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[Interactions in the system of copper ion-azalide (azithromycin)].

Interactions in the bio-inorganic systems of the copper ions and azalide (azithromycin) were analyzed by spectroscopic methods (atom-absorption spectroscopy, IR and UV spectrometry in the visible spectrum) and electrochemical methods (potentiometry). The system samples within molar ratios of the metal ion and ligand of 10:1 to 1:10 and wide pH ranges were tested. Formation of a compound consisting of the metal ion and ligand at a ratio of 1:1 was detected. The experimental data showed that the product of the compound solubility equaled 9.8.10(-14) (pH 7.0, 0.1 KNO3).

Azithromycin↗

Plasmid loss from gram-negative bacteria exposed to subinhibitory concentrations of beta-lactam drugs and azithromycin.

The stability of F'lac, pW101 and pHSG298 in Escherichia coli K12 exposed to subinhibitory concentrations of beta-lactam antibiotics, amikacin and tetracycline was studied. High molecular weight low copy plasmids (F'lac and pW101) were eliminated from bacteria treated with PBP-3 binding molecules, while a low molecular weight high copy extrachromosomal element (pHSG298) was not. None of the carbapenem antibiotics, mecillinam, amikacin or tetracycline promoted high rate plasmid loss from their hosts. Under the same conditions, plasmid-mediated ampicillin-resistance due to beta-lactamase production was also lost from F'lacTn1-carrying bacteria. In contrast, the high copy R6K plasmid was stably inherited in their hosts with the exception of those organisms treated with cefixime. When the same experiments were performed with a Klebsiella pneumoniae strain induced to form filaments by azithromycin at sub-MICs, F'lacTn1 and pW101 loss was detected, while pHSG298 was stably inherited. These results confirm previous observations that plasmid stability is correlated with cell shape and that recovery is more easily achieved when bacteria undergo an unbalanced division resulting in cell filamentation.

Anti-Bacterial Agents↗

[Comparative study of the antimicrobial activity of pefloxacin, ciprofloxacin, norfloxacin and azithromycin with respect to Strains of Yersinia pseudotuberculosis].

Ciprofloxacin (C), pefloxacin (P) and norfloxacin (N) had a marked effect on Yersinia pseudotuberculosis strains isolated from the infected humans and animals. The activity of C (MIC 0.0312-0.125 microgram/ml) was higher than that of P and N (MIC 0.0625-2.0 micrograms/ml). The isolates were resistant to azithromycin (MIC 3.1-100 micrograms/ml). The susceptibility of the strains did not depend on the source of their isolation. The polyresistant strains carrying the R plasmids preserved the susceptibility to the fluoroquinolones.

Animals↗

[Bacteriological, pharmacokinetic and clinical evaluation of azithromycin in the pediatric field].

Azithromycin (AZM), a new macrolide antibiotic, in fine granules and in capsules was studied for pharmacokinetic and clinical evaluation in the pediatric patients. Antibacterial activity of AZM against 43 clinical isolates: AZM exhibited slightly lower activity against Gram-positive bacteria and 2-8-fold higher activity against Gram-negative bacteria than erythromycin or clarithromycin. Plasma or urine samples were collected from eight patients receiving the drug in fine granular form, and two patients receiving it in capsules for the determination of drug levels. The elimination half-lives of AZM after administration at dose of 10 mg/kg/day for 3 days were 50.0 and 51.2 hours for fine granules, and 41.5 hours for capsules. AUC0-infinity was 11.7 and 24.3 micrograms.hr/ml for fine granules, and 8.3 micrograms.hr/ml for capsules. The cumulative excretion rates up to 120 hours after the start of treatment were 8.24 and 13.84% for fine granules, and 3.83% for capsules. AZM was administered to 123 patients once daily at 3.7-20.0 mg/kg body weight over 3 to 5 days with reference to the standard dose of 10 mg/kg. The drug was used to treat patients with pharyngitis, tonsillitis, scarlet fever, pneumonia, mycoplasmal pneumonia, chlamydial pneumonia, otitis media, pertussis, intestinal infection, and SSTI. The effectiveness of AZM was evaluated in 109 cases. The drug was rated "excellent" in 65.1% of the patients and "good" in 29.4%, resulting in an efficacy rate of 94.5%. Furthermore, AZM eradicated 43 of 46 (93.5%) bacteria that had been identified before the treatment. Three patients complained of side effects of urticaria (1 case) and diarrhea (2 cases). Abnormal laboratory changes were reported as follows: decreased leukocyte (3 cases), increased eosinophil (5), increased platelet (2), increased eosinophil and platelet, elevated GPT (1), and elevated GOT and GPT (1). The abnormalities, however, were mild enough to raise no clinically significant problems. In conclusion, AZM in once daily regimen was effective and safe in treatment of pediatric infections.

