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[Preclinical and clinical studies on aztreonam in the field of obstetrics and gynecology].

Penetration 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. By one shot intravenous injection of AZT 1 g, the uterus and the adnexal tissues showed favorable penetration with Cmax 27.0-48.5 micrograms/g, AUC 29.4-84.9 micrograms X hr/g and Tmax 0.10-0.44 hours. MIC50, MIC80 and MIC90 of AZT for Gram-negative bacteria measured prior to administration were very low being 0.10 micrograms/ml, 0.20 micrograms/ml and 1.56 micrograms/ml, respectively. 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. With regard to microbiological effect, 90.9% of the pathogens isolated prior to the administration were eliminated by AZT. During and after the administration of AZT, side effect due seemingly to AZT was not observed in subjective and objective symptoms and laboratory values.

Adult↗

[Clinical evaluation of aztreonam in the field of obstetrics and gynecology].

Aztreonam (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 1 g X 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.

Adolescent↗

[Tissue penetration and clinical experiences of aztreonam in obstetrics and gynecology].

Tissue penetration and clinical efficacy were studied on aztreonam (SQ 26,776, AZT) in obstetrics and gynecology with the following results. 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 1 g. Overall clinical effect for all the 6 cases reviewed was more than "good". Also, neither side effect nor abnormal laboratory findings were reported. From the above results, AZT was considered to be a highly useful antibiotic in obstetrics and gynecology.

Adult↗

[Basic and clinical studies of aztreonam in the field of obstetrics and gynecology].

Aztreonam (AZT), a new monobactam antibiotic, was basically and clinically applied to the field of obstetrics and gynecology, obtaining the following results. The pelvic dead space exudate level of AZT after 30 minutes-intravenous drip infusion of 1 g attained the peak of 22.66 micrograms/ml at 1 hour from initiation of infusion and thereafter declined gradually, contrasting the peak of 34.38 micrograms/ml of the cubital vein at 30 minutes. Total of 13 cases comprising 4 with intrauterine infection, 5 with adnexitis and 4 with pelveoperitonitis were intravenously treated with AZT at a dose of 1 g twice daily. The overall clinical results were excellent in 3 cases and good in 10 cases. No side effects were observed in any of the cases treated with AZT.

Adult↗

[Clinical experience on aztreonam].

Aztreonam (AZT), a new monobactam antibiotic, was studied for clinical efficacy in the field of gynecologic infection. AZT was administered at a daily dose of 2 g 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). Good response was seen in 10 patients out of 13. The overall efficacy rate of 76.9% was obtained. Slight increase in GOT, GPT and Al-P was seen in 1 case. It was normalized on 6th day after completion of the therapy. No notable side effects were observed.

Adult↗

[Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology].

The following results were obtained through the fundamental and clinical studies of aztreonam (AZT), a new monobactam antibiotic, in obstetrics and gynecology. Satisfactory tissue penetration was not recognized in 3-5 hours after intravenous injection of 1 g. However, the concentration was more than MIC for the majority of aerobic Gram-negative bacteria in intravenous drip infusion of AZT 1 g and in intravenous injection and intravenous drip infusion of 2 g. There was no difference of serum concentration of AZT between uterine arterial blood and cubital venous blood. 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. Neither subjective/objective side effects nor abnormal laboratory findings were noted in any case.

Adult↗

[Clinical trial of aztreonam in the field of obstetrics and gynecology].

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 2 g 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%. 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. There was a slight elevation of GOT and GPT in 1 case but no other appreciable side effect or abnormal laboratory value was observed.

Adult↗

[Tissue penetration of aztreonam in obstetrics and gynecology].

The following results were obtained by measuring serum and tissue concentrations of aztreonam, a new monobactam antibiotic. Penetration into each tissue was favorable, particularly, to the portio vaginalis, but there was no conspicuous difference of the penetration among other tissues. 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. No specific side effect was noted.

Adult↗

[Fundamental and clinical studies on aztreonam in the gynecological field].

Aztreonam (AZT), a new monocyclic beta-lactam antibiotic was studied on clinical efficacy for infectious disease in gynecological field. At about 80 minutes following intravenous injection of 1 g dose of AZT, it penetrated well into internal genital organs at therapeutic levels. Moreover it transferred very fast and enough into intrapelvic dead space exudate, and its level was kept still as high at 12 hours after administration. 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%) received intramuscularly. 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.

