PHARMACOKINETIC AND CLINICAL STUDIES OF CEFTIZOXIME IN NEWBORN INFANTS

• Published in: Japanese journal of antibiotics 1988/08/25, Vol.41(8), pp.1053-1064
• Main Authors: SATO, HAJIME, NAKAZAWA, SUSUMU, NARITA, AKIRA, NAKAZAWA, SHINICHI, MATSUMOTO, KIMIKO, SUZUKI, HIROYUKI, NAKANISHI, YOSHIKO, CHIKAOKA, HIDEJIRO, KAMIGAKI, MASATO, NIINO, KENJI
• Format: Article
• Language: Japanese
• Subjects: Acute Disease; Bacterial Infections - drug therapy; Bacterial Infections - metabolism; Ceftizoxime - administration & dosage; Ceftizoxime - pharmacokinetics; Ceftizoxime - therapeutic use; Drug Evaluation; Humans; Infant, Newborn - metabolism; Infant, Premature - metabolism; Infusions, Intravenous; Injections, Intravenous; Pneumonia - drug therapy
• ISSN: 0368-2781; 2186-5477
• DOI: 10.11553/antibiotics1968b.41.1053

Pharmacokinetic and clinical studies of ceftizoxime (CZX) were performed in infants given intravenously. The obtained results are summarized as follows. 1. Serum concentrations of CZX in 2 and 3 day-old mature infants given 20mg/kg by one shot intravenous injection peaked at 49.0 and 57.9μg/ml in 1 hour and decreased to 14.4 and 24.9μg/ml in 8 hours after dosing, respectively. Half-lives were 3.9 and 5.6 hours, respectively. In 5 day-old or older mature infants, peak serum levels ranged from 20.9 to 38.0μg/ml at 1 hour after the injection. Levels of CZX at 8 hours after injection were 1.31 to 7.32μg/ml. Half-lives were 1.6-3.0 hours in all the infants except one. 2. In a 3 day-old premature infant given the same dose by a bolus intravenous injection, the serum level peaked at 45.7μg/ml in 1 hour after the injection. The level at 8 hours after injection was 15.7μg/ml. The half-life was 4.2 hours. In 5-15 day-old premature infants, half-lives were 2.3-3.1 hours in all the infants except one. 3. Serum concentrations of CZX in 1 and 2 day-old infants given 20mg/kg by intravenous drip infusion peaked at 49.4 to 115.0μg/ml in 1 hour after dosing. Half-lives were rather long, 4.0 and 5.1 hours, in the 2 infants. 4. Peak serum levels and half-lives tended to be lower and shorter in 5 day-old or older ones than in the 3 day-old or younger infants. 5. No changes in the serum concentration were observed even after dosing with 20mg/kg of continuous one shot intravenous injection. 6. Urinary recovery rates during the first 8 hours (one is 6 hours, two is 9 hours) after 20mg/kg intravenous bolus injection of CZX tended to be lower in 3 day-old or younger infants than in 5 day-old or older infants. 7. Eleven infants with various bacterial infections were given CZX by intravenous bolus injection or drip infusion. Dosage of CZX used in the present study were 36-148mg/kg/day in 2-3 divided doses. Duration of treatment ranged from 3 to 12 days. Clinical efficacy of CZX was excellent or good in all the infants with acute bronchitis, acute pneumonia, suspected sepsis infected in uterine, acute otitis media, cellulitis, meningitis caused by Klebsiella pneumoniae and Escherichia coli, acute urinary tract infection and periproctic abscess except 1 case of acute bronchitis. 5 species of organisms identified from various cultures of 11 patients were all eradicated after treatment of CZX. 8. Neither systemic nor local adverse effect ascribed to CZX was encountered in any of the infa