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Reduction of haloperidol‐induced side effects by ACP‐103 in healthy volunteers
Author(s) -
Grahnen A. E.,
Vanover K. E.,
Weiner M.,
Nilsson L.,
Tolf B.,
Hacksell U.,
Davis M. R.
Publication year - 2005
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2005.01.004
Subject(s) - haloperidol , reduction (mathematics) , pharmacology , medicine , anesthesia , dopamine , mathematics , geometry
Background/Aims A novel serotonin 2 A (5‐HT2 A ) receptor inverse agonist, ACP‐103, was tested to determine the potential of ACP‐103 to inhibit central nervous system side effects produced by haloperidol. Methods Healthy male volunteers participated in a randomized, double blind, placebo‐controlled, single dose crossover study. All subjects received a single dose of haloperidol (7.5 mg) in combination with either a single dose of placebo or a single dose of ACP‐103 (100 mg). The washout period between treatment combinations was two weeks. Results Haloperidol caused measurable akathisia in 13 of 18 subjects and induced approximately a 3‐fold increase in prolactin secretion. ACP‐103 treatment caused a measurable and temporally consistent decrease in haloperidol‐induced akathisia compared to placebo treated subjects as measured by the Barnes Akathisia Scale. ACP‐103 significantly reduced haloperidol‐induced hyperprolactinemia. The pharmacokinetics of haloperidol and ACP‐103 were not affected by their co‐administration. No serious adverse events were reported. Conclusions Data suggest that ACP‐103, when co‐administered with existing antipsychotic drugs, may reduce their side effects and expand their range of efficacy. ACP‐103 is being developed as an adjunctive therapy for schizophrenia and as a therapy for treatment‐induced dysfunction in Parkinson's disease. Clinical Pharmacology & Therapeutics (2005) 77 , P98–P98; doi: 10.1016/j.clpt.2005.01.004