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Titolo:
Serotonergic and noradrenergic reuptake inhibitors: Prediction of clinicaleffects from in vitro potencies
Autore:
Frazer, A;
Indirizzi:
Univ Texas, Hlth Sci Ctr, Dept Pharmacol, San Antonio, TX 78229 USA Univ Texas San Antonio TX USA 78229 Pharmacol, San Antonio, TX 78229 USA Audie L Murphy Mem Vet Hosp, S Texas Vet Hlth Care Syst, San Antonio, TX 78284 USA Audie L Murphy Mem Vet Hosp San Antonio TX USA 78284 ntonio, TX 78284 USA
Titolo Testata:
JOURNAL OF CLINICAL PSYCHIATRY
, volume: 62, anno: 2001, supplemento:, 12
pagine: 16 - 23
SICI:
0160-6689(2001)62:<16:SANRIP>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN SYNAPTOSOMES; CEREBROSPINAL-FLUID; DEPRESSED-PATIENTS; DORSAL RAPHE; QUANTITATIVE AUTORADIOGRAPHY; 5-HYDROXYTRYPTAMINE RELEASE; ANTAGONIST MIRTAZAPINE; LOCUS-COERULEUS; PLASMA-LEVELS; UPTAKE SITES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Social & Behavioral Sciences
Clinical Medicine
Citazioni:
53
Recensione:
Indirizzi per estratti:
Indirizzo: Frazer, A Univ Texas, Hlth Sci Ctr, Dept Pharmacol, 7703 Floyd Curl Dr,Mail Code 7764, San Antonio, TX 78229 USA Univ Texas 7703 Floyd Curl Dr,Mail Code 7764 San Antonio TX USA 78229
Citazione:
A. Frazer, "Serotonergic and noradrenergic reuptake inhibitors: Prediction of clinicaleffects from in vitro potencies", J CLIN PSY, 62, 2001, pp. 16-23

Abstract

This article reviews the pharmacology of antidepressants, particularly focusing on those that act acutely by blocking the reuptake of norepinephrine (NE) and/or serotonin (5-HT). Such drugs have a very wide range of potencies, measured in vitro, to inhibit the reuptake of these biogenic amines. As a group, the selective serotonin reuptake inhibitors (SSRIs) are the most potent at inhibiting the reuptake of 5-HT Some tricyclic antidepressants (TCAs), such as desipramine and nortriptyline, are much more potent at blocking NE reuptake than 5-HT reuptake, as is the new non-TCA drug reboxetine. Among SSRIs, paroxetine is most potent at blocking the reuptake of NE. When considering whether such potencies measured in vitro translate into pharmacologic effects clinically, it is necessary to know how much drug gets to itssite of therapeutic action, presumably the brain. Most, but not all, antidepressants are extensively bound to plasma proteins, and this binding limits considerably the penetration of these drugs across the blood-brain barrier. The amount of drug present in the extracellular fluid (ECF) of brain approximates the non-protein-bound drug concentration in plasma. Comparison ofthe concentration of antidepressants in ECF with their potencies to inhibit the reuptake of 5-HT and/or NE reveals why some drugs block the reuptake of these biogenic amines in either a selective or nonselective manner. Thisanalysis reveals that venlafaxine may be unique among antidepressants in having a dose-dependent nonselectivity; at low doses it acts primarily as anSSRI, but at higher doses it inhibits the reuptake of NE as well.

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Documento generato il 25/01/20 alle ore 09:25:00