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Titolo:
Differential effects of fluvoxamine and other antidepressants on the biotransformation of melatonin
Autore:
Hartter, S; Wang, XM; Weigmann, H; Friedberg, T; Arand, M; Oesch, F; Hiemke, C;
Indirizzi:
Univ Mainz, Dept Psychiat, D-55131 Mainz, Germany Univ Mainz Mainz Germany D-55131 , Dept Psychiat, D-55131 Mainz, Germany Univ Mainz, Dept Toxicol, D-55131 Mainz, Germany Univ Mainz Mainz Germany D-55131 z, Dept Toxicol, D-55131 Mainz, Germany Tongji Med Univ, Wuhan, Peoples R China Tongji Med Univ Wuhan Peoples R China Med Univ, Wuhan, Peoples R China Univ Dundee, Ninewells Hosp & Med Sch, Biomed Res Ctr, Dundee DD1 9SY, Scotland Univ Dundee Dundee Scotland DD1 9SY ed Res Ctr, Dundee DD1 9SY, Scotland
Titolo Testata:
JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY
fascicolo: 2, volume: 21, anno: 2001,
pagine: 167 - 174
SICI:
0271-0749(200104)21:2<167:DEOFAO>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN LIVER-MICROSOMES; CLINICAL IMPLICATIONS; PLASMA MELATONIN; METABOLISM; SECRETION; PHARMACOKINETICS; BIOAVAILABILITY; INHIBITION; OXIDATION; BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Hiemke, C Univ Mainz, Dept Psychiat, Untere Zahlbachertr 8, D-55131 Mainz,Germany Univ Mainz Untere Zahlbachertr 8 Mainz Germany D-55131 Germany
Citazione:
S. Hartter et al., "Differential effects of fluvoxamine and other antidepressants on the biotransformation of melatonin", J CL PSYCH, 21(2), 2001, pp. 167-174

Abstract

Melatonin, the predominant product of the pineal gland, is involved in themaintenance of diurnal rhythms. Nocturnal blood concentrations of melatonin have been shown to be enhanced by fluvoxamine, but not by other serotoninreuptake inhibitors. Because fluvoxamine is an inhibitor of several cytochrome P450 (CYP) enzymes, the authors studied the biotransformation of melatonin and the effects of fluvoxamine on the metabolism of melatonin in vitrousing human liver microsomes and recombinant human CW isoenzymes. Melatonin was found to be almost exclusively metabolized by CYP1A2 to 6-hydroxymelatonin and N-acetylserotonin with a minimal contribution of CYP2C19. Both reactions were potently inhibited by fluvoxamine, with a K-i of 0.02 muM for the formation of 6-hydroxymelatonin and 0.05 muM for the formation of N-acetylserotonin. Other than fluvoxamine, fluoxetine, paroxetine, citalopram, imipramine, and desipramine were also tested at 2 and 20 muM. Among the other antidepressants, only paroxetine was able to affect the metabolism of melatonin at supratherapeutic concentrations of 20 muM, which did not reach byfar the magnitude of the inhibitory potency of fluvoxamine. The authors concluded that fluvoxamine is a potent inhibitor of melatonin degradation. Because this inhibitory action is also found in vivo, fluvoxamine might be used as an enhancer of melatonin, which might offer new therapeutic possibilities of fluvoxamine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 06:19:41