A pharmacokinetic and tolerance study of Ro13-9904, a new cephalosporin antibiotic.
1 Six healthy male volunteers received a total of 2500 mg of a new cephalosporin antibiotic Ro13-9904 by intramuscular injection in five divided doses at intervals of 12 h. 2 No significant systemic side-effects were observed and this was confirmed haematologically and biochemically. 3 The drug was distributed following intramuscular injection reaching a mean peak plasma concentration of 55 micrograms ml-1 (range 46-66) 1 to 2 h after the first injection. 4 Monoexponential elimination of drug was demonstrated. No significant difference was recorded in the plasma half-life after the initial dose (mean 6.7 h) and at steady state (mean 6.7 h). The half-life is long compared with other cephalosporin antibiotics. 5 On the basis of the observed half-life, steady state should be reached within 48 h. A mean peak plasma concentration of 74 micrograms ml-1 (range 65-87) was recorded at steady state. Steady state plasma concentrations of Ro13-9904 with a dose of 500 mg every 13 h may be predicted from the pharmacokinetics of a single dose.
D000328:Adult; D002439:Cefotaxime / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism; D002443:Ceftriaxone; D004361:Drug Tolerance; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D008297:Male
D002443:Ceftriaxone; D002439:Cefotaxime