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[Experiences using acylureido-penicillins (azlocillin, mezlocillin) in pediatrics]
Abstract:
The acylureidopenicillins azlocillin and mezlocillin cover a broad spectrum of bacteria, including gramnegative and grampositive species as well as anaerobes. Azlocillin is especially active against P. aeruginosa. Mezlocillin has a good activity against Klebsiella. Both antibiotics inhibit Hemophilus, N. meningitidis and D. pneumoniae in low concentrations. Clinical and kinetic studies were made in more than 300 pediatric patients. Elimination-constant halflife, distribution volume and area under the curve were determined to propose dosage recommendations. Concentrations of azlocillin (44) and mezlocillin (77) were measured in the bronchial secretions. Up to hour 5 after i.v. injection a wide range of concentration values were observed. Azlocillin was found in the meconium in different concentrations after a single injection into the newborn. Mezlocillin diffused into the CSF even in uninflamed meninges, 3 h after injection the mean concentrations were 5.5 mg/l. 39 patients, 35 of them infected by P. aeruginosa, were treated by azlocillin. Urinary tract infections, wound infections and dacryocystitis were cured with one exception. Less convincing were the results in complicated bronchopulmonary diseases. The clinical efficacy of mezlocillin was similar. In a group of 59 patients there were only 3 without effect and some with improvement again in complicated pulmonary diseases. Side effects worth to be mentioned were not seen. In 2 patients the azlocillin injection caused nausea. Mezlocillin led to some minor transitory elevations of the transaminases and dyspepsia in some patients.
Insights
Azlocillin and mezlocillin are effective acylureidopenicillins against various bacteria, including Pseudomonas aeruginosa and Klebsiella. Clinical studies in pediatric patients show good efficacy and safety profiles for these broad-spectrum antibiotics.
Area of Science:
- Pharmacology
- Microbiology
- Pediatric Infectious Diseases
Background:
- Acylureidopenicillins azlocillin and mezlocillin exhibit broad-spectrum antibacterial activity.
- These antibiotics are effective against Gram-negative, Gram-positive bacteria, and anaerobes.
- Specific activities include azlocillin against P. aeruginosa and mezlocillin against Klebsiella.
Purpose of the Study:
- To evaluate the clinical efficacy and pharmacokinetics of azlocillin and mezlocillin in pediatric patients.
- To determine dosage recommendations based on kinetic studies.
- To assess the penetration of these antibiotics into various body fluids and tissues.
Main Methods:
- Clinical and kinetic studies conducted in over 300 pediatric patients.
- Measurement of azlocillin and mezlocillin concentrations in bronchial secretions, meconium, and cerebrospinal fluid (CSF).
- Treatment of infections, including urinary tract, wound, and bronchopulmonary diseases, with azlocillin and mezlocillin.
Main Results:
- Azlocillin and mezlocillin demonstrated broad-spectrum activity, inhibiting common pathogens like H. influenzae, N. meningitidis, and D. pneumoniae.
- Pharmacokinetic parameters (half-life, distribution volume, AUC) were determined for dosage recommendations.
- Good concentrations were observed in bronchial secretions, meconium, and CSF (5.5 mg/l mean in uninflamed meninges).
- High cure rates were achieved for urinary tract and wound infections with azlocillin (35/39 P. aeruginosa infections).
- Clinical efficacy for mezlocillin was similar, with positive outcomes in most patients.
- Adverse effects were minimal, including nausea with azlocillin and transient transaminase elevations/dyspepsia with mezlocillin.
Conclusions:
- Azlocillin and mezlocillin are effective and well-tolerated broad-spectrum antibiotics for pediatric infections.
- Their pharmacokinetic profiles support established dosing regimens.
- Penetration into relevant sites like bronchial secretions and CSF is adequate for therapeutic effect.