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[Pharmacokinetic and clinical evaluation of cefozopran in the pediatric field]
1Department of Pediatrics, Meitetsu Hospital.
Insights
This study assessed cefozopran (CZOP), a new antibiotic, in pediatric patients. Cefozopran demonstrated favorable pharmacokinetics and significant clinical efficacy in treating various pediatric infections.
Area of Science:
- Pharmacology
- Infectious Diseases
- Pediatrics
Background:
- Cefozopran (CZOP) is a novel cephem antibiotic developed for intravenous administration.
- Understanding its pharmacokinetic profile and clinical effectiveness in pediatric populations is crucial.
Observation:
- Pharmacokinetic studies in pediatric patients (5-10 years) showed rapid absorption and elimination of CZOP, with serum half-lives averaging 1.85 hours.
- Significant urinary recovery rates (average 71.6%) were observed within 8 hours post-injection.
- Cerebrospinal fluid penetration was evaluated in meningitis and meningoencephalitis cases, indicating variable drug concentrations relative to serum levels.
Findings:
- CZOP exhibited favorable pharmacokinetic properties in pediatric patients, with predictable serum and urinary levels.
- The antibiotic demonstrated good penetration into the cerebrospinal fluid, particularly in purulent meningitis.
- Clinical evaluation in 29 pediatric patients (2 months to 15 years) with infectious diseases showed high efficacy, with 22 cases rated 'excellent' and 6 'good'.
Implications:
- Cefozopran shows promise as an effective treatment option for pediatric infectious diseases.
- Further research into optimal dosing and specific indications in pediatric patients is warranted.
- The pharmacokinetic and CSF penetration data support its potential use in central nervous system infections.
Abstract:
We conducted a pharmacokinetic and clinical studies on cefozopran (CZOP), a new cephem antibiotic for injection. 1. Changes in serum levels of the agent after intravenous bolus injection at a dose of 20 mg/kg to 4 pediatric patients (age: 5-10 years) were observed. The levels at 30 minutes after injection were 32.9-73.4 micrograms/ml average: 55.4 +/- 18.1 micrograms/ml), then the levels gradually decreased with half-lives of 1.67-2.24 hours (average: 1.85 +/- 0.27 hours) to 0.8-1.8 micrograms/ml (average: 1.2 +/- 0.4 micrograms/ml) at 8 hours after injections. Urinary levels reached at the maximum as, 1,773-3,450 micrograms/ml (average: 2,693 +/- 698 micrograms/ml) within 0-2 hours or 2-4 hours after injection, and recovery rates from urine in the first 8 hours after injection were 55.4-91.1% (average: 71.6 +/- 16.8%). 2. Transition to cerebrospinal fluid was examined in cases with purulent meningitis and aseptic meningoencephalitis. In the meningitis case, the level in cerebrospinal fluid 1 hour after administration was 8.8 micrograms/ml in the second day after the start of 4 times a day intravenous bolus injections with 42.5 mg/kg at each dose; The ratio of the drug level in cerebrospinal fluid to that in serum was 24.0%. In the meningoencephalitis, the levels in cerebrospinal fluid 1 hour after administrations were 1.1 micrograms/ml and 1.5 micrograms/ml in the second and the sixth days respectively, after the start of 4 times a day intravenous bolus injections with 50 mg/kg at each dose; the ratio of the levels in cerebrospinal fluid to those in sera were 0.93% and 2.41% respectively, at the second and the sixth day. 3. CZOP was clinically evaluated in 29 cases (ages: 2 months to 15 years) of pediatric infectious diseases. The agent was administered 3-4 times daily with 17-50 mg/kg at each dose, continued for 5-13 days. Total doses were 1.95-24.05 g. Clinical efficacy was evaluated in a total of 28 cases (1 case of purulent meningitis, 2 cases of acute purulent tonsillitis, 20 cases of acute pneumonia, 3 cases of urinary tract infections, 1 case of purulent lymphadenitis in cervical part and 1 case of cellulitis in face); The efficacies were "excellent" in 22 cases and "good" in 6 cases.(ABSTRACT TRUNCATED AT 400 WORDS)