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PubMed1990

[Pharmacokinetics and clinical studies on aztreonam in neonates].

Pharmacokinetic and clinical studies on aztreonam (AZT) were performed in neonates. Serum concentrations and urinary excretion of AZT were determined in 12 neonates with ages between 0 and 7 days (birth weights were between 1,260 and 3,500 g) upon intravenous injection or 1 hour drip intravenous infusion of AZT at 20 mg/kg. Serum concentrations of AZT at 1 hour after i.v. administration were 54.0 +/- 12.5 micrograms/ml, and half-lives were 6.01 +/- 0.70 hours. Serum concentrations of AZT reached their peaks at the end of drip infusion with levels of 42.1 +/- 17.6 micrograms/ml in the d.i.v. group and half-lives were 6.40 +/- 1.88 hours. Urinary recovery rates in the first 12 hours after administration were 28.5 +/- 6.4% for the i.v. group and 32.3 +/- 13.9% for the d.i.v. group. AZT was administered to 12 neonatal patients (2 cases of sepsis, 2 cases of suspected sepsis, 3 cases of pneumonia, 2 cases of urinary tract infection and 3 cases for prophylaxis), and clinical effectiveness, bacteriological efficacy and adverse reactions were evaluated. Clinical efficacies in 9 cases except 3 cases with prophylactic use were excellent in 1 case, good in 5 cases, fair in 1 case, poor in 1 case and unknown in 1 case, thus the efficacy rate was 75%. Bacteriological effects in 3 strains with Gram-negative bacilli were eradicated in 2 strains and unchanged in 1 strain, hence the bacteriological eradication rate was 66.7%. Increased GOT and GPT were observed in 1 cases as abnormal laboratory test results, but the abnormality was not serious.(ABSTRACT TRUNCATED AT 250 WORDS)

Aztreonam↗

PubMed1990

[Pharmacokinetic and clinical studies on aztreonam in neonates].

Pharmacokinetic and clinical studies on aztreonam (AZT) in mature and premature neonates were carried out. The results are summarized as follows. The mean serum peak level of AZT after intravenous administration at a single dose of 20 mg/kg in 3 to 4 day-old-neonates was 36.6 +/- 2.39 micrograms/ml at 1 hour after dosage. The mean serum level at 6 hours after dosage was 13.5 +/- 2.03 micrograms/ml. The mean half-life time was 3.86 +/- 0.92 hours. The mean urinary excretion rate was 25.1 +/- 5.18% in the first 6 hours after intravenous administration. AZT was administered in 4 cases, but the effects could not be evaluated. No side effect was observed except an elevation of GOT.

Ampicillin↗

PubMed1990

[Clinical evaluation of aztreonam in neonatal infections].

Serum concentration, urinary excretion and clinical application of aztreonam (AZT) were studied as follows: 1. Serum concentrations of AZT 1 hour after intravenous injection were 21.0 micrograms/ml in 1 case administered with approximately 10 mg/kg drug and 44.2 micrograms/ml on the average for 7 cases given approximately 20 mg/kg, indicating that serum concentrations are dose-dependent. Average serum half-life in 3 mature babies was 4.75 hours and that in 4 premature babies was 6.59 hours thus T 1/2 was longer in the latter. T 1/2 of 64 days of age newborn was 3.80 hours. Urinary recovery rates in 2 cases examined were 52.1 and 51.9%. 2. Daily dosages of AZT 39.9-63.3 mg/kg were intravenously administered to 10 newborns and prematures b.i.d. or t.i.d., 5 cases of which received AZT alone and the other 5 received AZT in combination with ampicillin (ABPC). Of the above 10 cases, AZT was given to 8 cases for treatment and to the other 2 cases for prophylaxis. Excluding 2 unascertainable cases, AZT showed good or better effectiveness in all the 6 cases in the treatment group, i.e., sepsis 1, suspected sepsis 1 and urinary tract infection 4 cases. All the identified pathogens (Escherichia coli 2 strains, Klebsiella pneumoniae 1 strain and Enterobacter 2 strains) were eliminated by the treatment. No onset of infection was observed in either of the 2 cases with prophylaxis. One of them was administered with AZT for 52 days consecutively but neither side effect nor abnormal laboratory test value was observed. 3. Side effect was not observed at all. One case each of minor degree of platelet increase and GOT elevation was recorded as an abnormal test value. The elevated GOT value continued to be high even after the completion of the administration and it was presumed to be due to the primary disease, heart failure. 4. As results of the above studies, AZT was considered to be effective and safe for neonatal infections caused by Gram-negative bacteria. It may be safer to initiate the treatment with AZT and ABPC in combination than with AZT alone before the identification of pathogen and to change the therapy to single administration of either AZT or ABPC when the pathogens are identified. With respect to method of administration, AZT 20 mg/kg 2 or 3 times a day appeared to show expected efficacy for the newborns with in 7 days after birth.

