Long-Acting Injectable Risperidone: Efficacy and Safety of the First Long-Acting Atypical Antipsychotic

Kane, John M.; Eerdekens, Mariëlle; Lindenmayer, Jean-Pierre; Keith, Samuel J.; Lesem, Michael D.; Karcher, Keith

doi:10.1176/appi.ajp.160.6.1125

Cited by 413 publications

(289 citation statements)

References 30 publications

(22 reference statements)

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“…Long-acting depot antipsychotic agents may improve long-term outcomes, especially among patients who frequently forget to take their medications or refuse treatment because of lack of insight. However, currently only one second-generation antipsychotic agent, risperidone, has a depot formulation available, and it must be administered once every 2 weeks (Gefvert et al, 2005;Kane et al, 2003;Remington et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

D2 Receptor Occupancy of Olanzapine Pamoate Depot Using Positron Emission Tomography: An Open-label Study in Patients with Schizophrenia

Mamo

Kapur

Keshavan

et al. 2007

Neuropsychopharmacol

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A long-acting depot formulation of olanzapine that sustains plasma olanzapine concentrations for over a month after a single injection is currently under development. This multicenter, open-label study explored D 2 receptor occupancy of a fixed dose of olanzapine pamoate (OP) depot given every 4 weeks. Patients (nine male, five female) with schizophrenia or schizoaffective disorder previously stabilized on oral olanzapine were switched to OP depot 300 mg by intramuscular injection every 4 weeks for 6 months. No visitwise within-group significant changes were found in Brief Psychiatric Rating Scale Total or Clinical Global Impressions-Severity of Illness scores, although seven patients received oral olanzapine supplementation during the first four injection cycles. To minimize impact on D 2 occupancy, positron emission tomography (PET) scans were not completed during injection cycles that required supplemental oral olanzapine. Two patients reported transient injection site adverse events, which did not result in discontinuation. The most frequently reported treatmentemergent adverse events were insomnia, aggravated psychosis, and anxiety. Mean striatal D 2 receptor occupancy, as measured by [ 11 C]-raclopride PET, was 69% on oral olanzapine (5-20 mg/day) and 50% (trough) on OP depot at steady state. Following an initial decline, occupancy returned to 84% of baseline oral olanzapine occupancy after six injections. Over the study period, D 2 receptor occupancy and plasma olanzapine concentrations were significantly correlated (r ¼ 0.76, Pp0.001). OP depot resulted in mean D 2 receptor occupancy of approximately 60% or higher at the end of the 6-month study period, a level consistent with antipsychotic efficacy and found during treatment with oral olanzapine. However, supplemental oral olanzapine or another dosing strategy may be necessary to maintain adequate therapeutic response during the first few injection cycles.

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Section: Introductionmentioning

confidence: 99%

D2 Receptor Occupancy of Olanzapine Pamoate Depot Using Positron Emission Tomography: An Open-label Study in Patients with Schizophrenia

Mamo

Kapur

Keshavan

et al. 2007

Neuropsychopharmacol

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“…Table 1 lists currently marketed formulations, indications for use, and duration of action. These depot formulations can deliver a sustained dose in vivo for varying periods of time, from weeks to months, [1][2][3][4][5][6] primarily owing to low degradation rates of the bulk eroding PLA and PLGA polymers.…”

