[The migration of cefotiam to cerebrospinal fluid]

The concentration of cefotiam (CTM), a newly synthesized cephem derivative antibiotic in serum and cerebrospinal fluid after single intravenous treatment was determined and its utility in the field of cerebral neurosurgery was studied. 1. One gram or 2 g of CTM was intravenously administered for 1 time to 10 patients admitted to our department. Dose dependency was observed in the progress of the mean serum concentration. There was no difference in the specific rate of constant, and the ratio of AUC between the group treated with 1 g and the one with 2 g was 1:1.9. The biological half-lives of the elimination phase for both dose levels were about 1.1 hours. 2. Disparity was recognized in the cerebrospinal fluid concentration in spite of the dose dependency. Although a case with comparatively high value of 1.37 micrograms/ml at 60 minutes after administration were seen in the 1 g treatment group, generally the migration concentration was low. Good cerebrospinal fluid concentration was attained in all of the cases in the 2 g treatment group, and the peak values ranged from 0.59 to 10.16 micrograms/ml. 3. The concentration ratio of cerebrospinal fluid to serum in the 2 g treatment group elevated till 360 minutes after administration, and the maximum values ranged from 15.8 to 89.8%. 4. The migration to the cerebrospinal fluid was faster in cases with slight inflammation than those without inflammation in the 2 g treatment group. 5. It was assumed that the prophylactic effect of CTM 2 g administration against staphylococci, streptococci and Klebsiella pneumoniae which are the major causative organisms can be expected in postoperative infection in the field of cerebral neurosurgery.