Administration, Oral↗

[Clinical evaluation of azithromycin in pediatric infections].

Azithromycin (AZM) was studied for its clinical efficacy in pediatric infections. The study on AZM was carried out in 43 patients whose diagnoses were given as follows: pharyngitis in five cases, tonsillitis in one, bronchitis in four, pneumonia in four, Mycoplasma pneumonia in 14, scarlet fever in nine, impetigo in four, pyodermia in one and Campylobacter enteritis in one. The patients received AZM once daily at 1.6 approximately 20.0 mg/kg body weight for three to five days. Effectiveness of AZM was evaluated in 39 cases and the drug was rated "excellent" in 15, "good" in 19, "fair" in one, "poor" in four, resulting in an efficacy rate of 87.2%. Twenty bacterial isolates were identified as causative isolates in 19 patients: Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, Campylobacter jejuni and Mycoplasma pneumoniae. AZM eradicated 16 isolates but four persisted after therapy. One patient complained of loose stool, while two patients were found with decreases in white blood cell counts, and seven showed increases in eosinophils. However, no serious case of adverse event was reported.

Administration, Oral↗

[Therapeutic efficacy of azithromycin in pediatrics].

Azithromycin (AZM), a newly developed azalide antibiotic, was administered at a standard dose of 10 mg/kg once daily for 3 days to pediatric patients with bacterial infections and the therapeutic efficacy of AZM was investigated. 1. A total of 12 patients with the following diseases was evaluated: pharyngitis in two, tonsillitis in four, bronchitis in one, Mycoplasma pneumonia in one, scarlet fever in two and enteritis in two. The drug was rated "excellent" in eight cases and "good" in four. 2. Eleven strains were isolated from patients: five strains of Streptococcus pyogenes, four strains of Haemophilus influenzae, and two strains of Haemophilus parainfluenzae. Isolated bacteria were eradicated in eight strains and persisting in one, resulting in 88.9% in eradication rate. No follow-up examinations in post-treatment were performed in two cases. 3. No adverse reaction was reported, while one case of eosinophilia was noted as an abnormal laboratory test value. 4. As far as compliance is concerned, patients claimed that the formulation of the drug is "easy to take" or "ordinary". With the results presented as above, we have concluded that AZM is a useful antibiotic in pediatric patients with bacterial infections.

Administration, Oral↗

[Therapy with azithromycin in pediatric infections].

Azithromycin (AZM) was orally administered to 12 pediatric patients with the following bacterial infections: pharyngitis in four cases, tonsillitis in one, pharyngo-bronchitis in two, and mycoplasmal pneumonia in five. In eleven of the twelve cases (91.7%) was the drug found effective. Neither abnormal clinical findings nor abnormal laboratory test results changes were observed. Eleven of the twelve pediatric patients claimed that the formulation of the drug is easy to take. The above results suggest that AZM is a useful antibiotic drug in the treatment of pediatric patients with bacterial infections.

Anti-Bacterial Agents↗

[Clinical studies on azithromycin in pediatrics].

Fine granules or capsules of azithromycin (AZM) were given to 32 pediatric patients for the treatment of the following diseases: pharyngitis in three cases; tonsillitis in one; bronchitis in six; pneumonia in six; mycoplasmal pneumonia in 14; pertussis and enteritis in one, each. Effectiveness of AZM was evaluated in 30 cases and the drug was rated "excellent" in 18 patients, "good" in 11 and "fair" in one, resulting in a total efficacy rate of 96.7%. Three strains of bacteria were isolated from 3 patients as the causative organisms including: Streptococcus pneumoniae, Haemophilus influenzae and Haemophilus parainfluenzae, from three different patients, respectively. One patient complained of mild diarrhea, another patient mild urticaria. Abnormal laboratory test results were reported as follows: one patient showed a slight decrease in leukocyte count, three patients showed slight increases in eosinophils, and one patient had slight elevations in GOT and GPT. The above results suggest that AZM is a useful antibiotic drug in the treatment of pediatric patients with various bacterial infections.

