PHARMACOKINETICS OF CARUMONAM IN HEALTHY VOLUNTEERS AND PATIENTS WITH RENAL INSUFFICIENCY

• Published in: CHEMOTHERAPY Vol. 35; no. Supplement2; pp. 237 - 246
• Main Authors: NASU, YOSHITSUGU, MIZUNO, AKIHIRO, NANBA, KATSUICHI, KUMON, HIROMI, KISHI, MIKIO, OHMORI, HIROYUKI
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 25.06.1987
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.35.Supplement2_237

Pharmacokinetics of carumonam, a new injectable monobactam antibiotic, were studied. Serum concentration and urinary excretion were determined after a single i.v. administration of lg of carumonam to healthy volunteers and to patients with renal insufficiency of various kinds. The drug concentration was determined by agar-well method using Escherichia coli NIHJ as the test organism. Pharmacokinetic analysis was performed with a two-compartment model, and 24 h endogenous creatinine clearance (Ccr) was used as a renal function index. In all cases the peak serum levels were detected immediately after administration, and similar values were noted regardless of the subject's renal function. However, serum clearance during the β-phase tended to be prolonged parallel with the degree of renal insufficiency, so that t1/2β, which was 1.20h in healthy volunteers, was prolonged to 4.22 h in patients with Ccr less than 30ml/min. The mean cumulative urinary recovery rate of carumonam within 24 h in healthy volunteers was 98%. Excretion of carumonam into urine was prolonged and cumulative urinary recovery tended to decrease parallel to a decrease in Ccr. However, in patients with Ccr of less than 30ml/min the mean cumulative urinary recovery rate was relatively high (66%).