Daniel W, Melzacka M
Institute of Pharmacology, Polish Academy of Sciences, Krakow.
J Pharm Pharmacol. 1992 May;44(5):429-32. doi: 10.1111/j.2042-7158.1992.tb03638.x.
Chronic intraperitoneal administration of desipramine led to an extensive cumulation of the drug in brain and blood compared with that after a single dose treatment, while chronic treatment with desipramine by the oral route produced a brain concentration comparable with its level after a single oral dose. Comparison of the present results with the corresponding data of published imipramine pharmacokinetics indicated that the cumulation of desipramine in the rat brain was nearly the same when rats received desipramine or imipramine twice a day for two weeks at a dose of 10 mg kg-1 orally, or imipramine, twice a day for two weeks at a dose of 10 mg kg-1 intraperitoneally. It is suggested that these three experimental paradigms may be used as models for differentiation of the pharmacological effects of imipramine and desipramine in-vivo.
与单次给药治疗相比，慢性腹腔注射地昔帕明导致药物在脑和血液中大量蓄积，而口服地昔帕明进行慢性治疗所产生的脑内浓度与其单次口服给药后的水平相当。将本研究结果与已发表的丙咪嗪药代动力学的相应数据进行比较表明，当大鼠以10mg/kg的剂量口服地昔帕明或丙咪嗪，每日两次，持续两周，或以10mg/kg的剂量腹腔注射丙咪嗪，每日两次，持续两周时，地昔帕明在大鼠脑内的蓄积情况几乎相同。提示这三种实验范式可作为体内区分丙咪嗪和地昔帕明药理作用的模型。
