Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field

Ryochi Fujii, Hidenori Meguro, Osamu Arimasu, Mitsuru Tagaya, Kozo Fujita, Hiroshi Sakata, Hajime Yoshioka, Shizuo Maruyama, Nobutaka Sanae, Ichimei Nagamatsu, Kazuo Abe, Akihiko Miyanoshita, Akira Watanabe, Masakazu Ohnuma, Yukio Izumi, Ryuzo Aoyama, Suzuko Uehara, Itaru Terashima, Akira Nakamura, Tsuyoshi Toba & 88 others Tatsuya Hayashi, Michio Hoshino, Suzuko Uehara, Itaru Terashima, Akira Nakamura, Tsuyoshi Toba, Tatsuya Hayashi, Michio Hoshino, Suzuko Uehara, Itaru Terashima, Akira Nakamura, Tsuyoshi Toba, Tatsuya Hayashi, Michio Hoshino, Suzuko Uehara, Itaru Terashima, Akira Nakamura, Tsuyoshi Toba, Tatsuya Hayashi, Michio Hoshino, Hajime Sato, Hidejiro Chikaoka, Shinichi Nakazawa, Katsumori Tazoe, Susumu Nakazawa, Hajime Sato, Hidejiro Chikaoka, Shinichi Nakazawa, Katsumori Tazoe, Susumu Nakazawa, Hajime Sato, Hidejiro Chikaoka, Shinichi Nakazawa, Katsumori Tazoe, Susumu Nakazawa, Haruo Ichihashi, Hiroki Hoshina, Kenichi Mikuni, Mikio Minamitani, Kei Hachimori, Kazutaka Kaneda, Yoshitake Sato, Satoshi Iwata, Hironobu Akita, Naoya Yamashita, Tadao Oikawa, Takayasu Murai, Shinya Hayano, Mitsuru Osano, Makoto Hori, Yoshiie Kurosu, Yoshikiyo Toyonaga, Morimasa Sugita, Makoto Hori, Yoshiie Kurosu, Yoshikiyo Toyonaga, Morimasa Sugita, Makoto Hori, Yoshiie Kurosu, Yoshikiyo Toyonaga, Morimasa Sugita, Hiroshi Hayakawa, Yukishige Yanagawa, Keisuke Sunakawa, Naoichi Iwai, Yoichi Taneda, Motohiro Shibata, Fumiko Mizoguchi, Michihiro Katayama, Shun Hashimoto, Yukitaka Murata, Jiro Yura, Tadafumi Nishimura, Toshio Takashima, Kazuo Tabuki, Michio Takagi, Tadafumi Nishimura, Toshio Takashima, Kazuo Tabuki, Michio Takagi, Yutaka Kobayashi, Tsunekazu Haruta, Shigekazu Kuroki, Kan etsu Ohkura, Takashi Motohiro, Tohru Nishiyama, Kaoru Tominaga, Fumio Yamashita

