Fluvoxamine is a potent inhibitor of cytochrome P4501A2

Biochemical Pharmacology
K BrøsenS Loft

Abstract

Fluvoxamine is a new antidepressant and selectively inhibits serotonin reuptake (SSRI). The present study demonstrates that fluvoxamine is a very potent inhibitor of the high-affinity O-deethylation of phenacetin, which is catalysed by cytochrome P4501A2 (CYP1A2), in microsomes from three human livers. Thus, the apparent inhibitor constant of fluvoxamine, Ki, ranged from 0.12 to 0.24 microM. Seven other SSRIs, citalopram, N-desmethylcitalopram, fluoxetine, norfluoxetine, paroxetine, sertraline and litoxetin either did not inhibit or were weak inhibitors of the O-deethylation of phenacetin. Our findings explain the mechanism of the pharmacokinetic interactions between fluvoxamine and drugs that are metabolized by CYP1A2, e.g. theophylline and imipramine.

References

Sep 1, 1992·British Journal of Clinical Pharmacology·E Skjelbo, K Brøsen
Jun 1, 1992·Therapeutic Drug Monitoring·E SpinaA P Caputi
May 1, 1992·Archives of Biochemistry and Biophysics·R W LambrechtJ F Sinclair
Nov 1, 1991·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·A D Sperber
Jan 1, 1991·European Journal of Clinical Pharmacology·G BertschyR Volmat
Jul 1, 1991·Journal of Psychiatry & Neuroscience : JPN·J M Kellett
Jan 1, 1991·Clinical Pharmacology and Therapeutics·E SkjelboL F Gram
Apr 15, 1991·Biochemical Pharmacology·S LoftH E Poulsen
Jan 1, 1990·Fundamental & Clinical Pharmacology·N H Holford
Jun 1, 1990·British Journal of Clinical Pharmacology·D SesardicD S Davies
Jan 1, 1988·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·E M Gillam, P E Reilly
Jan 1, 1987·British Journal of Clinical Pharmacology·E TarrusJ Segura

❮ Previous
Next ❯

Citations

Jan 1, 1996·The Psychiatric Quarterly·T B Cooper
Apr 30, 2005·Clinical Rehabilitation·Heleen BeckermanGustaaf J Lankhorst
Jul 12, 2008·Archives of Toxicology·Olavi PelkonenHannu Raunio
Jun 8, 2006·European Journal of Clinical Pharmacology·Janne T BackmanPertti J Neuvonen
Oct 24, 2007·European Journal of Clinical Pharmacology·Janne T BackmanPertti J Neuvonen
May 13, 2009·Journal of Neural Transmission·Arun K TiwariDaniel J Müller
Feb 22, 2011·European Journal of Drug Metabolism and Pharmacokinetics·Siamak Cyrus KhojastehAnthony Y H Lu
Mar 1, 1996·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·H J KoponenU Lepola
Jun 1, 1995·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·S VandelP Bizouard
Jan 13, 1999·Pediatric Clinics of North America·A P Ten EickM D Reed
Jan 7, 1998·Clinical Therapeutics·P E Stokes, A Holtz
Feb 16, 2000·Pharmacology & Therapeutics·C Hiemke, S Härtter
Mar 30, 2002·Advanced Drug Delivery Reviews·Marcel J de Groot, Sean Ekins
Jan 29, 2003·Progress in Neuro-psychopharmacology & Biological Psychiatry·Meera VaswaniSubramanyam Ramesh
Nov 26, 1999·European Psychiatry : the Journal of the Association of European Psychiatrists·S PallantiL M Koran
Sep 5, 2001·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·K Brøsen, C A Naranjo
Jul 28, 1999·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·W A DanielJ Wójcikowski
Jan 7, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·B Buur-Rasmussen, K Brøsen
Jul 19, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·C Lindsay DeVane
Sep 3, 2010·Journal of Child and Adolescent Psychopharmacology·Elana HarrisShannon N Saldaña
Jun 1, 1997·Journal of the American Academy of Child and Adolescent Psychiatry·H L LeonardA J Allen
Dec 1, 1993·British Journal of Clinical Pharmacology·V MartinelliM Del Zompo
Nov 1, 1994·British Journal of Clinical Pharmacology·L BertilssonJ Benitez
Jan 1, 1996·Fundamental & Clinical Pharmacology·J AhonenP J Neuvonen
May 5, 1998·Fundamental & Clinical Pharmacology·C IribarneF Berthou
Feb 1, 1996·Acta Psychiatrica Scandinavica·U A MeyerA Delini-Stula
Jan 1, 1997·Acta Psychiatrica Scandinavica. Supplementum·L BertilssonG Tybring
Feb 1, 1996·Pharmacology & Toxicology·H LuurilaP J Neuvonen
Apr 1, 1996·Pharmacology & Toxicology·M L Catterson, S H Preskorn
Dec 30, 1998·Pharmacology & Toxicology·B B RasmussenK Brøsen
Nov 12, 1998·The Journal of Pharmacy and Pharmacology·M ValotiG Sgaragli
Dec 21, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Rebecca StadelLindsay B Hough
Nov 8, 2001·Journal of Clinical Pharmacology·K VenkatakrishnanD J Greenblatt
Feb 28, 2002·Journal of Clinical Pharmacology·Emi YonezawaKazuhiko Tanaka
Sep 12, 2002·Drug Metabolism and Drug Interactions·Michael W JanDavid A Flockhart

❮ Previous
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