Lund J, Lomholt B, Fabricius J, Christensen J A, Bechgaard E
Acta Pharmacol Toxicol (Copenh). 1979 Apr;44(4):289-95. doi: 10.1111/j.1600-0773.1979.tb02332.x.
The tolerance of paroxetine (FG 7051), as well as its pharmacokinetics and reduction of 5-HT in blood, has been investigated in man. Three normal, healthy volunteers were administered the single doses 10, 25, 50, and 75 mg orally, and three volunteers received 10, 25, and 50 mg per day for seven or fourteen days. No toxic effect on blood, kidney, liver, heart or general condition was found by chemical and physical examinations. The pharmacokinetic studies revealed a dose dependent systemic availability, a rather slow elimination (t1-z2 = approximately 16 hrs), a good fit to one compartment open model, and an almost complete metabolism of the substance. 25 mg paroxetine per day gave a maximal reduction of 5-HT in the blood within 2--3 weeks (to approximately 0.03 microgram/ml). The 5-HT levels returned to the basic levels during a three to four weeks drug-free period.
已在人体中研究了帕罗西汀（FG 7051）的耐受性及其药代动力学以及血液中5-羟色胺（5-HT）的减少情况。三名正常、健康的志愿者口服了10、25、50和75毫克的单剂量药物，另外三名志愿者连续7天或14天每天服用10、25和50毫克。通过化学和体格检查未发现对血液、肾脏、肝脏、心脏或总体健康状况有任何毒性作用。药代动力学研究显示出剂量依赖性的全身利用率、相当缓慢的消除过程（t1/2约为16小时）、与单室开放模型的良好拟合以及该物质几乎完全的代谢。每天25毫克的帕罗西汀在2至3周内使血液中的5-HT最大程度降低（降至约0.03微克/毫升）。在停药3至4周期间，5-HT水平恢复到基础水平。