Adult↗

[Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology].

Aztreonam (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. 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 53.20 micrograms/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 12.79 micrograms/ml at 3.22 hours after the start of the infusion, and still showed the value of more than 7 micrograms/ml even at 8 hours after the start of the infusion. The AUC was 112.81 micrograms X hr/ml. Clinical evaluation AZT was administered at a daily dose of 2-4 g 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%.

Adult↗

[In vitro activity and clinical evaluation of aztreonam in the field of obstetrics and gynecology].

Antimicrobial 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 0.20 micrograms/ml of AZT. Anaerobic bacteria, however, were less susceptible 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 1 g. The concentrations of AZT in pelvic tissues were maximal 9.3 micrograms/g at 57 minutes but less than 0.6 micrograms/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.

Adult↗

[Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology].

Fundamental and clinical studies on aztreonam (AZT), a new synthetic monobactam antibiotic, were performed and following results were obtained. Concentration of AZT was examined in serum, internal genital tissues and retroperitoneal fluid after a single intravenous administration of 1 g dose. The venous serum level of AZT was 114.0 micrograms/ml at 10 minutes after the administration, then decreased to 7.0 micrograms/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 +/- 22.6 micrograms/ml at 1 hour after the administration, then slowly decreased to 13.4 +/- 3.2 micrograms/ml at 6 hours. Judging from above data, the transfer of AZT to retroperitoneal fluid was favorable. 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.

Adult↗

[Fundamental and clinical studies of aztreonam in the field of obstetrics and gynecology].

Aztreonam (AZT, E-0734), a new beta-lactam antibiotic, was fundamentally and clinically studied. The following results were obtained. The serum and internal genital tissue levels for AZT after 1 g intravenous injection had been kept at more than about 20 micrograms/ml and 3.0 micrograms/g, respectively, during 1 hour. AZT was administered at 1-2 g 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.

Adult↗

[Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology].

Aztreonam (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 1 g were highest 3 hours after administration in the ranges of between 18.6-23.4 micrograms/g 16.5-28.2 micrograms/g, respectively, and and rapidly decreased thereafter. Penetration of AZT into the pelvic dead space exudate was quickly recognized after intravenous injection of 1 g and its concentration 30 minutes after administration was 14.08 +/- 7.08 micrograms/ml and highest (22.35 +/- 5.85 micrograms/ml) 2 hours after administration. It gradually decreased to 8.50 +/- 2.07 micrograms/ml 6 hours after administration. Clinical effect was studied by administering 1-3 g 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.

Adult↗

[Fundamental and clinical studies on aztreonam in the field of obstetrics and gynecology].

Fundamental and clinical studies were performed on aztreonam (AZT), a new antibiotic with single beta-lactam ring, with the following results. Following intravenous drip infusion of 1 g, 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. 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. The above results demonstrated that AZT was a safe and effective drug.

Adult↗

[Study on transfer of aztreonam into female genital organs].

Aztreonam (AZT) is a newly developed beta-lactam antibiotic for use of intravenous injection. It is the first drug in the world of monobactam series with the structural characteristic of monocyclic beta-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. 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 68.0 micrograms/ml and 63.9 micrograms/ml, respectively. 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 50.0 micrograms/g, the cervix uteri 43.6 micrograms/g, the myometrium 29.8 micrograms/g, the oviduct 44.7 micrograms/g, the endometrium 27.3 micrograms/g, the ovary 29.0 micrograms/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.

Adult↗

[Fundamental and clinical studies on aztreonam].

Aztreonam (AZT), a new monocyclic beta-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. 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 1 g of AZT, the peak concentration of AZT in cubital venous blood was estimated 73.3 micrograms/ml at the end of infusion. The peak concentration of AZT in the pelvic dead exudate was estimated 18.6 micrograms/ml at 2.31 hours after infusion. Following intravenous 1-hour drip infusion of 1 g, 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. AZT was administered 2-4 g/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.

Adolescent↗

[Clinical studies on aztreonam in infections in obstetrics and gynecology].

Clinical 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.

Adult↗