Ampicillin↗

PubMed1990

[Pharmacokinetics and clinical studies of aztreonam in neonates and premature infants].

Pharmacokinetics and clinical evaluation of aztreonam (AZT) in the neonates and premature infants were studied with the following results: 1. Serum concentrations of AZT in 60 minutes intravenous drip infusion of AZT 20 mg/kg to 6 cases of neonates with 2 to 22 days of age were 45.5 +/- 0.87 micrograms/ml immediately after the completion of intravenous drip infusion, 37.8 +/- 1.62 micrograms/ml 1 hour after, 31.2 +/- 1.92 micrograms/ml 2 hours after and 19.7 +/- 2.36 micrograms/ml 4 hours after, respectively. Serum half-life was 3.61 +/- 0.53 hours on the average. 2. Urinary excretion rate 6 hours after intravenous drip infusion was 26.4 +/- 6.86% on the average. 3. Clinical evaluation was given to 1 sepsis case of 7-days of age and it was effective. There was no abnormal clinical or laboratory finding considered to be associated with AZT.

Ampicillin↗

PubMed1990

[Preclinical and clinical studies on aztreonam in pediatric surgery].

Aztreonam (AZT) was administered to immature infants, neonates and infants for preclinical and clinical studies. 1. Sufficient serum concentrations were obtained upon 1-hour intravenous drip infusion of AZT 40 mg/kg to infants with biliary atresia. The average T1/2 was about 1 hour and urinary recovery rates were in a range between 35.2 and 61.3%. Biliary recovery rates were 0.03-0.4%. 2. AZT was given to 5 cases for prophylaxis and the results showed its prophylactic effect in 3 cases. 3. AZT is effective against Gram-negative bacteria and its efficacies in the treatment of 4 infection-cases were "excellent" in 2 cases and "effective" and "somewhat effective" in 1 case each. 4. Neither side effects nor abnormal laboratory test values were observed in any of the 9 cases given AZT.

Aztreonam↗

PubMed1990

[Pharmacokinetics and clinical evaluation of aztreonam in pediatric surgery].

Pharmacokinetic and clinical studies on aztreonam (AZT) in pediatric surgery were performed and results obtained are summarized below. 1. Plasma and urinary levels of AZT were measured in 6 neonate patients following drip-infusion for 1 hour of AZT (dose of AZT: 20 mg/kg). Plasma levels reached their peak (42.3-50.4 micrograms/ml) at the end of infusion or in 1 hour thereafter except in case 2. In case 2, plasma level reached its peak (36.6 micrograms/ml) at 2 hours after the end of infusion. Plasma levels of AZT decreased rapidly after reaching their peaks, and plasma half-lives (T 1/2) were 1.85-2.84 hours. Urinary recovery rates were 15.7-65.3%. 2. Bile levels of AZT were determined in 8 patients with biliary atresia following 1 hour drip-infusion of AZT (dose of AZT: 20 mg/kg for 4 patients, 40 mg/kg for the other 4 patients). In the 20 mg/kg group, peak levels of AZT in bile were noted 2 hours after the end of infusion, and they were 3.7-7.1 micrograms/ml. Recovery rates in bile in the first 6 hours after the end of infusion were 0.34-0.9%. In the 40 mg/kg group, peak levels of AZT in bile were found at 2 hours and 2-4 hours after the end of infusion, and they were 4.9-8.8 micrograms/ml. Recovery rates in bile in the first 6 hours after the end of infusion were 0.03-0.33%. 3. AZT and ampicillin were administered to 6 patients as prophylaxis against postoperative infections. Another patient with postoperative cholangitis was given AZT alone.(ABSTRACT TRUNCATED AT 250 WORDS)

Aztreonam↗

PubMed1990

[Pharmacokinetic and clinical studies on aztreonam in perinatal period].

