OraSure Technologies, Research and Development, Bethlehem, PA, USA.
Ther Drug Monit. 2011 Feb;33(1):72-9. doi: 10.1097/FTD.0b013e3182018151.
Although current abuse of barbiturates is low compared with other classes of abused drugs, their narrow margin of safety, risk of dependence, and abuse liability remain a health concern. Limited information is available on the disposition of barbiturates in different biologic matrices.
The authors conducted a clinical study of the disposition of barbiturates in oral fluid, plasma, and urine after single-dose administration to healthy subjects.
Three parallel groups of 15 subjects were administered a single oral dose of one barbiturate: butalbital (50 mg), Phenobarbital (30 mg), or sodium secobarbital (100 mg). Subjects remained at the clinic for two confinement periods; the first was -1 to 36 hours postdose and again at 48 to 52 hours. Oral fluid specimens were collected by bilateral collection (Intercept; one on each side of the mouth simultaneously). Blood specimens were obtained by venipuncture and urine specimens were collected through separate collection pools of varying periods. Oral fluid specimens were analyzed for barbiturates by liquid chromatography-tandem mass spectroscopy with a limit of quantitation of 8 ng/mL. Plasma and urine specimens were analyzed by gas chromatography-mass spectroscopy with a limit of quantitation of 100 ng/mL.
Barbiturate side effects included dizziness, drowsiness, and somnolence. All effects resolved spontaneously without medical intervention. The three barbiturates were detectable in oral fluid and plasma within 15 to 60 minutes of administration and in the first urine pooled collection at 2 hours. Butalbital and Phenobarbital remained detectable in all specimens through 48 to 52 hours, whereas secobarbital was frequently negative in the last collection. Oral fluid to plasma ratios appeared stable over the 1- to 48-hour collection period.
This study demonstrated that single, oral therapeutic doses of butalbital, Phenobarbital, and secobarbital were excreted in readily detectable concentrations in oral fluid over a period of approximately 2 days. Oral fluid patterns of appearance and elimination were similar to that observed for plasma and urine.
尽管与其他滥用药物相比，目前巴比妥类药物的滥用情况较低，但它们的安全范围较窄、存在依赖风险和滥用倾向仍然是一个健康问题。关于不同生物基质中巴比妥类药物的处置情况，信息有限。
作者对健康受试者单次给药后口腔液、血浆和尿液中巴比妥类药物的处置情况进行了临床研究。
三组各 15 名受试者分别单次口服给予一种巴比妥类药物：戊巴比妥（50 mg）、苯巴比妥（30 mg）或司可巴比妥钠（100 mg）。受试者在诊所停留两个禁闭期；第一次是给药后-1 至 36 小时，再次是 48 至 52 小时。口腔液标本通过双侧采集（Intercept；每侧口腔同时采集一个）收集。通过静脉穿刺采集血样，通过不同时间段的单独采集池收集尿样。通过液相色谱-串联质谱法以 8 ng/mL 的定量下限分析口腔液标本中的巴比妥类药物。通过气相色谱-质谱法以 100 ng/mL 的定量下限分析血浆和尿液标本。
巴比妥类药物的副作用包括头晕、嗜睡和昏睡。所有的影响都没有医疗干预而自行缓解。所有三种巴比妥类药物在给药后 15 至 60 分钟内可在口腔液和血浆中检测到，并且在 2 小时的第一个尿液混合采集池中检测到。戊巴比妥和苯巴比妥在所有标本中直至 48 至 52 小时仍可检测到，而司可巴比妥则经常在最后一次采集时呈阴性。口腔液与血浆比值在 1 至 48 小时的采集期间似乎稳定。
本研究表明，单次口服治疗剂量的戊巴比妥、苯巴比妥和司可巴比妥在大约 2 天的时间内以可检测浓度排泄到口腔液中。口腔液中出现和消除的模式与血浆和尿液相似。
