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Source: Wikipedia, the free encyclopedia.
<
User:Qunho
Selected inducers, inhibitors and substrates of CYP3A4
Inhibitors
Inducers
Strong
protease inhibitors
ritonavir
indinavir
nelfinavir
saquinavir
some
macrolide antibiotics
clarithromycin
telithromycin
chloramphenicol
(
antibiotic
)
some
azole antifungals
ketoconazole
itraconazole
posaconazole
voriconazole
nefazodone
(
antidepressant
)
cobicistat
Moderate
amiodarone
aprepitant
(
antiemetic
)
some
calcium channel blockers
verapamil
diltiazem
some
macrolide antibiotics
erythromycin
some
azole antifungals
fluconazole
miconazole
bergamottin
(constituent of
grapefruit
juice)
cimetidine
ciprofloxacin
cyclosporine
donedarone
fluvoxamine
imatinib
Valerian
verapamil
Weak
buprenorphine
(
analgesic
)
cafestol
(in unfiltered coffee)
cilostazol
fosaprepitant
gabapentin
lomitapide
orphenadrine
ranitidine
ranolazine
tacrolimus
ticagrelor
valproic acid
Unspecified potency
cannabidiol
dithiocarbamate
(functional group)
mifepristone
(
abortifacient
)
norfloxacin
(antibiotic)
some non-nucleoside
reverse transcriptase inhibitors
delavirdine
gestodene
(
hormonal contraceptive
)
mibefradil
(in
angina pectoris
)
star fruit
milk thistle
niacinamide
ginkgo biloba
piperine
isoniazid
quercetin
Strong potency
antiandrogens
enzalutamide
apalutamide
phenytoin
Unspecified potency
anticonvulsants
,
mood stabilizers
carbamazepine
phenytoin
(
anticonvulsant
)
oxcarbazepine
topiramate
barbiturates
phenobarbital
Butalbital
St. John's wort
some
bactericidals
rifampicin
rifabutin
some non-nucleoside
reverse transcriptase inhibitors
efavirenz
nevirapine
some
hypoglycemics
pioglitazone
troglitazone
glucocorticoids
(
blood glucose
increase,
immunosuppressive
)
modafinil
(
stimulant
)
quercetin
capsaicin
Selected inducers, inhibitors and substrates of CYP3A4
Substrates
Inhibitors
Inducers
some
immunosuppressants
ciclosporin
(cyclosporin)
tacrolimus
sirolimus
many
chemotherapeutics
docetaxel
tamoxifen
paclitaxel
cyclophosphamide
doxorubicin
erlotinib
etoposide
ifosfamide
teniposide
vinblastine
vincristine
vindesine
imatinib
irinotecan
sorafenib
sunitinib
vemurafenib
temsirolimus
anastrozole
gefitinib
azole antifungals
ketoconazole
itraconazole
macrolides
clarithromycin
erythromycin
telithromycin
(not
azithromycin
)
dapsone
(in
leprosy
)
tricyclic antidepressants
amitriptyline
clomipramine
imipramine
cyclobenzaprine
SSRIs
citalopram
norfluoxetine
sertraline
some other antidepressants
mirtazapine
(
NaSSA
)
nefazodone
reboxetine
venlafaxine
(
SNRI
)
trazodone
(
SARI
)
vilazodone
buspirone
(
anxiolytic
)
antipsychotics
haloperidol
aripiprazole
risperidone
ziprasidone
pimozide
quetiapine
opioids
(mainly analgesics)
alfentanil
buprenorphine
(
analgesic
,
addiction maintenance treatment
)
codeine
(
analgesic
,
antitussive
,
antidiarrheal
)
fentanyl
hydrocodone
(partial involvement, not the bioactivation factor)
methadone
(
analgesic
,
addiction maintenance treatment
)
levacetylmethadol
tramadol
(to inactive metabolites, do not confuse with metabolism via
CYP2D6
)
benzodiazepines
alprazolam
midazolam
triazolam
diazepam
(bioactivation to
desmethyldiazepam
)
some
hypnotics
zopiclone
zaleplon
zolpidem
