and it was effective for all of them.
4. Neither subjective/objective side effects nor abnormal laboratory findings were noted in any case.View full abstractDownload PDF (848K) -
CHIZURU MARUYAMA, MASAYA TATENO1985 Volume 38 Issue 12 Pages 3599-3605
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1. Clinical effect and safety of aztreonam (AZT) in the obstetrics and gynecology were studied in 17 cases of obstetric and gynecological infections. AZT was administered at a dose of 2g per day by intravenous drip infusion, for 4-8 days depending on severity of the disease. The results showed that AZT was effective in 14 out of 17 cases and the overall efficacy rate was 82.4%.
2. E. coli, Enterobacter, E. faecalis, etc. were detected in 8 out of 17 cases, and after AZT treatment other strains appeared in 3 clinically effective cases.
3. There was a slight elevation of GOT and GPT in 1 case but no other appreciable side effect or abnormal laboratory value was observed.View full abstractDownload PDF (722K) -
HARUO TAKABAYASHI, SORYU KUWABARA1985 Volume 38 Issue 12 Pages 3606-3608
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe following results were obtained by measuring serum and tissue concentrations of aztreonam, a new monobactam antibiotic.
1. Penetration into each tissue was favorable, particularly, to the portio vaginalis, but there was no conspicuous difference of the penetration among other tissues.
2. Serum concentration tended to decrease with the lapse of time, but the concentration in each tissue did not show a specific pattern of change due to a considerable irregularity of the measured concentrations.
3. No specific side effect was noted.View full abstractDownload PDF (237K) -
EIJI HANADA, HARUHIKO IMANISHI, HIROSHI SAKAIDA, MASAHIRO IKEUCHI, SHI ...1985 Volume 38 Issue 12 Pages 3609-3618
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monocyclic β-lactam antibiotic was studied on clinical efficacy for infectious disease in gynecological field.
1. At about 80 minutes following intravenous injection of 1g dose of AZT, it penetrated well into internal genital organs at therapeutic levels.
Moreover it transfered very fast and enough into intrapelvic dead space exudate, and its level was kept still as high at 12 hours after administration.
2. AZT was given to 20 women affected with gynecological infectious disease. The outcome of AZT therapy was as follows: effective in 5 out of 6 patients (83.3%) administered intravenously and in all of 14 patients (100%) recieved intramuscularly.
3. Notable adverse effects or abnormal laboratory findings were not observed except 1 case of diarrhea and 2 cases of transient and slight elevation of serum CPK and transaminases.
Based on these results, we may conclude that AZT is a highly effective and a very safe antibiotic for the treatment of infectious disease in gynecological field.View full abstractDownload PDF (915K) -
KATSUMI NODA, KAZUTOSHI MATSUNAMI, KUNIIIIKO ITO, MOTOKI HAYASAKI1985 Volume 38 Issue 12 Pages 3619-3628
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT) was studied for the transfer into the pelvic dead space exudate in 5 patients who received radical hysterectomy due to uterocervical cancer, and for the clinical efficacy in the treatment of 5 cases of obstetrical and gynecological infections.
1. Transfer into the pelvic dead space exudate
Data analysis was performed by the simulation curves prepared from pharmacokinetic parameters using the two-compartment model. On examination, the serum concentration of cubital venous serum was found to be 53. 20ug/ml at 1 hour after the start of 1-hour intravenous drip infusion of 1 g of AZT. Also, the shifting concentration of the pelvic dead space exudate was found to have reached its peak value of 12. 79ug/ml at 3. 22 hours after the start of the infusion, and still showed the value of more than 7ug/ml even at 8 hours after the start of the infusion. The AUC was 112. 81μg·hr/ml.
2. Clinical evaluation
AZT was administered at a daily dose of 2-4g in 2 divided doses by intravenous injection and intravenous drip infusion for 60 minutes. Clinical efficacy of the 5 patients with acute and moderate degree obstetrical and gynecological infections was; excellent in 1 case, good in 3 cases and poor in 1 case, with the overall efficacy rate of 80. 0%.View full abstractDownload PDF (989K) -
FUTOSHI OHBAYASHI, KEIU NINOMIYA, YUKIO HASEGAWA1985 Volume 38 Issue 12 Pages 3629-3633
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAntimicrobial activity of aztreonam (AZT) against 231 clinical isolates in the field of obstetrics and gynecology was determined by agar-plates dilution method. Almost of all strains of E. coli (108 strains) tested were susceptible to the concentration of 0. 20μg/ml of AZT. Anaerobic bacteria, however, were lessu sceptible to this antibiotic than to cefazolin.
