Pharmacokinetics and clinical effects of cefozopran in pediatric patients

Ryochi Fujii, Toshiaki Abe, Tsuyoshi Tajima, Itaru Terashima, Hidenori Meguro, Susumu Nakazawa, Hajime Sato, Kenji Niinou, Keisuke Sunakawa, Takao Yokota, Hironobu Akita, Satoshi Iwata, Yoshitake Sato, Yoshikiyo Toyonaga, Hironori Nakamura, Kiwamu Seo, Ken Ichi Kawamura, Kuniyoshi Kuno, Kazue Ito, Naoichi Iwai & 37 others Haruhi Nakamura, Youichi Taneda, Minoru Sakurai, Masahiro Ito, Eiichi Azuma, Hitoshi Kamiya, Kenji Kitamura, Haruki Mikawa, Hajime Kimata, Tadafumi Nishimura, Kazuo Tabuki, Shigeyuki Aoki, Michio Takagi, Yohnosuke Kobayashi, Shoichiro Taniuchi, Yutaka Kobayashi, Tsunekazu Haruta, Kan Etsu Okura, Shigekazu Kuroki, Toshikazu Nishio, Hiroshi Matsuda, Kaichi Kida, Yukikazu Kainou, Takanobu Kurashige, Hideo Morita, Yasuhiro Kuroda, Etsuhisa Shirakawa, Takashi Okamoto, Takanori Sekiguchi, Yoshiro Tsuji, Izumi Gondo, Nobuo Kobayashi, Takashi Motohiro, Yasutaka Sakata, Hirokazu Sasaki, Youichiro Yoshinaga, Shuji Yamada

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

An investigation was made into pharmacokinetics and clinical effects of the newly developed cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), in pediatric patients. In 26 patients in whom pharmacokinetics were investigated, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by i.v injection were 21.3 ± 10.0 (mean ± standard deviation), 51.0 ± 9.9 and 68.3 ± 0.7 μg/ml, respectively. Serum concentrations at 6 hours after administration were 2.9 ± 17.2.3 ± 0.9 and 4.6 ± 2.6 μg/ml, with the levels roughly above MIC90s for dominating pathogenic bacteria being maintained until 6 hours after treatment. Urine concentrations were in the range between 200 and 560 μg/ml at 4 to 6 hours after dosing Cumulative urine excretion accounted for 70 to 80% of dose. In 11 patients in whom pharmacokinetic investigations were performed, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by 30- min. i. v. drip infusion were 37.1, 66.3 ± 25.5 and 95.7 ± 8.9 μg/ml, respectively. Serum concentrations at 6 hours after dosing were 1.6, 2.3 ± 0.8 and 3.0 ± 0.4 μg/ml, respectively, with the levels above MIC90s for dominating pathogenic bacteria also being maintained until 6 hours after administration. Urine concentrations were 190 μg/ml or more until 8 hours after dosing and the cumulative urinary excretion accounted for 50 to 70% of dose. In 9 patients with meningitis in whom CZOP penetration into cerebrospinal fluid was investigated, concentrations in the fluid of the compound i.v. injected at doses from 40 to 53 mg/kg were in the range between 1.6 and 43.4 μg/ml exceeding MICs for pathogenic bacteria at 1 to 1.5 hours after dosing. In all of the 38 patients in whom pharmacokinetic investigations and clinical evaluations were performed, CZOP was good to excellent (excellent in 22 patients and good in 16 patients). Also in bacteriological evaluations, all of the 31 strains of investigated pathogenic bacteria were eradicated. The clinical efficacy rates for the 335 subjects for clinical evaluations were 97.0% (195/201) for patients in whom pathogenic bacteria were detected (group A), and 95.5% (128/134) for patients in whom no pathogenic bacteria were detected (group B). In bacteriological evaluations, the eradication rates of Gram-positive and Gram-negative bacteria were 96.3% (77/80) and 04.5% (155/164), respectively, with the eradication rate in total being 95.1% (232/244). Safety investigations were performed in 364 patients. Adverse reactions were reported in 11 patients (3.0%), including diarrhea (aqueous stool and soft stool) in 7 patients (1.9%) and drug rash (rash, eruption and wheal) in 4 patients (1.1%). Abnormal laboratory test values were noted in 54 patients, including eosinophilia in 20 patients (6.3%) and elevated GPT in 20 patients (63%). The adverse reactions and abnormal laboratory test values were not serious, disappearing or improving during the continued treatment period or as a result of discontinuation of the treatment. Serum and urine concentrations of CZOP, when administered by i.v injection and 30-min iv drip infusion at doses of 10, 20 and 40 mg/kg, were higher than the MICs for pathogenic bacteria until 6 hours after dosing. The drug also showed favorable penetration into cerebrospinal fluid. It was therefore considered that CZOP was a highly useful drug for the treatment of pediatric infections with sufficient bacteriological and clinical efficacy when administered at a dose of 40 to 80 mg/kg three to four times daily.

