Metabolism
Cytochrome P-450 3A3/4 Isoenzyme
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Cytochrome P-450 3A3/4 Isoenzyme
, Cytochrome P-450 3A3, Cytochrome P-450 3A4, CYP3A3, CYP3A4, CYP3As
Background
Responsible for majority of P-450
Drug Interaction
s
Accounts for 40 to 60% of hepatic P-450 isoenzymes
Also present in intestinal epithelium
Interactions
Metabolized by CYP 3A3/4 (Substrates)
Neuropsychiatric drugs
Anticonvulsants
Carbamazepine
(
Tegretol
)
Ethosuximide (Zarontin)
Tertiary amine
Tricyclic Antidepressant
s
Amitriptyline
(
Elavil
)
Clomipramine
Imipramine
Antipsychotic
s
Clozapine
Benzodiazepine
s
Alprazolam
(
Xanax
)
Diazepam
(
Valium
)
Midazolam
(
Versed
)
Triazolam
(
Halcion
)
Other
Ergotamine
: Inhibitor
Cardiopulmonary Drugs
Antiarrhythmic
s
Amiodarone
(
Cordarone
)
Disopyramide (Norpace)
Lidocaine
(
Xylocaine
)
Propafenone
(
Rythmol
)
Quinidine
Lipid
lowering agents (i.e.
Statin
s)
Lovastatin
(Mevacor)
Simvastatin
(
Zocor
)
Atorvastatin
(
Lipitor
)
Cerivastatin
Antihypertensives
Felodipine (Plendil)
Diltiazem
(
Cardizem
)
Nifedipine
(
Procardia
,
Adalat
)
Verapamil
(
Calan
)
Amlodipine
(
Norvasc
)
Nisoldipine
Nimodipine
(Nimotop)
Antibiotics
Macrolide
antibiotics
Clarithromycin
Troleandomycin
HIV
Protease Inhibitor
s
Indinavir
Nelfinavir
Ritonavir
Saquinavir
Amprenavir
Miscellaneous
Alfentanil
Cisapride (Propulsid)
Estrogen
s (
Ethinyl Estradiol
, 17 B-estradiol)
Opioid
s
Codeine
Alfentanil
Fentanyl
Sufentanil
Sildenafil
(
Viagra
)
Testosterone
Tamoxifen
Vincristine
Vinblastine
Ifosfamide
Cyclophosphamide
Astemizole (Hismanal)
Terfenadine (Seldane)
Loratadine
(
Claritin
)
Cyclosporine
Tacrolimus
Zolpidem
(
Ambien
)
Corticosteroid
s (Budesonide, Cortisol)
Interactions
Inhibitor of CYP 3A3/4
Neuropsychiatric drugs
Midazolam
(
Versed
)
Nefazodone
(
Serzone
)
Cardiopulmonary Drugs
Quinidine
Diltiazem
(
Cardizem
)
Nifedipine
(
Procardia
,
Adalat
)
Verapamil
(
Calan
)
Zafirlukast
Antibiotics
Indinavir
Nelfinavir
Ritonavir
Fluconazole
Itraconazole
Ketoconazole
Erythromycin
Telithromycin
(
Ketek
)
Clarithromycin
Serious risk of
Hypotension
and
Acute Kidney Injury
when combined with
Calcium Channel Blocker
Gandhi (2013) JAMA 310(23):2544-53 [PubMed]
Miscellaneous
Bromocriptine
Cimetidine
Estrogen
s (
Ethinyl Estradiol
)
Grapefruit
juice
Mibefradil
Omeprazole
(
Prilosec
)
Interactions
Inducer of CYP 3A3/4
Neuropsychiatric drugs
Carbamazepine
Phenobarbital and other barbiturates
Phenytoin
Hypericum perforatum
(
St. John's Wort
)
Antibiotics
Rifampin
Miscellaneous
Dexamethasone
Troglitazone
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