Abstract
BL-P1654 is a new ureido-penicillin which has significant activity against both pseudomonas and klebsiella. Its pharmacokinetics were evaluated in five studies in four healthy adult male volunteers after 1-g doses given as: 5- and 30-min intravenous infusions, a 30-min infusion 1 h after the oral administration of 1 g of probenecid, and an intramuscular injection. For comparison, volunteers also received a 30-min infusion of 1 g of ampicillin. Serum levels of the antibiotic were found to fit a two-compartment open model using a Burroughs-5500 computer. After a 30-min infusion, peak serum levels of BL-P1654 (72.8 μg/ml [standard deviation] ± 5.9) were 50% greater than those of ampicillin (53.6 ± 8.9). Six hours later, the relative difference was even greater (4.58 ± 0.25 versus 0.35 ± 0.09). At 75 min after the 1-g intramuscular injection of BL-P1654, peak serum levels averaged 28.4 ± 10.3 μg/ml. The half-life of BL-P1654 (2.04 h) was significantly longer than for ampicillin (1.15 h), and the renal clearances of BL-P1654 and ampicillin were 79 versus 244 ml/min per 1.73 m2, respectively. Probenecid produced no significant change in blood levels, volume of distribution, half-life, or renal clearance, indicating that there is no net tubular secretion of this antibiotic.
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Selected References
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- Bennett J. V., Brodie J. L., Benner E. J., Kirby W. M. Simplified, accurate method for antibiotic assay of clinical specimens. Appl Microbiol. 1966 Mar;14(2):170–177. doi: 10.1128/am.14.2.170-177.1966. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bodey G. P., Horikoshi N., Rodriguez V. Human pharmacology of 6-[D-alpha-(3-guanylureido)-phenylacetamido]-penicillanic acid (BL-P1654). Antimicrob Agents Chemother. 1974 Apr;5(4):366–370. doi: 10.1128/aac.5.4.366. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Riegelman S., Loo J. C., Rowland M. Shortcomings in pharmacokinetic analysis by conceiving the body to exhibit properties of a single compartment. J Pharm Sci. 1968 Jan;57(1):117–123. doi: 10.1002/jps.2600570123. [DOI] [PubMed] [Google Scholar]
- Wagner J. G., Novak E., Leslie L. G., Metzler C. M. Absorption, distribution, and elimination of spectinomycin dihydrochloride in man. Int Z Klin Pharmakol Ther Toxikol. 1968 Apr;1(4):261–285. [PubMed] [Google Scholar]