Original languageEnglish
Pages (from-to)17-33
Number of pages17
JournalJapanese Journal of Antibiotics
Volume49
Issue number1
Publication statusPublished - 1996 Jan
Externally publishedYes

Fingerprint

Pharmacokinetics
Pediatrics
Bacteria
Urine
Serum
cefozopran
Exanthema
Intravenous Infusions
Injections
Cerebrospinal Fluid
Pharmaceutical Preparations
Eosinophilia
Therapeutics
Gram-Negative Bacteria
Meningitis
Diarrhea
Anti-Bacterial Agents
Safety

ASJC Scopus subject areas

  • Pharmacology
  • Molecular Medicine

Cite this

Fujii, R., Abe, T., Tajima, T., Terashima, I., Meguro, H., Nakazawa, S., ... Yamada, S. (1996). Pharmacokinetics and clinical effects of cefozopran in pediatric patients. Japanese Journal of Antibiotics, 49(1), 17-33.

Pharmacokinetics and clinical effects of cefozopran in pediatric patients. / Fujii, Ryochi; Abe, Toshiaki; Tajima, Tsuyoshi; Terashima, Itaru; Meguro, Hidenori; Nakazawa, Susumu; Sato, Hajime; Niinou, Kenji; Sunakawa, Keisuke; Yokota, Takao; Akita, Hironobu; Iwata, Satoshi; Sato, Yoshitake; Toyonaga, Yoshikiyo; Nakamura, Hironori; Seo, Kiwamu; Kawamura, Ken Ichi; Kuno, Kuniyoshi; Ito, Kazue; Iwai, Naoichi; Nakamura, Haruhi; Taneda, Youichi; Sakurai, Minoru; Ito, Masahiro; Azuma, Eiichi; Kamiya, Hitoshi; Kitamura, Kenji; Mikawa, Haruki; Kimata, Hajime; Nishimura, Tadafumi; Tabuki, Kazuo; Aoki, Shigeyuki; Takagi, Michio; Kobayashi, Yohnosuke; Taniuchi, Shoichiro; Kobayashi, Yutaka; Haruta, Tsunekazu; Okura, Kan Etsu; Kuroki, Shigekazu; Nishio, Toshikazu; Matsuda, Hiroshi; Kida, Kaichi; Kainou, Yukikazu; Kurashige, Takanobu; Morita, Hideo; Kuroda, Yasuhiro; Shirakawa, Etsuhisa; Okamoto, Takashi; Sekiguchi, Takanori; Tsuji, Yoshiro; Gondo, Izumi; Kobayashi, Nobuo; Motohiro, Takashi; Sakata, Yasutaka; Sasaki, Hirokazu; Yoshinaga, Youichiro; Yamada, Shuji.

In: Japanese Journal of Antibiotics, Vol. 49, No. 1, 01.1996, p. 17-33.

