rokitamycin and Respiratory-Tract-Infections

Topics: Animals; Bacterial Infections; Drug Resistance, Microbial; Humans; Leucomycins; Miocamycin; Mycoplasma pneumoniae; Respiratory Tract Infections; Staphylococcus

Rokitamycin (RKM), a newly developed macrolide antibiotic with a 16-membered ring, dissolves well under acidic conditions. It has been improved over other macrolides to minimize individual variations in its absorbability. We measured, using the GA-test, variations in gastric acidities of 43 children with ages between 1 to 14 years, and investigated the relationship between gastric acidities and pharmacokinetic values. Also activities (expressed in MICs) of antimicrobial agents were studied against clinically isolated 229 bacterial strains using an inoculum size of 10(6) cells/ml. Tested organisms included Streptococcus pyogenes (77 strains), Streptococcus agalactiae (29), Streptococcus pneumoniae (2), as Gram-positive cocci, and Haemophilus influenzae (1), Haemophilus parainfluenzae (1), Bordetella pertussis (12), Salmonella sp. (4) and Campylobacter jejuni (103) as Gram-negative bacilli. Against stock strains of bacteria, MICs of 10 drugs (RKM, erythromycin (EM), josamycin (JM), midecamycin (MDM), midecamycin acetate (MOM), clindamycin (CLDM), amoxicillin (AMPC), cefaclor (CCL), minocycline, ofloxacin (OFLX] were determined. Against isolates from patients who underwent treatment with RKM, MICs of only 4 drugs (RKM, EM, JM, MOM) were determined. Measurements were made on plasma and urinary concentrations of RKM and its urinary recovery rates after patients including 6 boys with ages between 5 years 1 month and 11 years 6 months were administered with RKM (dry syrup). Two groups of 6 boys were administered between meals with RKM at dose levels of 5 and 10 mg/kg, respectively. Clinical and bacteriological effects of RKM were evaluated for 175 patients including 5 cases of pharyngitis, 3 tonsillitis, 32 pneumonia, 17 mycoplasmal pneumonia, 34 atypical pneumonia, 28 streptococcal infections, 29 Campylobacter enteritis, 4 Salmonella gastroenteritis, and 23 enteritis due to unknown organisms. Five drop-out cases were excluded from the evaluations. In the evaluable cases, an average dose level used was 31.8 mg/kg/day, with a daily dose divided into 3 to 4 administrations and with an average treatment duration of 9 days. Adverse reactions of RKM and its effects on laboratory test values were investigated in these patients including the drop out cases. Obtained results of these studies are summarized below. 1. The GA-test produced pH values indicating that amounts of gastric acid were mostly either normal or high in 42 of the 43 subjects tested (97.7%), and only o

Topics: Administration, Oral; Blood Chemical Analysis; Campylobacter; Campylobacter Infections; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Enteritis; Female; Humans; Infant; Leucomycins; Male; Miocamycin; Multicenter Studies as Topic; Pneumonia; Pneumonia, Mycoplasma; Respiratory Tract Infections; Streptococcal Infections; Streptococcus; Tonsillitis

A new macrolide antibiotic preparation, TMS-19-Q.O tablet, was used to investigate the efficacy in the treatment of patients with respiratory tract infection, and the results obtained were as follows: Three hundred and seven cases were included in this report, and overall efficacy rate was 76.2%. Especially high clinical effect (86.0%) was observed in the treatment of patients with pneumonia including mycoplasmal pneumonia. Bacteriological effect was 87.5% in 51 cases identified as single infection of Gram-positive cocci and was 48.0% in 34 cases Gram-negative rods infection. Side effects were observed in 11 cases (3.50%): gastrointestinal disorder in 8, eruption in 2 and other in 1. Abnormality in laboratory tests was observed in 23 cases, hepatic disorder in 13, renal disorder in 3 and other laboratory tests in 7. It was considered from the results of clinical and bacteriological efficacy in different dose study that dose of TMS-19-Q should be 600 mg.