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Ceftriaxone (CTRX), a new injectable cephem antibiotic agent, was evaluated bacteriologically and clinically for its efficacy and safety in the pediatric field by a study group organized with pediatricians from all over the country. The following are a summary of the results of the evaluation. 1. Antibacterial effects: The inhibition of growth was attained for over 90% of strains of K. pneumoniae, H. influenzae and Salmonella spp. at the concentration of 0.10 µg/ml and of strains of S. pneumoniae and E. coli at the concentration of 2.0 µg/ml. The CTRX was proved to have excellent antibacterial effects. 2. Absorption and excretion: Thirty minutes after one shot intravenous administration with 10, 20, 40 and 50 mg/kg of CTRX, its serum levels were 73, 124, 169 and 190 µg/ml, respectively, a clear tendency of dose-response relationship being noticed. The serum levels decreased only gradually and stayed as high as 10 to 20 µg/ml even after 12 hours. The half-lives of the drug were 5.5, 6.3, 6.0 and 4.7 hours for the 4 different dose levels, respectively. Following the intravenous injection with 10, 20 and 40 mg/kg, the urinary excretion rates were 55, 52 and 54%, respectively. Following the one shot intravenous administration or by the drip infusion for 30 minutes with about 50 mg/kg, CTRX levels in the cerebrospinal fluid ranged from 1 to 20.3 µg/ml in case of purulent meningitis (5 to 10 µg/ml in most cases). 3. Clinical results: A total of 322 cases was enrolled. The efficacy of CTRX was evaluated in 295 cases out of the 322, excluding drop-outs and the cases which did not meet the protocols. The clinical efficacy rate was 94% of 191 cases where the causative bacteria were identified, CTRX being “excellent” in 108 cases and “effective” in 72. In the remaining 104 cases where the causative bacteria were not identified, the efficacy rate was 92%, CTRX being “excellent” in 42 cases and “effective” in 54. Furthermore, the efficacy rate was 89% of 18 cases infected with more than one kind of bacteria. The drug showed “excellent” or better effectiveness in 88% of 75 cases which had not responded to other antibiotics. Bacteriologically, 174 out of 216 strains (93%) which were judged to be causative bacteria disappeared with the use of CTRX. Eightyfive percent of 53 strains which had not responded to other antibiotics disappeared by the CTRX treatment. 4. Adverse reactions and over-ranged clinical laboratory parameters: Adverse reactions like diarrhea, loose passage and urticaria appeared in 28 cases out of 322 (8.7%). In clinical laboratory tests, increase in GOT, eosinophilia, increase in GPT, thrombocytosis, etc. were observed in 38 cases (48 symptoms). 5. Optimal clinical dose in children: The optimal clinical dose in children was 20 mg/kg twice a day by intravenous injection or by drip infusion. The dose was adjusted according to types and severities of diseases. The drug was considered to be a useful cephem antibiotic in the pediatric field especially because of the time-saving and cost-effective twice-a-day administration which was enabled due to the fairly long half-life, the broad antibacterial spectrum, the good transfer to the cerebrospinal fluid and the high safety. The administration to newborn babies, once-a-day administration and adverse reactions will have to be studied further for this new antibiotic agent.

Original languageEnglish
Pages (from-to)1988-2008
Number of pages21
JournalThe Japanese Journal of Antibiotics
Volume39
Issue number8
DOIs
Publication statusPublished - 1986

Fingerprint

Ceftriaxone
Pharmacokinetics
Pediatrics
Anti-Bacterial Agents
Bacteria
Intravenous Infusions
Intravenous Injections
Intravenous Administration
Cerebrospinal Fluid
Pneumonia
Pharmaceutical Preparations
Safety
Thrombocytosis
Urticaria
Eosinophilia
Serum
Meningitis
Salmonella
Human Influenza
Half-Life

ASJC Scopus subject areas

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

Cite this

Fujii, R., Meguro, H., Arimasu, O., Tagaya, M., Fujita, K., Sakata, H., ... Yamashita, F. (1986). Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field. The Japanese Journal of Antibiotics, 39(8), 1988-2008. https://doi.org/10.11553/antibiotics1968b.39.1988

Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field. / Fujii, Ryochi; Meguro, Hidenori; Arimasu, Osamu; Tagaya, Mitsuru; Fujita, Kozo; Sakata, Hiroshi; Yoshioka, Hajime; Maruyama, Shizuo; Sanae, Nobutaka; Nagamatsu, Ichimei; Abe, Kazuo; Miyanoshita, Akihiko; Watanabe, Akira; Ohnuma, Masakazu; Izumi, Yukio; Aoyama, Ryuzo; Uehara, Suzuko; Terashima, Itaru; Nakamura, Akira; Toba, Tsuyoshi; Hayashi, Tatsuya; Hoshino, Michio; Uehara, Suzuko; Terashima, Itaru; Nakamura, Akira; Toba, Tsuyoshi; Hayashi, Tatsuya; Hoshino, Michio; Uehara, Suzuko; Terashima, Itaru; Nakamura, Akira; Toba, Tsuyoshi; Hayashi, Tatsuya; Hoshino, Michio; Uehara, Suzuko; Terashima, Itaru; Nakamura, Akira; Toba, Tsuyoshi; Hayashi, Tatsuya; Hoshino, Michio; Sato, Hajime; Chikaoka, Hidejiro; Nakazawa, Shinichi; Tazoe, Katsumori; Nakazawa, Susumu; Sato, Hajime; Chikaoka, Hidejiro; Nakazawa, Shinichi; Tazoe, Katsumori; Nakazawa, Susumu; Sato, Hajime; Chikaoka, Hidejiro; Nakazawa, Shinichi; Tazoe, Katsumori; Nakazawa, Susumu; Ichihashi, Haruo; Hoshina, Hiroki; Mikuni, Kenichi; Minamitani, Mikio; Hachimori, Kei; Kaneda, Kazutaka; Sato, Yoshitake; Iwata, Satoshi; Akita, Hironobu; Yamashita, Naoya; Oikawa, Tadao; Murai, Takayasu; Hayano, Shinya; Osano, Mitsuru; Hori, Makoto; Kurosu, Yoshiie; Toyonaga, Yoshikiyo; Sugita, Morimasa; Hori, Makoto; Kurosu, Yoshiie; Toyonaga, Yoshikiyo; Sugita, Morimasa; Hori, Makoto; Kurosu, Yoshiie; Toyonaga, Yoshikiyo; Sugita, Morimasa; Hayakawa, Hiroshi; Yanagawa, Yukishige; Sunakawa, Keisuke; Iwai, Naoichi; Taneda, Yoichi; Shibata, Motohiro; Mizoguchi, Fumiko; Katayama, Michihiro; Hashimoto, Shun; Murata, Yukitaka; Yura, Jiro; Nishimura, Tadafumi; Takashima, Toshio; Tabuki, Kazuo; Takagi, Michio; Nishimura, Tadafumi; Takashima, Toshio; Tabuki, Kazuo; Takagi, Michio; Kobayashi, Yutaka; Haruta, Tsunekazu; Kuroki, Shigekazu; Ohkura, Kan etsu; Motohiro, Takashi; Nishiyama, Tohru; Tominaga, Kaoru; Yamashita, Fumio.

In: The Japanese Journal of Antibiotics, Vol. 39, No. 8, 1986, p. 1988-2008.

