Premium
Safety, Tolerability, and Effect of Food on the Pharmacokinetics of Iloperidone (HP 873), a Potential Atypical Antipsychotic
Author(s) -
Sainati Stephen M.,
Hubbard John W.,
Chi Eric,
Grasing Kenneth,
Brecher Martin B.
Publication year - 1995
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1995.tb04112.x
Subject(s) - tolerability , pharmacokinetics , atypical antipsychotic , pharmacology , medicine , antipsychotic , oncology , adverse effect , schizophrenia (object oriented programming) , psychiatry
Iloperidone (HP 873) is a D 2 and 5‐HT 2 receptor‐antagonist that is under development as a potential atypical antipsychotic agent. Two studies on iloperidone evaluated its safety and tolerability, made a preliminary pharmacokinetic assessment of single 3‐ and 5‐mg doses, and determined the effect of food on its tolerability and pharmacokinetics in healthy volunteers after single 3‐mg doses. Iloperidone was well absorbed orally in fasted subjects. The C max occurred approximately 2 to 3 hours after administration of a single 3‐ or 5‐mg dose. The pharmacokinetic parameters increased with the dose between 3 and 5 mg (from 2.2 to 5.2 ng/mL for C max , and 16 to 50 ng/mL•h for AUC). Iloperidone was eliminated slowly, with a mean t 1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t max , or C max . These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events. Coadministration of food reduced the incidence and severity of these events.