Topics: Adolescent; Adult; Aged; Anti-Bacterial Agents; Bronchitis; Child; Clinical Trials as Topic; Female; Humans; Leucomycins; Male; Middle Aged; Miocamycin; Pneumonia, Mycoplasma; Respiratory Tract Infections; Staphylococcus aureus; Streptococcus pneumoniae; Tablets; Tonsillitis

Twelve oral antimicrobial agents were tested for their antimicrobial activities against causative organisms isolated from pediatric infections. Activities of these antimicrobial agents against Streptococcus pyogenes were also examined in relation to T-antigen typing of the species. The results of the investigation are summarized as follows. 1. Against Staphylococcus aureus, rokitamycin (RKM), josamycin, ofloxacin, minocycline exhibited strong antimicrobial activities, and few strains of S. aureus showed resistance to these antimicrobial agents. More strains exhibited resistance to erythromycin (EM) than to other macrolide antibiotics (MLs) examined. Amoxicillin (AMPC)-resistance was often observed also. 2. Against S. pyogenes, beta-lactam antibiotics (beta-lactams) and RKM had MIC80 of 0.20 microgram/ml or below, and no resistant strains of this organism were observed against these antibiotics. Only 2 resistant strains (2.0%) of S. pyogenes to MLs were detected, but resistance to tetracyclines (TCs) was observed at a high frequency, with 71.4% or more strains among T-4, T-6, T-12 and T-28 antigen types exhibited resistance to TCs. Among the 21 strains of T-12 antigen type examined, only one strain (4.8%) was found resistant to MLs. These observations suggested that the reduction in the frequency of ML-resistant strains was not due to the reduction in the number of T-12 antigen type strains but due to losses of resistance factors against MLs of plasmids. 3. Antibacterial activities of beta-lactams and MLs against Streptococcus pneumoniae strains were good, similarly to activities against S. pyogenes. But many strains of S. pneumoniae were resistant to TCs. 4. New quinolone antimicrobial agents (quinolones) showed excellent activities against Branhamella catarrhalis strains with EM and RKM showing the next best activities. The number of resistant strains against quinolones, however, seemed to be on an increase. 5. Quinolones had strong antimicrobial activities against Haemophilus influenzae, few strains of which showed resistance to quinolones. AMPC had the next best activity, but approximately 10% of H. influenzae exhibited resistance to this antibiotic. 6. Against Campylobacter spp., quinolones and MLs showed the best activities with MIC80 values at or below 0.25 microgram/ml, and no resistant strains of the species against these antimicrobial agents were observed. Fosfomycin and TCs showed somewhat inferior activities to quinolones and MLs, with beta-lac

Topics: Anti-Bacterial Agents; Child; Drug Resistance, Microbial; Erythromycin; Haemophilus influenzae; Humans; Leucomycins; Miocamycin; Respiratory Tract Infections; Staphylococcus aureus; Streptococcus pyogenes

We have carried out laboratory and clinical studies on rokitamycin (RKM, TMS-19-Q). The results are summarized as follows. Serum and urinary concentrations of RKM were determined in 6 children with ages between 6 and 12 years given single oral doses of 5, 10 and 15 mg/kg. Mean serum concentrations peaked at 30 minutes after administration of 5, 10 and 15 mg/kg, and respective peak values were 0.30 microgram/ml, 0.79 microgram/ml and 1.32 micrograms/ml. Biological half-lives for 5, 10 and 15 mg/kg were 2.0 hours, 1.65 hours and 1.36 hours. The 6-hour urinary recovery ranged from 1.11% to 2.58% after administration of 5 mg/kg, and the mean 6-hour urinary recoveries were 1.35% after administration of 10 mg/kg and 2.28% after administration of 15 mg/kg. Therapeutic responses were recorded as excellent or good in 22 (73.3%) of the children, comprising 6 with tonsillitis, 2 with pharyngitis, 4 with bronchitis, 1 with bronchopneumonia, 1 with Mycoplasma pneumonia, 2 with whooping cough, 5 with streptococcal infections, 5 with Campylobacter enteritis, 3 with impetigo and 1 with SSSS. The microbiological effectiveness of RKM on identified pathogens comprising 4 strains of Staphylococcus aureus, 1 strain of Streptococcus pneumoniae, 6 strains of Streptococcus pyogenes, 4 strains of Haemophilus influenzae and 5 strains of Campylobacter spp. was not so satisfactory as evidenced by a eradication rate of 50.0%. No significant side effect due to the drug was observed in any cases. In conclusion, RKM was found to be efficacious and safe for the treatment of bacterial infections in children.

