Pharmacokinetics of total and unbound ertapenem in healthy elderly subjects

被引:39
作者
Musson, DG [1 ]
Majumdar, A [1 ]
Holland, S [1 ]
Birk, K [1 ]
Xi, L [1 ]
Mistry, G [1 ]
Sciberras, D [1 ]
Muckow, J [1 ]
Deutsch, P [1 ]
Rogers, JD [1 ]
机构
[1] Merck Res Labs, W Point, PA 19486 USA
关键词
D O I
10.1128/AAC.48.2.521-524.2004
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
Ertapenem is a new once-a-day parenteral carbapenem antimicrobial agent. The pharmacokinetics of unbound and total concentrations of ertapenem in plasma were investigated in elderly subjects and compared with historical data from young adults. In a single- and multiple-dose study, healthy elderly males and females (n = 14) 65 years old or older were given a 1-g intravenous (i.v.) dose once daily for 7 days. Plasma and urine samples collected for 24 h on days 1 and 7 following administration of the I-g doses were analyzed by reversed-phase high-performance liquid chromatography. Areas under the concentration-time curve from 0 h to infinity (AUC(0-infinity)) for elderly females and males were similar following administration of I-g single i.v. doses, and thus, the genders were pooled in subsequent analyses. Concentrations in plasma and the half-life of ertapenem were generally higher and longer, respectively, in elderly subjects than in young adults. The mean AUC(0-infinity) of total ertapenem in the elderly was 39% higher than that in young subjects following administration of a 1-g dose. The differences were slightly greater for the mean AUC(0-infinity) of unbound ertapenem (71%). The unbound fraction of ertapenem in elderly subjects (similar to5 to 11%) was generally greater than that in young adults (similar to5 to 8%). As in young adults, ertapenem did not accumulate upon multiple dosing in the elderly. The pharmacokinetics of ertapenem in elderly subjects, while slightly different from those in young adults, do not require a dosage adjustment for elderly patients.
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页码:521 / 524
页数:4
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