II. Background

  1. Responsible for majority of P-450 Drug Interactions
  2. Accounts for 40 to 60% of hepatic P-450 isoenzymes
  3. Also present in intestinal epithelium

III. Interactions: Metabolized by CYP 3A3/4 (Substrates)

  1. Neuropsychiatric drugs
    1. Anticonvulsants
      1. Carbamazepine (Tegretol)
      2. Ethosuximide (Zarontin)
    2. Tertiary amine Tricyclic Antidepressants
      1. Amitriptyline (Elavil)
      2. Clomipramine
      3. Imipramine
    3. Antipsychotics
      1. Clozapine
    4. Benzodiazepines
      1. Alprazolam (Xanax)
      2. Diazepam (Valium)
      3. Midazolam (Versed)
      4. Triazolam (Halcion)
    5. Other
      1. Ergotamine: Inhibitor
  2. Cardiopulmonary Drugs
    1. Antiarrhythmics
      1. Amiodarone (Cordarone)
      2. Disopyramide (Norpace)
      3. Lidocaine (Xylocaine)
      4. Propafenone (Rythmol)
      5. Quinidine
    2. Lipid lowering agents (i.e. Statins)
      1. Lovastatin (Mevacor)
      2. Simvastatin (Zocor)
      3. Atorvastatin (Lipitor)
      4. Cerivastatin
    3. Antihypertensives
      1. Felodipine (Plendil)
      2. Diltiazem (Cardizem)
      3. Nifedipine (Procardia, Adalat)
      4. Verapamil (Calan)
      5. Amlodipine (Norvasc)
      6. Nisoldipine
      7. Nimodipine (Nimotop)
  3. Antibiotics
    1. Macrolide antibiotics
      1. Clarithromycin
      2. Troleandomycin
    2. HIV Protease Inhibitors
      1. Indinavir
      2. Nelfinavir
      3. Ritonavir
      4. Saquinavir
      5. Amprenavir
  4. Miscellaneous
    1. Alfentanil
    2. Cisapride (Propulsid)
    3. Estrogens (Ethinyl Estradiol, 17 B-estradiol)
    4. Opioids
      1. Codeine
      2. Alfentanil
      3. Fentanyl
      4. Sufentanil
    5. Sildenafil (Viagra)
    6. Testosterone
    7. Tamoxifen
    8. Vincristine
    9. Vinblastine
    10. Ifosfamide
    11. Cyclophosphamide
    12. Astemizole (Hismanal)
    13. Terfenadine (Seldane)
    14. Loratadine (Claritin)
    15. Cyclosporine
    16. Tacrolimus
    17. Zolpidem (Ambien)
    18. Corticosteroids (Budesonide, Cortisol)

V. Interactions: Inducer of CYP 3A3/4

  1. Neuropsychiatric drugs
    1. Carbamazepine
    2. Phenobarbital and other barbiturates
    3. Phenytoin
    4. Hypericum perforatum (St. John's Wort)
  2. Antibiotics
    1. Rifampin
  3. Miscellaneous
    1. Dexamethasone
    2. Troglitazone

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Related Studies

Ontology: cytochrome P450 3A4 protein, human (C1142644)

Definition (NCI) Cytochrome P450 3A4 (503 aa, ~57 kDa) is encoded by the human CYP3A4 gene. This protein is involved in the oxidation of steroids, fatty acids and xenobiotics.
Concepts Amino Acid, Peptide, or Protein (T116) , Enzyme (T126)
MSH C510163
SnomedCT 422741004
English CYP3A4 protein, human, nifedipine oxidase, human, quinine 3-monooxygenase, human, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, human, CYP3A4, Cytochrome p450 CYP3A4 enzyme (substance), Cytochrome p450 CYP3A4 enzyme, albendazole monooxygenase, human, cytochrome P450, family 3, subfamily A, polypeptide 4, human, cytochrome p-450 3a4, cyp3a4, cytochrome p450 3a4, p450 3a4, cytochrome P450HLp3, cytochrome P-450 CYP3A3 (human), CYP3A3 protein, human, CYPIIIA4, Steroid-Inducible P450-III, Cytochrome P450 3A3, EC, CYPIIIA3, EC 1.14.13.-, EC, EC, Taurochenodeoxycholate 6-Alpha-Hydroxylase, Cytochrome P450 HLp, Albendazole Sulfoxidase, Albendazole Monooxygenase, Cytochrome P450 NF-25, Cytochrome P450-PCN1, cytochrome P450 3A4 protein, human, Cytochrome P450 3A4, P450-3A4, Cytochrome P450 Nifedipine Oxidase, Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 3, Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 4, Cytochrome P450, Subfamily IIIA, Polypeptide 4, Cytochrome P450PCN1, Glucocorticoid-Inducible P450, Nifedipine Oxidase, P450, FAMILY III, P450-III, Steroid Inducible, P450-III, Steroid-Inducible, Quinine 3-Monooxygenase
Spanish enzima CYP3A4 del citocromo p450 (sustancia), enzima CYP3A4 del citocromo p450, CYP3A4

Ontology: CYP3A4 wt Allele (C1705261)

Definition (NCI) Human CYP3A4 wild-type allele is located in the vicinity of 7q21.1 and is approximately 27 kb in length. This allele, which encodes cytochrome P450 3A4 protein, plays a role in the oxidation of steroids, drugs, carcinogens and other xenobiotics. CYP3A4 gene dysfunction is associated with both lung cancer and epipodophyllotoxin-induced leukemogenesis.
Concepts Gene or Genome (T028)
English CYP3A, CYPIIIA4, HLP, NF-25, P450-PCN1, P450C3, P450PCN1, CP33, CP34, CYP3A3, CYP3, Cytochrome P450, Family 3, Subfamily A, Polypeptide 4 wt Allele, CYP3A4 wt Allele