Research output: Contribution to journalArticle

Fujii, R, Abe, T, Tajima, T, Terashima, I, Meguro, H, Nakazawa, S, Sato, H, Niinou, K, Sunakawa, K, Yokota, T, Akita, H, Iwata, S, Sato, Y, Toyonaga, Y, Nakamura, H, Seo, K, Kawamura, KI, Kuno, K, Ito, K, Iwai, N, Nakamura, H, Taneda, Y, Sakurai, M, Ito, M, Azuma, E, Kamiya, H, Kitamura, K, Mikawa, H, Kimata, H, Nishimura, T, Tabuki, K, Aoki, S, Takagi, M, Kobayashi, Y, Taniuchi, S, Kobayashi, Y, Haruta, T, Okura, KE, Kuroki, S, Nishio, T, Matsuda, H, Kida, K, Kainou, Y, Kurashige, T, Morita, H, Kuroda, Y, Shirakawa, E, Okamoto, T, Sekiguchi, T, Tsuji, Y, Gondo, I, Kobayashi, N, Motohiro, T, Sakata, Y, Sasaki, H, Yoshinaga, Y & Yamada, S 1996, 'Pharmacokinetics and clinical effects of cefozopran in pediatric patients', Japanese Journal of Antibiotics, vol. 49, no. 1, pp. 17-33.
Fujii R, Abe T, Tajima T, Terashima I, Meguro H, Nakazawa S et al. Pharmacokinetics and clinical effects of cefozopran in pediatric patients. Japanese Journal of Antibiotics. 1996 Jan;49(1):17-33.
Fujii, Ryochi ; Abe, Toshiaki ; Tajima, Tsuyoshi ; Terashima, Itaru ; Meguro, Hidenori ; Nakazawa, Susumu ; Sato, Hajime ; Niinou, Kenji ; Sunakawa, Keisuke ; Yokota, Takao ; Akita, Hironobu ; Iwata, Satoshi ; Sato, Yoshitake ; Toyonaga, Yoshikiyo ; Nakamura, Hironori ; Seo, Kiwamu ; Kawamura, Ken Ichi ; Kuno, Kuniyoshi ; Ito, Kazue ; Iwai, Naoichi ; Nakamura, Haruhi ; Taneda, Youichi ; Sakurai, Minoru ; Ito, Masahiro ; Azuma, Eiichi ; Kamiya, Hitoshi ; Kitamura, Kenji ; Mikawa, Haruki ; Kimata, Hajime ; Nishimura, Tadafumi ; Tabuki, Kazuo ; Aoki, Shigeyuki ; Takagi, Michio ; Kobayashi, Yohnosuke ; Taniuchi, Shoichiro ; Kobayashi, Yutaka ; Haruta, Tsunekazu ; Okura, Kan Etsu ; Kuroki, Shigekazu ; Nishio, Toshikazu ; Matsuda, Hiroshi ; Kida, Kaichi ; Kainou, Yukikazu ; Kurashige, Takanobu ; Morita, Hideo ; Kuroda, Yasuhiro ; Shirakawa, Etsuhisa ; Okamoto, Takashi ; Sekiguchi, Takanori ; Tsuji, Yoshiro ; Gondo, Izumi ; Kobayashi, Nobuo ; Motohiro, Takashi ; Sakata, Yasutaka ; Sasaki, Hirokazu ; Yoshinaga, Youichiro ; Yamada, Shuji. / Pharmacokinetics and clinical effects of cefozopran in pediatric patients. In: Japanese Journal of Antibiotics. 1996 ; Vol. 49, No. 1. pp. 17-33.
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title = "Pharmacokinetics and clinical effects of cefozopran in pediatric patients",
abstract = "An investigation was made into pharmacokinetics and clinical effects of the newly developed cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), in pediatric patients. In 26 patients in whom pharmacokinetics were investigated, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by i.v injection were 21.3 ± 10.0 (mean ± standard deviation), 51.0 ± 9.9 and 68.3 ± 0.7 μg/ml, respectively. Serum concentrations at 6 hours after administration were 2.9 ± 17.2.3 ± 0.9 and 4.6 ± 2.6 μg/ml, with the levels roughly above MIC90s for dominating pathogenic bacteria being maintained until 6 hours after treatment. Urine concentrations were in the range between 200 and 560 μg/ml at 4 to 6 hours after dosing Cumulative urine excretion accounted for 70 to 80{\%} of dose. In 11 patients in whom pharmacokinetic investigations were performed, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by 30- min. i. v. drip infusion were 37.1, 66.3 ± 25.5 and 95.7 ± 8.9 μg/ml, respectively. Serum concentrations at 6 hours after dosing were 1.6, 2.3 ± 0.8 and 3.0 ± 0.4 μg/ml, respectively, with the levels above MIC90s for dominating pathogenic bacteria also being maintained until 6 hours after administration. Urine concentrations were 190 μg/ml or