Mullins Michael, Froelke Brian R, Rivera Maria Regina-Paz
Washington University, St. Louis, MO, USA.
Clin Toxicol (Phila). 2009 Feb;47(2):112-5. doi: 10.1080/15563650802093681.
To determine the effect of activated charcoal (AC) on acetaminophen (APAP) absorption kinetics when administered at 1, 2, or 3 h after combined oral overdose with oxycodone.
IRB-approved, prospective cross-over study of nine healthy human volunteers ingesting 5 g of APAP + 0.5 mg/kg of oxycodone on each of four study days. On the control day, subjects received no AC. On the remaining study days, subjects ingested 50 g of AC at 1, 2, or 3 h after drug ingestion. We measured serum APAP concentration hourly from 0 through 8 h and compared basic non-compartmental pharmacokinetic parameters.
Compared to the control, AC reduced area under the curve by 43% when given at 1 h (p < 0.0001), 22% when given at 2 h (p = 0.02), and 15% when given at 3 h (p = 0.26). AC at 1 h resulted in a 25% reduction in peak APAP concentration from 48.6 to 36.3 mcg/mL (p = 0.012) with no significant difference when given at 2 or 3 h. There was no significant difference in elimination half-life among the four study days.
The effect of AC rapidly declines between 1 and 3 h after combined oral overdose of APAP and oxycodone. AC is unlikely to be beneficial at or beyond 2 h after an overdose of acetaminophen and oxycodone.
确定在与羟考酮联合口服过量用药后1、2或3小时给予活性炭(AC)对乙酰氨基酚(APAP)吸收动力学的影响。
经机构审查委员会批准的前瞻性交叉研究,9名健康人类志愿者在四个研究日中的每一天摄入5克APAP + 0.5毫克/千克羟考酮。在对照日,受试者未接受AC。在其余研究日,受试者在服药后1、2或3小时摄入50克AC。我们从0至8小时每小时测量血清APAP浓度,并比较基本的非房室药代动力学参数。
与对照相比,AC在1小时给予时使曲线下面积减少43%(p < 0.0001),在2小时给予时减少22%(p = 0.02),在3小时给予时减少15%(p = 0.26)。1小时给予AC使APAP峰值浓度从48.6微克/毫升降至36.3微克/毫升,降低了25%(p = 0.012),在2或3小时给予时无显著差异。四个研究日之间的消除半衰期无显著差异。
在APAP和羟考酮联合口服过量用药后1至3小时内,AC的作用迅速下降。在对乙酰氨基酚和羟考酮过量用药后2小时及以后,AC不太可能有益。