Research output: Contribution to journalArticle

Fujii, R, Meguro, H, Arimasu, O, Tagaya, M, Fujita, K, Sakata, H, Yoshioka, H, Maruyama, S, Sanae, N, Nagamatsu, I, Abe, K, Miyanoshita, A, Watanabe, A, Ohnuma, M, Izumi, Y, Aoyama, R, Uehara, S, Terashima, I, Nakamura, A, Toba, T, Hayashi, T, Hoshino, M, Uehara, S, Terashima, I, Nakamura, A, Toba, T, Hayashi, T, Hoshino, M, Uehara, S, Terashima, I, Nakamura, A, Toba, T, Hayashi, T, Hoshino, M, Uehara, S, Terashima, I, Nakamura, A, Toba, T, Hayashi, T, Hoshino, M, Sato, H, Chikaoka, H, Nakazawa, S, Tazoe, K, Nakazawa, S, Sato, H, Chikaoka, H, Nakazawa, S, Tazoe, K, Nakazawa, S, Sato, H, Chikaoka, H, Nakazawa, S, Tazoe, K, Nakazawa, S, Ichihashi, H, Hoshina, H, Mikuni, K, Minamitani, M, Hachimori, K, Kaneda, K, Sato, Y, Iwata, S, Akita, H, Yamashita, N, Oikawa, T, Murai, T, Hayano, S, Osano, M, Hori, M, Kurosu, Y, Toyonaga, Y, Sugita, M, Hori, M, Kurosu, Y, Toyonaga, Y, Sugita, M, Hori, M, Kurosu, Y, Toyonaga, Y, Sugita, M, Hayakawa, H, Yanagawa, Y, Sunakawa, K, Iwai, N, Taneda, Y, Shibata, M, Mizoguchi, F, Katayama, M, Hashimoto, S, Murata, Y, Yura, J, Nishimura, T, Takashima, T, Tabuki, K, Takagi, M, Nishimura, T, Takashima, T, Tabuki, K, Takagi, M, Kobayashi, Y, Haruta, T, Kuroki, S, Ohkura, KE, Motohiro, T, Nishiyama, T, Tominaga, K & Yamashita, F 1986, 'Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field', The Japanese Journal of Antibiotics, vol. 39, no. 8, pp. 1988-2008. https://doi.org/10.11553/antibiotics1968b.39.1988
Fujii, Ryochi ; Meguro, Hidenori ; Arimasu, Osamu ; Tagaya, Mitsuru ; Fujita, Kozo ; Sakata, Hiroshi ; Yoshioka, Hajime ; Maruyama, Shizuo ; Sanae, Nobutaka ; Nagamatsu, Ichimei ; Abe, Kazuo ; Miyanoshita, Akihiko ; Watanabe, Akira ; Ohnuma, Masakazu ; Izumi, Yukio ; Aoyama, Ryuzo ; Uehara, Suzuko ; Terashima, Itaru ; Nakamura, Akira ; Toba, Tsuyoshi ; Hayashi, Tatsuya ; Hoshino, Michio ; Uehara, Suzuko ; Terashima, Itaru ; Nakamura, Akira ; Toba, Tsuyoshi ; Hayashi, Tatsuya ; Hoshino, Michio ; Uehara, Suzuko ; Terashima, Itaru ; Nakamura, Akira ; Toba, Tsuyoshi ; Hayashi, Tatsuya ; Hoshino, Michio ; Uehara, Suzuko ; Terashima, Itaru ; Nakamura, Akira ; Toba, Tsuyoshi ; Hayashi, Tatsuya ; Hoshino, Michio ; Sato, Hajime ; Chikaoka, Hidejiro ; Nakazawa, Shinichi ; Tazoe, Katsumori ; Nakazawa, Susumu ; Sato, Hajime ; Chikaoka, Hidejiro ; Nakazawa, Shinichi ; Tazoe, Katsumori ; Nakazawa, Susumu ; Sato, Hajime ; Chikaoka, Hidejiro ; Nakazawa, Shinichi ; Tazoe, Katsumori ; Nakazawa, Susumu ; Ichihashi, Haruo ; Hoshina, Hiroki ; Mikuni, Kenichi ; Minamitani, Mikio ; Hachimori, Kei ; Kaneda, Kazutaka ; Sato, Yoshitake ; Iwata, Satoshi ; Akita, Hironobu ; Yamashita, Naoya ; Oikawa, Tadao ; Murai, Takayasu ; Hayano, Shinya ; Osano, Mitsuru ; Hori, Makoto ; Kurosu, Yoshiie ; Toyonaga, Yoshikiyo ; Sugita, Morimasa ; Hori, Makoto ; Kurosu, Yoshiie ; Toyonaga, Yoshikiyo ; Sugita, Morimasa ; Hori, Makoto ; Kurosu, Yoshiie ; Toyonaga, Yoshikiyo ; Sugita, Morimasa ; Hayakawa, Hiroshi ; Yanagawa, Yukishige ; Sunakawa, Keisuke ; Iwai, Naoichi ; Taneda, Yoichi ; Shibata, Motohiro ; Mizoguchi, Fumiko ; Katayama, Michihiro ; Hashimoto, Shun ; Murata, Yukitaka ; Yura, Jiro ; Nishimura, Tadafumi ; Takashima, Toshio ; Tabuki, Kazuo ; Takagi, Michio ; Nishimura, Tadafumi ; Takashima, Toshio ; Tabuki, Kazuo ; Takagi, Michio ; Kobayashi, Yutaka ; Haruta, Tsunekazu ; Kuroki, Shigekazu ; Ohkura, Kan etsu ; Motohiro, Takashi ; Nishiyama, Tohru ; Tominaga, Kaoru ; Yamashita, Fumio. / Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field. In: The Japanese Journal of Antibiotics. 1986 ; Vol. 39, No. 8. pp. 1988-2008.
