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[Pharmacokinetic and clinical studies on cefozopran in the field of pediatrics]
Insights
Cefozopran (CZOP) demonstrated a 100% efficacy rate in pediatric patients with various infections, showing favorable pharmacokinetic profiles and good tolerability. Bacterial eradication was achieved in all cases, highlighting CZOP
Area of Science:
- Pediatric Infectious Diseases
- Pharmacokinetics and Pharmacodynamics
- Antimicrobial Susceptibility Testing
Background:
- Cefozopran (CZOP) is an injectable cephem antibiotic.
- Pediatric infections require effective and safe treatment options.
- Evaluating the clinical utility of novel antibiotics in pediatric populations is crucial.
Purpose of the Study:
- To determine the pharmacokinetic profile of cefozopran (CZOP) in pediatric patients.
- To evaluate the clinical efficacy and safety of CZOP in treating various pediatric infections.
- To assess the in vitro antimicrobial activity of CZOP against common clinical isolates.
Main Methods:
- Blood and urine samples were collected to determine CZOP levels after intravenous administration.
- Clinical efficacy was assessed in pediatric patients with respiratory tract infections, urinary tract infections, enteritis, skin infections, and lymphadenitis.
- Minimum inhibitory concentrations (MICs) of CZOP were determined against Staphylococcus aureus, MRSA, Streptococcus pneumoniae, Escherichia coli, and Moraxella (Branhamella) catarrhalis and compared to other cephems.
Main Results:
- CZOP exhibited peak blood levels within 0.5-1 hour post-administration, with half-lives of 1.5-2.3 hours.
- An overall clinical efficacy rate of 100% was observed across all treated pediatric patients.
- Bacteriological studies showed a 100% bacterial eradication rate; CZOP demonstrated potent activity against Gram-positive bacteria and E. coli, with higher MICs for M. (B.) catarrhalis.
- The most common side effect was diarrhea (1/22), with transient laboratory abnormalities noted in a small percentage of patients.
Conclusions:
- Cefozopran (CZOP) shows favorable pharmacokinetic properties and high clinical efficacy in pediatric patients.
- CZOP is effective in eradicating bacterial infections and possesses a generally good safety profile in the pediatric population.
- Further research may explore CZOP's utility against specific resistant pathogens, particularly M. (B.) catarrhalis.
Abstract:
Blood and urine levels of cefozopran (CZOP) were determined, and its efficacy and safety profile was evaluated in the field of pediatrics. The results of this study are summarized as follows. 1. Blood levels of CZOP peaked in 30 minutes to 1 hour (initial blood collection) after intravenous administration at a dose of 20 or 40 mg/kg. Its blood levels at 6 hours after intravenous administration were 1.6 micrograms/ml (HPLC) or 1.9 micrograms/ml (bioassay) at a dose of 20 mg/kg and 2.9 to 9.1 micrograms/ml (HPLC) or 2.9 to 8.4 micrograms/ml (bioassay) at a dose of 40 mg/kg. The half-lives were 1.58 to 2.27 hours (HPLC) and 1.53 to 1.85 hours (bioassay), respectively. The rate of recovery of CZOP in the urine in the first 8 hours after intravenous administration at a dose of 20 mg/kg was 61.5% (HPLC) or 54.6% (bioassay), and urine levels of CZOP at 6 to 8 hours after administration were 157.3 micrograms/ml (HPLC) and 129.7 micrograms/ml (bioassay). 2. When CZOP was administered to 16 patients with respiratory tract infections, 2 patients with urinary tract infections, 2 patients with acute enteritis, 1 patient with skin soft tissue infection, and 1 patient with purulent lymphadenitis, the responses were excellent in 68% of patients and good in 32% with an overall efficacy rate of 100%. 3. Bacteriological effect of CZOP was excellent and the rate of bacterial eradication was 100% (9/9). 4. MICs of CZOP against clinical isolates (Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Streptococcus pneumoniae, Escherichia coli, Moraxella (Branhamella) catarrhalis) were compared to those of other injectable cephems ceftazidime (CAZ), cefuzonam (CZON), flomoxef (FMOX), cefmetazole (CMZ). The MICs of cefozopran (CZOP) against Gram-positive organisms, S. aureus, MRSA, and S. pneumoniae, were nearly as low as those of CZON and were clearly lower than those of CAZ. MICs of CZOP against Gram-negative organisms were examined and the MIC against E. coli was as low as those of other antibiotics but the MIC of CZOP against M. (B.) catarrhalis was higher, at 1.56 micrograms/ml, than those of CAZ, FMOX, and CMZ. 5. Diarrhea was experienced by 1 of 22 patients as a side effect from CZOP, and abnormal laboratory tests including increases of eosinophil counts in 2 patients (9.1%), a decrease of neutrophil counts in 1 patient (4.5%), thrombocytosis in 1 patient (4.5%), and an elevation of GPT in 3 patients (13.6%).(ABSTRACT TRUNCATED AT 400 WORDS)