Omeprazole preferentially inhibits the metabolism of (+)-(S)-citalopram in healthy volunteers.

British Journal of Clinical Pharmacology
Adriana RochaVera L Lanchote

Abstract

Citalopram (CITA) pharmacokinetics are enantioselective in healthy volunteers and the metabolism of (+)-(S)-CITA to (+)-(S)-DCITA is dependent on CYP2C19. Omeprazole is a potent CYP2C19 inhibitor. This study indicates that omeprazole induces a loss of enantioselectivity in the CITA pharmacokinetics because of the selective inhibition of (+)-(S)-CITA metabolism. The study assessed the influence of omeprazole on the kinetic disposition of the (+)-(S)-citalopram (CITA) and (-)-(R)-CITA enantiomers in healthy volunteers. In a cross-over study, healthy volunteers (n = 9) phenotyped as extensive metabolizers of CYP2C19 and CYP2D6 and with an oral midazolam clearance ranging from 10.9 to 149.3 ml min(-1) kg(-1) received a single dose of racemic CITA (20 mg orally) in combination or not with omeprazole (20 mg day(-1) for 18 days). Serial blood samples were collected up to 240 h after CITA administration. CITA and demethylcitalopram (DCITA) enantiomers were analyzed by LC-MS/MS using a Chiralcel OD-R column. The kinetic disposition of CITA was enantioselective in the absence of treatment with omeprazole, with the observation of a greater proportion of plasma (-)-(R)-CITA [AUC S:R ratio of 0.53 (95% CI 0.41, 0.66) for CITA and 1.08 (95% ...Continue Reading

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Citations

Dec 17, 2011·CNS Drugs·Edoardo SpinaFilippo Caraci
Feb 20, 2014·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Ralph-Steven Wedemeyer, Henning Blume
Jul 18, 2014·Current Treatment Options in Gastroenterology·Marina KimJesse Green
May 6, 2015·British Journal of Clinical Pharmacology·Vera Lucia LanchoteGuilherme Suarez-Kurtz
Aug 8, 2013·British Journal of Clinical Pharmacology·Roberto LozanoErnesto Garcia-Arilla
Feb 11, 2015·Psychosomatics·Robert Joseph Morgan, Tamara J Dolenc
Oct 31, 2014·Biomedical Chromatography : BMC·R Nageswara Rao, K Guru Prasad
May 9, 2019·Journal of Child and Adolescent Psychopharmacology·Ethan A PoweleitLaura B Ramsey
Jun 11, 2020·Journal of Neural Transmission·Gudrun HefnerAnsgar Klimke
Nov 16, 2012·Deutsches Ärzteblatt International·Ingolf Cascorbi

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