Section: Introductionmentioning

confidence: 99%

A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres

2005

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The purpose of this study was to determine the feasibility of applying accelerated in vitro release testing to correlate or predict long-term in vitro release of leuprolide poly(lactideco-glycolide) microspheres. Peptide release was studied using a dialysis technique at 37°C and at elevated temperatures (50°C-60°C) in 0.1M phosphate buffered saline (PBS) pH 7.4 and 0.1M acetate buffer pH 4.0. The data were analyzed using a modification of the Weibull equation. Peptide release was temperature dependent and complete within 30 days at 37°C and 3 to 5 days at the elevated temperatures. In vitro release profiles at the elevated temperatures correlated well with release at 37°C. The shapes of the release profiles at all temperatures were similar. Using the modified Weibull equation, an increase in temperature was characterized by an increase in the model parameter, α, a scaling factor for the apparent rate constant. Complete release at 37°C was shortened from 30 days to 5 days at 50°C, 3.5 days at 55°C, 2.25 days at 60°C in PBS pH 7.4, and 3 days at 50°C in acetate buffer pH 4.0. Values for the model parameter β indicated that the shape of the release profiles at 55°C in PBS pH 7.4 (2.740) and 50°C in 0.1M acetate buffer pH 4.0 (2.711) were similar to that at 37°C (2.677). The E a for hydration and erosion were determined to be 42.3 and 19.4 kcal/mol, respectively. Polymer degradation was also temperature dependent and had an E a of 31.6 kcal/mol. Short-term in vitro release studies offer the possibility of correlation with long-term release, thereby reducing the time and expense associated with longterm studies. Accelerated release methodology could be useful in the prediction of long-term release from extended release microsphere dosage forms and may serve as a quality control tool for the release of clinical or commercial batches.

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“…Dentre eles, a natureza e gravidade dos episódios anteriores, o grau de consciência e resposta aos sinais prodrômicos de recaída, a vulnerabilidade aos efeitos adversos e o nível de estresse no ambiente e de apoio (4) .…”

Section: Variação Individual Da Dose E Do Intervalo Entre As Administunclassified

“…A introdução recente de um antipsicótico de nova geração com ação prolongada, risperidona AP (4,47) , abre nova perspectiva e possibilidade de, mais uma vez, melhorar o tratamento da esquizofrenia. O ambiente atual também favorece.…”

Section: Impacto Dos Antipsicóticos De Nova Geração E Perspectiva Comunclassified

Antipsicóticos de ação prolongada no tratamento de manutenção da esquizofrenia. Parte II. O manejo do medicamento, integração da equipe multidisciplinar e perspectivas com a formulação de antipsicóticos de nova geração de ação prolongada

Bechelli

2003

Rev. Latino-Am. Enfermagem

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Nesta segunda parte é abordado, entre os diversos tópicos, a indicação e o início do tratamento, a variação individual da dose e do intervalo entre as administrações, a freqüência das consultas e estratégias na recaída na vigência do tratamento. Considerando-se que a baixa adesão ao tratamento é um dos fatores principais associados à ocorrência de exacerbação da sintomatologia, que os agentes de nova geração, mesmo com menor freqüência de efeitos colaterais extrapiramidais e melhor tolerabilidade de forma geral, não modificaram esta condição em relação aos convencionais e tendo-se em conta a superioridade dos depot em relação aos compostos convencionais administrados v.o., a formulação de medicamentos de nova geração com ação prolongada certamente poderá favorecer a adesão, a regularidade ao tratamento e a prevenção de recaída em pacientes com esquizofrenia. Ao lado destas observações, é de grande importância a participação da família no tratamento, bem como a atitude e a integração da equipe na execução das diversas tarefas.

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Long-Acting Injectable Risperidone: Efficacy and Safety of the First Long-Acting Atypical Antipsychotic

Abstract: Long-acting injectable risperidone was efficacious and well tolerated and provides both clinicians and patients with a new mode of treatment that can improve the outcome of long-term therapy.

Cited by 413 publications

References 30 publications

D2 Receptor Occupancy of Olanzapine Pamoate Depot Using Positron Emission Tomography: An Open-label Study in Patients with Schizophrenia

D2 Receptor Occupancy of Olanzapine Pamoate Depot Using Positron Emission Tomography: An Open-label Study in Patients with Schizophrenia

A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres

Antipsicóticos de ação prolongada no tratamento de manutenção da esquizofrenia. Parte II. O manejo do medicamento, integração da equipe multidisciplinar e perspectivas com a formulação de antipsicóticos de nova geração de ação prolongada

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