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 |

ketoconazole

  • ketoconazole is a strong inhibitor of CYP3A.
  • ketoconazole is a weak inhibitor of CYP2C9, CYP2C19, and CYP2D6.
  • 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]
    Weak inhibitorsamiodarone [17]
    cimetidine [18]
    co-trimoxazole [19]
    disulfiram [20]
    echinacea [21]
    fluvastatin [22]
    fluvoxamine [23]
    ketoconazole [24]
    lovastatin [17]
    metronidazole [25]
    sertraline [26]
    simvastatin [17]
    sulfadiazine [27]
    voriconazole [28]
    zafirlukast [a]
    finasteride [29]
    interferon alpha-2b [30]
    ketoconazole [31]
    omeprazole [32]
    oral contraceptives [33]
    roxithromycin [34]
    amiodarone [35]
    amitriptyline [36]
    aspirin [37]
    celecoxib [38]
    cimetidine [39]
    darifenacin [b]
    desvenlafaxine [40]
    diltiazem [41]
    diphenhydramine [42]
    escitalopram [43]
    felodipine [44]
    fluvoxamine [45]
    gefitinib [46]
    hydralazine [47]
    imatinib [48]
    interferon alpha-2b [30]
    ketoconazole [49]
    methadone [50]
    metoprolol [51]
    nortriptyline [52]
    oral contraceptives [53]
    oxprenolol [51]
    pindolol [51]
    propranolol [51]
    ranitidine [54]
    risperidone [55]
    ritonavir [56]
    saw palmetto [57]
    sertraline [6]
    timolol [51]
    venlafaxine [58]
    alprazolam [59]
    amiodarone [60]
    aspirin [37]
    azithromycin [61]
    bicalutamide [62]
    cimetidine [63]
    co-trimoxazole [64]
    cyclosporine [65]
    fluvoxamine [66]
    isoniazid [67]
    maraviroc [68]
    oral contraceptives [69]
    ranitidine [70]
    roxithromycin [71]
    simvastatin [72]

    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.systemic preparations not available in Australia or New Zealand.
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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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    28.Purkins L, Wood N, Ghahramani P, Love ER, Eve MD, Fielding A. Coadministration of voriconazole and phenytoin: pharmacokinetic interaction, safety, and toleration. British Journal of Clinical Pharmacology 2003; 56: 37-44.[PubMed]
    29.Yasumori T, Narita H, Matsuda T, Takubo T, Ogawa M, Ishii M, Hara K, Ishii Y, Okuyama K, Fujimoto G, Ochiai H, Kano A, Hasegawa S, Sato K, Taniguchi T. Finasteride 1 mg has no inhibitory effect on omeprazole metabolism in extensive and poor metabolizers for CYP2C19 in Japanese. European Journal of Clinical Pharmacology 2006; 62: 939-46.[PubMed]
    30.Islam M, Frye RF, Richards TJ, Sbeitan I, Donnelly SS, Glue P, Agarwala SS, Kirkwood JM. Differential Effect of IFNalpha-2b on the Cytochrome P450 Enzyme System: A Potential Basis of IFN Toxicity and Its Modulation by Other Drugs. Clinical Cancer Research 2002; 8: 2480-87.[PubMed]
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    33.Laine K, Tybring G, Bertilsson L. No sex-related differences but significant inhibition by oral contraceptives of CYP2C19 activity as measured by the probe drugs mephenytoin and omeprazole in healthy Swedish white subjects. Clinical Pharmacology & Therapeutics 2000; 68: 151-59.[PubMed]
    34.Kees F, Holstege A, Ittner KP, Zimmermann M, Lock G, Scholmerich J, Grobecker H. Pharmacokinetic interaction between proton pump inhibitors and roxithromycin in volunteers. Alimentary Pharmacology & Therapeutics 2000; 14: 407-12.[PubMed]
    35.Fukumoto K, Kobayashi T, Tachibana K, Kat R, Tanaka K, Komamura K, Kamakura S, Kitakaze M, Ueno K. Effect of amiodarone on the serum concentration/dose ratio of metoprolol in patients with cardiac arrhythmia. Drug Metab Pharmacokinet 2006; 21: 501-05.[PubMed]
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    37.Chen XP, Tan ZR, Huang SL, Huang Z, Ou-Yang DS, Zhou HH. Isozyme-specific induction of low-dose aspirin on cytochrome P450 in healthy subjects. Clinical Pharmacology & Therapeutics 2003; 73: 264-71.[PubMed]
    38.Werner U, Werner D, Rau T, Fromm MF, Hinz B, Brune K. Celecoxib inhibits metabolism of cytochrome P450 2D6 substrate metoprolol in humans. Clinical Pharmacology & Therapeutics 2003; 74: 130-37.[PubMed]
    39.Steiner E, Spina E. Differences in the inhibitory effect of cimetidine on desipramine metabolism between rapid and slow debrisoquin hydroxylators. Clinical Pharmacology & Therapeutics 1987; 42: 278-82.[PubMed]
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