Anti-Bacterial Agents↗

[Pharmacokinetic and clinical evaluation of azithromycin using fine granules or capsules in the pediatric patients].

Azithromycin (AZM), a new macrolide antibiotic, in fine granules and in capsules was studied for pharmacokinetic and clinical evaluations. 1. Antibacterial activities. MIC profile of AZM was as follows: 0.78 approximately 1.56 micrograms/ml against Staphylococcus aureus, < or = 0.025 approximately 0.10 microgram/ml against Streptococcus pyogenes, 0.10 approximately 0.39 and 6.25 micrograms/ml against Streptococcus pneumoniae, < or = 0.025 approximately 0.39 microgram/ml against Moraxella(Branhamella) catarrhalis, 0.39 approximately 3.13 micrograms/ml against Haemophilus influenzae, and 0.20 approximately 6.25 micrograms/ml against Haemophilus parainfluenzae. 2. Absorption and excretion. The elimination half-life of AZM after its administration at 10 mg/kg/day for three days was 28.1 approximately 46.1 hours. The cumulative urinary excretion rate in the first 120 hours after start of treatment was 4.01 approximately 8.47%. 3. Clinical evaluation. AZM was given to 76 pediatric patients to treat following infections: pharyngitis in seven, tonsillitis in 11, bronchitis in 11, pneumonia in 19, Mycoplasma pneumonia in eight, scarlet fever in 13, infective enteritis in one, SSTI in four, and otitis media in two. Effectiveness of AZM was assessed in 75 patients and the drug was rated "excellent" or "good" in 71 resulting in an efficacy rate of 94.7%, 87.0% of the 46 cases indicated that AZM had eradicated bacteria identified before the treatment. One patient complained of moderate diarrhea which disappeared after treatment of anti-diarrheic. Abnormal laboratory changes were reported in 12 patients in the following: decreased leukocytes in eight, increased eosinophils in two, increased platelet count in one, and increased GPT in one. All cases of abnormality was deemed mild in severity and clinically insignificant.

Anti-Bacterial Agents↗

[Pharmacokinetic and clinical evaluation of azithromycin in pediatrics].

Azithromycin (AZM), a new macrolide antibiotic, in fine granules and in capsules was administered at a standard dose of 10 mg/kg once daily for 3 days to pediatric patients with bacterial infections. AZM was studied for its pharmacokinetic and clinical evaluation. 1. AZM possessed potent activity against Gram-positive bacteria and Gram-negative bacteria that had been clinically isolated. 2. Plasma samples were collected from two patients diagnosed as having pneumonia or enteritis, and urine samples were collected from one patient diagnosed as having pneumonia for drug level determination. The drug concentrations in plasma were 0.095 and 0.204 microgram/ml just before the end of treatment, and 0.017 and 0.096 microgram/ml at 48 hours post-treatment. The drug concentrations in urine were 5.16 micrograms/ml and 5.63 micrograms/ml during a period between 24 and 48 hours and between 48 and 72 hours after the start of treatment, respectively. 3. The drug was found effective in 37 of 38 cases with various pediatric infections. AZM treatment eradicated bacteria in 17 of 30 strains (56.7%). 4. One patient complained of mild vomiting, while abnormal laboratory test results indicating mild eosinophilia were reported in four cases.

Anti-Bacterial Agents↗

[Clinical study of a macrolide antibiotic, azithromycin, in pediatric patients].

Azithromycin (AZM), 10% fine granules or 100 mg capsules, were given orally to 27 children with various pediatric infections. The results of the study are shown below. 1. Pharmacokinetic investigation. We studied plasma and urinary concentrations after 100 mg AZM capsules were given. One patient received 8.3 mg/kg of AZM once a day for 3 days, and AZM concentration in plasma was 0.033 microgram/ml 48 hours after the final dosing. Doses of 8.3 and 12.5 mg/kg body weight of AZM were respectively given to two patients once daily for 3 days. As a result, AZM concentrations in urine during a period between 96 and 120 hours post-dosing were 1.67 and 4.53 micrograms/ml, respectively, and urinary excretion rate in 120 hours after the first dosing was 10.54% in the patient that was given 12.5 mg/kg. 2. Clinical investigation. Clinical efficacies were examined in 24 patients. Excellent results were obtained in 7 patients, good results in 14 patients, hence the clinical efficacy rate was 87.5%. Bacteriologically, Haemophilus influenzae strains isolates from 2 patients were eradicated in 1 and decreased in the other. Safety was evaluated in 26 patients. An adverse reaction was observed in 1 patient (urticaria). Abnormal laboratory test results were observed in 2 patients, decreased WBC in 1 and elevation of eosinophils in the other. The above results suggest that AZM is a useful oral antibiotic for pediatric patients with infection with susceptible organisms.

