Ticarcillin vs carbenicillin: Clinical pharmacokinetics

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Abstract
The pharmacokinetic characteristics of ticarcillin, a semisynthetic penicillin more active than carbenicillin against Pseudomonas, were compared to those of carbenicillin in 12 healthy volunteers. Following an intravenous infusion of 2 gm in 5 min, there was a lower average serum levelfor ticarcillin (218 µg/ml) thanfor carbenicillin (301 µg/ml), but after 2 hr the differences were not significant. The biologic half-life of ticarcillin was slightly longer than that of carbenicillin (72 and 65 min, P < 0.01 )and its volume of distribution was larger (15.7 and 12.31, P < 0.01). Eighty-six per cent of the dose of ticarcillin and 99% of the dose of carbenicillin was recovered in the urine in 24 hr. Similar but much less marked blood level differences were noted with 2 gm, 30-min infusions. An intravenous infusion of 1 gm Ihr gave average steady-state blood levels of about 124 µg/ml for both antibiotics. Probenecid, administered 1 hr before the infusion, caused significant and similar increases in blood levels, half-lives, and volumes of distribution of the 2 antibiotics. Protein binding in 100% human serum was 50% and 65% for carbenicillin and ticarcillin, respectively. These relatively small but definite differences in the pharmacokinetics of ticarcillin and carbenicillin are not likely to be of clinical signijicance.

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