@article{9504c8c2b6004c0b8a442242860bcb5e,
title = "Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field",
abstract = "Ceftriaxone (CTRX), a new injectable cephem antibiotic agent, was evaluated bacteriologically and clinically for its efficacy and safety in the pediatric field by a study group organized with pediatricians from all over the country. The following are a summary of the results of the evaluation. 1. Antibacterial effects: The inhibition of growth was attained for over 90{\%} of strains of K. pneumoniae, H. influenzae and Salmonella spp. at the concentration of 0.10 µg/ml and of strains of S. pneumoniae and E. coli at the concentration of 2.0 µg/ml. The CTRX was proved to have excellent antibacterial effects. 2. Absorption and excretion: Thirty minutes after one shot intravenous administration with 10, 20, 40 and 50 mg/kg of CTRX, its serum levels were 73, 124, 169 and 190 µg/ml, respectively, a clear tendency of dose-response relationship being noticed. The serum levels decreased only gradually and stayed as high as 10 to 20 µg/ml even after 12 hours. The half-lives of the drug were 5.5, 6.3, 6.0 and 4.7 hours for the 4 different dose levels, respectively. Following the intravenous injection with 10, 20 and 40 mg/kg, the urinary excretion rates were 55, 52 and 54{\%}, respectively. Following the one shot intravenous administration or by the drip infusion for 30 minutes with about 50 mg/kg, CTRX levels in the cerebrospinal fluid ranged from 1 to 20.3 µg/ml in case of purulent meningitis (5 to 10 µg/ml in most cases). 3. Clinical results: A total of 322 cases was enrolled. The efficacy of CTRX was evaluated in 295 cases out of the 322, excluding drop-outs and the cases which did not meet the protocols. The clinical efficacy rate was 94{\%} of 191 cases where the causative bacteria were identified, CTRX being “excellent” in 108 cases and “effective” in 72. In the remaining 104 cases where the causative bacteria were not identified, the efficacy rate was 92{\%}, CTRX being “excellent” in 42 cases and “effective” in 54. Furthermore, the efficacy rate was 89{\%} of 18 cases infected with more than one kind of bacteria. The drug showed “excellent” or better effectiveness in 88{\%} of 75 cases which had not responded to other antibiotics. Bacteriologically, 174 out of 216 strains (93{\%}) which were judged to be causative bacteria disappeared with the use of CTRX. Eightyfive percent of 53 strains which had not responded to other antibiotics disappeared by the CTRX treatment. 4. Adverse reactions and over-ranged clinical laboratory parameters: Adverse reactions like diarrhea, loose passage and urticaria appeared in 28 cases out of 322 (8.7{\%}). In clinical laboratory tests, increase in GOT, eosinophilia, increase in GPT, thrombocytosis, etc. were observed in 38 cases (48 symptoms). 