rokitamycin and Bacterial-Infections

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

Rokitamycin is a semisynthetic macrolide with a lactonic ring with 16 atoms, showing anti-bacterial action at concentrations near to MIC. A controlled clinical study is carried out, in parallel groups, whose aim was to assess the therapeutic action and safety of two dosage schemes of rokitamycin, in the short term treatment (5 days) of acute infective processes of odontostomatological origin.. Twenty patients (14 males, 6 females) were recruited for the trial, suffering from alveolitis, abscess, phlegmon, sialadenitis and suppurating cysts. The patients were divided in a randomized fashion into two groups: 10 patients were treated orally with 800 mg/day and 10 with 1200 mg/day. Rokitamycin was supplied in 400 mg tablets.. The 5 days of treatment with rokitamycin determined the complete resolution of the infective process, with eradication of the germs originally isolated, all belonging to the Streptococcus genus. Clinical efficacy was evident by the third day of treatment, with a prompt improvement of symptoms (functional limitation, pain, tumefaction) and the return of body temperature to within normal limits, in a totally superimposable fashion between the two groups. Safety was excellent with both doses, with no side effects observed.. The results of the study show that treatment with rokitamycin in the short term, at the usual dosage of 800 mg/day, is a valid therapeutic scheme in infective processes in odontostomatology.

Topics: Adolescent; Adult; Anti-Bacterial Agents; Bacterial Infections; Dose-Response Relationship, Drug; Female; Humans; Male; Miocamycin; Mouth Diseases

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

We obtained bacterial strains which were clinically isolated and identified from outpatients with various infections in medical institutions throughout Japan. Possible antibacterial activities of rokitamycin (RKM) were examined against these isolates. Minimum inhibitory concentrations (MICs) were determined through a comparative study with reference drugs. The results of the study are summarized as follows. 1. Resistance patterns of 400 isolates which were highly resistant to macrolides (MLs) with MIC values > 100 micrograms/ml were classified into 55 patterns. Staphylococcus spp. showed cross resistance to 14-membered ring MLs with 100% cross resistance observed between erythromycin (EM) and clarithromycin (CAM), and 85.2% between EM and oleandomycin (OL). Fewer isolates showed strong resistance to 16-membered ring MLs than to 14-membered ring MLs. Cross resistances observed among the Staphylococcus isolates were 100% between acetylmidecamycin (MDM-AC) and kitasamycin (leucomycin (LM)), 93.9% between MDM-AC and josamycin (JM), and 53.3% between MDM-AC and RKM. Streptococcus spp. and Peptococcus spp. showed very similar resistance patterns to both 14- and 16-membered ring MLs, but resistance patterns to RKM were quite different. Most of anaerobic streptococci and Bacteroides fragilis group had similar resistance patterns to 14- and 16-membered ring MLs, but in some cases a pattern similar to that of Staphylococcus spp. was observed. 2. When ML-resistant bacteria isolated during 1975 to 1980 were compared to those isolated in 1986 and 1989, it was observed that resistance of Staphylococcus aureus remained almost unchanged, that of Streptococcus pyogenes was lower in the later years than during 1975 to 1980, but that of Streptococcus pneumoniae increased. 3. Most of ML-resistances of the resistant isolates were inducible, but extents of induction varied depending on drugs tested. Strong inductions were observed when 14-membered ring MLs were used, but inductions were minimal with 16-membered ring MLs. RKM appeared to induce resistance to the least extent. From these results, it appears that the RKM is quite useful clinically even in the 1990s.

