PHARMACOKINETIC, BACTERIOLOGICAL, AND CLINICAL STUDIES ON PANIPENEM/BETAMIPRON IN CHILDREN

• Published in: Japanese journal of antibiotics 1992/03/25, Vol.45(3), pp.293-300
• Main Authors: TAJIMA, TAKESHI, NISHIMURA, SHUICHI, HIGA, AKIKO, KONDO, YASUO, NEGISHI, SACHIKO, HATA, MAMORU, ABE, TOSHIAKI, FUJII, RYOCHI
• Format: Article
• Language: Japanese
• Subjects: Bacterial Infections - drug therapy; beta-Alanine - analogs & derivatives; beta-Alanine - blood; beta-Alanine - pharmacokinetics; beta-Alanine - therapeutic use; Child; Child, Preschool; Drug Therapy, Combination - blood; Drug Therapy, Combination - pharmacokinetics; Drug Therapy, Combination - therapeutic use; Female; Humans; Infant; Male; Microbial Sensitivity Tests; Thienamycins - blood; Thienamycins - pharmacokinetics; Thienamycins - therapeutic use
• ISSN: 0368-2781; 2186-5477
• DOI: 10.11553/antibiotics1968b.45.293

Pharmacokinetic, bacteriological and clinical studies were performed on panipenem/betamipron (PAPM/BP) in children. The results are summarized as follow: 1. Twelve patients with various bacterial infectious diseases were treated with PAPM/BP. Each dose was 20mg/20mg/kg, administered 3 times daily, in 30-minute intravenous drip infusion. Treatments were continued for 5-22 days. Clinical efficacies of PAPM/BP in 12 patients with bacterial infections (1 with suspected sepsis, 5 with pneumonia, 1 with acute maxillary sinusitis, 2 with acute otitis media, 1 with cervical abscess and 2 with urinary tract infection complexed type) were evaluated as excellent in 7, good in 4 and fair in 1, with an efficacy rate of 91.7%. Seventeen causative organisms found in 10 patients (Haemophilus influenzae in 4, Branhamella catarrhalis in 3, Streptococcus pneumoniaein 2, Pseudomonas aeruginosa in 2, Staphylococcus aureus in 1, α-Streptococcus in 1, Corynebacterium sp. in 1, Peptostreptococcus micros in 1 and Klebsiella pneumoniae in 2) were eradicated except 2 strains (S. aureus and P. aeruginosa) from 1 patient (patient No.2). No adverse reactions were observed in any of the 12 patients. 2. MICs of PAPM were examined against 22 clinical isolates (H. influenzae 5, B. catarrhalis 3, α-Streptococcus 3, S. pneumoniae 2, Corynebacterium sp. 2, S. aureus 1, P. aeruginosa 1, P. micros 1, Enterobacter cloacae 1, Escherichia coli 1, Group D Streptococcus 1 and Staphylococcus epidermidis 1) from children with bacterial infections. PAPM showed a good antibacterial activity comparable to the activity of cefoperazone (CPZ) against S. pneumoniae strains relatively tolerant to penicillins. However, the activity of PAPM against H. influenzae was somewhat weaker than that of CPZ. 3. Pharmacokinetic studies. The peak of plasma concentrations of PAPM and BP were 53.39μg/ml (29.04-86.90μg/ml) and 29.91μg/ml (14.28-57.44μg/ml), respectively, at dose of 20mg/20mg/kg administered using a 30-minute intravenous drip infusion. Over a period of 8 hours, the urinary excretions of PAPM and BP were 30.65% (13.3-49.8%) and 74.73% (67.4-78.9%) of the dose administered, respectively. Plasma half-lives of PAPM and BP in the β-phase were 0.97 hour (0.77-1.15 hours) and 0.61 hour (0.39-0.92 hour), respectively. Based on the above results and the extremely broad spectrum of antibacterial activities of PAPM/BP, PAPM/BP may be a promising antibiotic which is suitable as a single agent for the primary therapy of s