The pharmacokinetics of escitalopram after oral and intravenous administration of single and multiple doses to healthy subjects

被引:112
作者
Sogaard, B
Mengel, H
Rao, N
Larsen, F
机构
[1] H Lundbeck & Co AS, Dept Clin Pharmacol & Pharmacokinet, Copenhagen, Denmark
[2] Forest Labs Inc, Forest Res Inst, Jersey City, NJ USA
关键词
escitalopram; citalopram; enantiomer; healthy volunteers; single dose; multiple dose; cross-over; pharmacokinetics; bioequivalence; tolerability;
D O I
10.1177/0091270005280860
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The pharmacokinetics of escitalopram (S-citalopram) and its principal metabolite, S-demethylcitalopram (S-DCT), were investigated after intravenous and oral administration to healthy subjects. After intravenous infusion of escitalopram, the mean systemic clearance and volume of distribution were 31 L/h and 1100 L, respectively After oral administration Of single or multiple doses, the absorption was relatively fast, with the maximum observed plasma or serum concentration attained after 3 to 4 hours. The mean half-lives were 27 and 33 hours, respectively, steady state was attained within 10 days. The area under the plasma or serum concentration-time curve from time zero to 24 hours and C-max was both linear and proportional to the dose. The apparent volume of distribution was around 20 L/kg. Comparison of the systemic and oral clearance implied a high absolute bioavailability, There was no evidence of interconversion from S-citaloprom to R-citalopram either in plasm a or in urine. Concurrent in take of food had no effect on the pharmacokinetics of escitalopram or its metabolite. All treatments were well tolerated.
引用
收藏
页码:1400 / 1406
页数:7
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