5. Optimal clinical dose in children: The optimal clinical dose in children was 20 mg/kg twice a day by intravenous injection or by drip infusion. The dose was adjusted according to types and severities of diseases. The drug was considered to be a useful cephem antibiotic in the pediatric field especially because of the time-saving and cost-effective twice-a-day administration which was enabled due to the fairly long half-life, the broad antibacterial spectrum, the good transfer to the cerebrospinal fluid and the high safety. The administration to newborn babies, once-a-day administration and adverse reactions will have to be studied further for this new antibiotic agent.",
author = "Ryochi Fujii and Hidenori Meguro and Osamu Arimasu and Mitsuru Tagaya and Kozo Fujita and Hiroshi Sakata and Hajime Yoshioka and Shizuo Maruyama and Nobutaka Sanae and Ichimei Nagamatsu and Kazuo Abe and Akihiko Miyanoshita and Akira Watanabe and Masakazu Ohnuma and Yukio Izumi and Ryuzo Aoyama and Suzuko Uehara and Itaru Terashima and Akira Nakamura and Tsuyoshi Toba and Tatsuya Hayashi and Michio Hoshino and Suzuko Uehara and Itaru Terashima and Akira Nakamura and Tsuyoshi Toba and Tatsuya Hayashi and Michio Hoshino and Suzuko Uehara and Itaru Terashima and Akira Nakamura and Tsuyoshi Toba and Tatsuya Hayashi and Michio Hoshino and Suzuko Uehara and Itaru Terashima and Akira Nakamura and Tsuyoshi Toba and Tatsuya Hayashi and Michio Hoshino and Hajime Sato and Hidejiro Chikaoka and Shinichi Nakazawa and Katsumori Tazoe and Susumu Nakazawa and Hajime Sato and Hidejiro Chikaoka and Shinichi Nakazawa and Katsumori Tazoe and Susumu Nakazawa and Hajime Sato and Hidejiro Chikaoka and Shinichi Nakazawa and Katsumori Tazoe and Susumu Nakazawa and Haruo Ichihashi and Hiroki Hoshina and Kenichi Mikuni and Mikio Minamitani and Kei Hachimori and Kazutaka Kaneda and Yoshitake Sato and Satoshi Iwata and Hironobu Akita and Naoya Yamashita and Tadao Oikawa and Takayasu Murai and Shinya Hayano and Mitsuru Osano and Makoto Hori and Yoshiie Kurosu and Yoshikiyo Toyonaga and Morimasa Sugita and Makoto Hori and Yoshiie Kurosu and Yoshikiyo Toyonaga and Morimasa Sugita and Makoto Hori and Yoshiie Kurosu and Yoshikiyo Toyonaga and Morimasa Sugita and Hiroshi Hayakawa and Yukishige Yanagawa and Keisuke Sunakawa and Naoichi Iwai and Yoichi Taneda and Motohiro Shibata and Fumiko Mizoguchi and Michihiro Katayama and Shun Hashimoto and Yukitaka Murata and Jiro Yura and Tadafumi Nishimura and Toshio Takashima and Kazuo Tabuki and Michio Takagi and Tadafumi Nishimura and Toshio Takashima and Kazuo Tabuki and Michio Takagi and Yutaka Kobayashi and Tsunekazu Haruta and Shigekazu Kuroki and Ohkura, {Kan etsu} and Takashi Motohiro and Tohru Nishiyama and Kaoru Tominaga and Fumio Yamashita",
year = "1986",
doi = "10.11553/antibiotics1968b.39.1988",
language = "English",
volume = "39",
pages = "1988--2008",
journal = "The Journal of antibiotics. Ser. B",
issn = "0368-2781",
publisher = "Japan Antibiotics Research Association",
number = "8",

