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Titolo:
MILNACIPRAN, A NEW SPECIFIC SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR
Autore:
BOYER P; BRILEY M;
Indirizzi:
INST RECH PIERRE FABRE,PARC IND CHARTREUSE F-81100 CASTRES FRANCE INST RECH PIERRE FABRE F-81100 CASTRES FRANCE INSERM PARIS FRANCE
Titolo Testata:
Medicamentos de actualidad
fascicolo: 8, volume: 34, anno: 1998,
pagine: 709 - 720
SICI:
0025-7656(1998)34:8<709:MANSSA>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
MAJOR DEPRESSION; RAT-BRAIN; TRICYCLIC ANTIDEPRESSANTS; MIDALCIPRAN; F-2207; PSYCHOPHARMACOLOGY; PHARMACOKINETICS; HYDROCHLORIDE; FLUOXETINE; EFFICACY;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
50
Recensione:
Indirizzi per estratti:
Citazione:
P. Boyer e M. Briley, "MILNACIPRAN, A NEW SPECIFIC SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR", Medicamentos de actualidad, 34(8), 1998, pp. 709-720

Abstract

Milnacipran is a new antidepressant which inhibits equipotently the reuptake of serotonin and noradrenaline both in vitro and in vivo with no effect on dopamine reuptake. Microdialysis studies have shown increased extracellular levels of both serotonin and noradrenaline after acute administration. Milnacipran is devoid of interactions at any knownneurotransmitter receptor. In particular, and unlike tricyclic antidepressants (TCAs), it has no activity at noradrenergic, muscarinic or histaminergic receptors. Contrary to TCAs, chronic administration of milnacipran does not modify beta-adrenoceptor binding or second messenger function. Milnacipran is active on various animal models of depression such as the forced swimming test in the mouse, learned helplessnessin the rat and the olfactory bulbectomized rat model. Milnacipran hasa high bioavailability, low plasma protein binding, and is largely eliminated in the urine as the parent drug or as a glucuronide. These features suggest that interactions with other drugs given concurrently are unlikely. Studies in patients with liver dysfunction and in the elderly suggest that dose adjustment is not necessary. In patients with renal impairment, decreased elimination of milnacipran is correlated tothe degree of renal impairment allowing an easy dosage adjustment. Anintermediate half-life of approximately 8 h is compatible with twice-daily administration. Clinical studies comparing milnacipran, placebo and other antidepressants provide evidence of its efficacy in moderateto severe depression in both hospitalized and outpatient settings. Meta-analyses of the original data of controlled trials comparing milnacipran with imipramine or selective serotonin reuptake inhibitors (SSRIs) show that milnacipran provides antidepressant efficacy similar to that of TCAs and significantly superior to that of SSRIs. An analysis of a database of over 3300 patients shows that both the general and cardiovascular tolerability of milnacipran are superior to those of TCAs with notably less cholinergic side effects. The tolerance of milnacipran was comparable to that of SSRIs with a higher incidence of dysuria with milnacipran but a higher frequency of nausea and anxiety with theSSRIs. Milnacipran represents an interesting new therapeutic option in depression, being as well tolerated as the SSRIs but offering clinical efficacy similar to the TCAs. (C) 1998 Prous Science. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 12:18:17