Pharmacokinetic and clinical studies were carried out on aztreonam (AZT), a monobactam antibiotic with a high activity against Gram-negative bacteria. The results obtained are summarized as follows: 1. Following 2 g bolus intravenous injection, transfers of AZT to umbilical cord serum and amniotic fluid were found to be satisfactory. AZT level in amniotic fluid was higher than 1 micrograms/ml at 40 minutes after administration and it was at 3.7 micrograms/ml in 23.5 hours. 2. In the treatment of 9 patients with perinatal infections, clinical efficacies of AZT were judged excellent in 3 cases and good in 6 cases. 3. No side effects and abnormal laboratory findings due to the drug were observed in any case. These results indicate that AZT may be a useful antibiotic for the treatment of perinatal infections.

Adult↗

PubMed1990

[Basic and clinical studies on aztreonam in obstetric and gynecologic infections during the perinatal period].

The basic and clinical efficacies of aztreonam (AZT) were evaluated in obstetric and gynecologic infections during the perinatal period. The results obtained are summarized below. 1. Concentrations of AZT in umbilical venous blood and amniotic fluid showed a good placental transfer of AZT. The rate of placental transfer of AZT was very similar to rates for cephalosporins. 2. Since the clinical efficacy rate of AZT in the treatment of Gram-negative bacterial infections was 80.0%, AZT appears to be a useful drug against Gram-negative bacterial infections.

Adult↗

PubMed1990

[Clinical studies on aztreonam in perinatal use].

Clinical effects of aztreonam (AZT), a monobactam antibiotic, on perinatal infections were studied with the following results: 1. Efficacy rate of AZT in the clinical application to 12 cases of perinatal infections via 2-4 g/day drip infusion (total dosage 8-24 g) was 91.7% (11/12). Breakdown of the effects according to diseases were "excellent" for mastitis (n = 3), pyelonephritis (n = 1) and urinary tract infection (n = 1), and "good" for a total of 6 cases, i.e., amnionitis (n = 2), amniotic fluid infections (n = 3) and external genital infection (n = 1). 2. Results of bacteriological studies were "eradicated" (n = 1), "replaced" (n = 4), "appeared" (n = 2) and "unknown" (n = 5). MIC values of AZT (10(6) cells/ml) were in a range of 25- greater than 100 micrograms/ml in 1 case of cervicitis (complicated with amnionitis) in the 13th week of pregnancy where AZT was found non-effective. 3. Neither subjective nor objective side effects nor abnormal clinical values were observed during the treatment with AZT.

Adult↗

PubMed1990

[Transplacental transfer and clinical application of aztreonam].

Preclinical and clinical studies on aztreonam (AZT) in the perinatal period were carried out and the results are summarized below. 1. Concentrations of AZT in maternal serum, umbilical cord serum and amniotic fluid were measured after intravenous injection of AZT 1 g and 2 g, and intravenous drip infusion of AZT 1 g. As results, the transfer of AZT into umbilical cord serum started to increase in 1 to 2 hours, and the transfer of AZT into amniotic fluid started to increase after an elapse of 2 hours. Upon the intravenous injection of 2 g, AZT concentration in amniotic fluid was as high as 27.1 micrograms/ml even at 10 hours 30 minutes after the injection, and it was still 6.9 micrograms/ml at 20 hours or more after the injection. 2. AZT 2 g/day (b.i.d.) was administered by intravenous drip infusion to 1 perinatal infection case with pyelonephritis. It was clinically effective and neither side effect nor abnormal laboratory test value was observed.

Adult↗

PubMed1990

[Pharmacokinetic and clinical studies on aztreonam in the perinatal period].

