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Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown risk associated with the use of Asenapine.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
The first-generation antipsychotics are known as “typical antipsychotics,” including chlorpromazine, chlorprothixene, haloperidol, flupentixol, fluphenazine, mesoridazine, perphen-azine, promazine, promethazine, thioridazine, trifluproma-zinc, and zuclopenthixol (Lieberman et al. 2008). Most of the drugs in the second generation, known as “atypical anti-psychotics,” have been developed. The second-generation antipsychotics include amisulpride, aripiprazole, clozapine, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, and zotepine (Lieberman et al. 2008; Vohora 2007; Worrel et al. 2000). Newer antipsychotic agents, such as asenapine, bifeprunox, norclozapine, and iloperidone, are being developed (Bishara and Taylor 2008). Antipsychotics are generally highly lipid soluble, subject to high clearance, and eliminated by metabolic rather than renal pathways. CYP2D6 is involved in the metabolism of a variety of anti-psychotics, including clozapine, thioridazine, perphenazine, chlorpromazine, fluphenazine, haloperidol, zuclopenthixol, risperidone, iloperidone, and sertindole (Gardiner and Begg 2006; Ingelman-Sundberg 2005; Zhou et al. 2008). CYP1A2 and 3A are also involved in the metabolism of antipsychotic drugs including clozapine, olanzapine, pimozide, and haloperidol (Gardiner and Begg 2006; Ingelman-Sundberg 2005; Zhou et al. 2008). There is preliminary evidence that CYP2D6 phenotype status may affect the clearance of this group and thus alter the clinical response to them.
Life Care Planning for Depressive Disorders, Obsessive-Compulsive Disorder, and Schizophrenia
Published in Roger O. Weed, Debra E. Berens, Life Care Planning and Case Management Handbook, 2018
Beginning with olanzapine in 1999, all of the atypical antipsychotics have FDA approval for the treatment of bipolar disorder with the exception of paliperidone and iloperidone. This includes asenapine, lurasidone, aripiprazole, ziprasidone, risperidone, and quetiapine. The conventional antipsychotic chlorpromazine is indicated for the treatment of bipolar disorder. Traditionally, antipsychotics have been used to treat acute mania and psychotic symptoms. However, there is evidence that they can also treat depressive symptoms and prevent future episodes (Gutman & Nemeroff, 2007; Suppes et al., 2016). Unlike lithium and valproate, atypical antipsychotics do not require serum monitoring. Common side effects associated with the use of atypicals include drowsiness, sedation, dry mouth, constipation, dizziness, orthostatic hypotension, nausea, and possibly extrapyramidal symptoms (but reduced in comparison with conventional antipsychotics). Atypical antipsychotics can have negative metabolic effects such as an increased risk of weight gain, hyperglycemia, diabetes mellitus, and dyslipidemia. It is recommended that clinicians monitor weight, waist circumference, blood pressure, glucose, and lipids regularly in patients taking these medications (Hirschfeld, 2005).
The treatment of acute agitation associated with schizophrenia or bipolar disorder: investigational drugs in early stages of their clinical development, and their clinical context and potential place in therapy
Published in Expert Opinion on Investigational Drugs, 2020
Dexmedetomidine film and intranasal olanzapine are novel formulations of preexisting medications for the management of acute agitation in patients with schizophrenia and bipolar disorder. Although these formulations require patient participation, they are important developments because they offer rapid, IM-like absorption rates without requiring an injection. The most comparable agents with this characteristic currently available are sublingual asenapine and inhalable loxapine. However, asenapine has not been investigated extensively for this indication and is not FDA-approved for this purpose. As for inhaled loxapine, although FDA-approved for agitation associated with schizophrenia or mania, the restrictions in place for use prevent its widespread adoption.
Safety considerations in the psychopharmacology of pediatric bipolar disorder
Published in Expert Opinion on Drug Safety, 2019
Amanda Y Sun, Steven Woods, Robert L Findling, Ekaterina Stepanova
The AEs profile of antipsychotics is different from lithium or anticonvulsants. Aripiprazole is associated with fatigue and dose-dependent increase in EPS, which has led to some cases of discontinuation [33,35]. Aripiprazole may also cause weight gain, but more likely during long-term treatment [35]. Unlike other antipsychotics, aripiprazole may decrease prolactin levels. Conversely, risperidone, quetiapine, and olanzapine may increase prolactin levels, contribute to weight gain and cause greater metabolic abnormalities [11,36,37,39,48]. Ziprasidone is associated with elevation in prolactin level and increased risk for QTc prolongation, but is weight neutral [40]. Treatment with olanzapine is associated with significant weight gain and metabolic changes in laboratory parameters, but not with substantial risk of EPS during acute treatment [39]. A single study of lurasidone shows good AEs profile with low incidence of weight gain, metabolic AEs, or EPS [41]. Asenapine may cause mild weight gain and increased rates of EPS [42]. Additionally, it may lead to orthostatic hypotension and increased suicidal thoughts in youth. Studies available to date show that most medications in the treatment of pediatric BPD have significant AEs, many potentially serious and may lead to discontinuation of treatment. It is a serious concern given the chronicity of BPD and potential need for life-long treatment. Unfortunately, less information is available on long-term treatment of pediatric BPD compared to acute management. It is essential that these studies are conducted to inform clinicians, patients and their families of efficacy and safety of psychopharmacological treatment of youth with BPD.
An update on potential pharmacotherapies for cognitive impairment in bipolar disorder
Published in Expert Opinion on Pharmacotherapy, 2023
Danica E. Johnson, Roger S. McIntyre, Rodrigo B. Mansur, Joshua D. Rosenblat
Asenapine is a second-generation antipsychotic (SGA) approved for treating manic episodes in BD [53]. However, the only study to explore its cognitive effects in bipolar disorder is a two-year observational study of inpatients with BD-II [57]. In the 11 subjects treated with asenapine, small, nonsignificant improvements were made in learning, short-term memory, and recognition tasks [57]. They report that significance may be found with a larger sample size since asenapine is similar to aripiprazole in its partial agonism of the 5-HT1A receptor [58], which has been shown to mediate a procognitive effect [55]. Therefore, these findings will need to be replicated, but this has yet to be done.