Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0348321 (Haemophilus)
 15,372 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Clarithromycin (TE-031, A-56268) is a new 14-membered ring macrolide antibiotic developed by Taisho Pharmaceutical Co., Ltd. TE-031 has a methoxy group at position 6 in its structure. In the present study, we carried out laboratory and clinical investigations on TE-031 in the field of pediatrics. The obtained results are summarized as follows. The antibacterial activity of TE-031 was investigated against 16 clinically isolated strains of Streptococcus pyogenes, Staphylococcus aureus, Haemophilus influenzae, Bordetella pertussis and Campylobacter jejuni. TE-031 showed antibacterial activity comparable to erythromycin. The pattern of changes in TE-031 concentrations in the blood after administration was investigated. In subjects administered the granular preparation of TE-031, Cmax values were 0.64 micrograms/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 micrograms/ml in 2 subjects administered with 10 mg/kg. The tablet form of TE-031 was administered to 3 subjects at 5 mg/kg, and Cmax values were 2.09-3.92 micrograms/ml, while T 1/2 values were in a range of 2.9-3.8 hours. When drug concentrations in the urine were investigated, it was found that 6-hour recovery rates were 9.9% (dose: 5 mg/kg) and 53.4% (dose: 10 mg/kg) in the subjects administered the granular form, whereas recovery rates averaged 36.8% in the tablet-administered subjects. In the clinical trial, TE-031 was administered in 2-3 doses/day for 2-18 days. In cases given the granular form, dosages were 12-38 mg/kg/day, while tablets were administered at 12-29 mg/kg/day. The overall clinical efficacy rate was 92.8%, i.e., the drug was effective in 64 of 69 patients. TE-031 was ineffective in 1 case of otitis media, but efficacious in 10 of 10 (100%) cases of upper respiratory infection, 15 of 18 (83.3%) cases of bronchitis and pneumonia, 5 of 6 (83.3%) cases of pertussis, 13 of 13 (100%) cases of mycoplasmal pneumonia, 4 of 4 (100%) cases of Chlamydia psittaci pneumonia, 16 of 16 (100%) cases of gastroenteritis (including 15 cases of Campylobacter gastroenteritis), and 1 (100%) case of impetigo. In bacteriological studies conducted on the patients, the overall elimination rate was 93.1%, i.e., bacterial elimination was obtained in 27 of 29 cases. TE-031 showed especially good bacteriological efficacy (100%) against C. jejuni and B. pertussis, which were eliminated from all of 15 and 2 cases examined, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Laboratory and clinical studies on clarithromycin in pediatrics]. 252 42

Laboratory and clinical studies on clarithromycin (TE-031, A-56268), a new macrolide antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows: 1. Serum concentrations, urinary concentrations and urinary recovery rates were determined upon oral administration on fasting of TE-031 at doses of 5 mg/kg granules in 1 case and tablets in 2 cases, and 10 mg/kg granules in 1 and 15 mg/kg granules in 1. Peak serum levels were obtained at 30 minutes in 2 cases, at 1 hour in 2 cases and at 2 hours in 1 case after administration of the drug with a range of 2.29-7.10 micrograms/ml with half-lives of 2.2-7.5 hours. Urinary recovery rates in 6 hours after administration ranged from 7.1-34.5%. 2. MICs of TE-031 against 49 clinical isolates (Streptococcus pyogenes 5 strains, Streptococcus pneumoniae 9, Staphylococcus aureus 3, Branhamella catarrhalis 4, Haemophilus influenzae 14, Haemophilus parainfluenzae 7, and Campylobacter jejuni 7) were compared with those of josamycin (JM), erythromycin (EM), and ampicillin (ABPC). The antibacterial activity of TE-031 was superior to those of JM and equal to those of EM. 3. Fifty-five pediatric patients with acute infectious diseases (scarlet fever 3 cases, pharyngitis and tonsillitis 15, pertussis 2, pneumonia 10, bronchitis 14, Campylobacter enteritis 11) were treated with TE-031 at daily doses of 10-35 mg/kg t.i.d. as a rule. The efficacy rates were 96% clinically and 72% bacteriologically. 4. Side effects or abnormal laboratory test values were not observed. 5. None of children refused TE-031.
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PMID:[Laboratory and clinical studies on clarithromycin in the field of pediatrics]. 252 45

