rokitamycin and Pneumonia

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

Topics: Bacterial Infections; Clinical Trials as Topic; Double-Blind Method; Humans; Leucomycins; Miocamycin; Pneumonia; Pneumonia, Mycoplasma

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

A dry syrup preparation for infants and children of a newly developed 16-membered macrolide antibiotic, rokitamycin, was administered to 5 neonates and low birth weight infants of 6 to 25 days after births at a dose level of 10 mg/kg on an empty stomach then plasma drug levels were determined. The dry syrup preparation was also given to a total of 19 Chlamydia trachomatis infection cases of 7 days to 8 months old neonates, low birth weight infants and infants including 12 cases of pneumonia, 2 cases of conjunctivitis and 5 non-symptomatic carriers at an average daily dose level of 48.1 mg/kg in 2 to 4 doses for an average of 19 days and its clinical effects, bacteriological effectiveness, side effects and effects on laboratory test values were examined. The obtained results are summarized as follows. 1. Because the test subjects were neonates and premature infants, obtainable amounts of blood samples were limited, thus it was not possible to determine time courses of plasma drug levels to reach their peaks. Peak plasma levels, however, were speculated to be similar to those in children. Plasma half-lives of the drug were also not determinable, but they seemed to be somewhat longer than those in children. 2. Clinical efficacies were determinable in the 2 cases of conjunctivitis and 10 of the 12 cases of pneumonia, with excellent or good results in both cases of the former and with excellent or good results in 9 of the 10 determinable cases of the latter. Thus, the overall efficacy rate was high, 91.7%. 3. Bacteriological efficacies were determinable in 18 cases including non-symptomatic carriers. C. trachomatis was eradicated in 16 of the cases with an overall efficacy rate of 88.9%. 4. Diarrhea was observed in 2 cases, which were suspected as side effects of the drug. 5. No abnormalities were observed in the laboratory test results. Judging from the above results, this drug appears to be useful for the treatment of C. trachomatis infections of neonates, low birth weight infants and infants.

Topics: Chlamydia Infections; Chlamydia trachomatis; Conjunctivitis, Bacterial; Drug Resistance, Microbial; Humans; Infant; Infant, Newborn; Infant, Premature; Leucomycins; Miocamycin; Pneumonia

The usefulness of a new macrolide antibiotic rokitamycin (RKM, TMS-19-Q) was evaluated in the field of pediatrics. 1. Twenty seven patients were enrolled in the study. One patient was excluded from the study because the illness was due to a viral infection. They included 14 boys and 13 girls with ages 7 months to 9 years 11 months. 2. The patients were treated with RKM at daily doses ranging 19.2-41.1 mg/kg, divided into 3 equal portions. The administration was done orally at fasting, lasting 2-15 days, with total doses of 22.2-500.0 mg/kg. 3. The patients were diagnostically classified into the following categories: 9 with acute pharyngitis, 15 with acute bronchitis, and one each with pneumonia, purulent lymphadenitis and Campylobacter enteritis. 4. The clinical response to the treatment was good or excellent in 22 of the patients with an overall efficacy rate of 81.5%. An efficacy rate of 88.9% was achieved for the patients with acute pharyngitis, 80.0% for those with acute bronchitis, and 100% for the patient with purulent lymphadenitis and the patient with Campylobacter enteritis. From the patient with pneumonia whose response was evaluated "fair" was Haemophilus influenzae isolated by culturing pharyngeal material. This organism was found resistant to RKM by the disk method. 5. Bacteriological responses were as follows; of 26 isolates presumed to be pathogens, 9 were eradicated, 5 decreased, 7 unchanged and 5 unknown, with an eradication rate of 42.9%. 6. Neither adverse reactions nor abnormal changes in laboratory findings were observed with the medication in any patients during and after the end of the treatment.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Bacterial Infections; Bronchitis; Child; Child, Preschool; Drug Evaluation; Enteritis; Female; Humans; Infant; Leucomycins; Lymphadenitis; Male; Miocamycin; Pharyngitis; Pneumonia