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Drug-Target Interaction

Drug

show drug details
PubChem ID:2554
Structure:
Synonyms:
2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene-2-ca
298-46-4
5-20-08-00247 (Beilstein Handbook Reference)
5-Carbamoyl-5H-dibenz(b,f)azepine
5-Carbamoyl-5H-dibenzo(b,f)azepine
5-Carbamoyl-5H-dibenz[b,f]azepine
5-Carbamoyldibenzo(b,f)azepine
5-Carbamyl-5H-dibenzo(b,f)azepine
5-Carbamyldibenzo(b,f)azepine
5H-Dibenz(b,f)azepine-5-carboxamide
5H-dibenzo[b,f]azepine-5-carboxamide
5H-Dibenz[b,f]azepine-5- carboxamide
5H-Dibenz[b,f]azepine-5-carboxamide
85756-57-6
85756-57-6 (di-hydrate)
AC-10560
AC1L1DXT
AC1Q4ZSU
AC1Q4ZSV
AIDS-055321
AIDS055321
AKOS003235644
Amizepin
Amizepine
Apo-Carbamazepine
Atretol
benzo[b][1]benzazepine-11-carboxamide
BIDD:GT0479
BIM-0050280.0001
Bio-0751
Bipotrol
Biston
BPBio1_000225
BRD-K71799949-001-06-7
BRN 1246090
BSPBio_000203
BSPBio_001929
C 4024
C06868
C15H12N2O
C4024_SIAL
C4024_SIGMA
C8981_SIAL
Calepsin
Carbamazepan
Carbamazepen
Carbamazepin
Carbamazepina
Carbamazepina [INN-Spanish]
Carbamazepine
Carbamazepine (JP15/USP/INN)
Carbamazepine (JP16/USP/INN)
carbamazepine (Tegretol)
Carbamazepine [USAN:BAN:INN:JAN]
Carbamazepine [USAN:INN:BAN:JAN]
CARBAMAZEPINE, U.S.P.
Carbamazepine-Supplied by Selleck Chemicals
Carbamazepinum
Carbamazepinum [INN-Latin]
Carbamezepine
CARBATROL
Carbatrol extended-release
Carbazepin
Carbazepine
Carbelan
CAS-298-46-4
CBChromo1_000350
CCG-38931
CDS1_002710
CHEBI:3387
CHEMBL108
ChemDiv1_018966
CPD001227191
D00252
DB00564
dibenzo[b,f]azepine-5-carboxamide
DivK1c_000388
DivK1c_003750
EINECS 206-062-7
Epitol
Epitol, Equetro, Tegretol, Biston, Calepsin, Carbamazepine
Equetro
Equetro (TN)
EU-0100292
Finlepsin
G 32883
G-32883
Geigy 32883
HMS1568K05
HMS1920I17
HMS2090M07
HMS2091O19
HMS2095K05
HMS2233G16
HMS3259B21
HMS3260L06
HMS501D10
HMS640O02
HSDB 3019
I06-0863
IDI1_000388
Karbamazepin
KBio1_000388
KBio2_000516
KBio2_003084
KBio2_005652
KBio3_001149
KBioGR_000724
KBioSS_000516
Lexin
Lopac-C-4024
Lopac0_000292
LS-60362
MLS000069652
MLS001055475
MLS001074172
NCGC00015234-01
NCGC00015234-02
NCGC00015234-03
NCGC00015234-04
NCGC00015234-05
NCGC00015234-06
NCGC00015234-07
NCGC00015234-08
NCGC00015234-09
NCGC00015234-10
NCGC00015234-11
NCGC00015234-12
NCGC00015234-13
NCGC00015234-14
NCGC00015234-15
NCGC00015234-16
NCGC00023877-03
NCGC00023877-04
NCGC00023877-05
NCGC00023877-06
NCGC00023877-07
NCGC00023877-08
nchem.859-comp7
Neurotol
Neurotop retard
NINDS_000388
Novo-Carbamaz
NSC 169864
NSC169864
Nu-Carbamazepine
Oprea1_790775
Prestwick0_000052
Prestwick1_000052
Prestwick2_000052
Prestwick3_000052
Prestwick_104
S1693_Selleck
SAM002264603
Sirtal
SMR000058201
SMR001227191
SPBio_000170
SPBio_002124
SPD-417
SPECTRUM1500159
Spectrum2_000125
Spectrum3_000325
Spectrum4_000262
Spectrum5_000936
Spectrum_000096
ST075773
Stazepin
Stazepine
STK177357
Taro-Carbamazepine
Taro-Carbamazepine Cr
Tegretal
Tegretol
Tegretol (TN)
Tegretol Chewtabs
Tegretol CR
TEGRETOL-XR
Telesmin
Teril
Timonil
Trimonil
UNII-33CM23913M
WLN: T C676 BNJ BVZ
ZINC00004785
ATC-Codes:
Side-Effects:
Side-EffectFrequency
dizziness0.14500001
rash0.13
infection0.12
somnolence0.11125
pain0.10666666
nausea0.09777778
ataxia0.087500006
headache0.08571429
dyspepsia0.083333336
amnesia0.08
asthenia0.07666667
manic depressive reaction0.07
anxiety0.07
dry mouth0.06333333
chest pain0.05666667
vomiting0.055714287
back pain0.05
diarrhea0.047142856
amblyopia0.046666667
pruritus0.0236
constipation0.016666668
vasculitis0.0010
macrocytic anemia0.0010
pancreatitis0.0010
abnormal liver function tests0.0010
interstitial nephritis0.0010
collapse0.0010
folic acid deficiency0.0010
pure red cell aplasia0.0010
neurodermatitis0.0010
cramp0.0010
psychosis0.0010
hallucinations0.0010
lymphoma0.0010
angioedema0.0010
megaloblastic anemia0.0010
hemolytic anemia0.0010
anaphylactic reaction0.0010
muscle pain0.0010
dyskinesia0.0010
acne0.0010
bradycardia0.0010
restlessness0.00075
loss of appetite0.00075
arrhythmias0.0006
leucocytosis0.0006
stomatitis0.0006
pneumonia0.0006
renal failure0.0006
aseptic meningitis0.0006
jaundice0.0006
aplastic anemia0.0006
agranulocytosis0.0006
arthralgia0.0006
leucopenia0.0006
hypotension0.0006
acute intermittent porphyria0.0006
eosinophilia0.0006
confusion0.0006
coronary artery disease0.0006
conjunctivitis0.0006
glossitis0.0006
dyspnea0.0006
purpura0.0006
toxic epidermal necrolysis0.0006
congestive heart failure0.0006
hepatitis0.0006
abdominal pain0.0006
thrombophlebitis0.0006
hypertension0.0006
hypersensitivity0.0006
diaphoresis0.0005
thrombocytopenia0.0005
erythema multiforme0.0005
photosensitivity0.0005
alopecia0.0005
systemic lupus erythematosus0.00042
lymphadenopathy0.00042
fever0.00042
paralysis0.0
chills0.0
fatigue0.0
av block0.0
albuminuria0.0
edema0.0
diplopia0.0
azotemia0.0
urinary frequency0.0
exfoliative dermatitis0.0
arterial insufficiency0.0
testicular atrophy0.0
elevated blood pressure0.0
blurred vision0.0
urinary retention0.0
glycosuria0.0
pancytopenia0.0
nystagmus0.0
peripheral neuritis0.0
hyperacusis0.0
myocardial infarction0.0
meningitis0.0
paresthesias0.0
stevens - johnson syndrome0.0
leg cramps0.0
hirsutism0.0
urticaria0.0
tinnitus0.0
hyponatremia0.0
impotence0.0
syncope and collapse0.0
coma0
rhinitis0
galactorrhea0
erythema nodosum0
dysarthria0
peripheral edema0
convulsions0
gynecomastia0
hypothermia0
cardiac arrest0
erythema0
tachycardia0
memory impairment0
visual hallucinations0
depersonalization0
metabolic acidosis0
suicide attempt0
retinopathy0
hearing loss0
insomnia0
osteomalacia0
status epilepticus0
nervousness0
heart failure0
flushing0
hypokalemia0
forgetful0
hepatic failure0
anemia0
muscle weakness0
urinary tract infection0
splenomegaly0
ear pain0
sinusitis0
alkaline phosphatase increased0
hyperglycemia0
hematuria0
weight gain0
allergic reaction0
tremor0
bronchitis0
pulmonary edema0
choreoathetosis0
vertigo0
pharyngitis0
porphyria0

