Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates

Y. Sato, K. Sunakawa, H. Akita, S. Iwata, T. Yokota, Y. Kusumoto

Research output: Contribution to journalArticle

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Abstract

We conducted fundamental and clinical evaluations of a cephem antibiotic, cefozopran (SCE-2787, CZOP), in infants with low birth weights and mature infants. (1) Blood concentrations. CZOP was intravenously given in bolus dose of 20 mg/kg to the newborn. The blood antibiotic concentrations were 69.7 μg/ml at 30 minutes after administration and the elimination half life was 2.99 hours in mature infants aged 1-3 days. They were 38.7 μg/ml and 2.85 hours in those aged 4-7 days, and 40.8 μg/ml and 3.81 hours in those aged 8 days or elder, respectively. In infants with lower birth weights aged 4-7 days the blood antibiotic concentrations were 48.6 μg/ml at 30 minutes after i.v. administration and the elimination half life was 3.77 hours. The blood antibiotic concentrations at 30 minutes after intravenous doses of 10, 20 and 50 mg/kg in mature infants aged 8 days or elder were 21.1, 40.8 and 153.6 μg/ml(value at 60 minutes) and the elimination half lives were 2.24, 3.81 and 3.07 hours, respectively. Administration of CZOP at doses of 20 and 40 mg/kg by intravenous drip infusion over 30 minutes gave the blood drug concentrations of 48.0 and 103.2 μg/ml at the end of infusion and the half lives were 2.60 and 3.33 hours, respectively. (2) Urinary excretion. The urinary excretion rates after i.v. bolus doses of 10, 20 and 40 mg/kg were 28.4-58.6% of dose. The urinary excretion rate after i.v. drip infusion of 40 mg/kg over 30 minutes was 49.0% of dose. (3) Transfer into cereblospinal fluid. The transfer of the antibiotic into cereblospinal fluid in patients with serous meningitis was 4.1-15.5μg/ml at 1 hour after administration. (4) Clinical results. The clinical efficacy was judged 'good' or 'excellent' in 2 of the 3 patients with septicemia and in all of the 10 patients with suspected septicemia. It was judged 'excellent' in all of the 9 patients with pneumonia, 3 with urinary tract infections and 3 with intrauterine infections. Prophylactic use of the antibiotic was effective in all of the 12 patients. Of the patients in whom bacteriological evaluation was successful, 7 of the 10 causative organisms were confirmed to be eradicated. No adverse drug reactions of signs and symptoms were recognized. Fourteen abnormal alterations of the laboratory test values such as elevation of γ-GTP and that of GPT were recognized in 8 patients (16.7%). None of them were particularly serious. These results indicate that CZOP is a drug useful for treatment and prevention of infections in infants with lower birth weights as well as in mature infants.

Original languageEnglish
Pages (from-to)917-935
Number of pages19
JournalJapanese Journal of Antibiotics
Volume50
Issue number12
Publication statusPublished - 1997
Externally publishedYes

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Low Birth Weight Infant
Newborn Infant
Anti-Bacterial Agents
Intravenous Infusions
Birth Weight
Half-Life
Sepsis
Guanosine Triphosphate
Infection
cefozopran
Drug-Related Side Effects and Adverse Reactions
Meningitis
Urinary Tract Infections
Pharmaceutical Preparations
Signs and Symptoms
Pneumonia

ASJC Scopus subject areas

  • Pharmacology
  • Molecular Medicine

Cite this

Sato, Y., Sunakawa, K., Akita, H., Iwata, S., Yokota, T., & Kusumoto, Y. (1997). Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates. Japanese Journal of Antibiotics, 50(12), 917-935.

Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates. / Sato, Y.; Sunakawa, K.; Akita, H.; Iwata, S.; Yokota, T.; Kusumoto, Y.

In: Japanese Journal of Antibiotics, Vol. 50, No. 12, 1997, p. 917-935.

Research output: Contribution to journalArticle

Sato, Y, Sunakawa, K, Akita, H, Iwata, S, Yokota, T & Kusumoto, Y 1997, 'Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates', Japanese Journal of Antibiotics, vol. 50, no. 12, pp. 917-935.
Sato Y, Sunakawa K, Akita H, Iwata S, Yokota T, Kusumoto Y. Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates. Japanese Journal of Antibiotics. 1997;50(12):917-935.
Sato, Y. ; Sunakawa, K. ; Akita, H. ; Iwata, S. ; Yokota, T. ; Kusumoto, Y. / Fundamental and clinical evaluation of cefozopran in low birth weight infants and neonates. In: Japanese Journal of Antibiotics. 1997 ; Vol. 50, No. 12. pp. 917-935.
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