Iloperidone

Iloperidone is an anti-psychotic combined dopamine (D2) and serotonin (5HT2) receptor antagonist.

Iloperidone in the treatment of schizophrenia: an evidence-based review of its place in therapy.[Pubmed:28008301]

Core Evid. 2016 Dec 14;11:49-61.

INTRODUCTION: Schizophrenia is a chronic and debilitating mental disorder that affects the patient's and their family's quality of life, as well as financial costs and health care settings. Despite the variety of available antipsychotics, optimal treatment outcomes are not always achieved. Novel drugs, such as Iloperidone, can provide more effective, tolerable and safer strategies. AIM: To review the evidence for the clinical impact of Iloperidone on the treatment of patients with schizophrenia. EVIDENCE REVIEW: Clinical trials, observational studies and meta-analyses reached a common consensus that Iloperidone is as effective as haloperidol, risperidone and ziprasidone in reducing schizophrenia symptoms. Similar amounts of adverse events and discontinuations were observed with Iloperidone compared to placebo and active treatments. Common adverse events are mild and include dizziness, hypotension, dry mouth and weight gain. Iloperidone can induce extension of QTc interval, and clinicians should be aware of its contraindications. In long-term trials, Iloperidone also showed promising safety and tolerability profiles. The low propensity to cause akathisia, extrapyramidal symptoms (EPS), increased prolactin levels or changes to metabolic laboratory parameters support its use in practice. Results showed that Iloperidone prevents relapse in stabilized patients, with a time to relapse superior to placebo and similar to haloperidol. Patients using a prior antipsychotic (eg, risperidone and aripiprazole) can easily switch to Iloperidone with no serious impact on safety or efficacy. However, the acquisition costs of Iloperidone may hamper its use. Further evidence comparing Iloperidone with other antipsychotics, and pharmacoeconomic studies would be welcome. PLACE IN THERAPY: Considering just the clinical profile of Iloperidone, it represents a promising drug for treating schizophrenia, particularly in patients who are intolerant to previous antipsychotics, as well as being suitable as first-line therapy. Cost-effectiveness comparisons are needed to justify its use in clinical practice.

A case of iloperidone overdose in a 27-year-old man with cocaine abuse.[Pubmed:27570623]

SAGE Open Med Case Rep. 2016 Aug 8;4:2050313X16660485.

INTRODUCTION: Iloperidone is a recently introduced antipsychotic medication. It is approved for the treatment of schizophrenia. There are no published reports of Iloperidone overdosage, but there are eight cases that have been reported to the US Food and Drug Administration. CASE REPORT: A case of a 27-year-old man who took 84 mg of Iloperidone while also smoking cocaine is described. He developed a prolonged QTc (527 ms) without arrhythmias and respiratory failure with mandated respiratory support. He ultimately recovered without sequelae. DISCUSSION: The information regarding previous cases of toxicity on the US Food and Drug Administration website is incomplete. However, there were no fatalities due to Iloperidone over-ingestion. Prolongation of the QTc may be a common feature.

Influences of CYP2D6(*)10 polymorphisms on the pharmacokinetics of iloperidone and its metabolites in Chinese patients with schizophrenia: a population pharmacokinetic analysis.[Pubmed:27665849]

Acta Pharmacol Sin. 2016 Nov;37(11):1499-1508.

AIM: Iloperidone is an atypical antipsychotic drug that is mainly metabolized by CYP2D6, CYP3A4, and cytosolic enzymes. Previous studies show that extensive and poor metabolizers of CYP2D6 exhibit different plasma concentrations of Iloperidone and its metabolites. The aim of this study was to develop a parent-metabolite population pharmacokinetic (PPK) model to quantify the effects of CYP2D6(*)10 allele on the pharmacokinetics of Iloperidone and its metabolites in Chinese schizophrenia patients. METHODS: Seventy Chinese schizophrenia patients were enrolled, from whom limited blood samples were collected on d 15 (0 h) and d 28 (0, 4 and 12 h after drug administration). The plasma concentrations of Iloperidone and its metabolites M1 (P-88) and M2 (P-95) were simultaneously detected using a validated HPLC-MS assay. CYP2D6(*)10 (rs1065852) genotyping was performed. A PPK model was developed based on data from the patients using the NONMEM software (version 7.2). A one-compartment model with first-order absorption and elimination was used to describe the pharmacokinetic data related to Iloperidone and its metabolites. RESULTS: Patients with the CYP2D6(*)10 T/T genotype had significantly higher concentrations of Iloperidone and M1, and lower concentrations of M2 than the patients with C/C or C/T genotypes. The CYP2D6(*)10 genotype affected the elimination constants for transformation of Iloperidone to the metabolites M1 (K23) and M2 (K24). The K23 value of the patients with T/T genotype was 1.34-fold as great as that of the patients with C/C or C/T genotype. The K24 value of the patients with C/T and T/T genotypes was 0.693- and 0.492-fold, respectively, as low as that of the patients with C/C genotype. CONCLUSION: CYP2D6(*)10 mutations affect the pharmacokinetics of Iloperidone and its metabolites in Chinese schizophrenia patients, suggesting that the clinical doses of Iloperidone for patients with CYP2D6(*)10 mutations need to be optimized.

Iloperidone(HP 873) is a D2/5-HT2 receptor antagonist, which is an atypical antipsychotic for the treatment of schizophrenia symptoms.

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