Asenapine: Pharmacological Aspects and Role in Psychiatric Disorders

Reyad, Ayman Antoun; Mishriky, Raafat

doi:10.24869/psyd.2019.157

Cited by 15 publications

(10 citation statements)

References 14 publications

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“…Current evidence from research examining first-line interventions should guide sequential medication selection (7,9,14,29,(32)(33)(34). Evidence-based antipsychotics for acute agitation include loxapine, haloperidol, droperidol, olanzapine, risperidone, ziprasidone, aripiprazole, and asenapine (13,(35)(36)(37)(38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53). Evidence-based benzodiazepines for acute agitation include midazolam and lorazepam (29,32,33,54,55).…”

Section: Repeated Use Of Emergent Medications: General Considerationsmentioning

confidence: 99%

Which Emergent Medication Should I Give Next? Repeated Use of Emergent Medications to Treat Acute Agitation

2021

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Agitation is a common symptom encountered among patients treated in psychiatric emergency settings. While there are many guidelines available for initial management of the acutely agitated patient, there is a notable dearth of guidelines that delineate recommended approaches to the acutely agitated patient in whom an initial medication intervention has failed. This manuscript aims to fill this gap by examining evidence available in the literature and providing clinical algorithms suggested by the authors for sequential medication administration in patients with persistent acute agitation in psychiatric emergency settings. We discuss risk factors for medication-related adverse events and provide options for patients who are able to take oral medications and for patients who require parenteral intervention. We conclude with a discussion of the current need for well-designed studies that examine sequential medication options in patients with persistent acute agitation.

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Section: Repeated Use Of Emergent Medications: General Considerationsmentioning

confidence: 99%

Which Emergent Medication Should I Give Next? Repeated Use of Emergent Medications to Treat Acute Agitation

2021

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“…Asenapine is rapidly metabolized by the liver via direct glucuronidation by uridine-diphosphoglucuronate glucuronosyl transferase 1A4 (UGT1A4) and oxidative metabolism by cytochrome P450 isoenzymes (predominantly CYP 1A2 and to a lesser degree CYP3A4 and CYP2D6). [11][12][13] First-pass effects exceed 95%, so that bioavailability (F or fraction in general circulation) is < 2% of oral dose. 13,14 Sublingual administration to escape immediate hepatic catabolism and deactivation results in 35% bioavailability in systemic circulation.…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…[11][12][13] First-pass effects exceed 95%, so that bioavailability (F or fraction in general circulation) is < 2% of oral dose. 13,14 Sublingual administration to escape immediate hepatic catabolism and deactivation results in 35% bioavailability in systemic circulation. 13 Peak plasma concentration of sublingual formulation (Cmax) is 4 ng/ mL and occurs within 1 hr (Tmax); 11 elimination half-life (t 1/2 ) is 24 hrs (range 13.4 to 39.2 h).…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…13,14 Sublingual administration to escape immediate hepatic catabolism and deactivation results in 35% bioavailability in systemic circulation. 13 Peak plasma concentration of sublingual formulation (Cmax) is 4 ng/ mL and occurs within 1 hr (Tmax); 11 elimination half-life (t 1/2 ) is 24 hrs (range 13.4 to 39.2 h). [14][15][16] Asenapine is highly bound (95%) to albumin and α 1 -acid glycoprotein.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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<p>Transdermal Asenapine in Schizophrenia: A Systematic Review</p>

Carrithers¹,

El‐Mallakh²

2020

PPA

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Background: Asenapine is a novel antipsychotic that has demonstrated efficacy in controlling psychosis in schizophrenia and mania in bipolar illness. It must be administered as a sublingual formulation because it is nearly completely metabolized in the first pass through the liver. Recently, a transdermal formulation of asenapine has been approved for schizophrenia by the Food and Drug Administration. Methods: A systematic review of transdermal asenapine was done utilizing the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) model. Discussion: There are several formulations of transdermal asenapine but only Secuado ® has been approved for clinical use. Total bioavailability is 35%. Peak plasma concentration (Cmax) is 4 ng/mL and occurs within 1 hr (Tmax); elimination half-life (t 1/2) is 24 hrs (range 13.4 to 39.2 h). Asenapine is highly bound (95%) to albumin and α 1-acid glycoprotein. It has a unique receptor profile in which it functions as an antagonist at multiple receptors with affinity that is higher than D 2 (K i = 1.3) including D 3 , D 4 , 5HT 2A , 5HT 2C , 5HT 2B , 5HT 7 , 5HT 6 , H 1 , and α2. This profile suggests that asenapine may be of particular value off label for bipolar depression, anxiety, and aggression. Transdermal asenapine was only tested in one randomized, placebo-controlled study of acute psychosis in schizophrenia. It was superior to placebo at week 6 with nearly onethird of patients experiencing >30% improvement in total PANSS score which translates in a number needed to treat (NNT) of 9.

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“…Schizophrenia is a chronic psychiatric disorder, where patient's perception and behavior are significantly altered; with diagnosis confirmed by a clinical psychiatrist after full psychiatric assessment (Reyad & Mishriky, 2019). In England, psychotic disorders annual incidence is 32 cases per 100,000 people, 15 of them schizophrenia (Kirkbride et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Efficacy and safety of brexpiprazole in acute management of psychiatric disorders: a meta-analysis of randomized controlled trials

Reyad

Girgis

Mishriky

2020

International Clinical Psychopharmacology

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Brexpiprazole is a new atypical antipsychotic for schizophrenia management and as adjunct in major depressive disorder (MDD). We searched randomized controlledtrials (RCT) to review brexpiprazole efficacy and tolerability in acute management of schizophrenia and MDD using PubMed, EUDRACT, ClinicalTrials.gov and Cochrane Central Register of Controlled-Trials. A meta-analysis was conducted using the identified 14 RCT to assess its efficacy using positive and negative syndrome scale (PANSS), clinical global impressionsseverity of Illness (CGI-S), Personal and Social Performance scale (PSP), Montgomery-Åsberg Depression Rating Scale (MADRS), Sheehan Disability Scale (SDS) and Hamilton Depression Rating Scale (HDRS17). The mean difference (MD) comparing brexpiprazole and placebo were PANSS -4.48, CGI-S -0.23 and PSP 3.24 favoring brexpiprazole. Compared to aripiprazole and quetiapine, brexpiprazole showed similar efficacy. In MDD, brexpiprazole showed efficacy compared to placebo demonstrated by MADRS -1.25, SDS -0.37 and HDRS17 -1.28. Brexpiprazole was associated with side effects including akathisia RR=1.72; weight increase RR=2.74 and somnolence RR=1.87.Compared to 4mg, brexpiprazole 2mg was associated with less risk of akathisia and Somnolence. Brexpiprazole demonstrated significant improvements in schizophrenia and MDD and is well-tolerated; however, associated with akathisia and somnolence. These findings will guide psychiatrists and pharmacists in their clinical role for supporting psychiatric patients care.

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Asenapine: Pharmacological Aspects and Role in Psychiatric Disorders

Cited by 15 publications

References 14 publications

Which Emergent Medication Should I Give Next? Repeated Use of Emergent Medications to Treat Acute Agitation

Which Emergent Medication Should I Give Next? Repeated Use of Emergent Medications to Treat Acute Agitation

<p>Transdermal Asenapine in Schizophrenia: A Systematic Review</p>

Efficacy and safety of brexpiprazole in acute management of psychiatric disorders: a meta-analysis of randomized controlled trials

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