Abstract
The pharmacokinetic and pharmacodynamic characteristics of a controlled-release (CR) formulation of trazodone were evaluated in healthy subjects who received acutely 150 mg and 75 mg of the CR trazodone and equal amounts of the conventional formulation on separate occasions. Plasma trazodone concentrations were measured by HPLC. The pharmacokinetic profile of CR trazodone was characterized by a slower increase in drug plasma levels and a lower and retarded peak plasma concentration without any modification in the total amount of trazodone absorbed over 24 hrs. The side effects were less severe and less frequent than with the conventional formulation.
Sommario
Le caratteristiche farmacocinetiche e farmacodinamiche di una formulazione di trazodone a rilascio controllato (CR) sono state studiate in volontari sani ai quali furono somministrati, in quattro differenti occasioni, 150 mg e 75 mg di trazodone CR e dosi equivalenti di trazodone in formulazione convenzionale. Le concentrazioni plasmatiche di trazodone furono misurate mediante HPLC. Rispetto alla formulazione convenzionale, il trazodone CR esibì un profilo farmacocinetico caratterizzato da un incremento più graduale dei livelli plasmatici e da una concentrazione massima più bassa e più ritar-data. Nessuna differenza nella quantità totale di farmaco assorbita nelle 24 ore fu osservata tra le due formulazioni. Dopo somministrazione del trazodone CR, gli effetti collaterali indesiderati furono meno severi e meno frequenti rispetto alla formulazione convenzionale.
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Monteleone, P., Delrio, G. Pharmacokinetic and pharmacodynamic characteristics of a controlled-release formulation of trazodone versus the conventional formulation in healthy volunteers. Ital J Neuro Sci 14, 443–449 (1993). https://doi.org/10.1007/BF02339174
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DOI: https://doi.org/10.1007/BF02339174