title: Single oral dose kinetics of zotepine and its relationship to prolactin response and side effects.
abstract: The authors investigated the single oral dose kinetics of zotepine and its relationship with prolactin response and side effects in 14 healthy male volunteers. Each subject took a single oral 25-mg dose of zotepine, and plasma concentrations of zotepine, prolactin, and their side effects were monitored up to 36 hours after dosing. The means +/- SD of the time of maximal plasma concentration (tmax), the apparent oral clearance, the apparent volume of distribution, and the elimination half-life (t1/2) were 3.8 +/- 1.2 hours, 4.6 +/- 4.2 1/h.kg, 109.0 +/- 59.0 1/kg, and 21.0 +/- 8.9 hours, respectively. The change in prolactin concentrations and side effect scores were parallel with that of drug concentrations, although no significant correlation was found between these three parameters at any time-point. The current results clearly indicate that the tmax and t1/2 of zotepine are much longer than those previously reported, which are reflected in the changes in prolactin concentrations and side effect scores.
authors.affiliation: Department of Neuropsychiatry, Hirosaki University School of Medicine, Japan.
authors.forename: O
authors.initials: O
authors.lastname: Tanaka
authors.forename: T
authors.initials: T
authors.lastname: Kondo
authors.forename: K
authors.initials: K
authors.lastname: Otani
authors.forename: N
authors.initials: N
authors.lastname: Yasui
authors.forename: N
authors.initials: N
authors.lastname: Tokinaga
authors.forename: S
authors.initials: S
authors.lastname: Kaneko
mesh_terms: D000284:Administration, Oral; D000328:Adult; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D003988:Dibenzothiepins / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D008297:Male; D011388:Prolactin / Q000097:blood*; D013607:Tablets
chemical_list: D014150:Antipsychotic Agents; D003988:Dibenzothiepins; D013607:Tablets; D011388:Prolactin; C022172:zotepine