CYP 450 interactions Flashcards

1
Q

3A4 inhibitors

A
Nefaozodone
Fluvoxaine
Fluoxetine
grapefruit juice
Antiretrovirals
antibiotics (macrolide like erythromycin)
Antifungals (like ketoconazole)
CCB
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2
Q

3A4 inducers

A
carbamazepine
phenytoin
barbiturates
modafinil
rifampicin
efavirenz
st John's wort
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3
Q

3A4 substrates

A
Benzos
many antipsychotics
Carbamazepine
OCP
statins
antiretrovirals
immunosuppressants
antineoplastic
cortecosteroids
CCB
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4
Q

1A2 inhibitors

A
fluvoxamine
caffiene
ciprofloxacin
estrogen
cimetidine Atazanavir
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5
Q

1A2 inducers

A
carbamazepine
?phenytoin
barbiturates
rifampicin
primidone
smoking
(not St.John's wort which induces 3A4, 2C9, 2C19)
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6
Q

1A2 substrates

A
Clozapine
Olanzapine
Mirtazapine
Ropinirole
Warfarin
Theophyline
caffiene
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7
Q

2D6 inhibitors

A
Paroxetine
Fluoxetine
Sertraline
Duloxetine
Buproprion

Terbenafine (antifungal)
Imatinib (anti-leukemia)
Quinidine (antiarrythmic)
Amiodarone (antiarrythmic)

there are poor metabolizers

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8
Q

2D6 inducers

A

none!

but there are ultra-rapid metabolizers

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9
Q

2 D6 Substrates

A
antidepressants:
TCA
SSRI
SNRI
Trazodone

AA:
Risperidone
Abilify

FGA: 
Haldol
chlorpromazoine
perphenazine
zuclopenthixole

betablockers
propranolol
metoprolol

anti-arrythmic:
flecainide
mexiletine

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10
Q

activation by 2D6

inhibitors of 2 D6 prevent drug from working

A

codeine
tramadolhydrocodone
tamoxifen

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11
Q

2C9 inhibitors

A

Valproate
Disulfiram
Fluoxetine

Clopidogrel (also 2C19-)
Amiodarone (also 2d6-)
Fluconazole (also 2C19-)
metronidazole

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12
Q

2C9 inducers

A
carbamazepine
phenytoin
barbiturates
rifampicin
Efavirenz (also 3A4 +)
St.John's wort (also  3A4+)

all of these are 3A4 inducers

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13
Q

2C9 substrates

A
phenytoin
barbiturates
Warfarin**
Glyburide (DM)
Glipizide (DM)
NSAIDs
ARB
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14
Q

2C19 inhibitors

A
Fluoxetine
Fluvoxaine
Moclobemide
Modafinil (also a 3A4 inducer)
Oxcarbazepine

Clopidogrel (2C9-)
Efavirenz (+ of 2C9 and 3A4)
Omeprazole
Fluconazole (2C9 -)

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15
Q

2C19 inducers

A
carbamazepine
phenytoin
barbiturates
rifampicin
st Johns wort

same as 3A4 and 2C9 inducer list (minus modafinil and efavirenz)

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16
Q

2C19 substrates

A
sertraline
escitalopram
citalopram
moclobemide
diazepam
pantoprazole
omeprazle
17
Q

St.John’s wort?

A

inducer of:
3A4
2C9
2C19

18
Q

Efavirenz?

A

inducer of
3A4
2C9

inhibitor of 2C19

no effect on 1A2

19
Q

inducers of 1A2, 3A4, 2C9, 2C19

A

carbamazepie
barbiturates
rifampicin
phenytoin (?1A2)

20
Q

polymorphism

A

2D6: 10% of caucasians, 1% of asians are poor
2C19: 20% of asians and blacks, 2% of caucasians are poor

21
Q

Paxil and phenytoin?

A

phenytoin goes up

2012

22
Q

least protein binding SSRIS?

most?

A

celexa and luvox

sertraline

23
Q

luvox plus celexa?

A

celexa goes up. 2C19

24
Q

Efavirenz and St.John’s wort have:
an effect on which enzymes (3)
no effect on which enzymes? (2)

A

effect on3A4, 2c9, 2c19

no effect on 2D6, 1A2

25
Q

what 2 enzymes do both fluoxetine and fluvoxamine strongly inhibit?

A

2C19

3A4

26
Q

which 2 enzymes are not affected by fluvoxamine?

A

2D6, 2C9

27
Q

which enzyme is not affected by fluoxetine?

A

1A2

28
Q

Enzymes inhibited by Fluoxetine from most to negligible?

A

2D6, 2C9
2C19
3A4
1A2

29
Q

Enzymes inhibited by Fluvoxamine from most to negligible?

A

1A2, 2C19
3A4
2D6
2C9