Once-monthly paliperidone injection for the treatment of schizophrenia

Delia BisharaPharmacy Department, South London and Maudsley NHS Foundation Trust, London, United KingdomAbstract: Paliperidone palmitate is a new long-acting antipsychotic injection for the treatment of acute and maintenance therapy in schizophrenia. Paliperidone (9-hydroxyrisperidone) is the major...

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Autor principal: Delia Bishara
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Publicado: Dove Medical Press 2010
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spelling oai:doaj.org-article:b457f0bcc8a3435f94ea09d714e9c6a82021-12-02T02:04:06ZOnce-monthly paliperidone injection for the treatment of schizophrenia1176-63281178-2021https://doaj.org/article/b457f0bcc8a3435f94ea09d714e9c6a82010-09-01T00:00:00Zhttp://www.dovepress.com/once-monthly-paliperidone-injection-for-the-treatment-of-schizophrenia-a5180https://doaj.org/toc/1176-6328https://doaj.org/toc/1178-2021Delia BisharaPharmacy Department, South London and Maudsley NHS Foundation Trust, London, United KingdomAbstract: Paliperidone palmitate is a new long-acting antipsychotic injection for the treatment of acute and maintenance therapy in schizophrenia. Paliperidone (9-hydroxyrisperidone) is the major active metabolite of risperidone and acts at dopamine D2 and serotonin 5HT2A receptors. As with other atypical antipsychotics, it exhibits a high 5HT2A:D2 affinity ratio. It also has binding activity as an antagonist at α1- and α2 adrenergic receptors and H1 histaminergic receptors, but has virtually no affinity for cholinergic receptors. Paliperidone palmitate has been shown to be effective in reducing Positive and Negative Syndrome Scale total scores in four short-term trials in acute schizophrenia. It was also effective as maintenance therapy in a long-term trial in which time to recurrence of symptoms was significantly longer in paliperidone-treated patients compared with placebo. In addition, paliperidone was shown to be noninferior to risperidone long-acting injection in one study, but this noninferiority was not established in another longer study comparing the two drugs. Treatment should be initiated with 234 mg on day 1 and 156 mg on day 8, followed by a recommended monthly maintenance dose of 39–234 mg based on efficacy and tolerability. Paliperidone palmitate is generally well tolerated, although it can cause weight gain and a rise in prolactin levels, which is generally greater in women than in men. Overall, paliperidone palmitate may have advantages over other currently available long-acting injections, and therefore may be a useful alternative for the treatment of schizophrenia, although further long-term trials comparing it with active treatments are warranted.Keywords: paliperidone palmitate, injection, schizophrenia, long-acting Delia BisharaDove Medical PressarticleNeurosciences. Biological psychiatry. NeuropsychiatryRC321-571Neurology. Diseases of the nervous systemRC346-429ENNeuropsychiatric Disease and Treatment, Vol 2010, Iss Issue 1, Pp 561-572 (2010)
institution DOAJ
collection DOAJ
language EN
topic Neurosciences. Biological psychiatry. Neuropsychiatry
RC321-571
Neurology. Diseases of the nervous system
RC346-429
spellingShingle Neurosciences. Biological psychiatry. Neuropsychiatry
RC321-571
Neurology. Diseases of the nervous system
RC346-429
Delia Bishara
Once-monthly paliperidone injection for the treatment of schizophrenia
description Delia BisharaPharmacy Department, South London and Maudsley NHS Foundation Trust, London, United KingdomAbstract: Paliperidone palmitate is a new long-acting antipsychotic injection for the treatment of acute and maintenance therapy in schizophrenia. Paliperidone (9-hydroxyrisperidone) is the major active metabolite of risperidone and acts at dopamine D2 and serotonin 5HT2A receptors. As with other atypical antipsychotics, it exhibits a high 5HT2A:D2 affinity ratio. It also has binding activity as an antagonist at α1- and α2 adrenergic receptors and H1 histaminergic receptors, but has virtually no affinity for cholinergic receptors. Paliperidone palmitate has been shown to be effective in reducing Positive and Negative Syndrome Scale total scores in four short-term trials in acute schizophrenia. It was also effective as maintenance therapy in a long-term trial in which time to recurrence of symptoms was significantly longer in paliperidone-treated patients compared with placebo. In addition, paliperidone was shown to be noninferior to risperidone long-acting injection in one study, but this noninferiority was not established in another longer study comparing the two drugs. Treatment should be initiated with 234 mg on day 1 and 156 mg on day 8, followed by a recommended monthly maintenance dose of 39–234 mg based on efficacy and tolerability. Paliperidone palmitate is generally well tolerated, although it can cause weight gain and a rise in prolactin levels, which is generally greater in women than in men. Overall, paliperidone palmitate may have advantages over other currently available long-acting injections, and therefore may be a useful alternative for the treatment of schizophrenia, although further long-term trials comparing it with active treatments are warranted.Keywords: paliperidone palmitate, injection, schizophrenia, long-acting
format article
author Delia Bishara
author_facet Delia Bishara
author_sort Delia Bishara
title Once-monthly paliperidone injection for the treatment of schizophrenia
title_short Once-monthly paliperidone injection for the treatment of schizophrenia
title_full Once-monthly paliperidone injection for the treatment of schizophrenia
title_fullStr Once-monthly paliperidone injection for the treatment of schizophrenia
title_full_unstemmed Once-monthly paliperidone injection for the treatment of schizophrenia
title_sort once-monthly paliperidone injection for the treatment of schizophrenia
publisher Dove Medical Press
publishDate 2010
url https://doaj.org/article/b457f0bcc8a3435f94ea09d714e9c6a8
work_keys_str_mv AT deliabishara oncemonthlypaliperidoneinjectionforthetreatmentofschizophrenia
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