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The Pharmacokinetics of Escitalopram After Oral and Intravenous Administration of Single and Multiple Doses to Healthy Subjects
Author(s) -
Søgaard B.,
Mengel H.,
Rao N.,
Larsen F.
Publication year - 2005
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005280860
Subject(s) - pharmacokinetics , citalopram , escitalopram , volume of distribution , bioavailability , oral administration , pharmacology , metabolite , urine , absorption (acoustics) , medicine , distribution (mathematics) , active metabolite , receptor , antidepressant , mathematical analysis , physics , mathematics , hippocampus , serotonin , acoustics
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 (C max ) 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‐citalopram to R‐citalopram either in plasma or in urine. Concurrent intake of food had no effect on the pharmacokinetics of escitalopram or its metabolite. All treatments were well tolerated .