Effects of Alcohol on the Pharmacokinetics of Blonanserin and N-Deethylated Blonanserin in Healthy Chinese Subjects

Journal of Clinical Psychopharmacology
Shuhua DengYu-Guan Wen

Abstract

Blonanserin is a novel antipsychotic drug approved for the treatment of schizophrenia in East Asia. The main objective of the present study was to investigate the effect of alcohol on the pharmacokinetic properties of blonanserin and its metabolite N-deethyl blonanserin in healthy Chinese male subjects under fasting conditions. The study was designed as a randomized, open-label, crossover clinical investigation in 10 male volunteers, each of whom received 2 treatments under fasted conditions: treatment A, blonanserin (8 mg) with water, and treatment B, blonanserin (8 mg) with alcohol (1 mL/kg). The average values of areas under the curve (AUCs) and mean peak plasma concentrations (Cmax) were noticeably increased by alcohol consumption. In treatment A, average values of AUC0-24h, AUC0-∞, and Cmax were 3178 ng/h/L, 3879 ng/h/L, and 492 ng/L for blonanserin, and 1932 ng/h/L, 4208 ng/h/L, and 137 ng/L for N-deethylated blonanserin, respectively. In treatment B, AUC0-∞ and Cmax were both increased 2.4-fold for blonanserin and 1.4-fold and 1.7-fold, respectively, for N-deethylated blonanserin (P < 0.05). Compared with treatment A, clearance (Clz/F) of blonanserin and N-deethylated blonanserin decreased significantly (2.4-fold and 1.7...Continue Reading

References

Aug 1, 1990·Alcoholism, Clinical and Experimental Research·M R PianoC L Melchior
May 1, 1985·Clinical Pharmacology and Therapeutics·P DorianD Abernethy
Feb 1, 1986·British Journal of Clinical Pharmacology·J M ScavoneR I Shader
Apr 1, 1984·Journal of Clinical Psychopharmacology·H R OchsR I Shader
Jan 1, 1981·Psychopharmacology·M DivollR I Shader
Dec 25, 2009·CNS Drugs·Emma D Deeks, Gillian M Keating
May 22, 2010·European Journal of Clinical Pharmacology·Junji SaruwatariSunao Kaneko
Jun 14, 2012·Progress in Neuro-psychopharmacology & Biological Psychiatry·Tomoko InoueNoboru Yamaguchi
Jul 24, 2012·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Yu-Guan WenDe-Wei Shang
Dec 12, 2012·The World Journal of Biological Psychiatry : the Official Journal of the World Federation of Societies of Biological Psychiatry·Alkomiet HasanWFSBP Task force on Treatment Guidelines for Schizophrenia
Jun 15, 2013·Neuropsychiatric Disease and Treatment·Tomomi TenjinNoboru Yamaguchi
Jul 3, 2013·Nutrition Reviews·Elhaseen E ElaminDaisy M Jonkers
Jun 28, 2014·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Manuela GrazianiRobert Nisticò
Oct 1, 2014·Clinical Pharmacokinetics·Lingtak-Neander Chan, Gail D Anderson
Oct 14, 2014·Handbook of Clinical Neurology·Bankole A Johnson, Chamindi Seneviratne
Dec 3, 2014·Redox Biology·Christopher B ForsythAli Keshavarzian
Jul 25, 2015·Digestive Diseases and Sciences·Sandeep B SubramanyaWim J Lammers
Sep 5, 2015·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Wei ShangJian Yang
Oct 5, 2017·European Journal of Clinical Pharmacology·De-Wei ShangYu-Guan Wen

Related Concepts

Lonasen
Ethanol
Central Nervous System Depressants
Drug Interactions
Fasting
Piperazines
Piperidines
Antipsychotic Effect
Cross-Over Studies
Human Volunteers

Related Feeds

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here