Laine K, Kivistö K T, Pelttari S, Neuvonen P J
Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland.
Pharmacol Toxicol. 1996 Nov;79(5):270-3. doi: 10.1111/j.1600-0773.1996.tb00272.x.
The effect of activated charcoal on fluoxetine (40 mg) absorption, with special reference to delayed charcoal administration, was investigated in a randomized study with four parallel groups of eight Healthy volunteers. The first group ingested fluoxetine on an empty stomach with water only (control). The second group received 25 g of activated charcoal as a suspension immediately after fluoxetine. The third and fourth groups took fluoxetine with water and received 25 g of charcoal 2 or 4 hr after fluoxetine. Timed blood samples were taken and plasma fluoxetine and norfluoxetine concentrations were measured by GC for 96 hr. When charcoal was administered immediately after fluoxetine, the AUC (0-96 hr) of fluoxetine was reduced by more than 96% (P < 0.0005) and the Cmax by more than 98% (P < 0.0005). The reduction in the AUC (0-96 hr) and Cmax of norfluoxetine was similar to that of fluoxetine. When the administration of charcoal was delayed 2 or 4 hr, there was a non-significant mean reduction of 16% and 23% in the AUC (0-96 hr) of fluoxetine. Similarly, the Cmax was not significantly reduced by charcoal given 2 or 4 hr later. Also, the half-life of fluoxetine was not significantly reduced (by 25%) by the late administration of charcoal. We conclude that activated charcoal, ingested immediately after fluoxetine, practically completely prevents the gastrointestinal absorption of fluoxetine. However, regardless of the relatively slow absorption of fluoxetine, delaying charcoal administration 2-4 hr greatly reduces its antidotal efficacy.
在一项有四组平行的八名健康志愿者参与的随机研究中,研究了活性炭对氟西汀(40毫克)吸收的影响,特别关注了活性炭给药延迟的情况。第一组仅在空腹时用水服用氟西汀(对照组)。第二组在服用氟西汀后立即接受25克活性炭悬浮液。第三组和第四组用水服用氟西汀,并在服用氟西汀后2或4小时接受25克活性炭。定时采集血样,并用气相色谱法测量血浆中氟西汀和去甲氟西汀的浓度,持续96小时。当在服用氟西汀后立即给予活性炭时,氟西汀的AUC(0 - 96小时)降低了96%以上(P < 0.0005),Cmax降低了98%以上(P < 0.0005)。去甲氟西汀的AUC(0 - 96小时)和Cmax的降低与氟西汀相似。当活性炭给药延迟2或4小时时,氟西汀的AUC(0 - 96小时)平均降低了16%和23%,差异无统计学意义。同样,在2或4小时后给予活性炭,Cmax没有显著降低。此外,延迟给予活性炭并没有显著降低氟西汀的半衰期(降低25%)。我们得出结论,在服用氟西汀后立即摄入活性炭,实际上能完全阻止氟西汀的胃肠道吸收。然而,尽管氟西汀吸收相对较慢,但将活性炭给药延迟2 - 4小时会大大降低其解毒效果。