Pharmacokinetic, bacteriological and clinical studies on neonates cefozopran

Ryochi Fujii, Akimasa Okuno, Kozo Fujita, Fujio Kakuya, Shizuo Maruyama, Hiroshi Sakata, Fumie Inyaku, Toshiaki Abe, Shintaro Hashira, Yutaka Nakazato, Masatoshi Sugiura, Takeshi Tajima, Shizuka Nagai, Noriaki Funamoto, Sumiko Sugimori, Shuichi Nishimura, Kohichi Yoshimura, Yasuo Kondoii, Yasuko Kawaoi, Itaru TerashimaHidenori Meguro, Yutaka Takeuchi, Masato Kantake, Keisuke Sunakawa, Satoshi Iwata, Hironobu Akita, Takao Yokota, Yoshitake Sato, Yutaka Kusumoto, Yoshikiyo Toyonaga, Toshihide Ishihara, Hironori Nakamura, Kenji Niinou, Naoichi Iwai, Haruhi Nakamura, Minoru Sakurai, Masahiro Itoh, Hideiuro Nishihara, Tadafumi Nishimura, Yutaka Kobayashi, Tsunekazu Haruta, Kan Etsu Ohkura, Takashi Motoniro, Yasutaka Sakata, Kensuke Nagai, Jun Morita, Tomoya Takagishi, Yusaku Matsuo, Takeo Hashimoto, Youichiro Yoshinaga, Masao Hayashi, Atsushi Toyota, Tamotsu Fujimoto, Masaomi Wada, Shintaro Kamizono, Yoshiro Tsuji, Kunio Tomimasu, Muneyoshi Yoshinaga, Toshimitsu Takayanagi, Seiko Nakashita, Takashi Kusumoto, Hiroya Tanaka, Katsutoshi Hayashi, Takeshi Miyano, Toshiki Oya, Yataro Hosoda, Tadao Manabe, Yasunobu Shimizu, Yosihhiro Otobe, Takashi Hashimoto, Morimasa Yagisawa

Research output: Contribution to journalArticlepeer-review

Abstract

(1) Half-lives (T 1/2's) of CZOP in 0-day-old (less than 24 hours after birth) neonates and premature infants were longer than those in 1-day-old or older infants. When half-lives were compared between 0-day-old neonates and 0-day-old premature infants, longer half-lives were observed in premature infants. (2) When CZOP was intravenously administered to 1-day-old or older neonates and premature infants at a dose of 20mgAg, no differences were noted in blood concentrations between neonates and premature infants from 30 minutes to 6 hours after administration as well as T 1/2's. (3) Blood concentrations of CZOP administered at doses of 10, 20 and 40mg/kg were dose-dependent. (4) Urine excretion rates of CZOP administered to 1-day-old or older neonates and premature infants were approximately 30 to 60% in the first 6 hours after administration. Urine excretion rates in 0-day-old neonates and premature infants were low. 2. Clinical results (1) Of a total of 136 cases to which CZOP was administered, clinical efficacy evaluation was possible in 96 cases, and safety evaluation in 132 cases. (2) The clinical efficacy rates were 78.6% (22/28) in 28 cases in which causative organisms were detected (Group A), and 97,1% (66/68) in 68 cases in which no such organisms were detected (Group B), with the total efficacy rate (Groups A and B) of as high as 91.7% (88/96). (3) Bacteriological evaluations were made with 33 strains isolated from the 28 cases of Group A. Elimination rates for Gram-positive and Gram-negative bacteria were 88.2% (15/17) and 92.3% (12/13), respectively, with the total elimination rate of 90.0% (27/30). No microbial substitution was noted. (4) As an adverse reaction, diarrhea was noted in one case (0.8%). Abnormal laboratory test values were noted in 15 cases (12.3%) including eosinophilia, elevated GPT, and elevated 7-GTP. All of these abnormalities were transitory, and none of them critical. As a result of above pharmacokinetic and clinical investigations, CZOP is considered to be highly useful in the treatment of indicated infections in neonates and premature infants. It appears that 20mg/kg of CZOP can be administered by intravenous injection or intravenous drip infusion to neonates and premature infants aged 0-day (less than 24 hours after birth) once or twice daily, to those aged 1 (24 or more hours after birth) to 7 days twice or three times daily, and to those aged 8 or more days three or four times daily, and that the dose can be increased up to 40mgAg in cases of critical or intractable infections.

Original languageEnglish
Pages (from-to)697-702
Number of pages6
JournalJapanese Journal of Antibiotics
Volume49
Issue number7
Publication statusPublished - 1996

ASJC Scopus subject areas

  • Microbiology (medical)
  • Pharmacology (medical)
  • Infectious Diseases

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