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Objective: To assess health-related quality of life and associated factors in patients treated with atypical antipsychotics, as well as to determine utility values using the EuroQol-5D-3L instrument. Methods: A cross-sectional study was conducted at a state-run pharmacy in the Brazilian National Health System. Individuals were included if they were using a single atypical antipsychotic and completed the EuroQol-5D-3L. Sociodemographic, behavioral, and clinical data were collected. The dependent variable was the EuroQol-5D-3L utility score. Associations between the independent variables and the dependent variable were analyzed in a multiple linear regression model. Results: A total of 394 patients were included, and their mean utility score was 0.664 ± 0.232. Patients treated with clozapine had the highest mean score (0.762 [0.202]), followed by olanzapine (0.687 [0.230]), risperidone (0.630 [0.252]), ziprasidone (0.622 [0.234]), and quetiapine (0.620 [0.243]). The following variables were related to higher utility scores: income, employment, clozapine use, no illicit psychoactive substance use, no suicide attempts, and no comorbidities. Conclusion: Evaluating health-related quality of life differences in the available atypical antipsychotics can facilitate the choice of treatment, improve health outcomes, and ensure rational prescriptions. [ABSTRACT FROM AUTHOR]

The aim of the present study was to formulate a controlled release Ziprasidone HCl oral matrix tablet using different proportions of hydroxyl propyl methylcellulose (HPMC) K15M to minimize dosing frequency. Matrix tablets were prepared with various proportions of HPMC by direct-compression to upgrade their compliance and safety profile. Micromeritic properties of blends, physical evaluation of tablets, swelling, and dissolution studies were performed to optimize the formulation. The drug release profile indicated the controlled release pattern of formulation with HPMC K15M 50% for 24 hours effectively. Ziprasidone CR matrix-based tablet was formulated successfully and it was shown that the release of drugs could be controlled by the inclusion of different ratios of various viscosity grade polymers. [ABSTRACT FROM AUTHOR]

Purpose Tardive dyskinesia (TD) is a hyperkinetic movement disorder that results from exposure to dopamine receptor antagonists and/or first- and second-generation antipsychotics. While cessation of the offending agent(s) through early detection is recommended, TD symptoms may be irreversible and require further treatment. Deutetrabenazine is approved by the Food and Drug Administration for treatment of persistent TD. Irreversible orofacial dyskinesia, a common affliction in TD, can progress to severe oropharyngeal dysphagia requiring alternate means of nutrition and medication delivery. Enteral administration of crushed deutetrabenazine has not been studied, and its use to treat TD in patients who cannot take medications by mouth has not been reported previously. Summary A 38-year-old female patient with a history of bipolar I disorder and TD secondary to atypical antipsychotic exposure developed worsening athetosis, hyperkinesia, and severe orofacial dyskinesia after initiation of ziprasidone. The patient had no improvement after discontinuation of atypical antipsychotics and required percutaneous endoscopic gastrostomy (PEG) placement for nutrition due to persistent aspiration and inability to tolerate oral nutrition. Despite a lack of information regarding administration of crushed deutetrabenazine tablets via PEG, that form of therapy was initiated and resulted in improvement of TD symptoms without noticeable adverse effects. Conclusion TD can result in significant orofacial dyskinesia with impaired delivery of needed medications and nutrition. We describe a case in which a patient with severe TD and orofacial dyskinesia experienced improvement of symptoms with use of crushed deutetrabenazine. Larger studies to further evaluate use of crushed deutetrabenazine for treatment of TD are needed. [ABSTRACT FROM AUTHOR]

The purpose of research work was to develop and optimize mucoadhesive microspheres of Ziprasidone hydrochloride for nasal del ivery with the aim to enhance the residence time and improve therapeutic efficacy. Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In our present work, mucoadhesive chitosan microspheres were prepared by emulsification method using liquid paraffin as external phase. Ten different formulations were developed. Results show that as the concentration of polymer increases it affects the particle size, production yield, encapsulation efficiency, swelling index, in-vitro mucoadhesion and in-vitro drug release of mucoadhesive microspheres. The in vitro mucoadhesion of microspheres was investigated using freshly isolated goat nasal mucosa. The mucoadhesion for M0, M1, M2, and M9 was tested. The mucoadhesion property was satisfactory. The M2 exhibited lowest mucoadhesion of 68.9%, and M0 displayed highest mucoadhesion of 87.5%. The In Vitro release studies it revealed that 84.1% of drug release from formulation M1 at 7hrs. The 50% of the drug was released from the formulation M2 and 70.67% from formulat ion M9.This formulations were further used for SEM for particles size analysis, mucoadhesion test and in-vitro drug release. The In-vitro % drug release data suggest that the maximum and sustained drug release was obtained for formulation M1.The present study showed that Ziprasidone hydrochloride chitosan microspheres can deliver intanasally which can improve the therapeutic outcome for the Epileptic seizure. [ABSTRACT FROM AUTHOR]

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone. [ABSTRACT FROM AUTHOR]

