Hansen L B, Thomsen I S, Vestergård P, Larsen N E, Hvidberg E F
Psychopharmacology (Berl). 1980;69(2):157-60. doi: 10.1007/BF00427642.
A new serotonin uptake inhibitor zimelidine was studied in 16 endogenously depressed inpatients, who received 150 mg/kg orally during 3--6 weeks in a phase II-type study. Plasma concentrations of zimelidine and its main metabolite norzimelidine were determined twice a week. Ten patients obtained a well-defined steady-state plasma level within 1--2 weeks, while three patients still had increasing concentrations of both substances or only norzimelidine within the investigation period. In two patients, biochemical affection of the liver could be demonstrated during the treatment; one associated with moderate clinical symptoms (dizziness and fever), the other without clinical symptoms. Both patients recovered upon cessation of the zimelidine treatment. In the former patient, very high concentrations of zimelidine at the time of hepatic symptoms were demonstrated, while the latter patient was within the average concentration range. Other adverse reactions were mild and few, particularly with respect to anticholinergic effects. With the applied, probably suboptimal, dosage the therapeutic response was only satisfactory in five cases.
在一项II期研究中，对16名内源性抑郁症住院患者使用了一种新型血清素摄取抑制剂齐美利定，患者在3至6周内口服剂量为150毫克/千克。每周两次测定齐美利定及其主要代谢产物去甲齐美利定的血浆浓度。10名患者在1至2周内达到明确的稳态血浆水平，而3名患者在研究期间两种物质或仅去甲齐美利定的浓度仍在升高。两名患者在治疗期间出现肝脏生化影响；一名伴有中度临床症状（头晕和发热），另一名无临床症状。两名患者在停用齐美利定治疗后均康复。前一名患者在出现肝脏症状时齐美利定浓度极高，而后一名患者处于平均浓度范围内。其他不良反应轻微且较少，尤其是抗胆碱能作用方面。使用的剂量可能未达最佳，仅5例患者的治疗反应令人满意。