Pharmacokinetic and clinical studies of aztreonam (AZT) in perinatal infections in the field of obstetrics and gynecology were performed with the following results. 1. At one shot intravenous injection, 1 g AZT showed rapid distribution to the umbilical-cord serum with concentrations higher than 15 micrograms/ml in 1 hour 36 minutes after injection and higher 10 micrograms/ml even in 4 hours 30 minutes after injection. Significant difference in concentrations was not observed between arterial serum sample and venous serum sample of the umbilical-cord in a single subject. The concentration in the amniotic fluid reached a level higher 10 micrograms/ml in 3 hours 37 minutes after injection. 2. Distribution into milk reached a concentration between less than 0.4 micrograms/ml to 1.0 micrograms/ml by 6 hours after administration. 3. AZT 1 g x 2/day was given by intravenous drip infusion to 4 cases of perinatal infection in obstetrics and gynecology for 5 to 9 days. Clinically, AZT was effective for all the cases. Neither side effect nor abnormal laboratory value was observed. Consequently, AZT was considered to be highly effective and safe for its clinical use in the parturition and the puerperium.

Adult↗

PubMed1990

[Pharmacokinetic and clinical studies on aztreonam in the perinatal period in obstetrics and gynecology].

Pharmacokinetic and clinical studies on aztreonam (AZT) in the perinatal period in obstetrics and gynecology were performed with the following results. 1. Concentrations of AZT in maternal serum, umbilical cord serum, amniotic fluid and neonatal serum were determined after 1 hour intravenous drip infusion of 1 g. The maternal serum concentration was 32.2 micrograms/ml at 26 minutes after administration, gradually decreasing thereafter to 13.2 micrograms/ml at 2 hours 33 minutes, 4.9 micrograms/ml at 3 hours 21 minutes and 2.9 micrograms/ml at 5 hours 3 minutes. Umbilical cord serum concentration was 17.0 micrograms/ml at 36 minutes after drip infusion and still remained at 4.0-16.1 micrograms/ml at 5 hours after administration. Amniotic fluid concentration was 9.9 micrograms/ml at 3 hours 21 minutes after drip infusion and showed 3.3 micrograms/ml at 16 hours 26 minutes after administration. Most of the maximum serum concentrations of newborns between 3 to 24 hours after delivery were not detectable, with only one case with 2.2 micrograms/ml at 9 hours after delivery. 2. AZT 1 or 2 g x 2/day was given by intravenous drip infusion to 12 cases of perinatal infections in obstetrics and gynecology for 5 to 8 days. Clinical efficacies were evaluated as excellent in 8 cases, effective in 2 and not effective in 2 with 83.3% efficacy rate. With respect to side effects, minor degree of urticaria was observed in 1 case. Another case showed a transient elevations of GOT, GPT and Al-P in laboratory tests.

Adult↗

PubMed1989

[Susceptibility of clinical isolates to aztreonam].

In vitro antibacterial activities of 9 antibiotics including aztreonam (AZT) against clinically isolated Gram-negative bacteria were determined using MIC-2000 plus system. Bacteria were isolated from clinical materials in Saga Medical School during a period from May 1987 to March 1988. Summarized results were as follows: 1. AZT showed excellent antibacterial activities against Escherichia coli, Klebsiella pneumoniae, Proteus sp. and Haemophilus influenzae, and MIC80 values of AZT against these organisms were lower than 0.20 microgram/ml. 2. Antibacterial activities of AZT were superior to cephem antibiotics compared against Enterobacter aerogenes, Enterobacter cloacae, Citrobacter freundii and Serratia marcescens. 3. The MIC50 and MIC80 of AZT against Pseudomonas aeruginosa were 12.5 micrograms/ml and 25 micrograms/ml, respectively. 4. AZT did not show any antibacterial activity against Acinetobacter sp. and Xanthomonas maltophilia.

Acinetobacter↗

PubMed1989

[Clinical reevaluation of aztreonam (AZT) on urinary tract infections].

The clinical effectiveness and safety of Aztreonam (AZT) were studied in 55 patients with complicated urinary tract infections. AZT was administered at a dose of 4 g/day for 5 days. The results as evaluated by the UTI criteria were excellent in 8 cases, moderate in 26 and poor in 21. The overall effectiveness rate was 61.8%. Out of 64 strains of bacteria isolated before treatment, 50 strains (78.0%) were eradicated by the treatment. Bacteriological eradication rates for gram negative rods and gram positive cocci were 79.6% and 66.7%, respectively. There were no obvious side effects, except for a temporary elevation of glutamic oxaloacetic transaminase, glutamic pyruvic transaminase alkalinephosphatase, and total bilirubin in some patients. The results indicate that AZT tablets are useful and safe for the treatment of complicated urinary tract infections.