The concentrations of AZT were determined in serum and pelvic tissue samples obtained at various intervals after 1 hour intravenous drip infusion with 1g. The concentrations of AZT in pelvic tissues were maximal 9. 3μg/g at 57 minutes but less than 0. 6%mug/g at 3 hours or more after injection.
Clinical efficacy of AZT was evaluated in 6 cases consisted of two each with BARTHOLIN'S abscess and intrauterine infection and one each with post partum endometritis and acute adnexitis. Clinical efficacies were seen in 5 cases.View full abstractDownload PDF (502K) -
HIROJI OKADA, JINSUKE YASUDA, MASAAKI KANAO, MEGUMI TOMIOKA, TAKAO YAM ...1985 Volume 38 Issue 12 Pages 3634-3644
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSFundamental and clinical studies on aztreonam (AZT), a new synthetic monobactam antibiotic, were performed and following results were obtained.
1. Concentration of AZT was examined in serum, internal genital tissues and retroperitoneal fluid after a single intravenous administration of 1g dose. The venous serum level of AZT was 114. 0μg/ml at 10 minutes after the administration, then decreased to 7. 0μg/ml at 3 hours. Since concentration of AZT in examined tissues showed wide variation, it was irrelevant to calculate transfer ratio. Concentration in retroperitoneal fluid made the peak of 40. 0 ± 22.6μg/ml at 1 hour after the administration, then slowly decreased to 13. 4± 3. 2μg/ml at 6 hours.
Judging from above data, the transfer of AZT to retroperitoneal fluid was favorable.
2. In clinical trial, AZT was given to 17 cases with obstetrical and gynecological infections such as endometritis, uterine adnexitis, pelvic peritonitis, parametritis and lymphocystitis. The efficacy was evaluated as excellent in 2 cases, good in 12 and poor in 3, and efficacy rate was 82. 4%.
No side effects were observed in any of the cases. In laboratory findings, transient elevation of liver function in 2 cases and eosinophilia in 1 case were noticed.View full abstractDownload PDF (1002K) -
ETSUO USHIODA, HIDEMITSU IIOKA, IKUKO SHIMAMOTO, MOTOHIKO ICHIJO1985 Volume 38 Issue 12 Pages 3645-3650
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT, E-0734), a new p-lactam antibiotic, was fundamentally and clinically studied. The following results were obtained.
1. The serum and internal genital tissue levels for AZT after 1g intravenous injection had been kept at more than about 20μg/ml and 3. 0μg/g, respectively, during 1 hour.
2. AZT was administered at 1-2g of daily dose by intravenous injection or intravenous drip infusion to 5 patients with obstetric and gynecological infections, comprising 1 of pyometra, parametritis, BARTHOLIN'S abscess, puerperal endometritis and diffuse peritonitis.
Clinical efficacy was; excellent in 1 puerperal endometritis case, good in 2 cases and poor in 2 cases. Neither side effect nor abnormal laboratory finding was observed.View full abstractDownload PDF (507K) -
AKIO MIYAZAKI, AKIRA YAMAMOTO, BUNPEI TANAKA, HIROSHI ONDA, ICHIRO TAT ...1985 Volume 38 Issue 12 Pages 3651-3659
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (SQ 26,776, AZT), a new monobactam antibiotic, was fundamentally and clinically studied with the following results.
Uterine and adnexal concentrations of AZT after intravenous injection of 1g were highest 3 hours after administration in the ranges of between 18.6-23.4μg/g and 16.5-28.2μg/g, respectively, and rapidly decreased thereafter. Penetration of AZT into the pelvic dead space exudate was quickly recognized after intravenous injection of 1g and its concentration 30 minutes after administration was 14.08±7.08μg/ml and highest (22.35±5.85μg/ml) 2 hours after administration. It gradually decreased to 8.50±2.07μg/ml 6 hours after administration.
Clinical effect was studied by administering 1-3g of AZT twice a day for 3-16 days by intravenous drip infusion for 18 patients with various infections in the field of obstetrics and gynecology. Efficacy of AZT for 9 genital infection cases were excellent for 4 cases, good for 4 cases and poor for 1 case, with an overall efficacy rate of 88.9%. For 2 UTI cases, it was excellent for one case and good for the other, and for 4 pelvioperitonitis cases, excellent for 3 cases and good for 1 case. For 2 inflammation cases of the pelvic dead space, efficacy of AZT was excellent for both of them.
