利福平引起的己巴比妥异构体口服清除率的年龄依赖性立体选择性增加。

Age-dependent stereoselective increase in the oral clearance of hexobarbitone isomers caused by rifampicin.

Smith D A, Chandler M H, Shedlofsky S I, Wedlund P J, Blouin R A

College of Pharmacy, University of Kentucky, Lexington 40536-0082.

Br J Clin Pharmacol. 1991 Dec;32(6):735-9.

The disposition of hexobarbitone enantiomers before and after rifampicin treatment (600 mg daily for 14 days) was investigated in six young (29 +/- 3 years old) and six elderly (71 +/- 4 years old) healthy male volunteers. Hexobarbitone was given as a single 500 mg oral dose of the racemate. 2. The mean (+/- s.d.) oral clearance of S-(+) hexobarbitone was 1.9 +/- 0.3 and 1.8 +/- 0.2 ml min-1 kg-1, respectively, in young and elderly subjects and increased approximately six fold following 14 days of rifampicin treatment in both young (to 11.9 +/- 2.2 ml min-1 kg-1) and elderly (to 10.7 +/- 2.8 ml min-1 kg-1) subjects. 3. In contrast, rifampicin treatment produced a larger and a differential increase in the oral clearance of R-(-) hexobarbitone in young and elderly subjects; an 89 fold change in the young (15.6 +/- 16.4 to 1146.7 +/- 1478.0 ml min-1 kg-1) and a 19 fold change (10.3 +/- 3.0 to 199.9 +/- 98.1 ml min-1 kg-1) in the elderly.

在6名年轻（29±3岁）和6名老年（71±4岁）健康男性志愿者中，研究了利福平治疗前后（每日600mg，共14天）异戊巴比妥对映体的处置情况。异戊巴比妥以500mg外消旋体单次口服给药。2. 在年轻和老年受试者中，S-(+)异戊巴比妥的平均（±标准差）口服清除率分别为1.9±0.3和1.8±0.2ml·min⁻¹·kg⁻¹，在年轻和老年受试者中，利福平治疗14天后均增加约6倍（年轻受试者增至11.9±2.2ml·min⁻¹·kg⁻¹，老年受试者增至10.7±2.8ml·min⁻¹·kg⁻¹）。3. 相比之下，利福平治疗使年轻和老年受试者中R-(-)异戊巴比妥的口服清除率有更大且不同的增加；年轻受试者增加了89倍（从15.6±16.4增至1146.7±1478.0ml·min⁻¹·kg⁻¹），老年受试者增加了19倍（从10.3±3.0增至199.9±98.1ml·min⁻¹·kg⁻¹）。

Age-dependent stereoselective increase in the oral clearance of hexobarbitone isomers caused by rifampicin.