Adolescent↗

[A clinical evaluation of azithromycin in the treatment of pediatric infection].

Fine granule preparation of azithromycin (AZM), a new macrolide antibiotic, was given to treat various infections in pediatric patients. Efficacies of AZM in a total of 21 patients (tonsillitis in six, bronchitis in five, pneumonia in five, impetigo contagiosa in three, staphylococcal scalded skin syndrome in one and bacterial enterogastritis in one) were rated "excellent" in 11 patients and "good" in eight. The remaining two cases were not included in the evaluation. AZM eradicated all strains of infection-causative bacteria identified in the 21 patients: Staphylococcus aureus in two, Streptococcus pneumoniae in four, Moraxella (Branhamella) catarrhalis in four, Haemophilus influenzae in six, Haemophilus parainfluenzae in three and Mycoplasma pneumoniae in one. One patient complained of mild diarrhea, while two patients showed increases in eosinophils as abnormal laboratory changes.

Anti-Bacterial Agents↗

[Pharmacokinetic and clinical evaluations of azithromycin in the pediatric field].

Azithromycin (AZM), an oral macrolide antibiotic drug, was studied for its efficacy and pharmacokinetics in the treatment of pediatric patients with respiratory tract infections. The results of the study are presented. Fifteen pediatric patients in an age range between 1 and 10 years were given 8.9 to 14.7 mg/ kg body weight of AZM once daily for 3 to 4 days. Pharmacokinetics of AZM in three patients were examined. AZM concentration in plasma was 0.037 microgram/ml at 72 hours after final dosing, while urine concentration was 10.9 micrograms/ml measured during a period between 72 and 96 hours post-dosing. Fourteen patient cases were included in analysis of drug efficacy for AZM. AZM was found "markedly effective" in all seven patients with pneumonia, and "effective" in all three patients with acute bronchitis, two patients with mycoplasmal pneumonia, and one patient with tonsillitis. In one patient with mycoplasmal bronchitis, AZM was found slightly effective. The efficacy rate was 92.9% (13/14). The study found one case of side effect, moderate diarrhea. No laboratory abnormality was documented. In conclusion, an antibiotic AZM was found useful in a treatment of pediatric respiratory tract infections.

Anti-Bacterial Agents↗

[Pharmacokinetic and clinical evaluation of azithromycin in pediatric infections].

Azithromycin (AZM) was studied for its concentrations in plasma and urine, efficacy and safety. 1. Plasma and urine samples were collected from one patient diagnosed as having Mycoplasma pneumonia for drug level determination. The drug was given once daily at 9.7 mg/kg body weight for three days. The drug concentrations in plasma was 0.149 microgram/ml in 12 hours after the start of the treatment, and 0.095 microgram/ml at the point of 24 hours after the end of the treatment. Urinary recovery rate up to 72 hours post-dosing was 6.39%. 2. The effectiveness of AZM was assessed in 19 patients with following diagnoses: pharyngitis in two patients, bronchitis in four, pneumonia in seven and Mycoplasma pneumonia in six. The drug was rated "excellent" in 11, "good" in seven, "poor" in one, resulting in an efficacy rate of 94.7%. 3. AZM eradicated two strains of Streptococcus pyogenes and Streptococcus pneumoniae identified in patients. 4. The AZM MIC's were 0.39 microgram/ml against Staphylococcus aureus, 0.20 microgram/ml against S. pneumoniae, < or = 0.0008 microgram/ml against Mycoplasma pneumoniae. 5. One patient complained of mild diarrhea, while another showed a slight increase in eosinophils, suggesting an abnormal laboratory change. In conclusion, AZM was found useful in treatment of pediatric infections.

Adolescent↗

[Pharmacokinetic and clinical studies on azithromycin in children].