more until 8 hours after dosing and the cumulative urinary excretion accounted for 50 to 70{\%} of dose. In 9 patients with meningitis in whom CZOP penetration into cerebrospinal fluid was investigated, concentrations in the fluid of the compound i.v. injected at doses from 40 to 53 mg/kg were in the range between 1.6 and 43.4 μg/ml exceeding MICs for pathogenic bacteria at 1 to 1.5 hours after dosing. In all of the 38 patients in whom pharmacokinetic investigations and clinical evaluations were performed, CZOP was good to excellent (excellent in 22 patients and good in 16 patients). Also in bacteriological evaluations, all of the 31 strains of investigated pathogenic bacteria were eradicated. The clinical efficacy rates for the 335 subjects for clinical evaluations were 97.0{\%} (195/201) for patients in whom pathogenic bacteria were detected (group A), and 95.5{\%} (128/134) for patients in whom no pathogenic bacteria were detected (group B). In bacteriological evaluations, the eradication rates of Gram-positive and Gram-negative bacteria were 96.3{\%} (77/80) and 04.5{\%} (155/164), respectively, with the eradication rate in total being 95.1{\%} (232/244). Safety investigations were performed in 364 patients. Adverse reactions were reported in 11 patients (3.0{\%}), including diarrhea (aqueous stool and soft stool) in 7 patients (1.9{\%}) and drug rash (rash, eruption and wheal) in 4 patients (1.1{\%}). Abnormal laboratory test values were noted in 54 patients, including eosinophilia in 20 patients (6.3{\%}) and elevated GPT in 20 patients (63{\%}). The adverse reactions and abnormal laboratory test values were not serious, disappearing or improving during the continued treatment period or as a result of discontinuation of the treatment. Serum and urine concentrations of CZOP, when administered by i.v injection and 30-min iv drip infusion at doses of 10, 20 and 40 mg/kg, were higher than the MICs for pathogenic bacteria until 6 hours after dosing. The drug also showed favorable penetration into cerebrospinal fluid. It was therefore considered that CZOP was a highly useful drug for the treatment of pediatric infections with sufficient bacteriological and clinical efficacy when administered at a dose of 40 to 80 mg/kg three to four times daily.",
author = "Ryochi Fujii and Toshiaki Abe and Tsuyoshi Tajima and Itaru Terashima and Hidenori Meguro and Susumu Nakazawa and Hajime Sato and Kenji Niinou and Keisuke Sunakawa and Takao Yokota and Hironobu Akita and Satoshi Iwata and Yoshitake Sato and Yoshikiyo Toyonaga and Hironori Nakamura and Kiwamu Seo and Kawamura, {Ken Ichi} and Kuniyoshi Kuno and Kazue Ito and Naoichi Iwai and Haruhi Nakamura and Youichi Taneda and Minoru Sakurai and Masahiro Ito and Eiichi Azuma and Hitoshi Kamiya and Kenji Kitamura and Haruki Mikawa and Hajime Kimata and Tadafumi Nishimura and Kazuo Tabuki and Shigeyuki Aoki and Michio Takagi and Yohnosuke Kobayashi and Shoichiro Taniuchi and Yutaka Kobayashi and Tsunekazu Haruta and Okura, {Kan Etsu} and Shigekazu Kuroki and Toshikazu Nishio and Hiroshi Matsuda and Kaichi Kida and Yukikazu Kainou and Takanobu Kurashige and Hideo Morita and Yasuhiro Kuroda and Etsuhisa Shirakawa and Takashi Okamoto and Takanori Sekiguchi and Yoshiro Tsuji and Izumi Gondo and Nobuo Kobayashi and Takashi Motohiro and Yasutaka Sakata and Hirokazu Sasaki and Youichiro Yoshinaga and Shuji Yamada",
year = "1996",
month = "1",
language = "English",
volume = "49",
pages = "17--33",
journal = "The Journal of antibiotics. Ser. B",
issn = "0368-2781",
publisher = "Japan Antibiotics Research Association",
number = "1",

