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Pharmacokinetics, Tolerability, and Safety of Aripiprazole following Multiple Oral Dosing in Normal Healthy Volunteers
Author(s) -
Mallikaarjun Suresh,
Salazar Daniel E.,
Bramer Steven L.
Publication year - 2004
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 - 10.1177/0091270003261901
Subject(s) - aripiprazole , tolerability , pharmacokinetics , placebo , dosing , medicine , adverse effect , antipsychotic , pharmacology , anesthesia , atypical antipsychotic , schizophrenia (object oriented programming) , psychiatry , alternative medicine , pathology
Two 14‐day, placebo‐controlled, double‐blind studies evaluated the fasting pharmacokinetics, safety, and tolerability of aripiprazole, a new antipsychotic, in healthy male subjects. In Study 1, 37 subjects were randomized to aripiprazole 5 mg, 10 mg, 15 mg, 20 mg, or placebo once daily. In Study 2, 11 subjects were randomized to aripiprazole, titrated from 10 to 30 mg/day, or placebo. Aripiprazole had linear pharmacokinetics over 5 to 30 mg/day, which were described by a two‐compartment open model, with first‐order absorption. In Study 1, mean elimination half‐life ranged from 47 to 68 hours with aripiprazole, with apparent systemic clearance (CL/F) of approximately 3.45 L/h. In Study 2, mean elimination half‐life was 59 hours (CL/F approximately 4.0 L/h). Adverse events were generally mild to moderate, were transient in nature, and commonly occurred within the first 3 days of dosing. Clinical laboratory assessments, electrocardiogram, electroencephalogram, and prolactin levels showed no clinically significant changes during the studies.