The Pharmacokinetics of Escitalopram After Oral and Intravenous Administration of Single and Multiple Doses to Healthy Subjects

Abstract

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.

Impact of CYP2C19 phenotypes on escitalopram metabolism and an evaluation of pupillometry as a serotonergic biomarker

“…These two mean values indicate a 1.6-fold higher AUC in the PM than in the EM, which is in good agreement with our data. In a recent study, the PK of escitalopram was determined in a group of 17 healthy subjects after multiple doses of escitalopram 10 mg/ day [18]. The results are fairly consistent with our results obtained in the group of EM subjects.…”

Acute escitalopram treatment inhibits REM sleep rebound and activation of MCH-expressing neurons in the lateral hypothalamus after long term selective REM sleep deprivation

“…The injections were administered at the beginning of sleep rebound to permit an undisturbed sleep for both REMS-deprived and HC animals during the 3-h EEG recording (Sogaard et al 2005;Vas et al 2013).…”

Increased Lower Limb Spasticity but Not Strength or Function Following a Single-Dose Serotonin Reuptake Inhibitor in Chronic Stroke

“…The half-life of escitalopram is 27 hours, 42 and 7 days between testing ensured drug elimination before reassessment. Agents were overencapsulated and block randomized (4 subjects per block) by the pharmacist who maintained blinding.…”

“…Agents were overencapsulated and block randomized (4 subjects per block) by the pharmacist who maintained blinding. Subjects were tested before and 4 to 5 hours after drug administration (time for peak plasma concentration 42 ). Testing was completed in 1.5 to 2 hours, and the time of day was similar for all procedures across drug conditions (ie, morning for pretesting, afternoon for posttraining).…”