Azithromycin (AZM) is a new oral macrolide antibiotic drug. AZM either in 10% fine granules form or in 100 mg capsule form was studied for its pharmacokinetics and treatment efficacy in pediatric patients with various infections. 1. Pharmacokinetics. Plasma and urine samples were collected from four patients with pharyngitis and post-dosing drug levels were determined. The drug was given once daily at 10 mg/kg body weight for 3 days. The drug concentrations found in plasma at 96 hours after the first dosing (48 hours after the final dosing) lay in a range of 0.02 and 0.04 microgram/ml and in urine at 120 hours after the first dosing (72 hours after the final dosing) in a range between 3.2 and 7.7 micrograms/ml. AZM was found in two patients but no effect was observed on blood levels of theophylline determined between 48 and 96 hours after the first dosing in the treatment of underlying bronchial asthma. 2. Clinical study results. Clinical studies of AZM was carried out in 25 pediatric patients with bacterial infections that mainly affected the respiratory tract. The patients received either 10% fine granules at 10 or 20 mg/ kg body weight or 100 mg capsules at 10 mg/kg body weight once daily over 3 to 6 days. The drug was found markedly effective in six patients, moderately effective in thirteen patients, while the investigators could not assess the drug efficacy in six patients. Although no side effect was reported in the study, two patients experienced slight decrease in WBC.

Adolescent↗

Evaluation of safety and efficacy of azithromycin in lower respiratory tract infections (LRTI)

Azithromycin was given to 55 cases of lower respiratory tract infections in the doses of 500 mg on day 1, followed by 250 mg on days 2-5. It produced bacteriological cure in 70.8% patients and clinical cure or improvement in 69.09% of patients. 4.27% of patients had throat colonisation with new organisms, of which 9.09% needed a second antibiotic. The drug was well tolerated and minor side effects were noted. Gastrointestinal disturbances (16.36%) headache and giddiness (14.55%), rash (3.64%) were the noted side effects. Reduction of platelet count by 50% occurred in 12.29% of the cases compared to 0.2% reported earlier. But this thrombocytopenia was clinically not significant, as it did not cause any symptoms.

Adolescent↗

[Pharmacokinetic, bacteriological and clinical studies on azithromycin in children].

Azithromycin (AZM) in fine granules was studied for its pharmacokinetics and clinical efficacies in eight child patients with ages between 1 month and 8 years. Informed consent was received from all of their parents. AZM was administered to the patients once a day at a dose of 10 mg/kg for 3 days. The clinical efficacies of AZM in 8 patients with microbial infections (pneumonia in one, Mycoplasma pneumonia in two, acute tonsillitis in one, pertussis in one, Campylobacter enteritis in one, infectious enteritis in one, Salmonella enteritis in one) were evaluated as "excellent" in five cases, "good" in two and "not evaluable" in one. As for the microbial efficacy, isolated strains were eradicated in 2 out of 3 patients. No adverse reaction was found except for one case with abnormal laboratory change, that is mildly increased GPT value. Plasma samples were collected from 3 cases. The elimination half-life of AZM was 45.8 hours. AUC0-infinity was 12.6 micrograms.hr/ml. Urine sample was collected from one. AZM concentration in urine was 35.0 micrograms/ml during a period between 48 and 72 hours after the start of treatment.

Anti-Bacterial Agents↗

[Pharmacokinetic and clinical evaluation of azithromycin in the pediatric field].

35 children between 9 months and 12 years of ages were given 9.1 to 12.2 mg/kg of azithromycin (AZM) once a day for 3 days. In the treatment of pediatric infectious diseases, we studied pharmacokinetics, efficacy and safetiness of AZM. After administration of 10 mg/kg/day of AZM for 3 days, the elimination half-life was calculated to be 3.8 +/- 16.3 hours (n = 6, mean +/- S.D.). The excretion rate of AZM in the urine within 120 hours of administration was 9.0 +/- 2.3% (n = 5). For the evaluation of efficacy of AZM, we treated 33 cases of children with pharyngotonsillitis, bronchitis, mycoplasma bronchitis, pneumonia, mycoplasma pneumonia, atypical pneumonia, and SSTI. The efficacy rate of these cases were 93.9%. 6 strains of bacteria were identified as causative agents. All strains were eradicated upon the treatment. One case of elevated GOT and GPT and two cases of elevated GPT were observed. No clinical adverse reactions were observed. In conclusion, AZM was useful for the treatment of pediatric infectious diseases were examined.

Anti-Bacterial Agents↗