Asenapine for the treatment of bipolar disorder

Marazziti, Donatella; Mucci, Federico; Falaschi, Valentina; Dell’Osso, Liliana

doi:10.1080/14656566.2019.1617849

Cited by 7 publications

(3 citation statements)

References 66 publications

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“…However, she soon stopped all drugs and began to suffer every year from two to three episodes characterized by mixed features that were quite resistant to common therapeutic strategies, as it is generally the case. 17,18 Since during the last hospitalization she showed an elevated fever paralleled by alterations of unspecific peripheral inflammatory markers, as well as by EEG abnormalities suggestive of VPA intoxication, she underwent a MRI that revealed the presence of an initial frontal-temporal cerebral atrophy, as supported also by lower CSF β-amyloid concentrations.…”

Section: Discussionmentioning

confidence: 99%

Effectiveness of clozapine, oxcarbazepine and rivastigmine combination in a bipolar disorder patient with initial cerebral atrophy

Morana¹,

Mucci

Baroni

et al. 2020

Clinical Case Reports

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Section: Discussionmentioning

confidence: 99%

Effectiveness of clozapine, oxcarbazepine and rivastigmine combination in a bipolar disorder patient with initial cerebral atrophy

Morana¹,

Mucci

Baroni

et al. 2020

Clinical Case Reports

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“…ASE exhibits its pharmacological effects by acting on serotonergic, dopaminergic, alpha-adrenergic, and histaminergic receptors. Having these pharmacological properties, it has been shown to have anti-anxiety, anti-stress, sedative, and anti-depressant properties (Grossini et al 2014;Marazziti et al 2019;Marston et al 2009;Vieta and Montes 2018). ASE has also been shown to improve phencyclidineinduced object recognition deficiency in rats due to its antagonistic properties on the dopamine d1 receptor (Snigdha et al 2011).…”

Section: Introductionmentioning

confidence: 99%

Investigation of efficacy of asenapine on passive avoidance learning and memory and oxidative stress in animal model of seizure-induced with pentylenetetrazole

Farhadi,

Mirazi,

Hosseini

2022

Acta Biol Szeged

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Asenapine (ASE) has been used for treatment of bipolar disorder. There is also evidence that it may be useful in the treatment of neurodegenerative disorders. In this regard, the efficacy of ASE in an experimental model of seizure and memory impairment caused by seizures in rats has been investigated in the present study. Seizures in male Wistar rats (200-250 g) were induced by pentylenetetrazole (PTZ, 60 mg/kg, intraperitoneally (i.p.)), and the anticonvulsant effect of ASE (0.5 and 1 mg/kg, i.p.) was evaluated. The effect on memory was assessed using passive avoidance (PA) test in a shuttle box apparatus. After behavioral tests, the animals underwent deep anesthesia and were euthanized painlessly. Serum was isolated for oxidative stress assays (nitric oxide (NO), and glutathione (GSH)). Intraperitoneal injection of ASE decreased the mean number of myoclonic jerks and duration of generalized tonic clonic seizures (GTCS) and increased the mean latency of myoclonic jerk and GTCS compared to the PTZ group. Moreover, in the PA test, ASE caused a significant increase in retention latency (RL) and total time spent in the light compartment (TLC) compared to the PTZ group. Biochemical tests showed that ASE was able to significantly increase GSH serum levels and significantly reduce NO serum levels compared to the PTZ group. Overall, this study suggests the potential neuroprotective effects of ASE in a model of memory impairment caused by seizures via the mechanism of inhibition of the oxidative stress pathway.

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“…Asenapine is a novel atypical antipsychotic drug approved for the treatment of schizophrenia, ameliorating both positive and negative symptoms [ 24 , 25 , 26 , 27 ]. Asenapine has been also recommended for the treatment of manic/mixed episodes with or without psychotic features associated with bipolar I disorder, such as manic-depressive bipolar disorder [ 28 , 29 , 30 ]. As asenapine is a tetracyclic member of the dibenzooxepinopyrroles, derived from the tetracyclic antidepressant mianserin, it would be expected to have also an antidepressant effect [ 31 , 32 ].…”

Section: Introductionmentioning

confidence: 99%

The Influence of Long-Term Treatment with Asenapine on Liver Cytochrome P450 Expression and Activity in the Rat. The Involvement of Different Mechanisms

2021

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Therapy of schizophrenia requires long-term treatment with a relevant antipsychotic drug to achieve a therapeutic effect. The aim of the present study was to investigate the influence of prolonged treatment with the atypical neuroleptic asenapine on the expression and activity of rat cytochrome P450 (CYP) in the liver. The experiment was carried out on male Wistar rats. Asenapine (0.3 mg/kg s.c.) was administered for two weeks. The levels of CYP mRNA protein and activity were determined in the liver and hormone concentrations were measured in the pituitary gland and blood serum. Asenapine significantly decreased the activity of CYP1A (caffeine 8-hydroxylation and 3-N-demethylation), CYP2B, CYP2C11 and CYP3A (testosterone hydroxylation at positions 16β; 2α and 16α; 2β and 6β, respectively). The neuroleptic did not affect the activity of CYP2A (testosterone 7α-hydroxylation), CYP2C6 (warfarin 7-hydroxylation) and CYP2E1 (chlorzoxazone 6-hydroxylation). The mRNA and protein levels of CYP1A2, CYP2B1, CYP2C11 and CYP3A1 were decreased, while those of CYP2B2 and CYP3A2 were not changed. Simultaneously, pituitary level of growth hormone-releasing hormone and serum concentrations of growth hormone and corticosterone were reduced, while that of triiodothyronine was enhanced. In conclusion, chronic treatment with asenapine down-regulates liver cytochrome P450 enzymes, which involves neuroendocrine mechanisms. Thus, chronic asenapine treatment may slow the metabolism of CYP1A, CYP2B, CYP2C11 and CYP3A substrates (steroids and drugs). Since asenapine is metabolized by CYP1A and CYP3A, the neuroleptic may inhibit its own metabolism, therefore, the plasma concentration of asenapine in patients after prolonged treatment may be higher than expected based on a single dose.

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Asenapine for the treatment of bipolar disorder

Cited by 7 publications

References 66 publications

Effectiveness of clozapine, oxcarbazepine and rivastigmine combination in a bipolar disorder patient with initial cerebral atrophy

Effectiveness of clozapine, oxcarbazepine and rivastigmine combination in a bipolar disorder patient with initial cerebral atrophy

Investigation of efficacy of asenapine on passive avoidance learning and memory and oxidative stress in animal model of seizure-induced with pentylenetetrazole

The Influence of Long-Term Treatment with Asenapine on Liver Cytochrome P450 Expression and Activity in the Rat. The Involvement of Different Mechanisms

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