Topics: Bacterial Infections; Bacteroides fragilis; Drug Resistance, Microbial; Humans; Miocamycin; Peptostreptococcus; Staphylococcus; Staphylococcus aureus; Streptococcus agalactiae; Streptococcus pneumoniae; Streptococcus pyogenes

YM133, the 4"-O-(4-methoxyphenyl)acetyltylosin, is a new macrolide. The in vitro activity of YM133 was compared with those of erythromycin, josamycin, and rokitamycin by an agar dilution method. YM133 inhibited 90% of the tested isolates of Streptococcus pneumoniae, Legionella spp., and anaerobic bacteria at less than or equal to 1.56 micrograms/ml. The drug inhibited 90% of erythromycin-resistant staphylococci and Streptococcus pyogenes at less than or equal to 50 micrograms/ml. YM133 showed activity against erythromycin-, josamycin-, and rokitamycin-resistant (MIC greater than or equal to 100 micrograms/ml) strains of staphylococci, streptococci, Bacteroides spp., and Clostridium spp. Enterococci were less susceptible to other YM133-like macrolides. Unlike other macrolides, YM133 showed killing activity, and the MBC/MIC ratios of YM133 for several strains were 1:32, whereas those of erythromycin were 4:1,024. In a time-kill curve study, the reduction of viable cells started within 2 h after the addition of YM133.

Topics: Anti-Bacterial Agents; Bacteria; Bacterial Infections; Clindamycin; Drug Resistance, Microbial; Erythromycin; Josamycin; Microbial Sensitivity Tests; Miocamycin; Oleandomycin

In a study of rokitamycin (RKM) dry syrup for its usefulness in pediatric infections, the following results were obtained: 1. Frequencies of RKM-resistant strains among fresh isolates from sick children were very low, and 4.4% of 68 isolates of Staphylococcus aureus, 4.2% of 48 isolates of Streptococcus pneumoniae, and none of 96 isolates of Streptococcus pyogenes were found to be RKM-resistant. 2. Hypo- to achlorhydria was found in 2 (3.77%) of 53 children. 3. When children were administered once orally with 5, 10 and 15 mg/kg of RKM dry syrup at fasting, mean peak values of plasma concentration were 0.25, 0.55 and 0.74 micrograms/ml with a T1/2 (beta) of 2.18, 1.97 and 2.00 hours, respectively. Urinary recovery rates during the first 0-6 hours were quite low, and values were 1.21, 1.38 and 2.23%, respectively. 4. The clinical efficacy of RKM dry syrup was studied on children chiefly with acute pneumonia, mycoplasmal pneumonia and tonsillitis. Among 379 children from whom pathogens had been determined, responses to the treatment were excellent in 186, good in 144, fair in 24, poor in 20 and unknown in 5 patients, the overall efficacy rate being 88.2%. Among all 598 treated patients, including those with undetermined pathogens, responses were excellent in 247, good in 269, fair in 42, poor in 35 and unknown in 5 patients, the efficacy rate being 87.0%. 5. The clinical efficacy of the drug in treating Chlamydia infection in 12 patients including a Chlamydia carrier and the clinical efficacy in treating Campylobacter enteritis in 36 patients were studied. All the cases showed "good" responses. Among 66 patients with mycoplasmal pneumonia, responses were excellent in 33 and good in 27 patients, with an efficacy rate of 90.9%. 6. The optimal dose of RKM dry syrup seemed to be in the range between 20 and 40 mg/kg. It appeared, however, that a dose of about 40 mg/kg would be required to eradicate the pathogen from the pharynx in S. pyogenes infection. 7. Adverse reactions to RKM dry syrup were found in 9 (1.45%) of 622 patients. The reactions were gastrointestinal symptoms except eruption occurred in 1 patient, but they were all mild. Laboratory examinations revealed eosinophilia in 19 and abnormal hepatic enzyme activities in 8 of 455 patients studied, but such abnormalities were all transient and mild.

