Dose-dependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine

@article{Jeppesen1996DosedependentIO,
  title={Dose-dependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine},
  author={Ulla Jeppesen and Lennart Gram and Kirsten Kjeldgaard Vistisen and Steffen H Loft and Henrik Enghusen Poulsen and Kim Br{\o}sen},
  journal={European Journal of Clinical Pharmacology},
  year={1996},
  volume={51},
  pages={73-78}
}
Objectives: The purpose of this pharmacokinetic study was to investigate the dose-dependent inhibition of model substrates for CYP2D6, CYP2C19 and CYP1A2 by four marketed selective serotonin reuptake inhibitors (SSRIs): citalopram, fluoxetine, fluvoxamine and paroxetine. [...] Key Method The volunteers received in randomised order, at weekly intervals, increasing single oral doses of one of the four SSRIs, followed 3 h later by sparteine (CYP2D6), mephenytoin (CYP2C19) and caffeine (CYP1A2) tests. Fluoxetine…Expand
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References

SHOWING 1-10 OF 45 REFERENCES
Pharmacokinetics of desipramine coadministered with sertraline or fluoxetine.
TLDR
Sertraline had less pharmacokinetic interaction with desipramine than did fluoxetine at their respective, minimum, usually effective doses. Expand
The effect of selective serotonin re-uptake inhibitors on cytochrome P4502D6 (CYP2D6) activity in human liver microsomes.
TLDR
It is suggested that compounds with SSRI activity are likely to interact with human CYP2D6 in vivo with the potential of causing drug interactions. Expand
Selective serotonin reuptake inhibitors and theophylline metabolism in human liver microsomes: potent inhibition by fluvoxamine.
TLDR
It is concluded that pharmacokinetic interaction between fluvoxamine and theophylline is due to potent inhibition of CYP1A2, which are equally important isoforms for the 8-hydroxylation of theophyLLine. Expand
Moclobemide, a substrate of CYP2C19 and an inhibitor of CYP2C19, CYP2D6, and CYP1A2: A panel study *
TLDR
A combined mephenytoin, sparteine, and caffeine test performed before, during, and after multiple dosing of moclobemide showed changes in the metabolic indexes compatible with a reversible inhibition of oxidation by way of the corresponding CYP enzymes—CYP2C19, CYP2D6, and CYP1A2—during moclOBemide treatment. Expand
A fluvoxamine-caffeine interaction study.
TLDR
The results confirm that CYP1A2 is the main enzyme catalysing the biotransformation of caffeine, in particular the N3-dem methylation and partly the N1- and N7-demethylation and the results indicate that intake of caffeine during fluvoxamine treatment may lead to caffeine intoxication. Expand
Pharmacokinetics of Citalopram in Relation to the Sparteine and the Mephenytoin Oxidation Polymorphisms
TLDR
It was shown that the citalopram elimination partially depends on the mephenytoin oxygenase, since steady-state serum concentration, half-life, and area under the serum concentration/time curve for cITALopram were significantly higher in poor metabolizers of mephenYtoin than in extensive metabolizer of me Pheny toin. Expand
Single‐dose kinetics of clomipramine: Relationship to the sparteine and S‐mephenytoin oxidation polymorphisms
TLDR
Evidence is provided that the 2‐ and 8‐hydroxylation of clomipramine are catalyzed by CYP2D6 and that the N‐demethylation is catalyzed in part by CYp2C. Expand
Fluvoxamine Inhibition and Carbamazepine Induction of the Metabolism of Clozapine: Evidence from a Therapeutic Drug Monitoring Service
TLDR
It is concluded that carbamazepine causes decreased clozapine plasma levels, while fluvoxamine increases the levels. Expand
Extremely slow metabolism of amitriptyline but normal metabolism of imipramine and desipramine in an extensive metabolizer of sparteine, debrisoquine, and mephenytoin.
TLDR
This patient illustrates two problems: (a) the erroneous phenotyping due to concurrent medication, and (b) the existence of a very slow amitriptyline elimination apparently not related to the sparteine/debrisoquine oxidation polymorphism. Expand
Are pharmacokinetic drug interactions with the SSRIs an issue?
  • K. Brøsen
  • Medicine
  • International clinical psychopharmacology
  • 1996
TLDR
It seems that citalopram and sertraline have the most favourable profile in relation to drug interactions in SSRIs and cytochrome P450. Expand
...
1
2
3
4
5
...