Oral Antipsychotic Update: A Brief Review of New and Investigational Agents for the Treatment of Schizophrenia

CNS Spectrums ◽  
2012 ◽  
Vol 17 (s1) ◽  
pp. 1-9 ◽  
Author(s):  
Leslie Citrome
Keyword(s):  
Second Generation ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Additional Information ◽  
Potential Association ◽  
Second Generation Antipsychotics ◽  
The Us ◽  
Glycine Transport ◽  
Oral Antipsychotic ◽  
Investigational Agents

This narrative review provides an overview of the three new oral second-generation antipsychotics that have become available in the US: iloperidone, asenapine and lurasidone. Although they are associated with less weight gain and fewer metabolic abnormalities than some of the older second-generation antipsychotics, iloperidone, asenapine and lurasidone have differences that make them unique from each other. Examples of these differences include dosing frequency, specific instructions on dosing with food, titration requirements, and potential association with sedation, extrapyramidal side effects, akathisia, and prolongation of the ECG QT interval. Additional information is provided regarding agents in late stage clinical development for the treatment of schizophrenia: cariprazine and brexpiprazole (both are dopamine D2 receptor partial agonists) and bitopertin (a glycine transport inhibitor that may have antipsychotic effects).

scholarly journals Evaluation of oral antipsychotic supplementation of select second-generation long-acting injectable antipsychotics in an acute-care psychiatric setting

2019 ◽  
Vol 9 (1) ◽  
pp. 18-23
Author(s):  
Jennifer N. Alastanos ◽  
Chris Paxos ◽  
Jessica Emshoff
Keyword(s):  
Confidence Interval ◽  
Odds Ratio ◽  
Second Generation ◽  
Patient Specific ◽  
Oral Supplementation ◽  
Psychiatric Setting ◽  
The Us ◽  
Oral Antipsychotic ◽  
Long Acting ◽  
Inpatient Psychiatric Unit

Abstract Introduction Long-acting injectable (LAI) antipsychotics were developed to increase medication adherence in patients with schizophrenia. The US Food and Drug Administration (FDA)-approved LAI dosing provides guidance regarding oral antipsychotic supplementation. Previous studies have concluded concomitant use of oral and LAI antipsychotics requires further investigation. The aim of this study was to examine oral antipsychotic supplementation among patients receiving select second-generation LAIs. Methods Patients were included if they were admitted to an inpatient psychiatric unit and received a second-generation LAI. The primary outcome was to determine the percentage of patients receiving oral antipsychotic supplementation prescribed in accordance with FDA recommendations. Secondary outcomes described oral supplementation prescribed in an inconsistent manner with FDA recommendations and identified patient-specific predictors associated with oral supplementation prescribed consistent with FDA recommendations. Results Of the 422 patients evaluated, 376 patients met inclusion criteria. Oral supplementation was prescribed in a manner consistent with FDA recommendations in 30% of patients. The following predictors were associated with oral supplementation prescribed in accordance with FDA recommendations: LAI initiation (odds ratio 1.868, 95% confidence interval 1.120-3.125) and the use of the once-monthly paliperidone LAI (odds ratio 20.278, 95% confidence interval 10.472-39.873). Discussion In the patient population evaluated, oral supplementation of LAI antipsychotics were prescribed in 30% of patients in a manner consistent with FDA recommendations. Of the patients who were prescribed oral antipsychotic supplementation inconsistent with FDA labeling, 223 patients were prescribed oral supplementation longer than the recommended duration and 8 patients received oral supplementation for a shorter duration than recommended.

scholarly journals Major Depressive Disorder (MDD) and Schizophrenia– Addressing Unmet Needs With Partial Agonists at the D2 Receptor: A Review

2019 ◽  
Vol 22 (10) ◽  
pp. 651-664
Author(s):  
Jasmina Mallet ◽  
Philip Gorwood ◽  
Yann Le Strat ◽  
Caroline Dubertret
Keyword(s):  
Major Depressive Disorder ◽  
Depressive Disorder ◽  
Unmet Needs ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Adjunctive Treatment ◽  
Major Depressive ◽  
Partial Agonism ◽  
Partial Agonists ◽  
Second Generation Antipsychotics

