title: [Clinic pharmacokinetics of a new original antipsychotic drug Dilept].
abstract: The pharmacokinetic study of a new original antipsychotic drug Dilept in healthy volunteers was performed. Volunteers received Dilept as single 20, 40 or 60 mg tablets. The parent drug in the human blood plasma was detected in low concentrations and short-term time due to intensive biotransformation with formation of two metabolites N-caproyl-L-prolyl-tyrosin (M-1) and N-caproyl-L-prolin (M-2). After 20 and 40 mg of Dilept parent drug was detected in certain time points and after 60 mg for 1 h. M-1 and M-2 metabolites were registered in the blood plasma for 4 - 8 h. Theirs concentrations were 10 - 100 times higher of unchanged drug ones. Metabolites pharmacokinetics in the studied dosage range was nonlinear.
authors.forename: R V
authors.initials: RV
authors.lastname: Shevchenko
authors.forename: A A
authors.initials: AA
authors.lastname: Litvin
authors.forename: G B
authors.initials: GB
authors.lastname: Kolyvanov
authors.forename: S S
authors.initials: SS
authors.lastname: Boĭko
authors.forename: V P
authors.initials: VP
authors.lastname: Zherdev
authors.forename: S Iu
authors.initials: SIu
authors.lastname: Serebrova
authors.forename: N Iu
authors.initials: NIu
authors.lastname: Ivashkina
authors.forename: G G
authors.initials: GG
authors.lastname: Neznamov
authors.forename: S A
authors.initials: SA
authors.lastname: Siuniakov
mesh_terms: D000328:Adult; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001711:Biotransformation; D004334:Drug Administration Schedule; D006801:Humans; D008297:Male; D011392:Proline / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D013607:Tablets; D014443:Tyrosine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics
chemical_list: D014150:Antipsychotic Agents; C401484:GZR 123; D013607:Tablets; D014443:Tyrosine; D011392:Proline