donepezil
(
acetylcholinesterase inhibitor
)
statins
atorvastatin
lovastatin
simvastatin
cerivastatin
(not
pravastatin
)
(not
rosuvastatin
)
calcium channel blockers
diltiazem
felodipine
nifedipine
verapamil
amlodipine
lercanidipine
nitrendipine
nisoldipine
amiodarone
(
class III antiarrhythmic
)
dronedarone
(
class III antiarrhythmic
)
quinidine
(
class I antiarrhythmic
)
PDE5 inhibitors
sildenafil
tadalafil
kinins
(
vasodilators
,
smooth muscle
contractors)
sex hormones
agonists and antagonists
finasteride
(
antiandrogen
)
estradiol
(
estrogen
)
progesterone
ethinylestradiol
(
hormonal contraceptive
)
testosterone
(
androgen
)
toremifene
(
SERM
)
bicalutamide
H1-receptor antagonists
terfenadine
astemizole
chlorphenamine
protease inhibitors
indinavir
ritonavir
saquinavir
nelfinavir
non-nucleoside
reverse transcriptase inhibitors
nevirapine
some
glucocorticoids
budesonide
hydrocortisone
dexamethasone
albendazole
(
antihelminthic
)
cisapride
(
5-HT4 receptor
agonist
)
aprepitant
(
antiemetic
)
caffeine
(
stimulant
)
cocaine
(
stimulant
)
cilostazol
(
phosphodiesterase inhibitor
)
dextromethorphan
(
antitussive
)
domperidone
(
antidopaminergic
)
eplerenone
(
aldosterone antagonist
)
lidocaine
(
local anesthetic
,
antiarrhythmic
)
ondansetron
(
5-HT3 antagonist
)
propranolol
(
beta blocker
)
salmeterol
(
beta agonist
)
warfarin
(
anticoagulant
)
clopidogrel
, becoming
bioactivated
(
antiplatelet
)
omeprazole
(
proton pump inhibitor
)
nateglinide
(
antidiabetic
)
methoxetamine
montelukast
(
leukotriene receptor antagonist
)
vilaprisan
(
selective progesterone receptor modulator
)
Strong
protease inhibitors
ritonavir
indinavir
nelfinavir
saquinavir
some
macrolide antibiotics
clarithromycin
telithromycin
chloramphenicol
(
antibiotic
)
some
azole antifungals
ketoconazole
itraconazole
posaconazole
voriconazole
nefazodone
(
antidepressant
)
cobicistat
Moderate
amiodarone
aprepitant
(
antiemetic
)
some
calcium channel blockers
verapamil
diltiazem
some
macrolide antibiotics
erythromycin
some
azole antifungals
fluconazole
miconazole
bergamottin
(constituent of
grapefruit
juice)
cimetidine
ciprofloxacin
cyclosporine
donedarone
fluvoxamine
imatinib
Valerian
verapamil
Weak
buprenorphine
(
analgesic
)
cafestol
(in unfiltered coffee)
cilostazol
fosaprepitant
gabapentin
lomitapide
orphenadrine
ranitidine
ranolazine
tacrolimus
ticagrelor
valproic acid
Unspecified potency
cannabidiol
dithiocarbamate
(functional group)
mifepristone
(
abortifacient
)
norfloxacin
(antibiotic)
some non-nucleoside
reverse transcriptase inhibitors
delavirdine
gestodene
(
hormonal contraceptive
)
mibefradil
(in
angina pectoris
)
star fruit
milk thistle
niacinamide
ginkgo biloba
piperine
isoniazid
quercetin
Strong potency
antiandrogens
enzalutamide
apalutamide
phenytoin
Unspecified potency
anticonvulsants
,
mood stabilizers
carbamazepine
phenytoin
(
anticonvulsant
)
oxcarbazepine
topiramate
barbiturates
phenobarbital
Butalbital
St. John's wort
some
bactericidals
rifampicin
rifabutin
some non-nucleoside
reverse transcriptase inhibitors
efavirenz
nevirapine
some
hypoglycemics
pioglitazone
troglitazone
glucocorticoids
(
blood glucose
increase,
immunosuppressive
)
modafinil
(
stimulant
)
quercetin
capsaicin