Which role for brexpiprazole, a new dopamine D2 partial agonist, in the treatment of schizophrenia?

Citrome, Leslie

doi:10.1136/eb-2015-102143

Cited by 2 publications

(3 citation statements)

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“…Newer atypical antipsychotics have been developed in an attempt to increase treatment efficacy and reduce side effects. Newer atypical antipsychotics include brexpiprazole, cariprazine, and aripiprazole, which bind to 5-HT receptors and also act as partial agonists at the D2 receptor [ 64 - 66 ]. These drugs differ from each other in DA and 5-HT receptor binding affinities, treatment efficacy, and side-effect profiles [ 66 ].…”

Section: Schizophreniamentioning

confidence: 99%

“…These drugs differ from each other in DA and 5-HT receptor binding affinities, treatment efficacy, and side-effect profiles [ 66 ]. Carpiprazine has a stronger affinity for the D2 and 5-HT1A receptors compared to aripiprazole and brexpiprazole [ 64 ]. When schizophrenia patients are assessed on the Positive and Negative syndrome Scale (PANSS), aripiprazole treatment results in the greatest reduction of scores compared to brexpiprazole and cariprazine [ 67 ].…”

Section: Schizophreniamentioning

confidence: 99%

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Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity

Tuplin

Holahan

2017

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Background: The treatment of schizophrenia is challenging due to the wide range of symptoms (positive, negative, cognitive) associated with the disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) are a common occurrence. Atypical antipsychotics targeting 5-HT2A and D2 receptors are more effective at treating cogni-tive and negative symptoms compared to typical antipsychotics, but these drugs also result in side-effects such as metabolic syndromes.Objective: To identify evidence in the literature that elucidates the pharmacological profile of aripiprazole.Methods: We searched PubMed for peer reviewed articles on aripiprazole and its clinical efficacy, side-effects, pharmacolo-gy, and effects in animal models of schizophrenia symptoms.Results: Aripiprazole is a newer atypical antipsychotic that displays a unique pharmacological profile, including partial D2 agonism and functionally selective properties. Aripiprazole is effective at treating the positive symptoms of schizophrenia and has the potential to treat negative and cognitive symptoms at least as well as other atypical antipsychotics. The drug has a favorable side-effect profile and has a low propensity to result in EPS or metabolic syndromes. Animal models of schizophrenia have been used to determine the efficacy of aripiprazole in symptom management. In these instanc-es, aripiprazole resulted in the reversal of deficits in extinction, pre-pulse inhibition, and social withdrawal. Because aripipra-zole requires a greater than 90% occupancy rate at D2 receptors to be clinically active and does not produce EPS, this suggests a functionally selective effect on intracel-lular signaling pathways.Conclusion: A combination of factors such as dopamine system stabilization via partial agonism, functional selectivity at D2 receptors, and serotonin-dopamine system interaction may contribute to the ability of aripiprazole to successfully manage schizophrenia symptoms. This review examines these mechanisms of action to further clarify the pharmacological actions of aripiprazole.

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Section: Schizophreniamentioning

confidence: 99%

Section: Schizophreniamentioning

confidence: 99%

Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity

Tuplin

Holahan

2017

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“…Poszczególne leki różnią się powinowactwem wobec receptorów dopaminowych i serotoninowych oraz profilem skuteczności i działań niepożądanych (Frankel i Schwartz, 2017). Kariprazyna charakteryzuje się silniejszym powinowactwem do D 2 i 5-HT 1A w porównaniu z arypiprazolem i brekspiprazolem (Citrome, 2016). Niemniej jednak w badaniach pacjentów chorujących na schizofrenię zaobserwowano większą redukcję punktacji w skali oceny objawów pozytywnych i negatywnych (Positive and Negative Syndrome Scale, PANSS) w trakcie terapii arypiprazolem w porównaniu z kariprazyną i brekspiprazolem (Citrome, 2015).…”

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Aripiprazole – therapeutic efficacy and safety in everyday practice

Nowakowska¹,

Kaźmierski²

2019

PSYCHIATR. PSYCHOL. KLIN.

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Arypiprazol wyróżnia się wśród leków przeciwpsychotycznych unikatowym mechanizmem działania: jako częściowy agonista receptorów D 2 i 5-HT 1A i agonista receptorów 5-HT 2A , wykazuje zdolność do "stabilizacji dopaminowej". Umożliwia kontrolę zarówno pozytywnych, jak i negatywnych oraz poznawczych objawów schizofrenii. Wskazania zawarte w charakterystyce produktu leczniczego obejmują również epizody maniakalne o nasileniu umiarkowanym do ciężkiego w przebiegu zaburzenia afektywnego dwubiegunowego typu I u dorosłych i młodzieży od 13. roku życia w leczeniu trwającym do 12 tygodni oraz zapobieganie nowym epizodom maniakalnym u dorosłych, u których występują głównie epizody maniakalne i którzy odpowiedzieli na leczenie arypiprazolem. Jak wskazują badania kliniczne, jest to lek dobrze tolerowany w porównaniu z innymi neuroleptykami. Stosowanie arypiprazolu wiąże się z relatywnie niskim ryzykiem wystąpienia objawów pozapiramidowych i nie zwiększa ryzyka pojawienia się zespołu metabolicznego. W piśmiennictwie można znaleźć opisy przypadków, w których dodanie arypiprazolu do innego neuroleptyku wpłynęło na redukcję sedacji, hipersomnii, ślinotoku, wzrostu masy ciała, dyslipidemii i dysfunkcji seksualnych. Dzięki dostępności różnych form preparatów arypiprazol może być stosowany także u pacjentów w stanach pobudzenia i katatonii, z problemami z przełykaniem czy przy uporczywym braku współpracy. Słowa kluczowe: arypiprazol, schizofrenia, choroba afektywna dwubiegunowa, przypadki kliniczneAripiprazole differs from other antipsychotics in its unique mechanism of action: as a partial D 2 and 5-HT 1A agonist and a 5-HT 2A antagonist, it acts as a dopamine system stabiliser. The drug allows controlling positive, negative and cognitive symptoms of schizophrenia. The indications in the summary of product characteristics also include treatment of up to 12 weeks of mild-tosevere manic episodes in type 1 bipolar affective disorder in adults and adolescents aged ≥13 years as well as prevention of new manic episodes in adults who experienced predominantly manic episodes and responded to aripiprazole treatment. Clinical trials have shown that the drug is well-tolerated compared to other neuroleptics. Aripiprazole therapy involves a relatively low risk of extrapyramidal symptoms and does not increase the risk of metabolic syndrome. Case reports where combining aripiprazole with another neuroleptic reduced sedation, hypersomnia, drooling, weight gain, dyslipidaemia and sexual dysfunction may be found in literature. Since the drug is available in different forms, it may be also used in agitated, catatonic or persistently uncooperative patients as well as in patients with swallowing problems.

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Which role for brexpiprazole, a new dopamine D2 partial agonist, in the treatment of schizophrenia?

Cited by 2 publications

References 4 publications

Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity

Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity

Aripiprazole – therapeutic efficacy and safety in everyday practice

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