Rigal J, Albin H, Fança X, Demotes-Mainard F, Vinçon G
Clinique Psychiatrique Les Pins, Bordeaux-Pessac, France.
J Clin Psychopharmacol. 1989 Oct;9(5):364-7.
Imipramine was used to treat 18 depressed inpatients for 22 days. Imipramine 2 mg/kg/day was administered from day 0 to day 14 intramuscularly, and 4 mg/kg/day was administered orally from days 15-21. Two pharmacokinetic studies were performed, the first at the end of the intramuscular phase (day 14) and the second at the end of the oral phase (day 21). Imipramine and desipramine blood levels were measured every hour from 8 a.m. to 4 p.m. Between these two pharmacokinetic evaluations, blood levels of imipramine and desipramine were measured every morning at 8 a.m. During intramuscular administration, the parent drug imipramine predominated in the plasma and, conversely, the desmethylated metabolite predominated during oral administration. With the changeover in route of administration, the doubling of the dose kept the blood levels of imipramine equal, while desipramine increased; the sum of imipramine and desipramine also increased, and the ratio of imipramine and desipramine decreased sharply, the median ratio changing over 3 days from 1.50 (day 15) to 0.62 (day 18).
丙咪嗪用于治疗18名住院抑郁症患者，为期22天。从第0天至第14天，丙咪嗪按2毫克/千克/天的剂量进行肌肉注射，从第15天至第21天，按4毫克/千克/天的剂量口服。进行了两项药代动力学研究，第一项在肌肉注射阶段结束时（第14天）进行，第二项在口服阶段结束时（第21天）进行。从上午8点到下午4点，每小时测量一次丙咪嗪和地昔帕明的血药浓度。在这两项药代动力学评估之间，每天上午8点测量丙咪嗪和地昔帕明的血药浓度。在肌肉注射期间，血浆中主要是母体药物丙咪嗪，相反，在口服给药期间，去甲基代谢产物占主导地位。随着给药途径的改变，剂量加倍使丙咪嗪的血药浓度保持相等，而地昔帕明的血药浓度增加；丙咪嗪和地昔帕明的总和也增加，丙咪嗪与地昔帕明的比值急剧下降，中位数比值在3天内从1.50（第15天）降至0.62（第18天）。
