[Pharmacokinetic and clinical studies on cefozopran in pediatrics]
Insights
Cefozopran (CZOP) demonstrates excellent efficacy and safety in treating pediatric infections, including meningitis and pneumonia. This parenteral cephalosporin achieved high clinical response rates with minimal side effects in young patients.
Area of Science:
- Pediatric Infectious Diseases
- Pharmacology
- Clinical Microbiology
Background:
- Cefozopran (CZOP), a novel parenteral cephalosporin, was evaluated for its pharmacokinetic and therapeutic profile in pediatric patients.
- Understanding the drug's penetration into cerebrospinal fluid (CSF) and its effectiveness against common pediatric pathogens is crucial.
Observation:
- Serum concentrations of CZOP reached 92.1 µg/ml and CSF concentrations reached 10.5 µg/ml one hour post-injection (50 mg/kg).
- CZOP exhibited an 11.4% penetration rate into CSF in patients with purulent meningitis.
- Twenty-five pediatric patients with various infections, including meningitis, pneumonia, and urinary tract infections, received CZOP.
Findings:
- All 25 patients showed excellent or good clinical responses to CZOP treatment.
- Bacteriological eradication was achieved for 22 out of 25 strains, with exceptions including Staphylococcus aureus and Salmonella sp.
- Adverse events were minimal, with diarrhea reported in one patient. Laboratory findings revealed mild eosinophilia, thrombocytosis, and elevated GPT in a few patients, with no impact on coagulation parameters.
Implications:
- Cefozopran is a safe and effective antibiotic for treating a range of pediatric infections.
- The recommended dosage for intravenous administration is 20-50 mg/kg every 6-8 hours.
- Further research may explore CZOP's utility in specific resistant bacterial infections in pediatric populations.
Abstract:
Cefozopran (CZOP, SCE-2787), a new parenteral cephalosporin antibiotic, was studied for its pharmacokinetics, bacteriological and clinical effects in the field of pediatrics. The serum and cerebrospinal fluid concentrations 1 hour after a bolus intravenous injection of 50 mg/kg were, respectively, 92.1, 10.5 micrograms/ml, and penetration rate to cerebrospinal fluid of CZOP in patients with purulent meningitis was 11.4%. 25 patients, including those with purulent meningitis, pneumonia, urinary tract infections, staphylococcal scalded skin syndrome (SSSS) etc., were treated with CZOP at dose levels of 16.0 to 50.0 mg/kg 3-4 times daily, via intravenous injection and intravenous drip infusion. CZOP gave "excellent" or "good" responses in all the 25 patients. In bacteriological examinations, 25 strains were identified and were eradicated except 1 strain of Staphylococcus aureus and 2 strains of Salmonella sp. As a side effect, diarrhea was observed in 1 patient among the 27 patients treated with the drug. As for abnormal laboratory findings, eosinophilia was observed in 1 patient, increases of thrombocytes in 3 and GPT in 2. Influences on blood coagulation parameters were studied. No changes in PIVKA II, HPT or APTT were observed during the treatment. Based on the above results, it has been concluded that CZOP is a safe and effective drug to use in the treatment of pediatric infections. The normal recommended dosage and administration should be 20 to 50 mg/kg of CZOP at a time, using intravenous injection or intravenous drip infusion 3 to 4 times a day.
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