We have carried out laboratory and clinical studies on clarithromycin (TE-031, A-56268). The results are summarized as follows. Serum and urinary concentrations of TE-031 were determined in 5 children with ages between 6 and 11 years given single oral doses of 5, 6.7, 10 and 15 mg/kg. Serum concentrations peaked at 1 hour after administration of 5, 6.7 and 15 mg/kg, and respective peak values were 1.98 micrograms/ml, 2.21 micrograms/ml and 5.58 micrograms/ml. Biological half-lives for the drug at 5, 6.7 and 15 mg/kg dose were 2.99 hours, 2.08 hours and 2.09 hours, respectively. Mean serum concentrations peaked at 2 hours after administration of 10 mg/kg, and peak values were 3.91 +/- 1.64 micrograms/ml. Biological half-lives were 3.00 +/- 0.58 hours. The 6-hour urinary recovery rates ranged from 22.7% to 23.8% after administration of 10 mg/kg, and the 6-hour urinary recoveries were 30.1%, 20.5% and 39.1% after administration of 5 mg/kg, 6.7 mg/kg and 15 mg/kg, respectively. Therapeutic responses were recorded as excellent or good in 35(89.7%) of the children, comprising 5 with tonsillitis, 3 with pharyngitis, 7 with bronchitis, 5 with pneumonia, 15 with Mycoplasma pneumonia, 1 with whooping cough and 3 with Campylobacter enteritis. The microbiological effectiveness of TE-031 on identified pathogens comprising 2 strains of Streptococcus pneumoniae, 5 strains of Haemophilus influenzae, 2 strains of Haemophilus parainfluenzae, 5 strains of Mycoplasma pneumoniae and Campylobacter spp. was satisfactory as evidenced by an eradication rate of 82.4%. No significant side effect due to the drug was observed in any cases. In conclusion, TE-031 was found to be efficacious and safe for the treatment of bacterial infections in children.
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PMID:[Laboratory and clinical studies of clarithromycin in pediatric fields]. 252 48

A newly developed macrolide clarithromycin (TE-031, A-56268), with antibacterial spectrum and antibacterial activity nearly equal to those of erythromycin (EM), shows beneficial characteristics such as a higher blood level, higher recovery rate in urine, and better penetration into each tissue than conventional macrolides (MLs). TE-031 has been studied in adults against various infections and proved to be useful. The present paper describes the results of a study in children to examine the usefulness of TE-031 granules and tablets with a potency of 50 mg. TE-031 granules were administered to 132 children with ages from 6 months to 13 years and 10 months. Excluded from the evaluation were 12 cases in which clinical effects were deemed unevaluable. The evaluable subjects consisted of 1 case with pharyngitis, 3 with tonsillitis, 9 with acute bronchitis, 19 with pneumonia, 19 with mycoplasmal pneumonia, 2 with scarlet fever, 20 with Campylobacter enteritis, 11 with impetigo, 2 with subcutaneous abscess, 18 with primary atypical pneumonia and 16 with acute enteritis of unidentified pathogens; a total of 120 subjects. An average daily dose of TE-031 was 25.9 mg/kg, divided into 3 doses except 1 case with 2 daily doses and lengths of the treatment averaged 7 days. TE-031 tablets each containing 50 mg potency, were administered to 49 subjects with ages from 3 year and a month to 14 years consisting of 8 cases with pharyngitis, 1 with tonsillitis, 1 with acute bronchitis, 4 with pneumonia, 14 with mycoplasmal pneumonia, 4 with scarlet fever, 5 with Campylobacter enteritis, 7 with impetigo, 1 with atypical pneumonia, 1 with Salmonella gastroenteritis and 3 with acute enteritis caused by unidentified pathogens, at an average daily dose of 13.5 mg/kg dived into 2-4 doses (2 doses/day for 12 cases, 3 doses for 32, 4 doses for 5) for 7 days on the average. In addition to examine the clinical and bacteriological effects of the 2 dosage forms of TE-031, minimum inhibitory concentrations (MICs) were determined for 9 antibiotics consisting of 5 MLs including TE-031, EM, josamycin (JM), midecamycin acetate (MDM acetate), and rokitamycin (RKM), 3 penicillins including ampicillin (ABPC), methicillin, cloxacillin and 1 cephem antibiotic, cefaclor (CCL), against 29 strains consisting of 12 strains of Staphylococcus aureus, 7 of Streptococcus pyogenes, 2 of Streptococcus pneumonia 2 of Haemophilus influenzae and 6 of Campylobacter jejuni, out of 71 strains of pathogens or possible pathogens that had been isolated from the cases given TE-031.
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PMID:[Clinical study on clarithromycin granule and tablet in the field of pediatrics]. 252 56