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TY - JOUR

T1 - Pharmacokinetics and clinical effects of cefozopran in pediatric patients

AU - Fujii, Ryochi

AU - Abe, Toshiaki

AU - Tajima, Tsuyoshi

AU - Terashima, Itaru

AU - Meguro, Hidenori

AU - Nakazawa, Susumu

AU - Sato, Hajime

AU - Niinou, Kenji

AU - Sunakawa, Keisuke

AU - Yokota, Takao

AU - Akita, Hironobu

AU - Iwata, Satoshi

AU - Sato, Yoshitake

AU - Toyonaga, Yoshikiyo

AU - Nakamura, Hironori

AU - Seo, Kiwamu

AU - Kawamura, Ken Ichi

AU - Kuno, Kuniyoshi

AU - Ito, Kazue

AU - Iwai, Naoichi

AU - Nakamura, Haruhi

AU - Taneda, Youichi

AU - Sakurai, Minoru

AU - Ito, Masahiro

AU - Azuma, Eiichi

AU - Kamiya, Hitoshi

AU - Kitamura, Kenji

AU - Mikawa, Haruki

AU - Kimata, Hajime

AU - Nishimura, Tadafumi

AU - Tabuki, Kazuo

AU - Aoki, Shigeyuki

AU - Takagi, Michio

AU - Kobayashi, Yohnosuke

AU - Taniuchi, Shoichiro

AU - Kobayashi, Yutaka

AU - Haruta, Tsunekazu

AU - Okura, Kan Etsu

AU - Kuroki, Shigekazu

AU - Nishio, Toshikazu

AU - Matsuda, Hiroshi

AU - Kida, Kaichi

AU - Kainou, Yukikazu

AU - Kurashige, Takanobu

AU - Morita, Hideo

AU - Kuroda, Yasuhiro

AU - Shirakawa, Etsuhisa

AU - Okamoto, Takashi

AU - Sekiguchi, Takanori

AU - Tsuji, Yoshiro

AU - Gondo, Izumi

AU - Kobayashi, Nobuo

AU - Motohiro, Takashi

AU - Sakata, Yasutaka

AU - Sasaki, Hirokazu

AU - Yoshinaga, Youichiro

AU - Yamada, Shuji

PY - 1996/1

Y1 - 1996/1

N2 - An investigation was made into pharmacokinetics and clinical effects of the newly developed cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), in pediatric patients. In 26 patients in whom pharmacokinetics were investigated, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by i.v injection were 21.3 ± 10.0 (mean ± standard deviation), 51.0 ± 9.9 and 68.3 ± 0.7 μg/ml, respectively. Serum concentrations at 6 hours after administration were 2.9 ± 17.2.3 ± 0.9 and 4.6 ± 2.6 μg/ml, with the levels roughly above MIC90s for dominating pathogenic bacteria being maintained until 6 hours after treatment. Urine concentrations were in the range between 200 and 560 μg/ml at 4 to 6 hours after dosing Cumulative urine excretion accounted for 70 to 80% of dose. In 11 patients in whom pharmacokinetic investigations were performed, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by 30- min. i. v. drip infusion were 37.1, 66.3 ± 25.5 and 95.7 ± 8.9 μg/ml, respectively. Serum concentrations at 6 hours after dosing were 1.6, 2.3 ± 0.8 and 3.0 ± 0.4 μg/ml, respectively, with the levels above MIC90s for dominating pathogenic bacteria also being maintained until 6 hours after administration. Urine concentrations were 190 μg/ml or more until 8 hours after dosing and the cumulative urinary excretion accounted for 50 to 70% of dose. In 9 patients with meningitis in whom CZOP penetration into cerebrospinal fluid was investigated, concentrations in the fluid of the compound i.v. injected at doses from 40 to 53 mg/kg were in the range between 1.6 and 43.4 μg/ml exceeding MICs for pathogenic bacteria at 1 to 1.5 hours after dosing. In all of the 38 patients in whom pharmacokinetic investigations and clinical evaluations were performed, CZOP was good to excellent (excellent in 22 patients and good in 16 patients). Also in bacteriological evaluations, all of the 31 strains of investigated pathogenic bacteria were eradicated. The clinical efficacy rates for the 335 subjects for clinical evaluations were 97.0% (195/201) for patients in whom pathogenic bacteria were detected (group A), and 95.5% (128/134) for patients in whom no pathogenic bacteria were detected (group B). In bacteriological evaluations, the eradication rates of Gram-positive and Gram-negative bacteria were 96.3% (77/80) and 04.5% (155/164), respectively, with the eradication rate in total being 95.1% (232/244). Safety investigations were performed in 364 patients. Adverse reactions were reported in 11 patients (3.0%), including diarrhea (aqueous stool and soft stool) in 7 patients (1.9%) and drug rash (rash, eruption and wheal) in 4 patients (1.1%). Abnormal laboratory test values were noted in 54 patients, including eosinophilia in 20 patients (6.3%) and elevated GPT in 20 patients (63%). The adverse reactions and abnormal laboratory test values were not serious, disappearing or improving during the continued treatment period or as a result of discontinuation of the treatment. Serum and urine concentrations of CZOP, when administered by i.v injection and 30-min iv drip infusion at doses of 10, 20 and 40 mg/kg, were higher than the MICs for pathogenic bacteria until 6 hours after dosing. The drug also showed favorable penetration into cerebrospinal fluid. It was therefore considered that CZOP was a highly useful drug for the treatment of pediatric infections with sufficient bacteriological and clinical efficacy when administered at a dose of 40 to 80 mg/kg three to four times daily.

