Role of sublingual asenapine in treatment of schizophrenia.
Article Details
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Citrome L
Role of sublingual asenapine in treatment of schizophrenia.
Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26.
- PubMed ID
- 21655346 [ View in PubMed]
- Abstract
Asenapine tablets are a new option for the treatment of schizophrenia. Sublingual administration is essential because bioavailability if ingested is less than 2%. Efficacy is supported by acute and long-term randomized controlled studies conducted by the manufacturer, with asenapine 5 mg twice daily evidencing superiority over placebo in six-week studies of acute schizophrenia, and flexibly-dosed asenapine (modal dose 10 mg twice daily) superior to placebo in a 26-week maintenance of response study. Tolerability advantages over some second-generation antipsychotics, such as olanzapine, include a relatively favorable weight and metabolic profile, as demonstrated in a 52-week randomized, head-to-head, double-blind clinical trial. Although dose-related extrapyramidal symptoms and akathisia can be present, the frequency of these effects is lower than that for haloperidol and risperidone. Somnolence may also occur, and appears to be somewhat dose-dependent when examining rates of this among patients receiving asenapine for schizophrenia and bipolar disorder. Prolactin elevation can occur, but at a rate lower than that observed for haloperidol or risperidone. Unique to asenapine is the possibility of oral hypoesthesia, occurring in about 5% of participants in the clinical trials. Obstacles to the use of asenapine are the recommendations for twice-daily dosing and the need to avoid food or liquids for 10 minutes after administration, although the bioavailability is only minimally reduced if food or liquids are avoided for only two minutes.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Asenapine 5-hydroxytryptamine receptor 1B Protein Humans UnknownAntagonistDetails Asenapine 5-hydroxytryptamine receptor 2A Protein Humans YesAntagonistDetails Asenapine 5-hydroxytryptamine receptor 2B Protein Humans UnknownAntagonistDetails Asenapine 5-hydroxytryptamine receptor 2C Protein Humans UnknownAntagonistDetails Asenapine 5-hydroxytryptamine receptor 5A Protein Humans UnknownAntagonistDetails Asenapine 5-hydroxytryptamine receptor 6 Protein Humans UnknownAntagonistDetails Asenapine 5-hydroxytryptamine receptor 7 Protein Humans UnknownAntagonistDetails Asenapine Dopamine D1 receptor Protein Humans UnknownAntagonistDetails Asenapine Dopamine D2 receptor Protein Humans YesAntagonistDetails Asenapine Dopamine D3 receptor Protein Humans UnknownAntagonistDetails Asenapine Dopamine D4 receptor Protein Humans UnknownAntagonistDetails Asenapine Histamine H1 receptor Protein Humans UnknownAntagonistDetails Asenapine Histamine H2 receptor Protein Humans UnknownAntagonistDetails - Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Asenapine Cytochrome P450 1A2 Protein Humans UnknownSubstrateDetails Asenapine Cytochrome P450 2D6 Protein Humans UnknownSubstrateInhibitorDetails