1994 Volume 42 Issue Supplement4 Pages 350-364
We studied a newly developed carbapenem, biapenem (BIPM), and obtained the following results.
1) Clinical pharmacological studies of BIPM were conducted in 10 patients with renal dysfunction. The drug was injected intravenously at a dose of 0.3g by drip infusion for 30 minutes, and its concentrations in plasma and urine were determined by bioassay. The concentrations of its metabolite (LJC 10, 905, LJC 10, 906) were determined by high-performance liquid chromatography. The patients were classified according to creatinine clearance (Ccr) values into group I (n=4, Ccr≥50ml/min), group II (n=3, 20Cc<50ml/min), group III (n=1, Ccr<20ml/min), group IV (n=2, uremic patients). The peak plasma levels of BIPM did not differ greatly among the four groups. T1/2β of BIPM was 2.02 hour in group I, 2.16 hour in group II, 3.52 hour in group III, 5.59 hour in group IV Thus, in plasma concentration decreased more slowly in patients with severely impaired renal function, than in those with slight or moderate renal dysfunction. The urinary recovery rate was 42.2% in group I and 39.3% in group II, but in patients with severely impaired renal function (group III), it was 20.7%. No discernible acumulation of the drug in plasma was observed.
2) BIPM was used to treat 34 patients with respiratory tract infections and 2 with acute pyelitis. Clinical response was good in 31, poor in 4, undetermined in 1. As an adverse reaction, diarrhea was observed in 1 case. Laboratory tests revealed an elevation of GOT and GPT, an elevation of BUN, a decrease of WBC in 1 case, and a decline in prothrombin activity and eosinophilia in 2 cases. However, these findings were slight and no severe side effects caused by drug were observed.