Keywords: bipolar disorder; gambling disorder; obsessive-compulsive disorder; ziprasidone EN bipolar disorder gambling disorder obsessive-compulsive disorder ziprasidone 425 428 4 06/12/20 20200601 NES 200601 Key message Bipolar disorder (BD) with comorbid obsessive-compulsive disorder (OCD) and gambling disorder (GD) is a severe and complex condition in clinical practice. In addition, the co-occurrence of other psychiatric disorders with BD is very high, with as many as 65%-95% meeting the diagnostic criteria for comorbid conditions.[1] Of these, about 25% are comorbid with obsessive-compulsive disorder (OCD), and 10.6% with gambling disorder (GD).[2] Moreover, BD patients with OCD are more likely to be comorbid with impulse-control disorder, including GD, than those without OCD. Recently, risperidone, quetiapine, olanzapine, and aripiprazole have been reported to be effective in the treatment of BD with OCD as an add-on therapy,[4] suggesting atypical antipsychotics might play a role in the treatment of BD with comorbid OCD. Learning points Bipolar disorder with comorbid obsessive-compulsive disorder (OCD) and gambling disorder (GD) is a severe and complex condition that confronts clinical psychiatrists. [Extracted from the article]

Hospitalized patients receiving haloperidol or ziprasidone for delirium while in intensive care experienced no increased risk of QTc interval prolongation relative to placebo, a secondary analysis of a randomized trial has found. None of the small number of cardiac events experienced by patients receiving one of the antipsychotics were determined to be associated with study drug administration. [ABSTRACT FROM AUTHOR]

В обзоре представлены данные об эффективности современного атипичного антипсихотика зипрасидона для внутримышечного применения при купировании острого психомоторного возбуждения различного генеза (шизофрения, биполярное аффективное расстройство, шизоаффек тивное расстройство, расстройства импульсивных влечений, алкогольная и другие виды интоксикации), в том числе в случаях недостаточ ной эффективности других инъекционных антипсихотиков (типичных и атипичных). Незначительная выраженность нежелательных эффектов и сходная эффективность внутримышечного зипрасидона у пациентов различного возраста позволяют применять препарат для купирования возбуждения у детей, подростков и пожилых людей, в том числе соматически неблагополучных. Разработанные схемы перевода больных с ле чения зипрасидоном с инъекционной на пероральную форму препарата позволяют обеспечить фармакологическую преемственность терапии без потери эффективности лечения.

The purpose of this study was to develop and evaluate a new formulation of ziprasidone (ZIP) for improved fasted state absorption and sustained drug release. ZIP solid dispersions were produced via spray drying using Soluplus®, an amphiphilic polymer, as the solubility enhancer. Physicochemical analysis proved that ZIP presented at amorphous state in the spray-dried microparticles and the dissolution rate of ZIP from the Soluplus®-ZIP composite microparticles was significantly increased compared with that of the physical mixtures. Commonly used encapsulation materials including Eudragit® RL, Eudragit® S100 and Ethyl Cellulose were incorporated into the solid dispersions to regulate the drug release kinetics. The formulation containing ethyl cellulose provided the most sustained release behaviors. Pharmacokinetic studies in beagle dogs confirmed that there was no significant difference in oral bioavailability of the microparticles under fasted and fed states, and a prolonged Tmax value was simultaneously achieved compared with the commercial ZIP capsules. [ABSTRACT FROM AUTHOR]

Vlad, not his real name, a 15 year old boy with an autism spectrum disorder and intellectual disability, was referred for psychiatric consultation due to aggression and other behavioural problems. He presented for initial psychiatric consultation on five psychotropic medications with associated severe obesity. A systematic deprescribing and crosstapering plan was implemented, removing all five psychotropic medications (which included olanzapine and quetiapine) and introducing ziprasidone. These changes were associated with a 44.8kg weight loss with no behavioral deterioration and overall lower rates of aggression. Vlad’s case may typify important deficiencies in the service system which create a context that allows for aggressive psychotropic polypharmacy without apparent concomitant increase in sophistication of behavioral management design and support, while also tolerating substantial treatment adverse effects (e.g., medication induced severe obesity) within a member of a vulnerable population (e.g., a youth with developmental disability in care). Suggestions to address some of these contextual factors are outlined. [ABSTRACT FROM AUTHOR]

Introduction The aim of this double-blind randomized study was to evaluate the response to antipsychotic treatment in schizophrenia patients with predicted high/low risk of nonresponse identified by applying a set of well-established scales and predictors of outcome and to compare efficacy between ziprasidone and haloperidol. Methods One hundred twelve schizophrenia patients (ziprasidone: n=54; haloperidol: n=58) were rated weekly on the Positive and Negative Syndrome Scale for Schizophrenia (PANSS), the Global Assessment of Functioning Scale (GAF), the Social and Occupational Functioning Scale (SOFAS), the Simpson-Angus Scale (SAS), and Hillside Akathisia Scale (HAS). Results Ninety-two patients (82%) were predicted to have a high risk of nonresponse. No significant difference regarding PANSS improvement in this subsample was found comparing ziprasidone and haloperidol (p=0.563). Also, for the total patient sample, no significant difference was found regarding the course of the PANSS total score, GAF (p=0.921), and SOFAS (p=0.658) between ziprasidone and haloperidol. Haloperidol resulted in higher scores on the SAS (p=0.001) and HAS (p=0.011). Discussion An alarmingly high number of patients were at high risk of nonresponse to antipsychotic treatment. [ABSTRACT FROM AUTHOR]

