Asunto(s)
Antipsicóticos/administración & dosificación , Antipsicóticos/farmacocinética , Interacciones Alimento-Droga , Piperidinas/administración & dosificación , Piperidinas/farmacocinética , Agonistas del Receptor de Serotonina 5-HT2 , Urea/análogos & derivados , Adolescente , Adulto , Antipsicóticos/efectos adversos , Antipsicóticos/sangre , Disponibilidad Biológica , Estudios Cruzados , Ayuno , Semivida , Humanos , Masculino , Persona de Mediana Edad , Piperidinas/efectos adversos , Piperidinas/sangre , Trastornos Psicóticos , Comprimidos , Equivalencia Terapéutica , Urea/administración & dosificación , Urea/efectos adversos , Urea/sangre , Urea/farmacocinéticaRESUMEN
The pharmacokinetics, safety, and tolerability of ACP-103, a selective serotonin 5-HT(2A) receptor inverse agonist, were evaluated in 2 double-blind, placebo-controlled, dose escalation studies in healthy male volunteers. Pharmacokinetic sampling was measured up to 216 hours after single oral/nasogastric doses of ACP-103 and after the last dose of once-daily oral administration of ACP-103 for 14 days. Single doses of ACP-103 (20-300 mg) resulted in dose-proportionate mean C(max) values (9-152 ng/mL) and AUC(0-infinity) (706-10 798 h x ng/mL), and multiple doses (50-150 mg) resulted in dose-proportionate mean C(max,ss) (93-248 ng/mL) and AUC(0-infinity,ss) (1839-4680 h x ng/mL). The half-life of ACP-103 was approximately 55 hours, with a t(max) at 6 hours. ACP-103 was well tolerated at single doses up to and including 300 mg and multiple doses up to 100 mg once daily for 14 days.
