The effect of cefotiam (CTM) on neonates and premature infants was examined in basic and clinical studies. Minimum inhibitory concentrations of CTM against 190 clinically isolated strains kept by this department were investigated. This drug was found to have a strong antibacterial effect against Escherichia coli, Klebsiella spp., Proteus mirabilis and Streptococcus agalactiae, Staphylococcus aureus and Staphylococcus epidermidis, although some strains were resistant. The CTM was given to 0-3, 4-7, and greater than or equal to 8 day-old premature infants and neonates by intravenous injection at the dose of 20 mg/kg, and we studied changes in serum CTM levels over time. Mean serum CTM levels were 62.3 micrograms/ml at 15 minutes and 16.4 micrograms/ml at 6 hours after the injection, with the half-life of 3.6 hours, for the 0-3 day-old premature infants. They were 38.5 micrograms/ml at 15 minutes and 10.1 micrograms/ml at 6 hours, with the half-life of 2.9 hours, for the 0-3 day-old neonates. Those levels were 22.5 micrograms/ml at 15 minutes and 2.9 micrograms/ml at 6 hours, with the half-life of 1.9 hours, for the 4-7 day-old neonates, and 51.8 micrograms/ml at 15 minutes and 1.0 micrograms/ml at 6 hours, with the half-life of 1.1 hours, for the greater than or equal to 8 day-old neonates. The CTM was given to 0-3 and greater than or equal to 8 day-old premature infants and neonates by 1-hour intravenous drip infusion at the dose of 20 mg/kg, and changes in serum CTM levels after the infusion were followed. The 0-3 day-old premature infant (there was only one subject) had a peak serum CTM level of 21.0 micrograms/ml 1 hour after the start of the infusion (that is, at the time of its completion), with the level decreased to 8.6 micrograms/ml at 7 hours and the half-life was 5.4 hours. The mean peak serum CTM level in 0-3 day-old neonates were 36.7 micrograms/ml at 1 hour, which decreased to a mean of 7.0 micrograms/ml at 7 hours; the half-life was 2.3 hours.(ABSTRACT TRUNCATED AT 400 WORDS)