Fundamental and clinical study of ceftizoxime suppository (CZX-S)

Abstract

Ceftizoxime suppository (CZX-S), a newly developed antibiotic preparation containing in each suppository 500 mg of CZX, was evaluated for pharmacokinetics and therapeutic effectiveness and safety in aged patients with urinary tract infection (UTI). The results are summarized as follows. 1. The average serum concentrations of CZX 30 minutes, 1 hour, and 6 hours after administration of one suppository (500 mg), were 0. 93 μg/ml, 1. 31 μg/ml, and 0. 40 μg/ml, respectively. The serum half-life was 3.02 hours. The average urinary concentrations of CZX in three successive collections of 0—2 hours, 2~4 hours, and 4—6 hours were 37. 9 μg/ml, 86.8 μg/ml, and 43. 0μg/ml. The average urinary recovery rate up to 6 hours was 2.15%. 2. Therapeutic effectiveness was “good” in 9 patients and “fair” in 2, with an effectiveness rate of 81. 8%. 3. Bacteriological effectiveness against the 13 causative strains was “eradicated” in 7 patients, reduced” in 1, and “replaced by other bacterial flora” in 5, with a bacterial elimination rate of 92.3%. 4. No side effects were observed in any patient. Abnormal laboratory findings were eosinophilia in 2 patients. © 1986, Japanese Society of Chemotherapy. All rights reserved.