Summary
The plasma concentrations of citalopram, a potent serotonin reuptake inhibitor, and its demethylated metabolite have been determined by a specific fluorescence coupling technique during single dose experiments in volunteers and in clinical tests. Citalopram was found to have linear kinetics within the dose range investigated, which were characterized by fairly rapid absorption and slow elimination (biological half-life 1–21/2 days). Steady state levels in the range 120–340 nM (i.e. slightly above those associated with pharmacodynamic activity in animals) were attained within a week. A drug/metabolite ratio of 2–3 was recorded.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Alexanderson, B.: Pharmacokinetics of desmethylimipramine and nortriptyline in man after single and multiple oral doses — A cross-over study. Europ. J. clin. Pharmacol.5, 1–10 (1972)
Borg, K. O., Westerlund, D.: Fluorometric determination of non-fluorescent amines by ion-pair extraction. Z. Anal. Chem.252, 275–278 (1970)
Christensen, A. V., Fjalland, B., Pedersen, V., Danneskiold-Samsøe, P., Svendsen, O.: Pharmacology of a new phthalane (Lu 10-171), with specific 5-HT uptake inhibiting properties. Eur. J. Pharmacol.41, 153–162 (1977)
Fredricson Overø, K., Svendsen, O.: Hepatotoxicity of citalopram in rats and first-pass metabolism. Proceedings of the 19th meeting of the European Society of Toxicology. Copenhagen, June 19–22, 1977 Arch. Toxicol. Suppl.1, 177–180 (1978)
Gram, L. F., Buch Andreasen, P., Fredricson Overø, K., Christiansen, J.: Comparison of single dose kinetics of imipramine, nortriptyline and antipyrine in man. Psychopharmacology50, 21–27 (1976)
Gram, L. F.: Plasma level monitoring of tricyclic antidepressant therapy. Clin. Pharmacokinetics2, 237–251 (1977)
Hald, A.: Statistiske metoder, p. 244. Copenhagen: Akademisk Forlag 1973
Hyttel, J.: Neurochemical characterization of a new potent and selective serotonin uptake inhibitor: Lu 10-171. Psychopharmacology51, 225–233 (1977a)
Hyttel, J.: Effect of a selective 5-HT uptake inhibitor — Lu 10-171 — on rat brain 5-HT turnover. Acta Pharmacol. Toxicol.40, 439–446 (1977b)
Hyttel, J.: Effect of a specific 5-HT uptake inhibitor, citalopram (Lu 10-171), on3H-5-HT uptake in rat brain synaptosomes in vitro. Psychopharmacology (1978) (in press)
Jørgensen, A., Staehr, P.: On the biological half-life of amitriptyline. J. Pharm. Pharmacol.28, 62–64 (1976)
Stahl, E.: Dünnschicht — Chromatographie. Berlin, Heidelberg, New York: Springer 1967
Westerlund, D., Borg, K. O.: Fluorimetric determinations by ion pair extractions. Part V. Studies on ion pair extraction with the fluorescent anion, 9, 10 — dimethoxyanthracene — 2 — sulphonate. Anal. Chim. Acta67, 89–98 (1973)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Overø, K.F. Preliminary studies of the kinetics of citalopram in man. Eur J Clin Pharmacol 14, 69–73 (1978). https://doi.org/10.1007/BF00560260
Received:
Revised:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00560260