PKIS v2.0 A clinical tool for identifying important pharmacokinetic drug-drug interactions
| 1. Accepted major perpetrators | 2. Rejected perpetrators | 3. Unclassifiable | 4. Full table |

fluoxetine

  • fluoxetine is a strong inhibitor of CYP2D6.
  • fluoxetine is a moderate inhibitor of CYP2C19.
  • fluoxetine is neither an inhibitor or inducer of CYP3A.
  • fluoxetine has not been evaluated in the literature showing its role of altering the activities of CYP2C9.
  • CYP2C9CYP2C19CYP2D6CYP3A
    Strong inhibitorsfluconazole [1]
    fluvoxamine [2]
    ticlopidine [3]
    bupropion [4]
    fluoxetine [5]
    paroxetine [6]
    perhexaline [7]
    clarithromycin [8]
    erythromycin [9]
    grapefruit juice [10]
    indinavir [a]
    itraconazole [11]
    ketoconazole [11]
    lopinavir/ritonavir [12]
    ritonavir [13]
    saquinavir [14]
    saquinavir/ritonavir [15]
    voriconazole [16]
    Moderate inhibitorsfluconazole [17]
    clarithromycin [18]
    fluoxetine [19]
    moclobemide [20]
    voriconazole [21]
    cinacalcet [22]
    doxepin [23]
    duloxetine [24]
    flecainide [25]
    moclobemide [26]
    quinine [27]
    terbinafine [28]
    aprepitant [29]
    atazanavir [15]
    atazanavir/ritonavir [15]
    cimetidine [30]
    cyclosporine [31]
    diltiazem [32]
    fluconazole [33]
    fluvoxamine [34]
    imatinib [35]
    posaconazole [a]
    verapamil [32]
    No apparent change in clearanceamodiaquine [36]
    darifenacin [a]
    modafinil [37]
    omeprazole [38]
    prednisone [39]
    St John's wort [40]
    amodiaquine [36]
    levonorgestrel [41]
    risperidone [42]
    topiramate [43]
    amodiaquine [36]
    dexamethasone [44]
    echinacea [45]
    ginko-biloba [46]
    maraviroc [47]
    omeprazole [48]
    smoking [49]
    cimetidine [50]
    echinacea [45]
    finasteride [51]
    fluoxetine [52]
    gatifloxacin [53]
    methylprednisolone [54]
    paroxetine [55]
    pioglitazone [56]
    saw palmetto [57]
    sertraline [58]
    tenofovir [59]
    tipranavir/ritonavir [15]
    venlafaxine [60]
    Not evaluated in the literatureatazanavir
    efavirenz
    5-fluorouracil
    fluoxetine
    imatinib
    isoniazid
    leflunomide
    phenobarbitone
    phenytoin
    ritonavir
    teniposide
    efavirenz [b]
    indomethacin
    modafinil
    oxcarbazepine
    phenobarbitone
    phenytoin
    prednisone
    artemether/ lumefantrine
    chlorpheniramine
    chlorpromazine
    cocaine
    doxorubicin
    haloperidol
    ibuprofen
    methadone
    metoclopramide
    nilotinib
    ticlopidine
    anastrozole
    atenolol
    atorvastatin
    caffeine
    cyproterone
    ethosuximide
    danazol
    delavirdine [c]
    digoxin
    gemfibrozil
    lapatinib
    metoprolol
    metronidazole
    mifepristone
    norfloxacin
    quinipristin-dalfopristin
    raloxifene
    repaglinide
    valproate

    Footnotes and References

    a.assessment based on product information accessed via the Therapeutic Goods Administration of Australia Product and Consumer Medicines Information website ( https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/PICMI?OpenForm&t=PI&q=&r=https://www.ebs.tga.gov.au/ ).
    b.poster found at http://www.klinikum.uni-heidelberg.de/fileadmin/medizinische_klinik/Abteilung_6/pdf/Posterpreis_VKliPha2008_Bayer.pdf
    c.likely to be a major inhibitor based on subjective evaluation (≥ 2-fold AUC increase or ≥ 50% decrease in clearance of in vivo CYP probe).
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    3.Ieiri I, Kimura M, He S, Urae A, Otsubo K, Ishizaki T. Interaction magnitude, pharmacokinetics and pharmacodynamics of ticlopidine in relation to CYP2C19 genotypic status. Pharmacogenetics and Genomics 2005; 15: 851-59.[PubMed]
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    15.Abel S, Russell D, Taylor-Worth RJ, Ridgway CE, Muirhead GJ. Effects of CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers. British Journal of Clinical Pharmacology 2008; 65: 27-37.[PubMed]
    16.Saari TI, Laine K, Leino K, Valtonen M, Neuvonen PJ, Olkkola KT. Effect of voriconazole on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Clinical Pharmacology & Therapeutics 2006; 79: 362-70.[PubMed]
    17.Neal JM, Kunze KL, Levy RH, O'Reilly RA, Trager WF. Kiiv, an in vivo parameter for predicting the magnitude of a drug interaction arising from competitive enzyme inhibition. Drug Metabolism and Disposition 2003; 31: 1043-48.[PubMed]
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