AB - An investigation was made into pharmacokinetics and clinical effects of the newly developed cephem antibiotic for injection, cefozopran (SCE-2787, CZOP), in pediatric patients. In 26 patients in whom pharmacokinetics were investigated, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by i.v injection were 21.3 ± 10.0 (mean ± standard deviation), 51.0 ± 9.9 and 68.3 ± 0.7 μg/ml, respectively. Serum concentrations at 6 hours after administration were 2.9 ± 17.2.3 ± 0.9 and 4.6 ± 2.6 μg/ml, with the levels roughly above MIC90s for dominating pathogenic bacteria being maintained until 6 hours after treatment. Urine concentrations were in the range between 200 and 560 μg/ml at 4 to 6 hours after dosing Cumulative urine excretion accounted for 70 to 80% of dose. In 11 patients in whom pharmacokinetic investigations were performed, peak serum concentrations of CZOP administered at doses of 10, 20 and 40 mg/kg by 30- min. i. v. drip infusion were 37.1, 66.3 ± 25.5 and 95.7 ± 8.9 μg/ml, respectively. Serum concentrations at 6 hours after dosing were 1.6, 2.3 ± 0.8 and 3.0 ± 0.4 μg/ml, respectively, with the levels above MIC90s for dominating pathogenic bacteria also being maintained until 6 hours after administration. Urine concentrations were 190 μg/ml or more until 8 hours after dosing and the cumulative urinary excretion accounted for 50 to 70% of dose. In 9 patients with meningitis in whom CZOP penetration into cerebrospinal fluid was investigated, concentrations in the fluid of the compound i.v. injected at doses from 40 to 53 mg/kg were in the range between 1.6 and 43.4 μg/ml exceeding MICs for pathogenic bacteria at 1 to 1.5 hours after dosing. In all of the 38 patients in whom pharmacokinetic investigations and clinical evaluations were performed, CZOP was good to excellent (excellent in 22 patients and good in 16 patients). Also in bacteriological evaluations, all of the 31 strains of investigated pathogenic bacteria were eradicated. The clinical efficacy rates for the 335 subjects for clinical evaluations were 97.0% (195/201) for patients in whom pathogenic bacteria were detected (group A), and 95.5% (128/134) for patients in whom no pathogenic bacteria were detected (group B). In bacteriological evaluations, the eradication rates of Gram-positive and Gram-negative bacteria were 96.3% (77/80) and 04.5% (155/164), respectively, with the eradication rate in total being 95.1% (232/244). Safety investigations were performed in 364 patients. Adverse reactions were reported in 11 patients (3.0%), including diarrhea (aqueous stool and soft stool) in 7 patients (1.9%) and drug rash (rash, eruption and wheal) in 4 patients (1.1%). Abnormal laboratory test values were noted in 54 patients, including eosinophilia in 20 patients (6.3%) and elevated GPT in 20 patients (63%). The adverse reactions and abnormal laboratory test values were not serious, disappearing or improving during the continued treatment period or as a result of discontinuation of the treatment. Serum and urine concentrations of CZOP, when administered by i.v injection and 30-min iv drip infusion at doses of 10, 20 and 40 mg/kg, were higher than the MICs for pathogenic bacteria until 6 hours after dosing. The drug also showed favorable penetration into cerebrospinal fluid. It was therefore considered that CZOP was a highly useful drug for the treatment of pediatric infections with sufficient bacteriological and clinical efficacy when administered at a dose of 40 to 80 mg/kg three to four times daily.

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