Topics: Bacterial Infections; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Infant, Newborn; Leucomycins; Male; Miocamycin

Twenty five children were treated with rokitamycin (RKM) and its clinical efficacy and side effects were evaluated. Ages of the patients ranged from 13 days to 10 years. Doses of RKM ranged 17.1-39.3 mg/kg/day for 2.3 to 17.7 days. Twenty four patients including 8 Mycoplasma pneumonia, 5 bronchopneumonia, 6 bronchitis, 2 streptococcosis, 1 otitis media, 1 tonsillitis and 1 Chlamydia conjunctivitis were evaluated for clinical efficacy. Results were excellent in 7, good in 12, fair in 4, and poor in 1 patient. One patient was excluded from the evaluation, because the patient was treated with erythromycin before entering this study. Out of the 25 patients, 3 cases showed eosinophilia, 2 cases showed elevated GOT and GPT but no adverse clinical signs due to RKM were observed. The pharmacokinetics of RKM was studied in 5 patients whose ages ranged from 8 to 12 years. Plasma peak concentrations of RKM in 2 patients were 0.14 and 0.16 micrograms/ml at 30 minutes after doses of 5 mg/kg. Peak concentrations in 3 patients ranged from 0.32 to 1.02 micrograms/ml after doses of 10 mg/kg. Portions of the drug excreted into urine within 6 hours were 0.49 and 1.03% in 2 patients each of whom was given doses of 5 mg/kg, and ranged from 1.16 to 1.30% in 3 patients, each given 10 mg/kg. Metabolic products in urine within 4 hours after doses of 5 to 10 mg/kg were studied in 4 patients. Leucomycin A7 and leucomycin V accounted for almost 90% of all the related compounds excreted.

Topics: Administration, Oral; Bacterial Infections; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Female; Humans; Infant; Infant, Newborn; Leucomycins; Male; Miocamycin

Clinical efficacies of a new macrolide antibiotic, rokitamycin (RKM, TMS-19-Q), were studied in acute pediatric infections. Responses to the RKM administration were evaluable in 62 out of 68 patients consisted of 7 patients with pharyngitis (efficacy rate of 85.7%, 6/7 patients), 4 with bronchitis (25.0%, 1/4), 9 with tonsillitis (100%, 9/9), 13 with mycoplasmal pneumonia (100%, 13/13), 13 with hemolytic streptococcal infections (92.3%, 12/13), 14 with pneumonia (57.1%, 8/14), one with pertussis (100%, 1/1) and another with Chlamydia pneumonia (100%, 1/1) thus an overall efficacy rate of 82.3% was achieved. Urticaria was observed in one of the patients as an adverse reaction to the drug, while abnormal laboratory test results were noted in 3 patients, but none of such changes were severe. The drug, even when administered in combination with a theophylline preparation, exerted no effects on the serum concentration of the latter.

Topics: Acute Disease; Administration, Oral; Bacterial Infections; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Infant, Newborn; Leucomycins; Male; Miocamycin; Theophylline; Urticaria

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

A total of 29 patients with pediatric infections was treated orally with 21.4-44.4 mg/kg/day of rokitamycin (RKM) dry syrup. The obtained results are summarized as follows. 1. Clinical responses to RKM in 24 evaluable patients were excellent in 2 and good in 3 of 5 patients with tonsillitis and laryngitis; excellent in 3 and good in 5 of 8 patients with bronchitis; excellent in 3, good in 2 and fair in one of 6 patients with bronchopneumonia; excellent in 2 and good in the other of 3 patients with psittacosis; and excellent in 2 of 2 patients with Campylobacter colitis. The overall efficacy rate was 95.8%. 2. Bacteriological responses to the drug were: reduction in 1 and no change in the other of 2 strains of Streptococcus pyogenes; eradication of a strain of Streptococcus pneumoniae and 2 strains of Staphylococcus aureus; eradication of 2 and no change in 3 of 5 strains of Haemophilus influenzae; and eradication of 2 out of 2 strains of Campylobacter spp. 3. Diarrhea was complained of as an adverse reaction to the RKM medication by 1 patient, abdominal pain was reported by another, and anorexia by another of the 27 patients treated. Laboratory examination was performed on some patients, but not abnormal test values were found except in 1 case showing an increase in platelet count from 27.6 to 78.2 X 10(4)/mm8. The results suggested that RKM dry syrup might be a very useful and safe drug for the treatment of pediatric infections.

Topics: Administration, Oral; Bacterial Infections; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Leucomycins; Male; Miocamycin