Topics: Administration, Oral; Blood Chemical Analysis; Bronchitis; Campylobacter; Child; Drug Evaluation; Drug Resistance, Microbial; Enteritis; Female; Humans; Leucomycins; Male; Miocamycin; Respiratory Tract Infections; Staphylococcus aureus; Streptococcal Infections; Streptococcus pyogenes; Tonsillitis

A total of 22 patients with acute pediatric infections was treated with rokitamycin (TMS-19-Q, RKM) dry syrup, a new macrolide antibiotic developed by Toyo Jozo Co., Ltd., Ohhito, Japan, to investigate its clinical efficacy. 1. A girl of an age 4 years 2 months (weighing 16.5 kg) was administered orally 10 mg/kg of RKM, and a boy of an age 8 years 7 months (weighing 24.5 kg), 15 mg/kg, and blood concentrations of RKM in these subjects were measured to investigate its absorption and excretion. Blood concentrations of the drug reached a peak of 0.84 microgram/ml in an hour after the administration in the girl, 0.72 microgram/ml in 30 minutes in the boy, with T1/2 of 0.86 and 1.82 hours, respectively. Their 6-hour cumulative urinary recovery rates were 2.79 and 2.13%, respectively. 2. A total of 20 patients was treated with RKM dry syrup. These patients included 3 with acute pharyngitis, one with acute tonsillitis, 4 with hemolytic streptococcal infections, 7 with acute bronchitis, 2 with pneumonia, another 2 with pertussis, and one with Campylobacter enteritis. The treatment was effective in 18 of them with a clinical efficacy of 90.0%. 3. Bacteriological responses to RKM dry syrup were as follows: eradication of pathogens in 5, pathogens decreased in 3, and no changes were observed in 3 of 12 patients from whom pathogens had been isolated prior to the treatment, thus the eradication rate was 45.5% with the exception of 1 patient whose bacteriological response was unknown.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Administration, Oral; Adolescent; Bronchitis; Child; Child, Preschool; Drug Evaluation; Humans; Infant; Leucomycins; Miocamycin; Pharyngitis; Respiratory Tract Infections

Laboratory and clinical studies on rokitamycin (RKM) dry syrup, a new macrolide antibiotic, were carried out in the field of pediatrics. The results are summarized as follows. 1. Plasma concentrations and urinary recovery rates after oral administration on fasting of RKM dry syrup at doses of 10 mg/kg and 20 mg/kg to 2 and 1 cases, respectively, were determined. Peak plasma levels were obtained in 30 minutes after administration of both dosages with half-lives of 1.5 to 2.2 hours. A clear-cut dose response was observed. Urinary recovery rates in the first 6 hours after administration ranged from 1.75 to 2.26%. 2. The MICs of RKM against 80 clinical isolates (Streptococcus pyogenes 9, Streptococcus pneumoniae 14, Branhamella catarrhalis 4, Haemophilus influenzae 27, Haemophilus parainfluenzae 9, Haemophilus haemolyticus 2, Haemophilus parahaemolyticus 14 and Campylobacter jejuni 1) were compared with MICs of midecamycin acetate (MOM), josamycin (JM) and erythromycin (EM). The antibacterial activity of RKM was superior to those of MOM and JM and slightly inferior to that of EM. 3. Twenty-eight pediatric patients with acute infectious diseases (acute tonsillitis 4, streptococcal infection 4, acute bronchitis 9, pneumonia 4, mycoplasmal pneumonia 2 and Campylobacter enteritis 5) were treated with RKM dry syrup at a daily dose of 12-42.9 mg/kg t.i.d. as a rule. Efficacy rates were 92.9% clinically and 58.6% bacteriologically. 4. No adverse reactions were observed. Abnormal laboratory findings were mild; thrombocytosis in 2 and eosinophilia in 1. 5. The taste and the odor of RKM dry syrup preparation were sufficiently tolerable for the pediatric patients to accept it.

