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Drug-Target Interaction

Drug

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PubChem ID:2448
Structure:
Synonyms:
1-Butanone, 4-(4-(4-bromophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-
1-Butanone, 4-[4-(4-bromophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-
10457-90-6
4-(4-(4-Bromophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
4-(4-(4-Bromophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
4-(4-(p-Bromophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
4-(4-(p-Bromophenyl)-4-hydroxypiperidinol)-4'-fluorobutyrophenone
4-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-on
4-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
5-21-02-00382 (Beilstein Handbook Reference)
BPBio1_000481
BRN 1552256
Bromperidol
Bromperidol (JAN/USAN/INN)
Bromperidol [USAN:BAN:INN:JAN]
Bromperidolum [INN-Latin]
BSPBio_000437
BUTYROPHENONE, 4-(4-(p-BROMOPHENYL)-4-HYDROXYPIPERIDINO)-4'-FLUORO-
C21H23BrFNO2
CAS-10457-90-6
CC 2489
D01101
EINECS 233-943-3
Impromen
Impromen (TN)
LS-48293
MLS002153852
NCGC00016692-01
NCGC00179558-01
PDSP1_001125
PDSP2_001109
Prestwick0_000509
Prestwick1_000509
Prestwick2_000509
Prestwick3_000509
Prestwick_781
R 11333
SMR001233211
SPBio_002358
ATC-Codes:

Target

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Uniprot ID:CP3A4_HUMAN
Synonyms:
Albendazole monooxygenase
Albendazole sulfoxidase
CYPIIIA3
CYPIIIA4
Cytochrome P450 3A3
Cytochrome P450 3A4
HLp
NF-25
Nifedipine oxidase
P450-PCN1
Quinine 3-monooxygenase
Taurochenodeoxycholate 6-alpha-hydroxylase
EC-Numbers:1.14.13.32
1.14.13.67
1.14.13.97
Organism:Homo sapiens
Human
PDB IDs:1TQN 1W0E 1W0F 1W0G 2J0D 2V0M
Structure:
2V0M

Binding Affinities:

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

References:

10463320
Effects of itraconazole on the steady-state plasma concentrations of bromperidol and reduced bromperidol in schizophrenic patients.. H Furukori; T Kondo; N Yasui; K Otani; N Tokinaga; U Nagashima; S Kaneko; Y Inoue (1999) Psychopharmacology display abstract
RATIONALE: A previously reported pharmacokinetic interaction between bromperidol and carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, suggests possible involvement of CYP3A4 in the metabolism of bromperidol. OBJECTIVE: We investigated pharmacokinetic interaction between bromperidol and itraconazole, a potent inhibitor of CYP3A4, to clarify the involvement of CYP3A4 in the metabolism of bromperidol and its reduced metabolite. METHODS: Itraconazole 200 mg/day for 7 days was coadministered to eight schizophrenic patients treated with a fixed dose of bromperidol 12 or 24 mg/day for at least 2 weeks. Blood samples were taken before and 1 week after itraconazole coadministration and 1 week after its discontinuation, together with clinical assessments using the Brief Psychiatric Rating Scale (BPRS) and the Udvalg for Kliniske Undersøgelser (UKU) Side Effect Rating Scale. RESULTS: Plasma concentrations of bromperidol during itraconazole coadministration (16.7+/-4.9 ng/ml) were significantly higher (P
10463320
Effects of itraconazole on the steady-state plasma concentrations of bromperidol and reduced bromperidol in schizophrenic patients.. H Furukori; T Kondo; N Yasui; K Otani; N Tokinaga; U Nagashima; S Kaneko; Y Inoue (1999) Psychopharmacology display abstract
RATIONALE: A previously reported pharmacokinetic interaction between bromperidol and carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, suggests possible involvement of CYP3A4 in the metabolism of bromperidol. OBJECTIVE: We investigated pharmacokinetic interaction between bromperidol and itraconazole, a potent inhibitor of CYP3A4, to clarify the involvement of CYP3A4 in the metabolism of bromperidol and its reduced metabolite. METHODS: Itraconazole 200 mg/day for 7 days was coadministered to eight schizophrenic patients treated with a fixed dose of bromperidol 12 or 24 mg/day for at least 2 weeks. Blood samples were taken before and 1 week after itraconazole coadministration and 1 week after its discontinuation, together with clinical assessments using the Brief Psychiatric Rating Scale (BPRS) and the Udvalg for Kliniske Undersøgelser (UKU) Side Effect Rating Scale. RESULTS: Plasma concentrations of bromperidol during itraconazole coadministration (16.7+/-4.9 ng/ml) were significantly higher (P
10752674
11133003
9592806
Involvement of cytochromeP4503A4 in the metabolism of haloperidol and bromperidol. H Furukori (1998) Nihon shinkei seishin yakurigaku zasshi display abstract
To clarify the involvement of cytochromeP450 (CYP) 3A4 in the metabolism of haloperidol and bromperidol in humans, the effects of itraconazole, a potent inhibitor of CYP3A4, on steady-state plasma concentrations of both drugs and their reduced metabolites were investigated using 21 schizophrenic patients. Patients treated with haloperidol 12 or 24 mg/day (n = 13) or bromperidol 12 or 24 mg/day (n = 8) for at least 2 weeks were then given itraconazole 200 mg/day for 7 days. Blood samplings were performed before administration, 1 week during itraconazole coadministration and 1 week after its discontinuation together with clinical assessments. Plasma concentrations of haloperidol and bromperidol and their reduced metabolites were significantly higher during itraconazole treatment (P < 0.01). Deterioration in the neurological side effects of haloperidol was observed during itraconazole coadministration. Thus, this study suggests that itraconazole inhibits the metabolism of haloperidol and bromperidol, and that CYP3A4 is involved in the metabolism of both drugs.
9592806
Involvement of cytochromeP4503A4 in the metabolism of haloperidol and bromperidol. H Furukori (1998) Nihon shinkei seishin yakurigaku zasshi display abstract
To clarify the involvement of cytochromeP450 (CYP) 3A4 in the metabolism of haloperidol and bromperidol in humans, the effects of itraconazole, a potent inhibitor of CYP3A4, on steady-state plasma concentrations of both drugs and their reduced metabolites were investigated using 21 schizophrenic patients. Patients treated with haloperidol 12 or 24 mg/day (n = 13) or bromperidol 12 or 24 mg/day (n = 8) for at least 2 weeks were then given itraconazole 200 mg/day for 7 days. Blood samplings were performed before administration, 1 week during itraconazole coadministration and 1 week after its discontinuation together with clinical assessments. Plasma concentrations of haloperidol and bromperidol and their reduced metabolites were significantly higher during itraconazole treatment (P < 0.01). Deterioration in the neurological side effects of haloperidol was observed during itraconazole coadministration. Thus, this study suggests that itraconazole inhibits the metabolism of haloperidol and bromperidol, and that CYP3A4 is involved in the metabolism of both drugs.