Seifritz E, Baumann P, Müller M J, Annen O, Amey M, Hemmeter U, Hatzinger M, Chardon F, Holsboer-Trachsler E
Depression Research Unit, Psychiatric University Hospital, Basel, Switzerland.
Neuropsychopharmacology. 1996 Apr;14(4):253-63. doi: 10.1016/0893-133X(95)00117-V.
Pharmacokinetic measurements, neuroendocrine responses, and side effects profiles of intravenous infusions of 20 mg citalopram over 30 minutes during the early afternoon have been studied. Eight healthy male volunteers were enrolled in a placebo- (saline) controlled, single-blind, cross-over protocol. Plasma concentrations of the parent compound showed a double exponential decay. Demethyl and didemethyl metabolites were not detectable, but low concentrations of the propionic acid derivative of citalopram were found. Determination of the citalopram enantiomers yielded a balanced S(+)/R(-) ratio of 0.9 to 1.2. The endocrine response to the drug was characterized by significant increases in plasma prolactin and cortisol. Except for one subject, who developed pronounced side effects, human growth hormone showed a surge following saline that was inhibited following citalopram. Rectal temperature and heart rate were not affected and tolerability was favorable. Because of citalopram's extremely high selectivity for the presynaptic 5-hydroxytryptamine nerve terminals, the present data suggest that it might be a promising tool for the investigation of serotonergic function in the human brain in vivo.
已对20毫克西酞普兰在午后早期30分钟内静脉输注的药代动力学测量、神经内分泌反应和副作用情况进行了研究。八名健康男性志愿者参与了一项安慰剂（生理盐水）对照、单盲、交叉试验方案。母体化合物的血浆浓度呈双指数衰减。去甲基和双去甲基代谢物未被检测到，但发现了低浓度的西酞普兰丙酸衍生物。西酞普兰对映体的测定得出S(+)/R(-)平衡比为0.9至1.2。该药物的内分泌反应表现为血浆催乳素和皮质醇显著增加。除一名出现明显副作用的受试者外，人体生长激素在输注生理盐水后出现激增，而在输注西酞普兰后受到抑制。直肠温度和心率未受影响，耐受性良好。由于西酞普兰对突触前5-羟色胺神经末梢具有极高的选择性，目前的数据表明它可能是体内研究人脑5-羟色胺能功能的一种有前景的工具。
