CYP3A4: The Workhorse

  • Jennifer DeCou
  • Nathaniel Birgenheier
  • Randal O. Dull


This chapter discusses the genetics, metabolic actions, substrates, inducers, and inhibitors of cytochrome P450 3A4.


Cytochrome P450 CYP P450 3A4 CYP3A4 Pharmacokinetic Metabolism Metabolic pathway Enzyme Induction Inhibitor Substrate Oxidase Mixed-function oxidase Liver Intestine Hepatocytes Enterocytes Chromosome Gene locus 7q21.3-7q22.1 MDR gene Multi-drug resistance P-glycoprotein Pregname X receptor PXR receptor Constitutive androstane receptor CAR receptor Vitamin D Vitamin D response Polymorphism Aliphatic oxidation Aromatic hydroxylation N-dealkylation O-demethylation Oxidative deamination Sulfoxide formation N-hydroxylation Felodipine Tertiary amine tricyclic anti-depressants Antipsychotics Macrolide antibiotics Dihydropyridine calcium-channel blockers HMG CoA reductase inhibitors Statins Carbamazepine Steroid compounds Protease inhibitors Ritonavir Anticonvulsants Rifampin St. John’s Wort SSRI’s Quinolone antibiotics Azole antifungals Grapefruit juices Bergamottin Dihydroxybergamottin Torsade de pointes Rhabdomyolysis Midazolam Rifampin Intraconazole Midazolam Ketamine Fentanyl Alfentanil Sufentanil Methadone Local anesthetics Lidocaine Bupivacaine Ketamine Methadone 


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Jennifer DeCou
    • 1
  • Nathaniel Birgenheier
    • 1
  • Randal O. Dull
    • 2
  1. 1.Department of AnesthesiologyUniversity of Utah School of MedicineSalt Lake CityUSA
  2. 2.Department of AnesthesiologyUniversity of Illinois at ChicagoChicagoUSA

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