With regard to side effect, there was only one rash case experienced. It was considered from the above results that AZT is sufficiently useful for the infections in the field of obstetrics and gynecology and also useful for various gynecologic surgery cases.View full abstractDownload PDF (879K) -
KIICHIRO NODA, MASANORI IKEDA, MITSURU SHIOTA, TAKAHISA HORII, YOH WAT ...1985 Volume 38 Issue 12 Pages 3660-3665
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSFundamental and clinical studies were performed on aztreonam (AZT), a new antibiotic with single β-lactam ring, with the following results.
1. Following intravenous drip infusion of 1g, transfer of AZT to the internal genital organs was found to be good. Transfer of AZT to exudate of pelvic dead space was also good.
2. AZT was given to 6 cases, who had gynecological or obstetrical infectious disease. AZT was effective in the 5 cases out of 6, although it showed high MIC against bacteria isolated from the effective cases.
3. The above results demonstrated that AZT was a safe and effective drug.View full abstractDownload PDF (555K) -
KATSUHIKO TADA, KATSUYOSHI SAKAE, MASAAKI ANDO, MOTOHIRO HONGO, REIKO ...1985 Volume 38 Issue 12 Pages 3666-3673
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT) is a newly developed β-lactam antibiotic for use of intravenous injection. It is the first drug in the world of monobactam series with the structural characteristic of monocyclic β-lactam. The antimicrobial spectrum of AZT is unique, having little or no susceptibility against Gram-positive organisms and anaerobes, but showing high susceptibility against aerobic Gram-negative rods including Pseudomonas.
One gram of AZT was given intravenously to 32 patients prior to abdominal total hysterectomy for uterine myoma. Bilateral uterine arteries were clamped at 0.25, 0.5, 1, 2, 4, 8 or 12 hours after administration, and serum samples and uterine tissues were taken for the measurement of AZT concentration by bioassay method.
1. Little difference was found in the serum concentration between cubital venous and uterine arterial serum, the half-lives of both being 2.11 hours. The initial concentrations were estimated to be 68.0μg/ml and 63.9μg/ml, respectively.
2. While the peak concentrations of the portio vaginalis, cervix uteri, myometrium and oviduct were obtained at about 10 minutes, those of the endometrium and ovary were at 18.2 minutes and 31.3 minutes, respectively. They were as follows; the portio vaginalis 50.0μg/g, the cervix uteri 43.6μg/g, the myometrium 29.8μg/g, the oviduct 44.7μg/g, the endometrium 27.3μg/g, the ovary 29.0μg/g. After showing peak, tissue levels were kept fairly high up to 3 hours, then decreased gradually as time passed up to approximately 8 hours.
Judging from its favorable transfer into the uterine tissues and MICs against main clinical isolates in the field of obstetrics and gynecology, AZT is evaluated to be clinically useful in the treatment of obstetrical and gynecological infections.View full abstractDownload PDF (889K) -
ETSUKO OKADA, KOJI HIRABAYASHI1985 Volume 38 Issue 12 Pages 3674-3682
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT), a new monocyclic β-lactam antibiotic, was studied on the transfer into intrapelvic tissues and on the clinical efficacy in the treatment of 19 cases of obstetrical and gynecological infections.
1. The AZT levels were examined in the pelvic dead space exudate in 6 patients who received radical hysterectomy due to uterocervical cancer.
The simulation curves for AZT were well performed after the decision of the pharmacokinetic parameters using the two-compartment model. Following 1-hour intravenous drip infusion of 1g of AZT, the peak concentration of AZT in cubital venous blood was estimated 73.3μg/ml at the end of infusion. The peak concentration of AZT in the pelvic dead exudate was estimated 18.6μg/ml at 2.31 hours after infusion.
2. Following intravenous 1-hour drip infusion of 1g, the transferred level of AZT into uterine tissues was maintained at the effective concentration which means the excess level of the MIC against clinical isolates often observed in the field of obstetrics and gynecology.
3. AZT was administered 2-4g/day in 2 times a day by intravenous drip infusion for 60-90 minutes. The subjects were 19 patients with the following infections; pyometra (1), puerperal intrauterine infection (4), postoperative parametritis (4), pelvioperitonitis (2), purulent lymphocyst (1), acute salpingoophoritis (1), vaginal stump abscess (1), DOUGLAS abscess (2), pelvioperitonitis+pyosalpinx (2), vulval abscess (1).
Clinical efficacy was; excellent in 2 cases, good in 11 cases and poor in 6 cases. No notable side effect or abnormal laboratory finding was noted.View full abstractDownload PDF (939K) -
HIDEAKI WATANABE, HIDEKI KATABUCHI, JUNYA UMEZU, MICHIAKI YAKUSHIJI, T ...1985 Volume 38 Issue 12 Pages 3683-3686
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSClinical effect was studied for aztreonam (AZT) on 2 patients being treated for malignant tumors.
