rokitamycin and Streptococcal-Infections

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

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

Rokitamycin (RKM, TMS-19-Q) was used for the treatment of infections in patients with underlying diseases. Many antibiotics are tended to be used on these patients with underlying diseases mainly for prophylactic purposes and, as a consequence, microbes resistant to antibiotics frequently become pathogens in these cases. Responses of our patients to RKM, however, were generally excellent but one who had EB virus infection.

Topics: Administration, Oral; Child; Drug Evaluation; Female; Humans; Infectious Mononucleosis; Laryngitis; Leucomycins; Male; Miocamycin; Streptococcal 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

Rokitamycin dry syrup (RKM), a new macrolide antibiotic preparation, was evaluated for its safety, efficacy and pharmacokinetics in 19 children. RKM was effective in mycoplasmal pneumonia, Chlamydia trachomatis pneumonitis and Campylobacter gastroenteritis. Efficacies of RKM in streptococcal pharyngitis and Haemophilus influenzae pneumonia, however, were insufficient. Pharmacokinetic observations seemed to indicate that RKM achieved higher blood concentrations than older macrolides, but a large individual variation was observed. Diarrhea which was the only type of side effect observed in our cases, was encountered in 2 of 17 evaluable cases. From these data, RKM seems to have a place in the treatment of pediatric infectious diseases.

Topics: Campylobacter Infections; Child; Child, Preschool; Chlamydia Infections; Drug Evaluation; Female; Haemophilus Infections; Humans; Infant; Infant, Newborn; Leucomycins; Male; Miocamycin; Pneumonia, Mycoplasma; Streptococcal Infections