P450 药物相互作用表P450 Drug Interaction Table
http://medicine.iupui.edu/clinpharm/DDIs/table.aspx
SUBSTRATES
1A2
2B6
2C8
2C9
2C19
2D6
2E1
3A4,5,7
amitriptyline
caffeine2
clomipramine
clozapine
cyclobenzaprine
estradiol
fluvoxamine
haloperidol
imipramine N-DeMe
mexileti...
P450 Drug Interaction Table
http://medicine.iupui.edu/clinpharm/DDIs/table.aspx
SUBSTRATES
1A2
2B6
2C8
2C9
2C19
2D6
2E1
3A4,5,7
amitriptyline
caffeine2
clomipramine
clozapine
cyclobenzaprine
estradiol
fluvoxamine
haloperidol
imipramine N-DeMe
mexiletine
naproxen
olanzapine
ondansetron
phenacetin1→
acetaminophen→NAPQI
propranolol
riluzole
ropivacaine
tacrine2
theophylline2
tizanidine
verapamil
(R)warfarin
zileuton
zolmitriptan
bupropion1
cyclophosphamide
efavirenz1
ifosphamide
methadone
sorafenib
amodiaquine2
cerivastatin
paclitaxel
repaglinide
sorafenib
torsemide
NSAIDs:
diclofenac1
ibuprofen
lornoxicam
meloxicam
S-naproxen→Nor
piroxicam
suprofen
Oral Hypoglycemic Agents:
tolbutamide1
glipizide
Angiotensin II Blockers:
losartan
irbesartan
Sulfonylureas:
glyburide
glibenclamide
glipizide
glimepiride
tolbutamide
amitriptyline
celecoxib
fluoxetine
fluvastatin
glyburide
nateglinide
phenytoin-4-OH2
rosiglitazone
tamoxifen
torsemide
S-warfarin1
PPIs:
lansoprazole
omeprazole2
pantoprazole
rabeprazole
Anti-epileptics:
diazepam→Nor
phenytoin(O)
S-mephenytoin1
phenobarbitone
amitriptyline
carisoprodol
citalopram
chloramphenicol
clomipramine
clopidogrel
cyclophosphamide
hexobarbital
imipramine N-DeME
indomethacin
R-mephobarbital
moclobemide
nelfinavir
nilutamide
primidone
progesterone
proguanil
propranolol
teniposide
R-warfarin→8-OH
tamoxifen:
TAMOXIFEN GUIDE
Beta Blockers:
carvedilol
S-metoprolol
propafenone
timolol
Antidepressants:
amitriptyline
clomipramine
desipramine
fluoxetine
imipramine
paroxetine
venlafaxine
Antipsychotics:
haloperidol
perphenazine
risperidone→9-OH
thioridazine
zuclopenthixol
alprenolol
amphetamine
aripiprazole
atomoxetine
bufuralol1
chlorpheniramine
chlorpromazine
clonidine
codeine (→O-desMe)
debrisoquine2
dexfenfluramine
dextromethorphan1
donepezil
duloxetine
encainide
flecainide
fluvoxamine
lidocaine
metoclopramide
methoxyamphetamine
mexiletine
minaprine
nebivolol
nortriptyline
ondansetron
oxycodone
perhexiline
phenacetin
phenformin
promethazine
propranolol
sparteine
tramadol
Anesthetics:
enflurane
halothane
isoflurane
methoxyflurane
sevoflurane
acetaminophen→NAPQI
aniline2
benzene
chlorzoxazone1
ethanol
N,N-dimethylformamide
theophylline→8-OH
Macrolide antibiotics:
clarithromycin
erythromycin2 (not 3A5)
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine→3-OH (not 3A5)
Benzodiazepines:
alprazolam
diazepam→3OH
midazolam1
triazolam2
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Antivirals:
indinavir
nelfinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
terfenadine2
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
lercanidipine
nifedipine2
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
NOT rosuvastatin
simvastatin
Steroid 6beta-OH:
estradiol
hydrocortisone
progesterone
testosterone1
Miscellaneous:
alfentanil
aprepitant
aripiprazole
boceprevir
buspirone
cafergot
caffeine→TMU
cilostazol
cocaine
codeine-N-demethylation
dapsone
dexamethasone
dextromethorphan2
docetaxel
domperidone
eplerenone
fentanyl
finasteride
gleevec
haloperidol
irinotecan
LAAM
lidocaine
methadone
nateglinide
ondansetron
pimozide
propranolol
quetiapine
quinine
risperidone
salmeterol
sildenafil
sirolimus
sorafenib
sunitinib
tamoxifen
taxol
telaprevir
terfenadine
torisel
trazodone
vincristine
zaleplon
ziprasidone
zolpidem
INHIBITORS
Inhibitors compete with other drugs for a particular enzyme thus affecting the optimal level of metabolism of the substrate drug which in many cases affect the individual's response to that particular medication, e.g. making it ineffective.