One-two grams of AZT was administered b. i. d. by intravenous drip infusion for 6-7 days. In case 1 with pyometra, there were excellent improvements in WBC, CRP and fever pattern. Unfavorable BUN and S-Cr. values were found, but these were considered to be side effects due to cisplatin. These improved finally, and clinical effect was also excellent. Case 2, a urinary tract infection+prophylactic postoperative administration case, was treated in combination with another drug presuming mixed infection and AZT was shown to be effective clinically and overall.
No side effects in cases 1 or 2 were considered to be due to AZT.View full abstractDownload PDF (414K) -
HIROMICHI YAMAO, ISAO MIYAKAWA, KEIICHI TANIYAMA, KIMIHIRO NAGAI, KYOG ...1985 Volume 38 Issue 12 Pages 3687-3693
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe concentrations of aztreonam (SQ 26,776, AZT, Squibb) in peripheral venous serum, uterine arterial serum and intrapelvic female ograns were determined by bioassay, using the cylinder-plate diffusion method, in 27 women with simple total hysterectomy.
With an intravenous injection of AZT 1g, the maximum levels of peripheral venous serum and uterine arterial serum were 76.39μg/ml and 76.38μg/ml, respectively.
Also, the biological half-life (T1/2) was 1.56 hours in peripheral venous serum and 1.54 hours in uterine arterial serum. The concentration in uterine arterial serum was more than 1.8μg/ml at 8 hours after injection and maintained at a high level than the minimal inhibitory concentration necessary for most Gram-negative bacteria for at least 8 hours.
The concentrations of AZT in female genital organs were kept higher than the minimal inhibitory concentration against E. coli at 4 hours after injection, and the ratios of the concentrations in uterine tube and endometrium to that in peripheral venous serum were 0.40±0.18 and 0.30±0.20, respectively.
Since AZT is characterized by more potent antibacterial activity against Gram-negative bacteria and the minimal side effects, intravenous administration of AZT at 1g or 2g per day may be an adequate dose for infections of the female urogenital tract.View full abstractDownload PDF (784K) -
AKITO MORI, EIICHIRO YAMADA, HIROYUKI HARAGUCHI, TEPPEI UEDA, YUKIHIRO ...1985 Volume 38 Issue 12 Pages 3695-3699
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreoman (SQ 26,776, AZT), a synthetic monobactam antibiotic, was applied clinically in the field of obstetrics and gynecology. AZT was administered by intravenous drip infusion for 6 to 8 days at a daily dose of 2g divided in 2 times to 5 cases. Klebsiella in 1 case with puerperal endometritis, Enterococcus, Propionibacterium and Bacteroides in each 1 case with pyometra was isolated. The clinical effect of Klebsiella was excellent. Bacteroides in 1 not-examined case was good. Enterococcus and Bacteroides with pyometra was not effective. Side effects were observed in 2 cases. One case with eclampsia arised LDH and Al-P in serum and 1 case with hepatitis arised GOT and GPT in serum.View full abstractDownload PDF (512K) -
HIDEAKI IJUIN1985 Volume 38 Issue 12 Pages 3700-3703
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAztreonam (AZT) was evaluated for its clinical efficacy in a total of 10 cases, namely 3 cases of endometritis, 6 cases of intrapelvic infections, 1 case of puerperal pyelonephritis.
The clinical results of AZT were as follows; excellent in 5 cases and moderate in 5 cases, the overall efficacy rate was 100%.
No clinical side effect was observed, however in laboratory finding slightly elevated transaminase (GOT, GPT) was observed in 1 case.View full abstractDownload PDF (347K) -
SHINICHI TAKAMURA1985 Volume 38 Issue 12 Pages 3704-3710
Published: December 25, 1985
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSFundamental and clinical studies on gynecological use of aztreonam (AZT), a new monobactam, were performed with following results.
1. Following the intravenous administration of 1g dose of AZT, the transfer of AZT to pelvic dead space exudate was good, in which the concentration of that was 14.9μg/ml (2 hours), 15.3μg/ml (3 hours) after injection. The transfer of AZT to serum of umbilical cord and amniotic fluid was excellent.
2. In a clinical trial, AZT was given to 5 patients with obstetric and gynecological infections. The clinical efficacy was evaluated as excellent in 1 case and good in the other 4 cases.
No adverse effects were observed in any of the patients treated with AZT.View full abstractDownload PDF (653K)
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