Adherence and Long-Acting Injectable Antipsychotics in Schizophrenia: An Update

Mohr, Pavel; Volavka, Jan

doi:10.5350/dajpn20122504001

Cited by 4 publications

(7 citation statements)

References 49 publications

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“…All benefits of antipsychotic medication are attenuated or directly invalidated by a crucial problem in the long‐term schizophrenia treatment: partial or complete non‐adherence with medication. Various sources report the rate of 40%‐50% schizophrenia patients who are non‐adherent; 50%‐55% of all hospitalisations can be attributed to non‐adherence . Relapse following discontinuation of medication reduces treatment response, contributes to unfavourable course and outcome of illness, it has a severe negative impact on patients, their carers, and the whole health and social system .…”

Section: Introductionmentioning

confidence: 99%

“…Increasing evidence suggests that long‐acting injectable antipsychotics (LAI), also called “depot,” can play an important role in improving adherence to antipsychotic medication . The advantage of LAI in comparison with oral formulations was not apparent in randomised controlled trials, perhaps because these tend to exclude non‐adherent patients .…”

Section: Introductionmentioning

confidence: 99%

“…Various sources report the rate of 40%-50% schizophrenia patients who are non-adherent; 50%-55% of all hospitalisations can be attributed to non-adherence. 11 Relapse following discontinuation of medication reduces treatment response, contributes to unfavourable course and outcome of illness, it has a severe negative impact on patients, their carers, and the whole health and social system. 12 The causal link between drug withdrawal and relapse/recurrence of illness cannot be overlooked.…”

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confidence: 99%

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Long-acting injectable antipsychotics for prevention and management of violent behaviour in psychotic patients

et al. 2017

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Long-acting injectable antipsychotics for prevention and management of violent behaviour in psychotic patients

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“…Depot agents have a number of advantages over oral medication, including stabilization of serum drug levels, avoidance of first‐pass metabolism, and assured medication delivery . In contrast to the expected 40–50% of non‐adherent patients receiving oral antipsychotic drugs, the non‐adherent rate dropped to less than 10% in patients treated with LAI antipsychotics …”

Section: Introductionmentioning

confidence: 99%

“…7,8 In contrast to the expected 40-50% of non-adherent patients receiving oral antipsychotic drugs, 9 the non-adherent rate dropped to less than 10% in patients treated with LAI antipsychotics. 10 RBP-7000 has been designed to be a sustained-release (once-monthly injection for subcutaneous administration) formulation of risperidone using the ATRIGEL 1 Delivery system. This biodegradable polymer drug delivery system uses an in situ poly-DL-lactide-co-glycolide (PLGH) implant formed by subcutaneous (SC) injection of a viscous, liquid formulation that forms an implant upon contact with tissue fluids.…”

Section: Introductionmentioning

confidence: 99%

A model‐based approach to characterize the population pharmacokinetics and the relationship between the pharmacokinetic and safety profiles of RBP‐7000, a new, long‐acting, sustained‐released formulation of risperidone

Goméni

Heidbreder

Fudala

et al. 2013

The Journal of Clinical Pharma

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RBP-7000 is a sustained-release (once-monthly injection for subcutaneous administration) formulation of risperidone using the ATRIGEL® Delivery System, developed for treatment of schizophrenia to address compliance issues associated with oral administration. The objective of this analysis was to report the results of a population pharmacokinetic analysis and to describe the relationship between risperidone and 9-hydroxyrisperidone levels with dopamine (DA) D2-receptor occupancy, prolactin levels, and adverse events using data collected in 45 clinically stable schizophrenic patients receiving RBP-7000 in single ascending doses (risperidone) of 60, 90, and 120 mg. The population PK model accounted for an initial peak, a delayed and slow delivery, the disposition of risperidone, and the conversion of risperidone to 9-hydroxyrisperidone. BMI was a covariate affecting absorption of risperidone and ultimately formation of 9-hydroxyrisperidone. A logistic analysis indicated a correlation between the increase in Active Moiety (risperidone + 9-OH-risperidone) exposure (Cmax ) and the probability of observing GI disorders. An Emax population PK/prolactin model best described the relationship between the circulating Active Moiety and the serum prolactin levels. Gender was a significant covariate associated with Emax . These data provided a comprehensive characterization of the relationship between circulating Active Moiety and the efficacy/safety profile of RBP-7000 in clinically stable schizophrenic patients.

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Striatal Dopamine D2 Receptor Occupancy Induced by Daily Application of Blonanserin Transdermal Patches: Phase II Study in Japanese Patients With Schizophrenia

Nishibe

Tateno

Sakayori

et al. 2020

International Journal of Neuropsychopharmacology

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Background Transdermal antipsychotic patch formulations offer potential benefits, including improved adherence. This study investigated the striatal dopamine D2 receptor occupancy with daily blonanserin transdermal patch application. Methods This open-label, Phase 2 study enrolled 18 Japanese outpatients (20 to <65 years) with schizophrenia (DSM-IV-TR criteria; total Positive and Negative Syndrome Scale [PANSS] score <120 at screening) treated with blonanserin 8 mg or 16 mg tablets. Patients continued tablets for 2-4 weeks at their current dose and were then assigned to once-daily blonanserin patches (10/20/40/60/80 mg daily) for 2-4 weeks based on the oral dose. [ 11C]raclopride PET scanning determined blonanserin striatal dopamine D2 receptor occupancy (primary endpoint). Secondary endpoints included assessment of receptor occupancy by dose, changes in PANSS and CGI-S scores, patient attitudes towards adherence, and patch adhesiveness. Results Of 18 patients who started the blonanserin tablet treatment period, 14 patients completed treatment. Mean D2 receptor occupancy for blonanserin tablets 8 mg/day (59.2%, n=5) and 16 mg/day (66.3%, n=9) was within the values for blonanserin patches: 10 mg/day (33.3%, n=3), 20 mg/day (29.9%, n=2), 40 mg/day (61.2%, n=3), 60 mg/day (59.0%, n=3), and 80 mg/day (69.9%, n=3). Occupancy generally increased with increasing blonanserin dose for both formulations with the half maximal receptor occupancy for tablets and patches associated with doses of 6.9 mg/day and 31.9 mg/day, respectively. Diurnal variability in occupancy was lower during transdermal patch treatment than during tablet treatment. Blonanserin transdermal patches were well tolerated with no major safety concerns. Conclusions Blonanserin patches (40/80 mg/day) have lower diurnal variability in occupancy than blonanserin tablets (8/16 mg/day) and patches at doses of 40 mg/day and 80 mg/day appear to be suitable alternative for blonanserin tablets at doses of 8 mg and 16 mg/day, respectively. Blonanserin patches represent a potential new treatment option for patients with schizophrenia.

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Adherence and Long-Acting Injectable Antipsychotics in Schizophrenia: An Update

Cited by 4 publications

References 49 publications

Long-acting injectable antipsychotics for prevention and management of violent behaviour in psychotic patients

Long-acting injectable antipsychotics for prevention and management of violent behaviour in psychotic patients

A model‐based approach to characterize the population pharmacokinetics and the relationship between the pharmacokinetic and safety profiles of RBP‐7000, a new, long‐acting, sustained‐released formulation of risperidone

Striatal Dopamine D2 Receptor Occupancy Induced by Daily Application of Blonanserin Transdermal Patches: Phase II Study in Japanese Patients With Schizophrenia

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