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[Laboratory and clinical studies on cefoperazone in pediatrics treatment (author's transl)]
Insights
Cefoperazone (CPZ) demonstrates effective blood and urine concentrations in pediatric patients, with significant antibacterial activity against Gram-negative bacteria. Clinical trials show an 80.4% efficacy rate in treating various infections with manageable side effects.
Area of Science:
- Pharmacology
- Microbiology
- Clinical Medicine
Context:
- New semisynthetic cephalosporin, cefoperazone (CPZ), evaluated for laboratory and clinical efficacy.
- Previous research on cephalosporins highlighted their broad-spectrum activity and pharmacokinetic profiles.
Purpose:
- To investigate the pharmacokinetic properties of cefoperazone (CPZ) in pediatric patients.
- To evaluate the in vitro antibacterial activity of CPZ against clinical isolates.
- To assess the clinical efficacy and safety of CPZ in treating various infections.
Summary:
- Pharmacokinetic studies revealed dose-dependent blood levels and half-life of CPZ, with significant urinary excretion.
- Cerebrospinal fluid penetration was observed in a bacterial meningitis case.
- In vitro tests showed CPZ possessed antibacterial activity against Gram-negative bacteria comparable to cefotaxime and piperacillin.
- Clinical application in 46 patients resulted in an 80.4% overall efficacy rate and 78.9% bacteriological effectiveness.
- Observed side effects included gastrointestinal, dermatological, and hematological changes, generally not severe.
Impact:
- Cefoperazone (CPZ) shows promising therapeutic potential for bacterial infections, particularly those caused by Gram-negative pathogens.
- The pharmacokinetic and efficacy data support CPZ's use in clinical settings.
- Further research may explore optimal dosing regimens and comparative effectiveness against emerging resistant strains.
Abstract:
Laboratory and clinical studies of cefoperazone (CPZ), a new semisynthetic cephalosporin, were investigated and following results were obtained. (1) Blood level: CPZ was given intravenous dose of 25 mg/kg and 50 mg/kg to each 3 children. In the former, the blood level of 15 minutes after injection was 194.2 mcg/ml on average and the half life was 106.2 minutes. In the latter, the blood level was 320.0 mcg/ml on average and half life was 102.2 minutes. (2) Urinary concentration: In the cases of the dose of 25 mg/kg, 35.9% of CPZ was recovered on average from the urine within 6 hours after injection, and the urinary concentration reached to 2,148.6 mcg/ml (0 approximately 2 hours). And in the cases of the dose of 50 mcg/kg, the recovery rate in urine was 43.6%, and the urinary concentration was 3,008.3 mcg/ml. (3) Cerebrospinal fluid level: CSF level was determined in a patient with bacterial meningitis by S. pneumoniae. Ninety mg/kg of CPZ were given intravenous injection. After 60 minutes CSF level was 3.35 mcg/ml, and after 80 minutes the blood level was 192.0 mcg/ml. (4) Bacteriological evaluation: Against 164 strains isolated clinical specimens, the bacteriological evaluation on CPZ was performed in comparison with cefotaxime (CTX), cefazolin (CEZ) and piperacillin (PIPC) by inoculum size of 10(8) cells/ml. CPZ showed antibacterial activity against Gram-negative bacteria almost similar to CTX and PIPC. (5) CLINICAL RESULTS: CPZ was given 48.3 approximately 360 mg/kg/day (average 146.1 mg/kg/day) by intravenous route to 46 patients with various infection. The overall efficacy rate was 80.4%. The rate of bacteriological effectiveness was 78.9% in 19 cases. (6) Side effects: As side effects, diarrhea, fever, rash, urticaria, leukopenia, eosinophilia, elevation of GOT, GPT, and LDH were observed, but not seriously.