}

TY - JOUR

T1 - Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field

AU - Fujii, Ryochi

AU - Meguro, Hidenori

AU - Arimasu, Osamu

AU - Tagaya, Mitsuru

AU - Fujita, Kozo

AU - Sakata, Hiroshi

AU - Yoshioka, Hajime

AU - Maruyama, Shizuo

AU - Sanae, Nobutaka

AU - Nagamatsu, Ichimei

AU - Abe, Kazuo

AU - Miyanoshita, Akihiko

AU - Watanabe, Akira

AU - Ohnuma, Masakazu

AU - Izumi, Yukio

AU - Aoyama, Ryuzo

AU - Uehara, Suzuko

AU - Terashima, Itaru

AU - Nakamura, Akira

AU - Toba, Tsuyoshi

AU - Hayashi, Tatsuya

AU - Hoshino, Michio

AU - Uehara, Suzuko

AU - Terashima, Itaru

AU - Nakamura, Akira

AU - Toba, Tsuyoshi

AU - Hayashi, Tatsuya

AU - Hoshino, Michio

AU - Uehara, Suzuko

AU - Terashima, Itaru

AU - Nakamura, Akira

AU - Toba, Tsuyoshi

AU - Hayashi, Tatsuya

AU - Hoshino, Michio

AU - Uehara, Suzuko

AU - Terashima, Itaru

AU - Nakamura, Akira

AU - Toba, Tsuyoshi

AU - Hayashi, Tatsuya

AU - Hoshino, Michio

AU - Sato, Hajime

AU - Chikaoka, Hidejiro

AU - Nakazawa, Shinichi

AU - Tazoe, Katsumori

AU - Nakazawa, Susumu

AU - Sato, Hajime

AU - Chikaoka, Hidejiro

AU - Nakazawa, Shinichi

AU - Tazoe, Katsumori

AU - Nakazawa, Susumu

AU - Sato, Hajime

AU - Chikaoka, Hidejiro

AU - Nakazawa, Shinichi

AU - Tazoe, Katsumori

AU - Nakazawa, Susumu

AU - Ichihashi, Haruo

AU - Hoshina, Hiroki

AU - Mikuni, Kenichi

AU - Minamitani, Mikio

AU - Hachimori, Kei

AU - Kaneda, Kazutaka

AU - Sato, Yoshitake

AU - Iwata, Satoshi

AU - Akita, Hironobu

AU - Yamashita, Naoya

AU - Oikawa, Tadao

AU - Murai, Takayasu

AU - Hayano, Shinya

AU - Osano, Mitsuru

AU - Hori, Makoto

AU - Kurosu, Yoshiie

AU - Toyonaga, Yoshikiyo

AU - Sugita, Morimasa

AU - Hori, Makoto

AU - Kurosu, Yoshiie

AU - Toyonaga, Yoshikiyo

AU - Sugita, Morimasa

AU - Hori, Makoto

AU - Kurosu, Yoshiie

AU - Toyonaga, Yoshikiyo

AU - Sugita, Morimasa

AU - Hayakawa, Hiroshi

AU - Yanagawa, Yukishige

AU - Sunakawa, Keisuke

AU - Iwai, Naoichi

AU - Taneda, Yoichi

AU - Shibata, Motohiro

AU - Mizoguchi, Fumiko

AU - Katayama, Michihiro

AU - Hashimoto, Shun

AU - Murata, Yukitaka

AU - Yura, Jiro

AU - Nishimura, Tadafumi

AU - Takashima, Toshio

AU - Tabuki, Kazuo

AU - Takagi, Michio

AU - Nishimura, Tadafumi

AU - Takashima, Toshio

AU - Tabuki, Kazuo

AU - Takagi, Michio

AU - Kobayashi, Yutaka

AU - Haruta, Tsunekazu

AU - Kuroki, Shigekazu

AU - Ohkura, Kan etsu

AU - Motohiro, Takashi

AU - Nishiyama, Tohru

AU - Tominaga, Kaoru

AU - Yamashita, Fumio

PY - 1986

Y1 - 1986

N2 - Ceftriaxone (CTRX), a new injectable cephem antibiotic agent, was evaluated bacteriologically and clinically for its efficacy and safety in the pediatric field by a study group organized with pediatricians from all over the country. The following are a summary of the results of the evaluation. 1. Antibacterial effects: The inhibition of growth was attained for over 90% of strains of K. pneumoniae, H. influenzae and Salmonella spp. at the concentration of 0.10 µg/ml and of strains of S. pneumoniae and E. coli at the concentration of 2.0 µg/ml. The CTRX was proved to have excellent antibacterial effects. 2. Absorption and excretion: Thirty minutes after one shot intravenous administration with 10, 20, 40 and 50 mg/kg of CTRX, its serum levels were 73, 124, 169 and 190 µg/ml, respectively, a clear tendency of dose-response relationship being noticed. The serum levels decreased only gradually and stayed as high as 10 to 20 µg/ml even after 12 hours. The half-lives of the drug were 5.5, 6.3, 6.0 and 4.7 hours for the 4 different dose levels, respectively. Following the intravenous injection with 10, 20 and 40 mg/kg, the urinary excretion rates were 55, 52 and 54%, respectively. Following the one shot intravenous administration or by the drip infusion for 30 minutes with about 50 mg/kg, CTRX levels in the cerebrospinal fluid ranged from 1 to 20.3 µg/ml in case of purulent meningitis (5 to 10 µg/ml in most cases). 3. Clinical results: A total of 322 cases was enrolled. The efficacy of CTRX was evaluated in 295 cases out of the 322, excluding drop-outs and the cases which did not meet the protocols. The clinical efficacy rate was 94% of 191 cases where the causative bacteria were identified, CTRX being “excellent” in 108 cases and “effective” in 72. In the remaining 104 cases where the causative bacteria were not identified, the efficacy rate was 92%, CTRX being “excellent” in 42 cases and “effective” in 54. Furthermore, the efficacy rate was 89% of 18 cases infected with more than one kind of bacteria. The drug showed “excellent” or better effectiveness in 88% of 75 cases which had not responded to other antibiotics. Bacteriologically, 174 out of 216 strains (93%) which were judged to be causative bacteria disappeared with the use of CTRX. Eightyfive percent of 53 strains which had not responded to other antibiotics disappeared by the CTRX treatment. 4. Adverse reactions and over-ranged clinical laboratory parameters: Adverse reactions like diarrhea, loose passage and urticaria appeared in 28 cases out of 322 (8.7%). In clinical laboratory tests, increase in GOT, eosinophilia, increase in GPT, thrombocytosis, etc. were observed in 38 cases (48 symptoms). 5. Optimal clinical dose in children: The optimal clinical dose in children was 20 mg/kg twice a day by intravenous injection or by drip infusion. The dose was adjusted according to types and severities of diseases. The drug was considered to be a useful cephem antibiotic in the pediatric field especially because of the time-saving and cost-effective twice-a-day administration which was enabled due to the fairly long half-life, the broad antibacterial spectrum, the good transfer to the cerebrospinal fluid and the high safety. The administration to newborn babies, once-a-day administration and adverse reactions will have to be studied further for this new antibiotic agent.

