rokitamycin and Enteritis

The clinical efficacy, safety and usefulness of Rokitamycin (RKM), a new macrolide antibiotic, were compared with those of Ofloxacin (OFLX) for the treatment of Campylobacter enteritis by a double blind method. The daily dose level of RKM or OFLX was 600 mg. They were orally administered in three divided doses for 5 days. Of 223 cases studied, 106 cases were diagnosed as Campylobacter enteritis. Ninety cases (RKM group: 50, OFLX group: 40) except for 16 excluded or drop-out cases were analysed. There was no significant difference between the two groups in any background factors. The effectiveness and usefulness was evaluated in 88 cases (RKM group: 48, OFLX group: 40). The results obtained were as follows: 1. In a total of 82 strains of Campylobacter jejuni/coli (RKM group: 42, OFLX group: 40), the bacteriological efficacy rate of RKM (95.2%) was superior to that of OFLX (70.0%) with a significant difference (p = 0.006). 2. In 76 symptomatic patients (RKM group: 42, OFLX group: 34) on the day of the beginning of drug administration, the clinical efficacy rate was 97.6% in the RKM group and 85.3% in the OFLX group with no significant difference between the two groups. 3. In 88 evaluable patients, the global clinical efficacy rate of RKM (95.8%) was superior to that of OFLX (67.5%) with a significant difference (p = 0.001). 4. Side effect was observed in 1 (1.9%) of the 54 patients in the RKM group and none of the 44 patients in the OFLX group. Slightly abnormal laboratory findings were seen in 4 (10.8%) of the 37 patients treated with RKM and 3 (9.7%) of the 31 patients treated with OFLX, but there was no significant difference between the two groups. 5. In 88 evaluable patients, the clinical usefulness of RKM (91.7%) was superior to that of OFLX (67.5%) with a significant difference (p = 0.01). From these results, RKM is considered to be a very useful agent for the treatment of Campylobacter enteritis.

Topics: Adolescent; Adult; Aged; Campylobacter coli; Campylobacter Infections; Campylobacter jejuni; Double-Blind Method; Enteritis; Female; Humans; Male; Middle Aged; Miocamycin; Ofloxacin

Because Campylobacter jejuni is most frequently identified as a causative organism of bacterial enteritis in pediatrics, a study was done to evaluate the clinical efficacy against Campylobacter enteritis and the safety of a macrolide antibiotic, rokitamycin (RKM). In case of acute enteritis, RKM was used in a form of dry syrup at a dose level of approximately 30 mg (in potency)/kg body weight and its efficacy and safety were compared to those of fosfomycin (FOM) dry syrup which is currently in use at a dose level of 60 mg (in potency)/kg. Both drugs were administered, as a rule, in 3 divided daily dose (RKM before meal and FOM after meal) for 5 consecutive days. Comparisons of the drugs were made using a well-controlled method. Obtained results are summarized as follows. 1. No significant differences in background factors of the 2 drug groups were apparent, hence it was deemed that no obstacles existed in making comparative studies of the 2 groups with regard to their efficacies and safeties. 2. Overall efficacy rate against Campylobacter enteritis was 100% in the RKM group with a rate of excellent efficacy of 91.3% and the former was 94.4% in the FOM group with the latter of 72.2%. Though the RKM group apparently showed higher rates by 5.6% and 19.1%, respectively, for overall and excellent efficacies, they were not statistically significant as both drugs showed good efficacies. When acute cases of enteritis other than those caused by Campylobacter were included in the analysis, overall efficacy rates and rates of excellent efficacy were, respectively, 97.6% and 85.7% for the RKM group and 88.6% and 68.2% for the FOM group, thus RKM showed higher efficacy rates by 9.0% and 17.5%, respectively. These differences were deemed statistically significant using the U-test. 3. Numbers of days required for most of the major symptoms to subside were 3 days or less for the group for which RKM was used against Campylobacter enteritis. Similar results were observed for the FOM group also. In cases of acute enteritis due to other causes than Campylobacter, slower recoveries were observed for both the RKM and the FOM groups than in Campylobacter enteritis cases, with the latter group slower than the former. In cases of puruloid stool, the recovery in the RKM group was significantly faster by U-test than the FOM group, and a similar trend was observed overall. 4. Bacteriologically, the eradication rate of Campylobacter in the RKM group was very good at 91.3% with the FO

