Quetiapine Extended Release

Abstract

Quetiapine is an atypical antipsychotic agent with well established efficacy and tolerability in the acute and maintenance treatment of adults with schizophrenia. The extended-release formulation of quetiapine (quetiapine XR) was developed to provide more convenient once-daily administration, as well as allowing simple and rapid dose escalation, with the aim of improving compliance (known to be a substantial issue in patients with schizophrenia). In several short-term clinical trials, oral quetiapine XR 400-800 mg once daily was generally effective across a range of symptoms in the acute treatment of schizophrenia. As a long-term maintenance treatment, quetiapine XR prevented relapse in patients with stable disease, with significantly longer times to relapse in patients treated with quetiapine XR compared with placebo. Quetiapine XR was generally well tolerated in clinical trials. According to pooled results from three 6-week trials, events occurring in >or=5% of quetiapine XR recipients with an incidence>or=2-fold that seen in placebo recipients were dry mouth, somnolence and dizziness. A generally low incidence of extrapyramidal symptoms (EPS) is seen in quetiapine XR recipients. The most common potentially EPS-associated adverse events seen with quetiapine treatment were akathisia, restlessness and tremor. Rates of worsening of Simpson-Angus Scale and Barnes Akathisia Rating Scale scores were not dissimilar among quetiapine XR, quetiapine immediate release and placebo.

Comparison of D2 dopamine receptor occupancy after oral administration of quetiapine fumarate immediate-release and extended-release formulations in healthy subjects

“…Thus, during treatment with clinically recommended doses, it is unlikely that D 2 receptor occupancy reaches the 80% threshold suggested for EPS. This is in agreement with clinical studies showing a low incidence of EPS in quetiapine-treated patients (Baldwin & Scott, 2009; Weiden, 2007). …”

Use of quetiapine XR and quetiapine IR in clinical practice for hospitalized patients with schizophrenia: a retrospective study

“…2009; Barnes and Paton, 2011], real world evidence on the proven efficacy and clinical use of AAPs is clearly lacking [Gorwood, 2006; Altamura and Glick, 2010], as is the case for quetiapine fumarate, an established first-line oral AAP for schizophrenia [Riedel et al . 2007; Baldwin and Scott, 2009]. …”

“…Quetiapine XR is characterized by sustained drug exposure with once-daily dosing, a faster dose titration and different pharmacological and tolerability profiles than quetiapine IR [Peuskens et al . 2007; Baldwin and Scott, 2009; Figueroa et al . 2009; Meulien et al .…”

Change in daytime sleepiness and cognitive function in a 6-month, double-blind study of lurasidone and quetiapine XR in patients with schizophrenia

“…Lurasidone has no appreciable affinity for H 1 and M 1 receptors (Ishibashi et al, 2010). In contrast, quetiapine is associated with a high affinity at the H 1 receptor where it acts as an antagonist (Baldwin and Scott, 2009); this mechanism is associated with sedation in both animal models and human studies (Witek et al, 1995). The short-term effects of lurasidone on neurocognitive performance were demonstrated in a 3-week double-blind, active-controlled study of lurasidone and ziprasidone (Harvey et al, 2011), as well as a 6-week, double-blind, placebo- and active-controlled study of lurasidone and quetiapine XR (Harvey et al, 2013).…”