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Titolo:
Effects of itraconazole on the steady-state plasma concentrations of bromperidol and reduced bromperidol in schizophrenic patients
Autore:
Furukori, H; Kondo, T; Yasui, N; Otani, K; Tokinaga, N; Nagashima, U; Kaneko, S; Inoue, Y;
Indirizzi:
Hirosaki Univ, Sch Med, Dept Neuropsychiat, Hirosaki, Aomori 0368652, Japan Hirosaki Univ Hirosaki Aomori Japan 0368652 rosaki, Aomori 0368652, Japan Yamagata Univ, Sch Med, Dept Neuropsychiat, Yamagata 99023, Japan YamagataUniv Yamagata Japan 99023 Neuropsychiat, Yamagata 99023, Japan Yoshitomi Pharmaceut Ind Ltd, Pharmaceut Technol Ctr, Fukuoka, Japan Yoshitomi Pharmaceut Ind Ltd Fukuoka Japan Technol Ctr, Fukuoka, Japan
Titolo Testata:
PSYCHOPHARMACOLOGY
fascicolo: 2, volume: 145, anno: 1999,
pagine: 189 - 192
Fonte:
ISI
Lingua:
ENG
Soggetto:
DEBRISOQUINE HYDROXYLATION PHENOTYPE; SYSTEMIC ANTIMYCOTICS KETOCONAZOLE; PHARMACOKINETIC DRUG-INTERACTIONS; HALOPERIDOL DISPOSITION; CYP2D6 GENOTYPE; HUMAN LIVER; IN-VIVO; METABOLITE; CARBAMAZEPINE; AGENTS;
Keywords:
bromperidol; reduced bromperidol; steady-state plasma concentration; itraconazole; cytochrome P450 3A4;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
25
Recensione:
Indirizzi per estratti:
Indirizzo: Kondo, T Hirosaki Univ, Sch Med, Dept Neuropsychiat, Hirosaki, Aomori 0368652, Japan Hirosaki Univ Hirosaki Aomori Japan 0368652 omori 0368652, Japan
Citazione:
H. Furukori et al., "Effects of itraconazole on the steady-state plasma concentrations of bromperidol and reduced bromperidol in schizophrenic patients", PSYCHOPHAR, 145(2), 1999, pp. 189-192

Abstract

Rationale: A previously reported pharmacokinetic interaction between bromperidol and carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, suggestspossible 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 CYP3A4in 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 clinicalassessments using the Brief Psychiatric Rating Scale (BPRS) and the Udvalgfor Kliniske Undersogelser (UKU) Side Effect Rating Scale. Results: Plasmaconcentrations of bromperidol during itraconazole coadministration (16.7+/-4.9 ng/ml) were significantly higher (P<0.01) than before itraconazole coadministration (8.9+/-4.4 ng/ml) and 1 week after its discontinuation (9.9+/-4.3 ng/ml). Plasma concentrations of reduced bromperidol during itraconazole coadministration (3.6+/-2.9 ng/ml) were significantly higher (P<0.01) than before itraconazole coadministration (1.8+/-1.3 ng/ml). No changes were observed in BPRS and UKU scores throughout the study. Conclusions: The pharmacokinetic interaction between bromperidol and itraconazole is probably due to the inhibitory effect of itraconazole on the metabolism of bromperidol. This study provides in vivo evidence of involvement of CYP3A4 in the metabolism of bromperidol and reduced bromperidol.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/20 alle ore 20:57:11