Abstract Second-generation antipsychotics are common candidates for the adjunctive treatment of major depressive disorder and for the treatment of schizophrenia. However, unmet needs remain in the treatment of both disorders. Considering schizophrenia, antipsychotics are the most common treatment and have demonstrated good efficacy. Still, side effects of these treatments are commonly reported and may impact adherence to the medication and functioning in patients with schizophrenia. Regarding major depressive disorder, despite the availability of several classes of antidepressants, many patients do not achieve remission. Adjunctive treatment with antipsychotics may improve clinical and functional outcomes. Compared with dopamine D2 receptor antagonism that is exhibited by most antipsychotics, partial agonism may result in improved outcomes in major depressive disorder and in schizophrenia. Aripiprazole, cariprazine, and brexpiprazole have partial agonism at the dopamine D2 receptor and could potentially overcome limitations associated with D2 antagonism. The objectives of this review were (1) to discuss the goal of treatment with second-generation antipsychotics in major depressive disorder and schizophrenia, and the clinical factors that should be considered, and (2) to examine the short- and long-term existing data on the efficacy and safety of D2 receptor partial agonists (aripiprazole, cariprazine, and brexpiprazole) in the adjunctive treatment of major depressive disorder and in the treatment of schizophrenia.

Effect of amphetamine on dopamine D2 receptor binding in the primate brain with the agonist ligand [11C]MNPA

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S646-S646
Author(s):  
Nicholas Seneca ◽  
Sjoerd Finnema ◽  
Masanori Ichise ◽  
Balazs Gulyas ◽  
Håkan Wikstrom ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Dopamine D2 ◽  
Primate Brain

Assessment of endocrine disorders of the hypothalamicpituitary axis by nuclear medicine techniques

2002 ◽  
Vol 41 (02) ◽  
pp. 80-90 ◽  
Author(s):  
F. Jockenhövel ◽  
P. Theissen ◽  
M. Dietlein ◽  
W. Krone ◽  
H. Schicha ◽  
...  
Keyword(s):  
Nuclear Medicine ◽  
Pituitary Adenomas ◽  
Dopamine D2 Receptor ◽  
Somatostatin Receptor ◽  
D2 Receptor ◽  
Ectopic Acth Syndrome ◽  
Endocrine Disorders ◽  
Ectopic Acth ◽  
Number Of Patients ◽  
Hypothalamic Pituitary Axis

SummaryThe following article reviews nuclear medicine techniques which can be used for assessment of endocrine disorders of the hypothalamic-pituitary axis. For planar and SPECT imaging somatostatin-receptor- and dopamine- D2-receptor-scintigraphy are the most widely distributed techniques. These nuclear medicine techniques may be indicated in selected cases to answer differential diagnostic problems. They can be helpful to search for presence and localization of receptor positive tissue. Furthermore they can detect metastasis in the rare cases of a pituitary carcinoma. Scintigraphy with Gallium-67 is suitable for further diagnostic evaluation in suspected hypophysitis. Other SPECT radiopharmaca do not have relevant clinical significance. F-18-FDG as PET radiopharmacon is not ideal because obvious pituitary adenomas could not be visualized. Other PET radiopharmaca including C-11-methionine, C-11-tyrosine, F-18-fluoroethylspiperone, C-11-methylspiperone, and C-11-raclopride are available in specialized centers only. Overall indications for nuclear medicine in studies for the assessment of endocrine disorders of the hypothalamic-pituitary-axis are rare. Original studies often report only about a small number of patients. According to the authors’ opinion the relevance of nuclear medicine in studies of clinically important endocrinologic fields, e. g. localization of small ACTH-producing pituitary adenomas, tumor localization in ectopic ACTH syndrome, localization of recurrent pituitary tissue, assessment of small incidentalomas, can not be definitely given yet.

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