Topics: Administration, Oral; Bronchitis; Campylobacter Infections; Child; Child, Preschool; Drug Evaluation; Enteritis; Humans; Leucomycins; Miocamycin; Pneumonia; Respiratory Tract Infections; Streptococcal Infections

Pharmacokinetic, bacteriological and clinical studies on a new macrolide antibiotic, rokitamycin (RKM) dry syrup for pediatric use, were done, and results as summarized below were observed: 1. Five children with ages between 6 and 10 years were administered orally with RKM at a dose level of 10 mg/kg either at 30 minutes before or 30 minutes after meal on a crossover design, and plasma concentrations and urinary excretion rates of the drug were measured. Plasma concentrations of RKM following the administration before meal were 0.50 microgram/ml at 1/2 hour, 0.43 microgram/ml at 1 hour, 0.15 microgram/ml at 2 hours, 0.03 microgram/ml at 4 hours, and not detectable at 6 hours. Plasma concentrations following the administration after meal were 0.11 microgram/ml at 1/2 hour, 0.15 microgram/ml at 1 hour, 0.09 microgram/ml at 2 hours, 0.03 microgram/ml at 4 hours, and not detectable at 6 hours. The 0-6 hour urinary recovery rates were 1.41% following the administration before meal, and 0.93% following the administration after meal. These results suggested that the drug might be absorbed more rapidly, giving a higher plasma concentration, when administered before meal than when administered after meal. Changes in plasma concentrations of RKM following the administration of 10 mg/kg before meal were similar to those of two 100 mg RKM tablets (TMS-19-Q.GC tablets) to adult patients. Therefore, it seemed optimal to administer 10 mg/kg 3 times daily at fasting to children as a rule.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Acute Disease; Administration, Oral; Blood Chemical Analysis; Bronchitis; Child; Child, Preschool; Drug Evaluation; Enteritis; Female; Humans; Leucomycins; Male; Miocamycin; Pharyngitis; Pneumonia; Respiratory Tract Infections

Rokitamycin (RKM) dry syrup was administered to a group of pediatric patients. The results obtained are summarized as follows. 1. Of the recent isolates of Streptococcus pyogenes, fewer strains were highly resistant to RKM than to josamycin (JM), midecamycin (MDM), erythromycin and lincomycin. Also, macrolides (MLs)-resistant strains proved to be susceptible to RKM. 2. Recent isolates of Staphylococcus aureus, Streptococcus agalactiae, group G Streptococci, S. pyogenes, Streptococcus pneumoniae and Haemophilus influenzae were more susceptible to RKM than to midecamycin acetate and JM. Oral administrations of 10-15 mg/kg of the drug were followed by its peak concentrations of 0.07-0.77 micrograms/ml in the blood at 30 minutes in many patients, and by an undetectable level at 6 hours also in many of them. T1/2 values were 1.2-2.6 hours, and first 6-hour urinary excretion rates were 1.26-1.74%. 3. Fifty-two patients with acute upper and lower respiratory tract infections, Campylobacter enteritis, etc. were treated with RKM at about 20-40 mg/kg daily for 4-14 days, with an overall efficacy rate of 88.5%. 4. An eradication rate of 81.4% was achieved for 43 strains of 7 species isolated from the patients. 5. No abnormal laboratory test values were observed after treatment with drug 4 approximately 14 days. A side effect, stomach discomfort, was observed in 1 patient.

Topics: Administration, Oral; Child; Child, Preschool; Drug Evaluation; Female; Haemophilus; Humans; Infant; Leucomycins; Male; Miocamycin; Respiratory Tract Infections; Streptococcus

1. A total of 15 patients with pediatric respiratory tract infections were mediated with rokitamycin (RKM) dry syrup, and its clinical effects were excellent in 2, good in 10, fair in 1 and poor in 1. 2. The efficacy rate in Streptococcus pneumoniae pneumonia and mycoplasmal pneumonia was 100%. 3. Clinical effects on 7 patients with Haemophilus influenzae were excellent in 1, good in 4, fair in 1 and poor in 1. 4. No adverse reaction was observed, and the taste and odor of RKM was well accepted by the children. 5. RKM is useful and one of the first choice antibiotics on respiratory tract infections in pediatric field.

Topics: Child; Drug Resistance, Microbial; Haemophilus influenzae; Humans; Leucomycins; Miocamycin; Respiratory Tract Infections; Streptococcus pneumoniae