AB - Ceftriaxone (CTRX), a new injectable cephem antibiotic agent, was evaluated bacteriologically and clinically for its efficacy and safety in the pediatric field by a study group organized with pediatricians from all over the country. The following are a summary of the results of the evaluation. 1. Antibacterial effects: The inhibition of growth was attained for over 90% of strains of K. pneumoniae, H. influenzae and Salmonella spp. at the concentration of 0.10 µg/ml and of strains of S. pneumoniae and E. coli at the concentration of 2.0 µg/ml. The CTRX was proved to have excellent antibacterial effects. 2. Absorption and excretion: Thirty minutes after one shot intravenous administration with 10, 20, 40 and 50 mg/kg of CTRX, its serum levels were 73, 124, 169 and 190 µg/ml, respectively, a clear tendency of dose-response relationship being noticed. The serum levels decreased only gradually and stayed as high as 10 to 20 µg/ml even after 12 hours. The half-lives of the drug were 5.5, 6.3, 6.0 and 4.7 hours for the 4 different dose levels, respectively. Following the intravenous injection with 10, 20 and 40 mg/kg, the urinary excretion rates were 55, 52 and 54%, respectively. Following the one shot intravenous administration or by the drip infusion for 30 minutes with about 50 mg/kg, CTRX levels in the cerebrospinal fluid ranged from 1 to 20.3 µg/ml in case of purulent meningitis (5 to 10 µg/ml in most cases). 3. Clinical results: A total of 322 cases was enrolled. The efficacy of CTRX was evaluated in 295 cases out of the 322, excluding drop-outs and the cases which did not meet the protocols. The clinical efficacy rate was 94% of 191 cases where the causative bacteria were identified, CTRX being “excellent” in 108 cases and “effective” in 72. In the remaining 104 cases where the causative bacteria were not identified, the efficacy rate was 92%, CTRX being “excellent” in 42 cases and “effective” in 54. Furthermore, the efficacy rate was 89% of 18 cases infected with more than one kind of bacteria. The drug showed “excellent” or better effectiveness in 88% of 75 cases which had not responded to other antibiotics. Bacteriologically, 174 out of 216 strains (93%) which were judged to be causative bacteria disappeared with the use of CTRX. Eightyfive percent of 53 strains which had not responded to other antibiotics disappeared by the CTRX treatment. 4. Adverse reactions and over-ranged clinical laboratory parameters: Adverse reactions like diarrhea, loose passage and urticaria appeared in 28 cases out of 322 (8.7%). In clinical laboratory tests, increase in GOT, eosinophilia, increase in GPT, thrombocytosis, etc. were observed in 38 cases (48 symptoms). 5. Optimal clinical dose in children: The optimal clinical dose in children was 20 mg/kg twice a day by intravenous injection or by drip infusion. The dose was adjusted according to types and severities of diseases. The drug was considered to be a useful cephem antibiotic in the pediatric field especially because of the time-saving and cost-effective twice-a-day administration which was enabled due to the fairly long half-life, the broad antibacterial spectrum, the good transfer to the cerebrospinal fluid and the high safety. The administration to newborn babies, once-a-day administration and adverse reactions will have to be studied further for this new antibiotic agent.

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U2 - 10.11553/antibiotics1968b.39.1988

DO - 10.11553/antibiotics1968b.39.1988

M3 - Article

VL - 39

SP - 1988

EP - 2008

JO - The Journal of antibiotics. Ser. B

JF - The Journal of antibiotics. Ser. B

SN - 0368-2781

IS - 8

ER -