CYP 450 interactions Flashcards
3A4 inhibitors
Nefaozodone Fluvoxaine Fluoxetine grapefruit juice Antiretrovirals antibiotics (macrolide like erythromycin) Antifungals (like ketoconazole) CCB
3A4 inducers
carbamazepine phenytoin barbiturates modafinil rifampicin efavirenz st John's wort
3A4 substrates
Benzos many antipsychotics Carbamazepine OCP statins antiretrovirals immunosuppressants antineoplastic cortecosteroids CCB
1A2 inhibitors
fluvoxamine caffiene ciprofloxacin estrogen cimetidine Atazanavir
1A2 inducers
carbamazepine ?phenytoin barbiturates rifampicin primidone smoking (not St.John's wort which induces 3A4, 2C9, 2C19)
1A2 substrates
Clozapine Olanzapine Mirtazapine Ropinirole Warfarin Theophyline caffiene
2D6 inhibitors
Paroxetine Fluoxetine Sertraline Duloxetine Buproprion
Terbenafine (antifungal)
Imatinib (anti-leukemia)
Quinidine (antiarrythmic)
Amiodarone (antiarrythmic)
there are poor metabolizers
2D6 inducers
none!
but there are ultra-rapid metabolizers
2 D6 Substrates
antidepressants: TCA SSRI SNRI Trazodone
AA:
Risperidone
Abilify
FGA: Haldol chlorpromazoine perphenazine zuclopenthixole
betablockers
propranolol
metoprolol
anti-arrythmic:
flecainide
mexiletine
activation by 2D6
inhibitors of 2 D6 prevent drug from working
codeine
tramadolhydrocodone
tamoxifen
2C9 inhibitors
Valproate
Disulfiram
Fluoxetine
Clopidogrel (also 2C19-)
Amiodarone (also 2d6-)
Fluconazole (also 2C19-)
metronidazole
2C9 inducers
carbamazepine phenytoin barbiturates rifampicin Efavirenz (also 3A4 +) St.John's wort (also 3A4+)
all of these are 3A4 inducers
2C9 substrates
phenytoin barbiturates Warfarin** Glyburide (DM) Glipizide (DM) NSAIDs ARB
2C19 inhibitors
Fluoxetine Fluvoxaine Moclobemide Modafinil (also a 3A4 inducer) Oxcarbazepine
Clopidogrel (2C9-)
Efavirenz (+ of 2C9 and 3A4)
Omeprazole
Fluconazole (2C9 -)
2C19 inducers
carbamazepine phenytoin barbiturates rifampicin st Johns wort
same as 3A4 and 2C9 inducer list (minus modafinil and efavirenz)
2C19 substrates
sertraline escitalopram citalopram moclobemide diazepam pantoprazole omeprazle
St.John’s wort?
inducer of:
3A4
2C9
2C19
Efavirenz?
inducer of
3A4
2C9
inhibitor of 2C19
no effect on 1A2
inducers of 1A2, 3A4, 2C9, 2C19
carbamazepie
barbiturates
rifampicin
phenytoin (?1A2)
polymorphism
2D6: 10% of caucasians, 1% of asians are poor
2C19: 20% of asians and blacks, 2% of caucasians are poor
Paxil and phenytoin?
phenytoin goes up
2012
least protein binding SSRIS?
most?
celexa and luvox
sertraline
luvox plus celexa?
celexa goes up. 2C19
Efavirenz and St.John’s wort have:
an effect on which enzymes (3)
no effect on which enzymes? (2)
effect on3A4, 2c9, 2c19
no effect on 2D6, 1A2
what 2 enzymes do both fluoxetine and fluvoxamine strongly inhibit?
2C19
3A4
which 2 enzymes are not affected by fluvoxamine?
2D6, 2C9
which enzyme is not affected by fluoxetine?
1A2
Enzymes inhibited by Fluoxetine from most to negligible?
2D6, 2C9
2C19
3A4
1A2
Enzymes inhibited by Fluvoxamine from most to negligible?
1A2, 2C19
3A4
2D6
2C9
