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[Pharmacokinetic and clinical evaluation of cefpirome in the pediatric field]
Y Toyonaga1, K Yamori, N Sakaguchi
1Department of Pediatrics, Yamanashi Red Cross Hospital.
Insights
Cefpirome (CPR), an aminothiazolylmethoxyiminoacetamido cephalosporin, demonstrates favorable pharmacokinetics and high efficacy in pediatric patients. This antibiotic achieved a 96.4% efficacy rate in treating various bacterial infections, showing good penetration into cerebrospinal fluid.
Area of Science:
- Pharmacology and Infectious Diseases
- Clinical Microbiology
- Pediatric Pharmacology
Background:
- Cefpirome (CPR) is an aminothiazolylmethoxyiminoacetamido cephalosporin (ATOIC) antibiotic.
- Understanding the pharmacokinetic and clinical profile of CPR is crucial for its effective use in pediatric populations.
- Previous studies have established the general properties of cephalosporins, but specific data for CPR in children is needed.
Purpose of the Study:
- To evaluate the pharmacokinetic properties of cefpirome (CPR) in children.
- To assess the clinical efficacy of CPR in treating various bacterial infections in pediatric patients.
- To determine CPR's penetration into the cerebrospinal fluid (CSF).
Main Methods:
- Pharmacokinetic study involving intravenous bolus injections and drip infusions (30-min and 1-hr) of CPR at dosages of 10, 20, and 40 mg/kg in children.
- Measurement of blood concentrations, half-lives, and urinary excretion rates.
- Clinical evaluation of CPR in 56 pediatric subjects with diverse bacterial infections, including meningitis, pneumonia, and urinary tract infections.
Main Results:
- Pharmacokinetic parameters in children were comparable to those observed in adults, with dose-dependent blood concentrations and predictable half-lives (1.09-1.43 hours).
- Urinary excretion rates ranged from 60.6-71.1% after bolus injections and 50.2-83.8% after drip infusions.
- CPR demonstrated moderate penetration into the cerebrospinal fluid (0.28-5.19 µg/ml at 50 mg/kg) and achieved an overall clinical efficacy rate of 96.4% across treated infections.
Conclusions:
- Cefpirome exhibits favorable pharmacokinetic properties in children, similar to adults, supporting its use across different administration routes.
- The antibiotic shows significant efficacy in treating a broad spectrum of pediatric bacterial infections.
- CPR's moderate CSF penetration suggests potential utility in managing CNS infections, warranting further investigation.
Abstract:
We conducted a pharmacokinetic and clinical study on cefpirome (HR 810, CPR), an aminothiazolylmethoxyiminoacetamido cephalosporin (ATOIC), and obtained the following results. 1. Concentrations in blood/excretion in urine. We studied pharmacokinetic in children upon intravenous bolus injections and 30-minute and 1-hour intravenous drip infusions in single dosages of 10, 20, and 40 mg/kg, and obtained virtually the same results as those found in adult subjects. Upon intravenous bolus injections, mean blood concentrations 30 minutes after administration of 10, 20, and 40 mg/kg were 26.1, 47.8, and 82.8 micrograms/ml, respectively, and half-lives were 1.13, 1.43, and 1.26 hours, respectively. Upon 30-minute intravenous drip infusion, mean blood concentrations on completion of the drip infusions of 10, 20, and 40 mg/kg were 43.2, 106.9, and 163.0 micrograms/ml, respectively, and half-lives were 1.15, 1.09, and 1.15 hours, respectively. In addition, upon 1-hour intravenous drip infusion, mean blood concentrations on completion of infusion were 27.1 micrograms/ml for 10 mg/kg and 47.5 micrograms/ml for 20 mg/kg, and half-lives were 1.09 and 1.40 hours, respectively. A clear dose response was observed at all dosages for either administration method. Mean excretion rates in urine in the first 8 hours after administration were 60.6-71.1% upon intravenous bolus injections of 10-40 mg/kg, and upon intravenous drip infusion, the values were 50.2-83.8% for administration of 10-40 mg/kg 6 or 7 hours after completion of drip infusion. 2. Concentrations in the cerebrospinal fluid Penetration into the cerebrospinal fluid was studied in 2 subjects, and a concentration of 0.28-5.19 micrograms/ml was observed upon administration of 50 mg/kg, a moderate degree of penetration compared to the penetration of cephalosporins of group 5 studied up to now. 3. Clinical results Evaluation of clinical effects of CPR on various types of bacterial infections was conducted in 56 subjects, excluding 3 subjects who had diseases which were excluded from the study. The breakdown was as follows: 3 cases of meningitis, 1 case of septicemia, 25 cases of bronchial pneumonia, 1 case each of tonsillitis and infection of the external acoustic meatus, 2 cases each of scarlet fever and phlegmon, 8 cases each of lymphadenitis and urinary tract infections, and 5 cases of staphylococcal scalded skin syndrome. Results of excellent or good were obtained in 54 subjects for an efficacy rate of 96.4%.(ABSTRACT TRUNCATED AT 400 WORDS)