- Lithium Neurotoxicity Due to Second-Generation Antipsychotics Combined With Lithium: A Systematic Review. [Journal Article]
- PCPrim Care Companion CNS Disord 2019 Jun 20; 21(3)
- CONCLUSIONS: LN, both reversible and irreversible, due to SGAs combined with lithium presents with certain causative factors and a clinical profile. Early detection and prompt management will help prevent LN.
- Medication-Induced Akathisia with Newly Approved Antipsychotics in Patients with a Severe Mental Illness: A Systematic Review and Meta-Analysis. [Review]
- CDCNS Drugs 2019; 33(6):549-566
- CONCLUSIONS: The use of a NAP raises the akathisia risk more than two-fold when compared with patients receiving placebo. Although distinctions between the different NAPs were not clear in placebo-controlled trials, the results of our meta-analyses and systematic review generally indicate that these differences more than likely reflect real differences, with iloperidone showing the most and cariprazine showing the least benign akathisia profile. Moreover, due to patient characteristics and methodological issues, incidence rates of akathisia with NAPs found in this meta-analysis may even be an underestimation of true incidence rates.
- Novel Adverse Events of Iloperidone: A Disproportionality Analysis in US Food and Drug Administration Adverse Event Reporting System (FAERS) Database. [Journal Article]
- CDCurr Drug Saf 2019; 14(1):21-26
- CONCLUSIONS: Iloperidone associated five potential signals were generated by data mining in the FDA AERS database. The result requires an integration of further clinical surveillance for the quantification and validation of possible risks for the adverse events reported of iloperidone.
- A Focused Review on the Treatment of Pediatric Patients with Atypical Antipsychotics. [Journal Article]
- JCJ Child Adolesc Psychopharmacol 2018; 28(9):582-605
- CONCLUSIONS: Evidence regarding the efficacy and tolerability of antipsychotic medications for mental health disorders in children and adolescents has expanded exponentially in recent years. However, more information is needed so that evidence-based comparisons between medications can be made. In the future, data enabling the selection of medications based upon individual patient characteristics could potentially lead to greater efficacy and efficiency in treating what are frequently debilitating medical conditions. Maladaptive aggression in children, often treated with antipsychotics, is one such area in which there is a dearth of actual information available to the clinician. It is to be hoped that additional, longer-term studies of these medications will further inform evidence-based practice in clinical settings.
- A Review of the Pharmacological and Clinical Profile of Newer Atypical Antipsychotics as Treatments for Bipolar Disorder: Considerations for Use in Older Patients. [Review]
- DADrugs Aging 2018; 35(10):887-895
- Bipolar disorder prevalence rates vary in the older adult population (defined as age ≥ 65 years), ranging from 1% in community dwellers to as high as 8-10% in hospital inpatients. Although older agen…
Bipolar disorder prevalence rates vary in the older adult population (defined as age ≥ 65 years), ranging from 1% in community dwellers to as high as 8-10% in hospital inpatients. Although older agents, including lithium and valproic acid, offer significant antimanic efficacy, as supported by a recent randomized controlled trial (RCT), there is growing interest in using atypical antipsychotics to treat bipolar disorder in older adults. Newer atypical antipsychotics are of interest based on their tolerability and efficacy in the general adult bipolar population. The aim of this review was to systematically examine efficacy and tolerability of newer atypical antipsychotics for older adult bipolar disorder (OABD). We conducted a systematic search utilizing the MEDLINE, EMBASE, PsycINFO and Cochrane Library electronic databases, with the aim of identifying all RCTs comparing newer atypical antipsychotics approved by the US FDA since 2002 (including brexpiprazole, cariprazine, lurasidone, iloperidone, asenapine, paliperidone, and aripiprazole) with placebo or another comparator, in the treatment of any phase of bipolar disorder (including mania, depression or mixed episodes while used as an acute or maintenance treatment) in older adults (> 65 years). We found no RCT data on any of the examined agents. Hence, we changed our search criteria to include studies with a lower age cut-off (≥ 55 years), as well as the inclusion of post hoc studies. Two post hoc studies on lurasidone suggest its reasonable safety and efficacy profile in the acute and maintenance treatment of OABD; however, there are no pharmacoeconomic data on the use of lurasidone in the treatment of OABD. Research data from open-label studies on oral asenapine and aripiprazole as add-on therapy suggest that these two agents are adequately tolerated and improved symptoms of depression and mania in OABD; hence, there is an urgent need to conduct RCTs on these two agents. Lastly, we found no studies for the treatment of OABD with brexpiprazole, cariprazine, iloperidone, or paliperidone.
