Bareggi S R, Pirola R, Truci G, Leva S, Smirne S
Department of Pharmacology, School of Medicine, Università degli Studi, Milan, Italy.
J Clin Pharmacol. 1988 Apr;28(4):371-5. doi: 10.1002/j.1552-4604.1988.tb03161.x.
The pharmacokinetics of two benzodiazepine hypnotics, flunitrazepam and loprazolam, was determined on two occasions in two groups of eight healthy volunteers. Single 2-mg oral doses of either drug were given in the fasting state at morning on one occasion and after a standard dinner at night on another. Compared with administration of drugs in the fasting state, administration of the drugs after dinner decreased peak plasma concentrations, delayed the time to reach maximum concentration, and prolonged the absorption half-life. The extent of absorption was reduced for flunitrazepam but not for loprazolam. The elimination half-life of both flunitrazepam and loprazolam was not changed in the two conditions. These changes may be of clinical significance because they can delay and reduce the effects of the drugs.
在两组各八名健康志愿者中,分两次测定了两种苯二氮䓬类催眠药氟硝西泮和氯普唑仑的药代动力学。在一次实验中,于早晨空腹状态下给予单剂量2毫克的任一药物,在另一次实验中,于晚上进食标准餐后给予。与空腹状态下给药相比,餐后给药降低了血浆峰浓度,延迟了达到最大浓度的时间,并延长了吸收半衰期。氟硝西泮的吸收程度降低,但氯普唑仑未降低。在两种情况下,氟硝西泮和氯普唑仑的消除半衰期均未改变。这些变化可能具有临床意义,因为它们会延迟和降低药物的效果。