Estimation of brain receptor occupancy for trazodone immediate release and once a day formulations.

ABSTRACT: Trazodone is approved for the treatment of major depressive disorders, marketed as immediate release (IR), prolonged release, and once a day (OAD) formulation. The different formulations allow different administration schedules and may be useful to facilitate patients' compliance to the antidepressant treatment. A previously verified physiologically-based pharmacokinetic model based on in vitro and in vivo information on trazodone pharmacokinetics was applied, aiming at predicting brain receptor occupancy (RO) after single and repeated dosing of the IR formulation and repeated dosing of the OAD formulation in healthy subjects. Receptors included in the simulations were selected using static calculations of RO based on the maximum unbound brain concentration (C_max,brain,u ) of tr

SUBMITTER: Oggianu L 

PROVIDER: S-EPMC9200067 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature