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[Pharmakokinetic and clinical studies with azlocillin in paediatrics (author's transl)]
Insights
Azlocillin, a potent penicillin antibiotic, demonstrates significant bactericidal activity against key pathogens like Pseudomonas and E. coli. Pharmacokinetic studies in children confirm effective dosing strategies for various age groups, ensuring therapeutic azlocillin serum levels.
Area of Science:
- Pharmacology
- Microbiology
- Pediatrics
Context:
- Azlocillin is an acylureido penicillin antibiotic.
- It exhibits bactericidal activity against Gram-negative bacteria, including Pseudomonas, E. coli, and Proteus species.
- It is also effective against enterococci, Haemophilus influenzae, and Bacteroides.
Purpose:
- To conduct pharmacokinetic studies of azlocillin in children of various ages.
- To determine optimal intravenous (i.v.) and intramuscular (i.m.) dosing regimens.
- To evaluate azlocillin's efficacy and safety in pediatric patients.
Summary:
- Pharmacokinetic studies involved 138 children (prematures to schoolchildren) receiving 50-100 mg/kg azlocillin.
- Therapeutic serum levels were achieved with specific dosing frequencies based on age.
- Azlocillin was detected in bronchial secretions and meconium, indicating good distribution.
- Clinical treatment of 39 children, primarily with Pseudomonas infections, showed very good results in urinary tract, wound infections, and meningitis.
- Bronchopulmonary infections showed less favorable outcomes, potentially due to underlying conditions.
Impact:
- Establishes effective azlocillin dosing for pediatric populations.
- Demonstrates good pharmacokinetic profile and tissue penetration.
- Highlights clinical efficacy against specific bacterial infections in children.
- Suggests a favorable safety profile with no serious side effects observed.
Abstract:
Azlocillin, an acylureido penicillin with bactericidal activity, is particularly effective against Pseudomonas, enterococci and Haemophilus influenzae. It is also very active against E. coli, various Proteus species and Bacteroides. Pharmacokinetic studies were carried out in 138 children of various ages (prematures, newborns, infants, schoolchildren) after administering 50-75-100 mg/kg/ body weight azlocillin via the i.v. or i.m. routes; The constant of elimination and the distribution volumes were calculated besides the serum levels. In prematures and newborns, therapeutically effective serum levels were obtained on administering 50 or 100 mg/kg body weight twice daily. Infants and older children required 100 or 75 mg/kg body weight t.i.d. Determination of azlocillin in the bronchial secretion after i.v. doses of 75 mg/kg body weight showed good elimination. Azlocillin was always identified up to the 5th hour post injectionem. Inspite of parenteral administration, azlocillin was identified in different concentrations in the meconium as well. 39 children were treated with azlocillin, 35 of whom had Pseudomonas infection. Very good results were obtained in infections of the urinary tract, wound infections, conjunctivitis, dacryocystitis and in one case of meningitis. Bronchopulmonary diseases did not take an equally good course, but in these cases the conditions had not been favourable. No serious side effects were revealed by testing several laboratory parameters.