Topics: Acute Disease; Administration, Oral; Age Factors; Campylobacter fetus; Campylobacter Infections; Child; Child, Preschool; Clinical Trials as Topic; Dosage Forms; Enteritis; Female; Fosfomycin; Humans; Infant; Male; Miocamycin; Multicenter Studies as Topic

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

Rokitamycin, a newly developed macrolide, was administered to a total of 107 cases, 16 years old or more, in order to evaluate its clinical efficacy, safety and usefulness on Campylobacter enteritis. Daily dosage of 600 mg of rokitamycin was administered orally in three divided doses for 5 days. Bacteriological and clinical efficacies were judged by the attending doctors from the evaluation criteria made by the committee and from the days required for improvement of diarrhea, defervescence and so on, respectively. Antibacterial activities against the isolates were tested of rokitamycin (RKM), erythromycin (EM), josamycin (JM) and ofloxacin (OFLX). The results were as follows; 41 symptomatic patients and 5 carriers were evaluated. Clinical efficacy (n = 41) was 100% (excellent; 34.1%, good; 65.9%). Bacteriological efficacy (n = 41) was 97.6%. Eight of the 9 cases with consecutive stool cultures were free of the bacteria on and after one day of the drug administration. Clinical usefulness (n = 46) was 97.8%. Slight epigastric pain was seen in only one as a side effect. The items of abnormal laboratory findings were 4 elevated GPT and/or GOT and one increased number of WBC in 4 cases. MIC90 of RKM, EM, JM and OFLX against 41 clinical isolates of C. jejuni were 1.56, 3.13, 3.13 and 0.78 micrograms/ml, respectively. Rokitamycin was considered clinically useful to treat Campylobacter enteritis.

Topics: Adolescent; Adult; Aged; Campylobacter coli; Campylobacter Infections; Campylobacter jejuni; Drug Evaluation; Enteritis; Female; Humans; Male; Middle Aged; Miocamycin

We determined the minimum inhibitory concentrations (MICs) of rokitamycin (TMS-19-Q, RKM), a macrolide antimicrobial agent, against strains of various bacterial species isolated from enteritis patients, and compared them with those of josamycin (JM), erythromycin (EM) and ofloxacin (OFLX). MIC90 of RKM against 147 strains of Campylobacter jejuni, and each 25 strains of Shigella spp., Salmonella spp. and diarrheagenic Escherichia coli were 1.56, 200, 800 and 200 micrograms/ml, respectively. There was only one RKM resistant (MIC greater than 100 micrograms/ml) C. jejuni strain, while most of the strains of the other species were resistant to RKM. MIC values of the other drugs were all similar to those of RKM. MIC90 of OFLX against 147 strains of C. jejuni was 0.78 micrograms/ml, lower than other drugs.

Topics: Campylobacter; Enteritis; Enterobacteriaceae; Humans; Microbial Sensitivity Tests; Miocamycin

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

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

We studied the absorption and excretion as well as the clinical effect of rokitamycin (RKM, TMS-19-Q) dry syrup. The results we found are summarized as follows: 1. When 3 pediatric patients were medicated orally with a single dose of 10 mg/kg of the drug, its peak concentrations of 0.75 and 0.51 microgram/ml appeared in the blood in 30 minutes after administration in 2 patients, and of 0.21 microgram/ml in 1 hour in the other patient. At 4 hours after administration, its concentration in the blood was 0.07-0.08 microgram/ml in all of the patient, and at 6 hours, it was undetectable. T1/2 values were 1.05-2.08 hours. First 6-hour urinary recovery rates of the drug in the first 2 patients were 1.52 and 1.11%, respectively. 2. Twenty-four patients with 25 diseases were medicated with 7.14-12.5 mg/kg of the drug 3-4 times daily for 4-10 days. The patients consisted of 12 with tonsillitis, 7 with bronchitis, 3 with colitis, one each with Haemophilus influenzae pneumonia, mycoplasmal pneumonia, and pertussis. Clinical responses to the treatment were excellent in 7, good in 13, and poor in 5, with an efficacy rate of 80.0%. Bacteriologically, of 17 isolates whose changes were followed, 8 were eradicated, 1 decreased, and 8 remained unchanged, with an eradication rate of 47.1%. 3. No adverse reactions to the drug were observed in any of these patients, while abnormal laboratory test values observed were slight eosinophilia and also slight elevations of S-GOT and S-GPT in one of the patients.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Administration, Oral; Bronchitis; Child; Child, Preschool; Drug Evaluation; Enteritis; Female; Humans; Infant; Leucomycins; Male; Miocamycin; Pneumonia, Mycoplasma; Tonsillitis

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