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首页> 外文期刊>International clinical psychopharmacology >Measuring citalopram in blood and central nervous system: revealing a distribution pattern that differs from other antidepressants
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Measuring citalopram in blood and central nervous system: revealing a distribution pattern that differs from other antidepressants

机译：测量血液和中枢神经系统中西酞普兰：揭示与其他抗抑郁药不同的分布模式

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The aim of this study was to measure blood and cerebrospinal fluid concentrations of citalopram and its weakly active N-demethylated metabolite desmethylcitalopram to account for the distribution between the two compartments. The findings are discussed in the context with own preceding studies on the distribution pattern of different antidepressants. Concentrations of citalopram were measured in blood serum and cerebrospinal fluid of 18 patients treated with daily doses of 10-40mg. Daily doses were correlated with serum and cerebrospinal fluid concentrations, and serum concentrations were correlated with concentrations in cerebrospinal fluid. Serum concentrations of citalopram and desmethylcitalopram showed no significant correlation to the daily dose, r=0.164, P=0.515, and r=0.174, P=0.505, respectively, whereas citalopram concentrations in serum and cerebrospinal fluid were highly correlated (r=0.763, P<0.001). The cerebrospinal fluid/serum ratio for citalopram (total=bound+unbound concentration) varied between 0.14 and 0.86 (mean 0.35, SD 0.16). By correcting the mean cerebrospinal fluid/serum ratio for 80% plasma protein binding, cerebrospinal fluid concentrations of citalopram were on average 77% higher than the calculated unbound serum concentration with a ratio of 1.77 (SD 0.81, range 0.68-4.29). Findings indicate a very good ability of citalopram to cross the blood-brain and cerebrospinal fluid barrier. High concentrations of citalopram in the cerebrospinal fluid are indicative of active transport of citalopram into or missing active transport out of the cerebrospinal fluid. The results suggest a high ability of citalopram to enter the brain with sufficiently high drug concentrations at the target sites within the brain, contributing toward clinical efficacy.
机译：这项研究的目的是测量西酞普兰及其弱活性的N-去甲基代谢产物desmethylcitalopram的血液和脑脊液浓度，以说明两个区室之间的分布。在与之前有关不同抗抑郁药分布模式的研究一起讨论了这些发现。在每日剂量为10-40mg的18例患者中，测定其血清和脑脊液中西酞普兰的浓度。每日剂量与血清和脑脊液浓度相关，血清浓度与脑脊液中浓度相关。西酞普兰和去甲基西酞普兰的血清浓度与日剂量无显着相关性，分别为r = 0.164，P = 0.515和r = 0.174，P = 0.505，而血清和脑脊液中西酞普兰的浓度高度相关（r = 0.763， P ＜0.001）。西酞普兰的脑脊液/血清比率（总量=结合+未结合浓度）在0.14和0.86之间变化（平均值0.35，SD 0.16）。通过校正80％血浆蛋白结合的平均脑脊液/血清比率，西酞普兰的脑脊液浓度平均比计算出的未结合血清浓度高77％，比率为1.77（SD 0.81，范围0.68-4.29）。研究结果表明西酞普兰具有很好的穿越血脑和脑脊液屏障的能力。脑脊液中高浓度西酞普兰指示西酞普兰主动转运到脑脊液中或缺少主动转运出脑脊液。结果表明，西酞普兰具有进入大脑的高能力，并且在大脑内的靶位具有足够高的药物浓度，有助于临床疗效。

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