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Titolo:
Pharmacokinetics of selective serotonin reuptake inhibitors
Autore:
Hiemke, C; Hartter, S;
Indirizzi:
Univ Mainz, Dept Psychiat, D-55101 Mainz, Germany Univ Mainz Mainz Germany D-55101 , Dept Psychiat, D-55101 Mainz, Germany
Titolo Testata:
PHARMACOLOGY & THERAPEUTICS
fascicolo: 1, volume: 85, anno: 2000,
pagine: 11 - 28
SICI:
0163-7258(200001)85:1<11:POSSRI>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN LIVER-MICROSOMES; OBSESSIVE-COMPULSIVE DISORDER; ANTIDEPRESSANT PLASMA-LEVELS; SPARTEINE OXIDATION POLYMORPHISM; IMPROVES NEGATIVE SYMPTOMS; IN-VITRO; DRUG-INTERACTIONS; DOUBLE-BLIND; THERAPEUTIC EFFICACY; FLUVOXAMINE MALEATE;
Keywords:
fluoxetine; fluvoxamine; paroxetine; citalopram; sertraline; drug-drug interactions;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
204
Recensione:
Indirizzi per estratti:
Indirizzo: Hiemke, C Univ Mainz, Dept Psychiat, Untere Zahlbacher Str 8, D-55101 Mainz, Germany Univ Mainz Untere Zahlbacher Str 8 Mainz Germany D-55101 ermany
Citazione:
C. Hiemke e S. Hartter, "Pharmacokinetics of selective serotonin reuptake inhibitors", PHARM THERA, 85(1), 2000, pp. 11-28

Abstract

The five selective serotonin reuptake inhibitors (SSRIs), fluoxetine, fluvoxamine, paroxetine, sertraline, and citalopram, have similar antidepressant efficacy and a similar side effect profile. They differ, however, in their pharmacokinetic properties. Under steady-state concentrations, their half-lives range between 1 and 4 days for fluoxetine (7 and 15 days for norfluoxetine) and between 21 (paroxetine) and 36 (citalopram) hr for the other SSRIs. Sertraline and citalopram show linear and fluoxetine, fluvoxamine, andparoxetine nonlinear pharmacokinetics. SSRIs underlie an extensive metabolism with high interindividual variability, whereby cytochrome P450 (CYP) isoenzymes play a major role. Therefore, resulting blood concentrations are highly variable between individuals. Except for N-demethylated fluoxetine, metabolites of SSRIs do not contribute to clinical actions. Therapeutically effective blood concentrations are unclear so far, although there is evidence for minimal effective and upper-threshold concentrations that should notbe exceeded. Paroxetine and, to a lesser degree, fluoxetine and norflouxetine are potent inhibitors of CYP2D6 and fluvoxamine of CYP1A2 and CYP2C19. This can give rise to drug-drug interactions that may have no effect, lead to intoxication, or improve the therapeutic response. These different pharmacokinetic properties of the five SSRIs, especially their drug-drug interaction potential, should be considered when selecting a distinct SSRI for treatment of depression or other disorders with a suggested dysfunction of theserotonergic system in the brain. (C) 1999 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 18:43:19