The Pharmacokinetic and Safety Profiles of Blonanserin in Healthy Chinese Volunteers After Single Fasting Doses and Single and Multiple Postprandial Doses

  title={The Pharmacokinetic and Safety Profiles of Blonanserin in Healthy Chinese Volunteers After Single Fasting Doses and Single and Multiple Postprandial Doses},
  author={Xia Chen and Hongyun Wang and Ji Jiang and Rui Chen and Ying Zhou and Wen Zhong and Hongzhong Liu and Pei Hu},
  journal={Clinical Drug Investigation},
Background and ObjectivesBlonanserin is a novel atypical antipsychotic drug acting as a mixed serotonin 5-HT2A and dopamine D2 receptor antagonist. This study investigated the pharmacokinetics and safety of blonanserin in healthy Chinese males.MethodsThis was an open-label trial with two parts. Twenty-four subjects were enrolled in part A to receive a single fasting dose of 4 or 8 mg blonanserin (each n = 12); part B recruited 12 subjects and administered single and sequentially twice-daily… 

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

Alcohol increased the bioavailability of blonanserin and N-deethylated blon Lanserin in healthy subjects and the marked effect of alcohol on blonANSerin bioavailability should be taken into consideration in deciding dosing schedules in clinical therapy.

Effects of food and grapefruit juice on single-dose pharmacokinetics of blonanserin in healthy Chinese subjects

It is suggested that blonanserin was largely metabolised in the intestinal tract before becoming systemically available, and both food and grapefruit juice enhanced exposure to blonANSerin and N-desethyl blonoserin.

Atypical antipsychotic properties of AD-6048, a primary metabolite of blonanserin


Article history The present research work describe a rapid, simple, validated and stability indicating RP- HPLC method for analysis of blonanserin in bulk and tablet dosage form performed

Psychotropics and Male Reproduction.

Psychotropic drugs, including antidepressants, antipsychotics, and anticonvulsants, all have negative effects on sexual function and semen quality and are less pronounced for some medications, allowing their effects to be managed to some extent.

An Ultra Performance Liquid Chromatography-PDA Method for the Determination of a Novel Antipsychotic-Blonanserin in Bulk and its Tablet Dosage Form

To develop a new ultra-high-resolution liquid chromatographic technique for determining Blonanserin concentrations in APIs and tablets. A DIKMA Endoversil (2.1 x 50mm, 1.7µm) column with a flow rate



Effect of dose timing in relation to food intake on systemic exposure to blonanserin

Food intake increased the systemic exposure to blonanserin for all time intervals investigated in this study, and the marked effect of food on the bioavailability of blonANSerin should be taken into account in its dosing schedules.

A Double Blind, Placebo-Controlled, Randomized Crossover Study of the Acute Metabolic Effects of Olanzapine in Healthy Volunteers

Olanzapine exerts some but not all of the early endocrine/metabolic changes observed in rodent models of the metabolic side effects, and this suggest that antipsychotic effects are not limited to perturbations in glucose metabolism alone.

Profile of blonanserin for the treatment of schizophrenia

Results suggest that blonanserin may be a promising candidate for a first-line antipsychotic for acute and maintenance therapy for schizophrenia.

Simultaneous determination of blonanserin and its metabolite in human plasma and urine by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study.

Blonanserin: a review of its use in the management of schizophrenia.

Clinical data suggest that blonanserin is an effective and generally well tolerated option for the short-term treatment of schizophrenia and for those requiring longer-term therapy.

Atypical antipsychotic properties of blonanserin, a novel dopamine D2 and 5-HT2A antagonist

Striatal and Extrastriatal Dopamine D2 Receptor Occupancy by a Novel Antipsychotic, Blonanserin: A PET Study With [11C]Raclopride and [11C]FLB 457 in Schizophrenia

The clinical implications obtained in this study were the optimal therapeutic dose range of 12.9 to 22.1 mg/d of blonanserin required for 70% to 80% dopamine D2 receptor occupancy in the striatum, and the good blood-brain barrier permeability that suggested a relatively lower risk of hyperprolactinemia.

Potential mechanisms of atypical antipsychotic-induced hypertriglyceridemia

There is evidence that AAPs may cause hypertriglyceridemia through several possible mechanisms: a direct effect on triglyceride metabolism either by stimulation of hepatic triglyceride production and secretion or by inhibition of lipoprotein lipase-mediated triglyceride hydrolysis and an indirect mechanism associated with obesity and insulin resistance.

Gut instincts: CYP3A4 and intestinal drug metabolism.

  • K. Thummel
  • Medicine, Biology
    The Journal of clinical investigation
  • 2007
It is shown in this issue of the JCI that first-pass metabolism of the anticancer agent docetaxel by the gut wall, and not the liver, is likely to be the major cause of its low oral bioavailability in humans.