Target

show target details
Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----
----
----

References:

10096433
11760814
7974626
Fluvoxamine inhibition and carbamazepine induction of the metabolism of clozapine: evidence from a therapeutic drug monitoring service.. M Jerling; L Lindstr÷m; U Bondesson; L Bertilsson (1994) Therapeutic drug monitoring display abstract
Therapeutic drug monitoring data for clozapine were used to study interactions with other drugs. The distribution of the ratio concentration/dose (C/D) of clozapine was compared in four matched groups--patients simultaneously treated with benzodiazepines, patients on drugs that inhibit the cytochrome P450 enzyme CYP2D6, patients taking carbamazepine, and those not taking any of these drugs. No difference was seen among the monotherapy, CYP2D6, and benzodiazepine groups. Patients on carbamazepine had a mean 50% lower C/D than the monotherapy group (p < 0.001), indicating that carbamazepine is an inducer of the metabolism of clozapine. The C/D was inversely correlated to the daily dose of carbamazepine. Intraindividual comparisons in eight patients, with analyses both on and off carbamazepine, confirmed a substantial decrease of the clozapine concentration when carbamazepine was introduced. Four patients treated with clozapine were concomitantly given the antidepressant fluvoxamine. Three of them exhibited a much higher C/D ratio when on fluvoxamine compared with the monotherapy group. Two had their clozapine levels analyzed when on and off fluvoxamine. The dose-normalized clozapine concentration increased by a factor of 5-10 when fluvoxamine was added. We conclude that carbamazepine causes decreased clozapine plasma levels, while fluvoxamine increases the levels. The pathways are not known with certainty, but CYP1A2 may be of major importance for the metabolism of clozapine, since fluvoxamine is a potent inhibitor of this enzyme. A recent panel study suggests that determination of CYP1A2 activity with the caffeine test may be very useful for the dosing of clozapine. The induction of clozapine metabolism by carbamazepine might be partly mediated by CYP3A4.
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