rokitamycin and Tonsillitis

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

The clinical study for TMS-19-Q.O tablet was performed with multicenter trial. The results obtained were as follows; Final global improvement rating in 332 cases of otorhinolaryngological infections were excellent in 99, good in 142, fair in 40 and poor in 51 and the effective rate was 72.6%. Those of 266 cases with acute infection were excellent in 93 and good in 121 and the effective rate was 80.5%. Optimum daily doses would be 600 mg based on the analysis of 144 cases of the acute infection with sensitive bacteria (MIC: less than or equal to 3.13 micrograms/ml). In acute infection, major causative bacteria were Gram-positive cocci (GPC) indicating the frequency of 72.0% in total isolates and 87.5% in singly isolated cases. In chronic infection, although GPC were also dominant, Gram-negative bacilli were observed in 31.9%. Clinical and bacteriological effective rates of 160 cases of acute infection with single species were 80.6% and 90.3%, and those of 43 cases in chronic infection were 44.2% and 72.7%, respectively. The resistant rates of isolates in acute infection to TMS-19-Q were 13.3% in S. aureus, 7.7% in S. epidermidis, 6.0% in S. pyogenes and 0% in S. pneumoniae. Those in chronic infection were 20.0% in S. aureus and 25.0% in S. epidermidis. Slight adverse reactions, such as skin eruption or gastrointestinal disorders were observed in 14 cases and no severe one was observed. Slight elevation of GOT, GPT, Al-P, BUN, S-Cr. or eosinophil were observed in 12 cases. These results suggest that TMS-19-Q would be useful antibiotic for otorhinolaryngological infections.

Topics: Adolescent; Adult; Aged; Anti-Bacterial Agents; Clinical Trials as Topic; Female; Humans; Laryngitis; Leucomycins; Male; Microbial Sensitivity Tests; Middle Aged; Miocamycin; Otitis Media, Suppurative; Otorhinolaryngologic Diseases; Sinusitis; Staphylococcus aureus; Staphylococcus epidermidis; Tonsillitis

In order to compare the clinical efficacy and safety of TMS-19-Q.GC tablet (TMS) with josamycin tablet (JM) in acute tonsillitis, the double blind trial was carried out with the daily dosage of 200 mg X 3 in TMS and 400 mg X 3 in JM. Number of cases evaluated for clinical efficacy were 154 cases (73 treated with TMS and 81 treated with JM). The effective rating of TMS and JM were 89.0% and 88.9% judged by doctors in charge, and 82.2% and 85.2% judged by committee respectively. Bacteriological effects were satisfactory to yield the eradication rates of 93.8% in TMS and 94.7% in JM. Number of cases evaluated for safety were 199 cases (101 treated with TMS and 98 treated with JM). The incidence of side effect was 4.0% (4/101) in TMS and 5.1% (5/98) in JM and most of them were mild gastro-intestinal disorders. Number of cases evaluated for utility were 156 cases (74 treated with TMS and 82 treated with JM). The usefulness rates were 85.1% in TMS and 86.6% in JM. There was no significant difference between TMS and JM, in clinical effect, bacteriological effect, safety and utility. From these results, daily 600 mg dosage of TMS was as useful as daily 1,200 mg dosage of JM in the treatment for acute tonsillitis.

Topics: Acute Disease; Adolescent; Adult; Aged; Clinical Trials as Topic; Double-Blind Method; Female; Humans; Leucomycins; Male; Middle Aged; Miocamycin; Tablets; Tonsillitis

Tonsillitis is the most common disease in the otorhinolaryngeal location. For most patients, tonsillitis is attributed to a group A streptococcal infection if the throat culture is positive for that organism or to a viral infection if the throat culture is negative. However, recent studies have shown that Chlamydia trachomatis can produce tonsillar infection. In this study, we evaluated the efficacy of Rokitamycin, a 16-membered ring macrolide antibiotic agent, in the treatment of tonsillitis associated with C. trachomatis. In 26 of 28 (92.9%) patients from whom C. trachomatis was isolated, the organism was eradicated by antimicrobial treatment with Rokitamycin of five days to three weeks' duration. In 25 of the 26 patients, they were totally free of tonsillar symptoms.

Topics: Adult; Aged; Child; Chlamydia Infections; Chlamydia trachomatis; Drug Evaluation; Female; Humans; Male; Middle Aged; Miocamycin; 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

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

Pharmacokinetic and clinical evaluations of rokitamycin (RKM, TMS-19-Q), a new macrolide antibiotic, were carried out. RKM was administered orally to 14 patients with congenital heart diseases before cardiocatheterization and angiography. Peak plasma levels of RKM were observed at 30 minutes after the administration at dosages of 5, 10, 15 mg/kg. Although the reason is not clear, there were great variations among plasma levels. Peak plasma levels of patients with relatively good absorption were high enough against bacteria such as beta-hemolytic Streptococcus, Mycoplasma pneumoniae and Chlamydia trachomatis. Clinical responses were evaluated in 5 children comprising 2 cases of mycoplasmal pneumonia, 2 cases of Chlamydia infection and 1 case of beta-hemolytic streptococcal tonsillitis. All of these cases had excellent or good responses without any side effect. Furthermore, no child refused to take RKM dry syrup.

Topics: Adolescent; Child; Child, Preschool; Chlamydia Infections; Drug Evaluation; Female; Humans; Leucomycins; Male; Miocamycin; Pneumonia, Mycoplasma; Tonsillitis