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3a4_inhibitors.md

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CYP3A4 Inhibitors

Strong: ≥5-fold increase in the plasma AUC values (>80% decrease in clearance)

Moderate: ≥2-fold increase in the plasma AUC values (50–80% decrease in clearance)

Weak: ≥1.25-fold and <2-fold increase in the plasma AUC values (20–50% decrease in clearance)

Strong inhibitors

  • protease inhibitors
    • boceprevir
    • ritonavir
    • indinavir
    • nelfinavir
    • saquinavir
  • macrolide antibiotics
    • clarithromycin
    • erythromycin
    • telithromycin
  • ceritinib
  • mibefradil
  • nefazodone
  • ribociclib
  • tucatinib
  • chloramphenicol
  • azole antifungals
    • ketoconazole
    • itraconazole
    • posaconazole
    • voriconazole
  • cobicistat
  • green tea extract
  • grape seed extract
  • dillapiole
  • apigenin

Moderate inhibitors

  • amiodarone
  • aprepitant
  • ciprofloxacin
  • conivaptan
  • crizotinib
  • rutin
  • tofisopam
  • calcium channel blockers
    • verapamil
    • diltiazem
  • azole antifungals
    • fluconazole
    • miconazole
  • bergamottin
  • cyclosporine
  • donedarone
  • fluvoxamine
  • imatinib
  • valerian

Weak inhibitors

  • berberine
  • buprenorphine
  • cafestol (in unfiltered coffee)
  • cilostazol
  • cimetidine
  • fosaprepitant
  • lomitapide
  • orphenadrine
  • omeprazole
  • quercetin
  • ranitidine
  • ranolazine
  • tacrolimus
  • ticagrelor
  • valproic acid
  • amlodipine
  • azithromycin

Inhibitors of unspecified potency

  • cannabidiol
  • dithiocarbamate
  • mifepristone
  • norfloxacin
  • antiretroviral drugs
    • delavirdine
  • gestodene
  • star fruit
  • milk thistle
  • niacin
  • ginkgo biloba
  • sesamin
  • piperine
  • isoniazid
  • serenoa