- Efficacy and Tolerability of Atypical Antipsychotics in the Treatment of Delirium: A Systematic Review of the Literature. [Journal Article]
- PPsychosomatics 2019 Jan - Feb; 60(1):18-26
- CONCLUSIONS: Although the current evidence of the efficacy and tolerability of AAPs in the treatment of delirium is limited and the heterogeneity of the data precluded a meta-analysis, olanzapine and quetiapine seem to be adequate alternatives to haloperidol, especially in patients who are vulnerable for extrapyramidal symptoms, who require sedation or who have a history of haloperidol intolerance. Evidently, larger-scale RCTs are urgently required.
- Long-Term Effects of Iloperidone on Cerebral Serotonin and Adrenoceptor Subtypes. [Journal Article]
- JMJ Mol Neurosci 2018; 66(1):59-67
- The atypical antipsychotic drug iloperidone has high affinity for a wide range of neurotransmitter receptors, including serotonin and adrenoceptors. We examined the long-term effects of multiple dose…
The atypical antipsychotic drug iloperidone has high affinity for a wide range of neurotransmitter receptors, including serotonin and adrenoceptors. We examined the long-term effects of multiple doses of iloperidone (0.5, 1.5, or 5 mg/kg) on serotonin (5-HT) 5-HT1A, 5-HT2A receptor subtypes, and adrenoceptors α1 and α2 subtypes. Rats received daily intraperitoneal injections of different doses of iloperiodone or vehicle for 4 weeks. Receptor autoradiography quantified the levels of 5-HT and adrenoceptors in medial prefrontal cortex (MPC), dorsolateral frontal cortex (DFC), caudate putamen (CPu), nucleus accumbens (NAc), and hippocampal CA1 (HIP-CA1) and CA3 (HIP-CA3) regions. Four weeks of iloperidone treatment significantly and dose-dependently increased 5-HT1A and decreased 5-HT2A receptors in the MPC and DFC. Higher doses of iloperidone (1.5 and 5 mg/kg) increased 5-HT1A and decreased 5-HT2A receptors in HIP-CA1 and HIP-CA3 regions. In addition, repeated iloperidone treatment produced significant increases in α1- and α2-adrenoceptors in MPC, DFC, HIP-CA1, and HIP-CA3 regions. No changes in 5-HT and adrenoceptors were observed in other brain regions examined. These results suggest that long-term iloperidone treatment exerts region- and dose-specific effects on forebrain 5-HT and adrenoceptors, which may contribute to its therapeutic benefits in improving positive and negative symptoms of schizophrenia as well as maintaining a benign safety profile.
- Drugs and Lactation Database (LactMed): Iloperidone [BOOK]
- BOOKNational Library of Medicine (US): Bethesda (MD)
- Because no information is available on the use of iloperidone during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Because no information is available on the use of iloperidone during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
- Supported liquid extraction and LC-MS-MS determination of iloperidone and olanzapine in rat plasma: Application to a pharmacokinetic study. [Journal Article]
- JCJ Chromatogr Sci 2018 Nov 01; 56(10):879-887
- A sensitive, selective rapid bioanalytical assay method was developed and quantification of iloperidone (ILP) and olanzapine (OLZ) in rat plasma was done by mass spectrometry. Systematic sample prepa…
A sensitive, selective rapid bioanalytical assay method was developed and quantification of iloperidone (ILP) and olanzapine (OLZ) in rat plasma was done by mass spectrometry. Systematic sample preparation and extraction procedure were carried out by supported liquid extraction using dichloromethane to extract both the eluents (ILP and OLZ) from rat plasma samples. The extorted samples were injected on a selective Waters XTerra® C18 reverse-phase bonded column (250 × 4.6 mm i.d., 5 μm) using acetonitrile and 15 mM ammonium formate containing 0.05% trifluoroacetic acid (60:40 v/v) for isocratic elution mode and detected by mass spectrometry. Calibration curves were drawn with the respective assay statistical data and showed linear regression coefficients greater than 0.9996 over the concentration ranges 2-5,000 ng/mL for ILP and OLZ, respectively. The absolute mean recoveries were found to be in the replicate range of 87.12-94.47%, respectively. The obtained results by the method revealed good intra and interday assay performance in terms of 1.70-5.90% precision and 0-5% accuracy. The validated bioassay method has been successfully applied to the pharmacokinetics in rats.
New Search Next
- Graphic representation of pharmacology: Development of an alternative model. [Journal Article]
- MHMent Health Clin 2017; 7(5):201-206
- Providing clinicians with an easy to grasp and understandable representation of pharmacology is important to allow optimal clinical decisions to be made. Two of the most clinically relevant dimension…
Providing clinicians with an easy to grasp and understandable representation of pharmacology is important to allow optimal clinical decisions to be made. Two of the most clinically relevant dimensions are receptor binding affinity and functional activity. The binding affinity for an agonist is described by the dissociation constant (KA ), and an antagonist by the inhibition constant (Ki ). Functionally, medications can act as superagonists, agonists, partial agonists, antagonists, partial inverse agonists, or inverse agonists at several receptor sites, transporters, or ion channels. Comprehending the differences between agents is complicated by the number and types of binding sites.