A Strong inhibitor is one that causes a > 5-fold increase in the plasma AUC values or more than 80% decrease in clearance.
A Moderate inhibitor is one that causes a > 2-fold increase in the plasma AUC values or 50-80% decrease in clearance.
A Weak inhibitor is one that causes a > 1.25-fold but < 2-fold increase in the plasma AUC values or 20-50% decrease in clearance.
All other inhibitors.
FDA preferred1 and acceptable2 inhibitors for in vitro experiments.*
1A2
2B6
2C8
2C9
2C19
2D6
2E1
3A4,5,7
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/1A2references.aspx" \l "fluvoxamineInh" fluvoxamine
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/1A2references.aspx" \l "ciprofloxacinInh" ciprofloxacin
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/1A2references.aspx" \l "cimetidineInh" cimetidine
amiodarone
fluoroquinolones
furafylline1
interferon
methoxsalen
mibefradil
ticlopidine
thiotepa
ticlopidine2
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2C8references.aspx" \l "gemfibrozilInh" gemfibrozil2
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2C8references.aspx" \l "trimethoprimInh" trimethoprim2
glitazones
montelukast1
quercetin1
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2C9references.aspx" \l "fluconazoleInh" fluconazole2
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2C9references.aspx" \l "amiodaroneInh" amiodarone
fenofibrate
fluvastatin
fluvoxamine2
isoniazid
lovastatin
phenylbutazone
probenicid
sertraline
sulfamethoxazole
sulfaphenazole1
teniposide
voriconazole
zafirlukast
PPIs:
lansoprazole
omeprazole2
pantoprazole
rabeprazole
chloramphenicol
cimetidine
felbamate
fluoxetine
fluvoxamine
indomethacin
ketoconazole
modafinil
oxcarbazepine
probenicid
ticlopidine2
topiramate
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "bupropionInh" bupropion
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "cinacalcetInh" cinacalcet
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "fluoxetineInh" fluoxetine
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "paroxetineInh" paroxetine
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "quinidineInh" quinidine1
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "duloxetineInh" duloxetine
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "sertralineInh" sertraline
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "terbinafineInh" terbinafine
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "amiodaroneInh" amiodarone
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/2D6references.aspx" \l "cimetidineInh" cimetidine
celecoxib
chlorpheniramine
chlorpromazine
citalopram
clemastine
clomipramine
cocaine
diphenhydramine
doxepin
doxorubicin
escitalopram
halofantrine
histamine H1 receptor antagonists
hydroxyzine
levomepromazine
methadone
metoclopramide
mibefradil
midodrine
moclobemide
perphenazine
ranitidine
reduced-haloperidol
ritonavir
ticlopidine
tripelennamine
diethyl-dithiocarbamate2
disulfiram
HIV Antivirals:
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "indinavirInh" indinavir
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "nelfinavirInh" nelfinavir
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "ritonavirInh" ritonavir
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "clarithromycinInh" clarithromycin
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "itraconazoleInh" itraconazole1
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "ketoconazoleInh" ketoconazole1
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "nefazodoneInh" nefazodone
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "saquinavirInh" saquinavir
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "telithromycinInh" telithromycin
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "aprepitantInh" aprepitant
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "erythromycinInh" erythromycin
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "fluconazoleInh" fluconazole
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "grapefruitInh" grapefruit juice
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "verapamilInh" verapamil2
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "diltiazemInh" diltiazem
HYPERLINK "http://medicine.iupui.edu/clinpharm/DDIs/3A457references.aspx" \l "cimetidineInh" cimetidine
amiodarone
NOT azithromycin
chloramphenicol
boceprevir
ciprofloxacin
delaviridine
diethyl-dithiocarbamate
fluvoxamine
gestodene
imatinib
mibefradil
mifepristone
norfloxacin
norfluoxetine
starfruit
telaprevir voriconazole
INDUCERS
1A2
2B6
2C8
2C9
2C19
2D6
2E1
3A4,5,7
broccoli
brussel sprouts
char-grilled meat
insulin
methylcholanthrene1
modafinil
nafcillin
beta-naphthoflavone1
omeprazole1
tobacco
phenobarbital
phenytoin
rifampin
rifampin1
rifampin
secobarbital
carbamazepine
norethindrone
NOT pentobarbital
prednisone
rifampicin1
dexamethasone
rifampin
ethanol
isoniazid
HIV Antivirals:
efavirenz
nevirapine
barbiturates
carbamazepine
glucocorticoids
modafinil
oxcarbazepine
phenobarbital2
phenytoin2
pioglitazone
rifabutin
rifampin1
St. John's wort
troglitazone1
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