Laboratory and clinical studies on clarithromycin in pediatrics

H. Akita, Y. Sato, S. Iwata, K. Sunakawa

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

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, C(max) values were 0.64 μg/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 μg/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 C(max) values were 2.09 ~ 3.92 μg/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. Analysis for side effects was conducted in 82 patients administered with TE-031. Adverse symptoms occurred in 6 of those patients, for an incidence rate of 7.3%. These side effects consisted of digestive tract symptoms in 5 patients (1 case each of abdominal pain, vomiting, and abdominal pain and vomiting, and 2 cases of diarrhea or loose stool) and urticaria in 1 patient. Various laboratory test abnormalities were also detected: eosinophilia in one of 38 (2.6%) patients examined, elevated GOT in 3 of 39 (7.7%) patients, and elevated GOT and GPT in one of 39 (2.6%) patients. In addition, studies were carried out to determine whether or not TE-031 exerts any effect on the hemostatic mechanism, but no change was detected in the blood clotting factors by the TE-031 administration regimen. On the basis of the basic and clinical study results summarized above, it is surmised that TE-031 will be an effective and safe oral antibiotic for use in the treatment of infections in children when administered 2 ~ 3 times per day in a dose of 5 ~ 10 mg/kg.

Original languageEnglish
Pages (from-to)264-280
Number of pages17
JournalJapanese Journal of Antibiotics
Volume42
Issue number2
Publication statusPublished - 1989
Externally publishedYes

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Clarithromycin
Pediatrics
Tablets
Bordetella pertussis
Campylobacter jejuni
Gastroenteritis
Abdominal Pain
Vomiting
Clinical Studies
Pneumonia
Impetigo
Chlamydophila psittaci
Chlamydophila pneumoniae
Campylobacter
Blood Coagulation Factors
Bronchitis
Whooping Cough
Streptococcus pyogenes
Urticaria
Dosage Forms

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Akita, H., Sato, Y., Iwata, S., & Sunakawa, K. (1989). Laboratory and clinical studies on clarithromycin in pediatrics. Japanese Journal of Antibiotics, 42(2), 264-280.

Laboratory and clinical studies on clarithromycin in pediatrics. / Akita, H.; Sato, Y.; Iwata, S.; Sunakawa, K.

In: Japanese Journal of Antibiotics, Vol. 42, No. 2, 1989, p. 264-280.

Research output: Contribution to journalArticle

Akita, H, Sato, Y, Iwata, S & Sunakawa, K 1989, 'Laboratory and clinical studies on clarithromycin in pediatrics', Japanese Journal of Antibiotics, vol. 42, no. 2, pp. 264-280.
Akita, H. ; Sato, Y. ; Iwata, S. ; Sunakawa, K. / Laboratory and clinical studies on clarithromycin in pediatrics. In: Japanese Journal of Antibiotics. 1989 ; Vol. 42, No. 2. pp. 264-280.
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abstract = "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, C(max) values were 0.64 μg/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 μg/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 C(max) values were 2.09 ~ 3.92 μg/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. Analysis for side effects was conducted in 82 patients administered with TE-031. Adverse symptoms occurred in 6 of those patients, for an incidence rate of 7.3{\%}. These side effects consisted of digestive tract symptoms in 5 patients (1 case each of abdominal pain, vomiting, and abdominal pain and vomiting, and 2 cases of diarrhea or loose stool) and urticaria in 1 patient. Various laboratory test abnormalities were also detected: eosinophilia in one of 38 (2.6{\%}) patients examined, elevated GOT in 3 of 39 (7.7{\%}) patients, and elevated GOT and GPT in one of 39 (2.6{\%}) patients. In addition, studies were carried out to determine whether or not TE-031 exerts any effect on the hemostatic mechanism, but no change was detected in the blood clotting factors by the TE-031 administration regimen. On the basis of the basic and clinical study results summarized above, it is surmised that TE-031 will be an effective and safe oral antibiotic for use in the treatment of infections in children when administered 2 ~ 3 times per day in a dose of 5 ~ 10 mg/kg.",
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N2 - 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, C(max) values were 0.64 μg/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 μg/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 C(max) values were 2.09 ~ 3.92 μg/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. Analysis for side effects was conducted in 82 patients administered with TE-031. Adverse symptoms occurred in 6 of those patients, for an incidence rate of 7.3%. These side effects consisted of digestive tract symptoms in 5 patients (1 case each of abdominal pain, vomiting, and abdominal pain and vomiting, and 2 cases of diarrhea or loose stool) and urticaria in 1 patient. Various laboratory test abnormalities were also detected: eosinophilia in one of 38 (2.6%) patients examined, elevated GOT in 3 of 39 (7.7%) patients, and elevated GOT and GPT in one of 39 (2.6%) patients. In addition, studies were carried out to determine whether or not TE-031 exerts any effect on the hemostatic mechanism, but no change was detected in the blood clotting factors by the TE-031 administration regimen. On the basis of the basic and clinical study results summarized above, it is surmised that TE-031 will be an effective and safe oral antibiotic for use in the treatment of infections in children when administered 2 ~ 3 times per day in a dose of 5 ~ 10 mg/kg.

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