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

Author(s): Sogaard B, Mengel H, Rao N, Larsen F

Affiliation(s): Department of Clinical Pharmacology and Pharmacokinetics, H. Lundbeck A/S, Copenhagen, Denmark.

Publication date & source: 2005-12, J Clin Pharmacol., 45(12):1400-6.

Publication type: Clinical Trial, Phase I; Randomized Controlled Trial

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 1,100 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.