Are pharmacokinetic drug interactions with the SSRIs an issue?

K. Brøsen*

*Kontaktforfatter for dette arbejde

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

Resumé

The development of the selective serotonin reuptake inhibitors (SSRIs) began 20 years ago, around the time when it was discovered that the cytochrome P450 system consists of multiple drug-metabolizing enzymes. There are 5-10 important drug-metabolizing P450 enzymes in the human liver, and their relationship with SSRIs has been studied intensively during the last 5 years. Thus, among the SSRIs, fluvoxamine is the only very potent inhibitor of cytochrome P4501A2 (CYP1A2). All of the SSRIs inhibit CYP2D6 ('sparteine/debrisoquine oxygenase') but fluoxetine and paroxetine are clearly the most potent in this regard. Fluoxetine and fluvoxamine are moderate inhibitors of CYP2C19 ('S-mephenytoinhydroxylase'), and fluvoxamine might also be a moderate inhibitor of CYP2C9. Thus, although much still has to be learned about SSRIs and cytochrome P450, it seems that citalopram and sertraline have the most favourable profile in relation to drug interactions.

OriginalsprogEngelsk
TidsskriftInternational Clinical Psychopharmacology
Vol/bind11
Udgave nummerSUPPL. 1
Sider (fra-til)23-27
Antal sider5
ISSN0268-1315
StatusUdgivet - 1. mar. 1996

Fingeraftryk

Serotonin Uptake Inhibitors
Drug Interactions
Fluvoxamine
Pharmacokinetics
Cytochrome P-450 Enzyme System
Fluoxetine
Debrisoquin
Sertraline
Oxygenases
Cytochrome P-450 CYP2D6
Paroxetine
Citalopram
Cytochromes
Pharmaceutical Preparations
Liver
Enzymes

Citer dette

@article{2af3f0fc5d0f46ccbe8da4ac336ee5c0,
title = "Are pharmacokinetic drug interactions with the SSRIs an issue?",
abstract = "The development of the selective serotonin reuptake inhibitors (SSRIs) began 20 years ago, around the time when it was discovered that the cytochrome P450 system consists of multiple drug-metabolizing enzymes. There are 5-10 important drug-metabolizing P450 enzymes in the human liver, and their relationship with SSRIs has been studied intensively during the last 5 years. Thus, among the SSRIs, fluvoxamine is the only very potent inhibitor of cytochrome P4501A2 (CYP1A2). All of the SSRIs inhibit CYP2D6 ('sparteine/debrisoquine oxygenase') but fluoxetine and paroxetine are clearly the most potent in this regard. Fluoxetine and fluvoxamine are moderate inhibitors of CYP2C19 ('S-mephenytoinhydroxylase'), and fluvoxamine might also be a moderate inhibitor of CYP2C9. Thus, although much still has to be learned about SSRIs and cytochrome P450, it seems that citalopram and sertraline have the most favourable profile in relation to drug interactions.",
keywords = "Cytochrome P450, Drug interactions, Drug oxidation, Genetic polymorphism, SSRI",
author = "K. Br{\o}sen",
year = "1996",
month = "3",
day = "1",
language = "English",
volume = "11",
pages = "23--27",
journal = "International Clinical Psychopharmacology",
issn = "0268-1315",
publisher = "Lippincott Williams and Wilkins Ltd.",
number = "SUPPL. 1",

}

Are pharmacokinetic drug interactions with the SSRIs an issue? / Brøsen, K.

I: International Clinical Psychopharmacology, Bind 11, Nr. SUPPL. 1, 01.03.1996, s. 23-27.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

TY - JOUR

T1 - Are pharmacokinetic drug interactions with the SSRIs an issue?

AU - Brøsen, K.

PY - 1996/3/1

Y1 - 1996/3/1

N2 - The development of the selective serotonin reuptake inhibitors (SSRIs) began 20 years ago, around the time when it was discovered that the cytochrome P450 system consists of multiple drug-metabolizing enzymes. There are 5-10 important drug-metabolizing P450 enzymes in the human liver, and their relationship with SSRIs has been studied intensively during the last 5 years. Thus, among the SSRIs, fluvoxamine is the only very potent inhibitor of cytochrome P4501A2 (CYP1A2). All of the SSRIs inhibit CYP2D6 ('sparteine/debrisoquine oxygenase') but fluoxetine and paroxetine are clearly the most potent in this regard. Fluoxetine and fluvoxamine are moderate inhibitors of CYP2C19 ('S-mephenytoinhydroxylase'), and fluvoxamine might also be a moderate inhibitor of CYP2C9. Thus, although much still has to be learned about SSRIs and cytochrome P450, it seems that citalopram and sertraline have the most favourable profile in relation to drug interactions.

AB - The development of the selective serotonin reuptake inhibitors (SSRIs) began 20 years ago, around the time when it was discovered that the cytochrome P450 system consists of multiple drug-metabolizing enzymes. There are 5-10 important drug-metabolizing P450 enzymes in the human liver, and their relationship with SSRIs has been studied intensively during the last 5 years. Thus, among the SSRIs, fluvoxamine is the only very potent inhibitor of cytochrome P4501A2 (CYP1A2). All of the SSRIs inhibit CYP2D6 ('sparteine/debrisoquine oxygenase') but fluoxetine and paroxetine are clearly the most potent in this regard. Fluoxetine and fluvoxamine are moderate inhibitors of CYP2C19 ('S-mephenytoinhydroxylase'), and fluvoxamine might also be a moderate inhibitor of CYP2C9. Thus, although much still has to be learned about SSRIs and cytochrome P450, it seems that citalopram and sertraline have the most favourable profile in relation to drug interactions.

KW - Cytochrome P450

KW - Drug interactions

KW - Drug oxidation

KW - Genetic polymorphism

KW - SSRI

UR - http://www.scopus.com/inward/record.url?scp=0029928537&partnerID=8YFLogxK

M3 - Journal article

C2 - 8732441

AN - SCOPUS:0029928537

VL - 11

SP - 23

EP - 27

JO - International Clinical Psychopharmacology

JF - International Clinical Psychopharmacology

SN - 0268-1315

IS - SUPPL. 1

ER -