Nakra B R, Glass R C, Rees J A
J Int Med Res. 1977;5(6):391-7. doi: 10.1177/030006057300100202.
Five healthy volunteers took part in a crossover study which examined the serum concentrations of dothiepin and northiaden after a 25 mg three times a day and a 75 mg once a day dosage regimen of Prothiaden. The inter-individual variation of serum levels was large after either schedule which is to be expected with this group of drugs. The minimum steady-state level of dothiepin tended to be lower after the single daily dose, but the differences were small and not statistically significant. The approximate maximum steady-state levels of dothiepin showed large intra-and inter-subject variation and no obvious trend. The values of the desmethylated metabolite, norhiaden, tended to follow the dothiepin concentrations but were lower than the parent drug. Average steady-state levels tended, with one exception, to be very similar after both regimens with no evidence with no evidence fo any trend when comparing the two regiments. The study showed that the two regimens yielded similar steady-state serum concentrations both of drug and metabolite but inter-individual differences were large.
五名健康志愿者参与了一项交叉研究，该研究检测了在接受丙咪嗪每日三次25毫克和每日一次75毫克给药方案后多塞平及去甲替林的血清浓度。两种给药方案后血清水平的个体间差异都很大，这在这类药物中是可预期的。单剂量给药后，多塞平的最低稳态水平往往较低，但差异较小且无统计学意义。多塞平的近似最大稳态水平在个体内和个体间均表现出较大差异，且无明显趋势。去甲基化代谢产物去甲替林的值往往与多塞平浓度变化一致，但低于母体药物。除一个例外情况外，两种给药方案后的平均稳态水平往往非常相似，比较两种给药方案时没有任何趋势的证据。该研究表明，两种给药方案产生的药物和代谢产物的稳态血清浓度相似，但个体间差异很大。