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.
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PMID:[Laboratory and clinical studies of rokitamycin in pediatric fields]. 305 Jan 85

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 one low acid case (2.3%) was observed.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Microbiological, pharmacokinetic and clinical studies of rokitamycin dry syrup in the pediatric field]. 305 Jan 86

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.
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PMID:[Laboratory and clinical studies of rokitamycin dry syrup in the field of pediatrics]. 317 61

Rokitamycin (RKM) dry syrup was administered to a group of pediatric patients. The results obtained are summarized as follows. 1. Of the recent isolates of Streptococcus pyogenes, fewer strains were highly resistant to RKM than to josamycin (JM), midecamycin (MDM), erythromycin and lincomycin. Also, macrolides (MLs)-resistant strains proved to be susceptible to RKM. 2. Recent isolates of Staphylococcus aureus, Streptococcus agalactiae, group G Streptococci, S. pyogenes, Streptococcus pneumoniae and Haemophilus influenzae were more susceptible to RKM than to midecamycin acetate and JM. Oral administrations of 10-15 mg/kg of the drug were followed by its peak concentrations of 0.07-0.77 micrograms/ml in the blood at 30 minutes in many patients, and by an undetectable level at 6 hours also in many of them. T1/2 values were 1.2-2.6 hours, and first 6-hour urinary excretion rates were 1.26-1.74%. 3. Fifty-two patients with acute upper and lower respiratory tract infections, Campylobacter enteritis, etc. were treated with RKM at about 20-40 mg/kg daily for 4-14 days, with an overall efficacy rate of 88.5%. 4. An eradication rate of 81.4% was achieved for 43 strains of 7 species isolated from the patients. 5. No abnormal laboratory test values were observed after treatment with drug 4 approximately 14 days. A side effect, stomach discomfort, was observed in 1 patient.
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PMID:[Bacteriological, pharmacokinetic and clinical studies of a rokitamycin syrup in pediatrics]. 322 34

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)
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PMID:[Studies on efficacy, safety and dosage of rokitamycin in the treatment of pediatric infections]. 322 35

Azithromycin (AZM) was studied for its clinical efficacy in pediatric infections. The study on AZM was carried out in 43 patients whose diagnoses were given as follows: pharyngitis in five cases, tonsillitis in one, bronchitis in four, pneumonia in four, Mycoplasma pneumonia in 14, scarlet fever in nine, impetigo in four, pyodermia in one and Campylobacter enteritis in one. The patients received AZM once daily at 1.6 approximately 20.0 mg/kg body weight for three to five days. Effectiveness of AZM was evaluated in 39 cases and the drug was rated "excellent" in 15, "good" in 19, "fair" in one, "poor" in four, resulting in an efficacy rate of 87.2%. Twenty bacterial isolates were identified as causative isolates in 19 patients: Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, Campylobacter jejuni and Mycoplasma pneumoniae. AZM eradicated 16 isolates but four persisted after therapy. One patient complained of loose stool, while two patients were found with decreases in white blood cell counts, and seven showed increases in eosinophils. However, no serious case of adverse event was reported.
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PMID:[Clinical evaluation of azithromycin in pediatric infections]. 898 54


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