Adolescent↗

PubMed1989

[Pharmacokinetic evaluations and analysis of aztreonam in children].

Aztreonam (AZT), monocyclic beta-lactam antimicrobial agent, was administered to 9 children at a dose level of 30 mg/kg through intravenous drip infusion for half-hour. Using serum levels of the drug obtained in blood samples, pharmacokinetic parameters were calculated and a simulation curve of serum levels was drawn automatically using a micro-computer. The mean values (n = 9) for elimination constant (Kel) and half-life (T 1/2) were 0.67 hr-1 and 1.08 hours, respectively. The mean apparent volume of distribution was 4.29 L, and serum clearance was 0.17 L/kg/hr. A basic analysis for the efficacy dose of AZT was performed using above mentioned parameters.

Adolescent↗

PubMed1989

[Clinical evaluation of a combination therapy with aztreonam and clindamycin for severe infections in leukemia and related disorders].

A combination of aztreonam (AZT) and clindamycin (CLDM) was evaluated for severe infections associated with leukemia and related disorders. AZT is a monobactam antibiotic which has strong bactericidal effect against Gram-negative bacteria including Pseudomonas aeruginosa. CLDM which has strong antibacterial spectrum against Gram-positive and anaerobic bacteria, was chosen as a partner of AZT in order to complement the weak points of AZT. Fifty six patients were treated with the combination therapy. Among them, 51 patients were evaluable for the effectiveness. Five patients were excluded from the evaluation because 3 patients were subjected to additional therapy with other agents such as amikacin, miconazole and pulse therapy of a large dose of methylprednisolone, one had a fever episode apparently due to primary disease, and the remaining one was discontinued of the combination therapy of administration due to mild nausea after 3 days. Excellent responses were obtained in 17 (33.3%) patients and good responses in 20 (39.2%) patients, with a total rate of effectiveness of 72.5%. One patient with whom the combination therapy was stopped due to nausea, was included in the final evaluation of side effects. Side effects were observed in 2 patients of 50 and 40 years of ages (2/52, 3.8%), both of whom suffered with nausea. In the 50 years patient of acute myeloblastic leukemia, nausea occurred in a slight degree in 3 hours after the combined regimen was started. But, it disappeared during the continuation of the combination therapy. In the 40 years patient of acute myelomonocytic leukemia, mild nausea occurred after 3 day administration of the combined regimen. It disappeared soon after the cessation of the treatment. These results indicated that a combination of AZT and CLDM was an effective and safe regimen for the treatment of severe infections in patients with hematological disorders.

Adult↗

PubMedDate not supplied

[Effect of sub-bacteriostatic doses of aztreonam on the adhesion of Pseudomonas aeruginosa].

The effect of sub-inhibitory concentrations of Aztreonam towards the adhesiveness of an uropathogenic strain of P. aeruginosa was tested. The filamentous forms, morphologically altered by the action of the antibiotic, were not capable of adhering to human uroepithelial cells. This phenomenon was due to an alteration of bacterial structures responsible for the adhesion and was not related to a steric hindrance caused by the antibiotic on either the bacterial structures or the cell receptors.

Aztreonam↗

PubMed1988

[Clinical efficacy of aztreonam in patients with complicated urinary tract infections].

Aztreonam (AZT) (2 g daily) was intravenously administered for 5 to 7 days to 65 patients with complicated urinary tract infections (UTI). Ninety one organisms were isolated from these patients' urine. Among them 66 organisms were eliminated following AZT administration. The elimination rate for Gram negative organisms was 94.7% and that for Gram positive organisms was 33.3%. Thirty one organisms appeared newly by the replacement of organisms. Among them, 12 organisms were E. faecalis. The efficacy rate of AZT in single infection and in mixed infection was 55.8% and 13.7%, respectively. The overall clinical efficacy rate of AZT in the present study was 41.5%. As side effects, skin rash and itching were observed in 3 patients and slight elevations in blood chemistry were observed in 10 patients. The results indicate that AZT is an effective drug for the treatment of patients with complicated UTI, especially those caused by Gram negative organisms.

Adult↗