Aims: Pregnancy is associated with physiological changes that alter the pharmacokinetics (PK) of drugs. The aim of this study was to predict the PK of ziprasidone in pregnant women. Methods: A full physiologically‐based pharmacokinetic (PBPK) model of ziprasidone was developed and validated for the non‐pregnant population (healthy adults, paediatrics, geriatrics), and this was extended to the pregnant state to assess the change in PK profile of ziprasidone throughout pregnancy. Results: The PBPK model successfully predicted the ziprasidone disposition in healthy adult volunteers, wherein the predicted and observed AUC, Cmax and tmax were within the fold‐difference of 0.94–1.09, 0.89–1.40 and 0.80–1.08, respectively. The paediatric and geriatric population, also showed predicted AUC, Cmax and tmax within a two‐fold range of the observed values. The simulated exposure in pregnant women using a p‐PBPK model showed no significant difference when compared to non‐pregnant women. Conclusions: The PBPK model predicted the impact of physiological changes during pregnancy on PK and exposure of ziprasidone, suggesting that dose adjustment is not necessary in this special population. [ABSTRACT FROM AUTHOR]

OBJECTIVES An increasing number of pediatric patients with psychiatric chief complaints present to emergency departments (EDs) nationwide. Many of these patients require treatment with antipsychotic medications to treat agitation. We sought to examine the use of antipsychotic medications in pediatric patients presenting to a tertiary care pediatric ED. METHODS We performed a retrospective electronic medical record review of patients presenting to a tertiary care pediatric hospital from January 2009 through February 2016 with a psychiatric chief complaint who received an antipsychotic medication in the ED. RESULTS A total of 229 patients were identified, 54.1% of whom were male. Mean age was 14.4 ± 2.6 years. Commonly administered medications included olanzapine (51.1%), aripiprazole (26.6%), haloperidol (24.0%), and risperidone (11.8%). Eighty-seven patients (38.0%) were given at least 1 intravenous or intramuscular dose of antipsychotic medication. A total of 113 patients (49.3%) received only 1 antipsychotic medication, 65 (28.4%) received 2, 30 (13.1%) received 3, and 21 (9.2%) received 4 or more antipsychotics. Median length of stay (minutes) increased significantly with increasing number of medications administered (p < 0.001). Length of stay was significantly shorter in patients given only oral medications (675.6 minutes, IQR 418-1194) compared to those given at least one intramuscular or intravenous dose (951 minutes, IQR 454-1652) (p = 0.014). CONCLUSIONS In this retrospective series, the majority of patients were treated with newer oral antipsychotics. Administration of multiple medications was associated with a significantly longer length of stay in the ED, as was parenteral administration of antipsychotics. [ABSTRACT FROM AUTHOR]

Objective An important clinical question is how many patients with acute schizophrenia do not respond to antipsychotics despite being treated for adequate time and with an effective dose. However, up to date, the exact extent of the phenomenon remains unclear. Methods We calculated the nonresponse and nonremission percentages using individual patient data from 16 randomized controlled trials (RCTs). Six thousand two hundred twenty-one patients were assigned to one antipsychotic (amisulpride, flupenthixol, haloperidol, olanzapine, quetiapine, risperidone, or ziprasidone) at an adequate dose; the response was assessed at 4–6 weeks. As various definitions of nonresponse have been used in the literature, we applied 4 different cut-offs covering the whole range of percent Positive and Negative Syndrome Scale (PANSS)/Brief Psychiatric Rating Scale (BPRS) reduction (≤0%, <25%, <50%, <75%).For symptomatic remission, we used the definition proposed by Andreasen without employing the time criterion. Results The overall nonresponse for the cut-off of ≤0% PANSS/BPRS reduction was 19.8% (18.8%–20.8%); for the cut-off of <25% reduction it was 43% (41.7%–44.3%); for the cut-off of <50% reduction it was 66.5% (65.3%–67.8%); and for the cut-off of <75% reduction it was 87% (86%–87.9%). The overall percentage of no symptomatic remission was 66.9% (65.7%–68.1%). Earlier onset of illness, lower baseline severity and the antipsychotic used were significantly associated with higher nonresponse percentages. Conclusions Nonresponse and nonremission percentages were notably high. Nevertheless, the patients in our analysis could represent a negative selection since they came from short-term RCTs and could have been treated before study inclusion; thus, further response may not have been observed. Observational studies on this important question are needed. [ABSTRACT FROM AUTHOR]

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