Side Effects of cariprazine: A Synthesis of Findings from 24 Studies

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Original Abstract of the Article

Main research findings

Cariprazine is a novel antipsychotic drug that has shown promise in treating schizophrenia and bipolar disorder. 22 12 14 10 It is unique in its mechanism of action, acting as a partial agonist at both the dopamine D2 and D3 receptors, with a higher affinity for the D3 receptor. 22 12 14 10 This unique profile has been linked to its effectiveness in treating both positive and negative symptoms of schizophrenia. 22 14 4 10 It has also demonstrated effectiveness in treating acute manic episodes in bipolar disorder. 12 19 A notable benefit of cariprazine is its lower tendency to cause weight gain and metabolic abnormalities compared to some older antipsychotics. 16 24 22 6 12 11

Reasons for side effects

Cariprazine's mechanism of action, specifically its partial agonism at dopamine D2 and D3 receptors, can contribute to the development of side effects. 8 9

Common side effects

Akathisia

Cariprazine can cause akathisia, a condition characterized by restlessness and a feeling of inner unease. 22 12 19 3 2

Extrapyramidal symptoms

Cariprazine may lead to extrapyramidal symptoms, which include muscle stiffness, tremors, and difficulty with movement. 22 12 19 2

Nausea

Nausea and other digestive issues can be experienced while taking cariprazine. 12 19

Headache

Headaches are a potential side effect of cariprazine treatment. 19

Constipation

Cariprazine can cause constipation as a side effect. 19

Dyspepsia

Dyspepsia, or indigestion, can also be a side effect of cariprazine. 19

Countermeasures for side effects

Akathisia

If akathisia develops, it is important to consult your doctor. They may adjust your dosage, consider switching to a different medication, or recommend other treatment options. 3

Extrapyramidal symptoms

Similar to akathisia, if extrapyramidal symptoms emerge, discuss these with your doctor. They may adjust your treatment plan, potentially reducing the dosage or exploring alternative medications. 3

Comparison between studies

Commonalities between studies

Multiple studies have shown that cariprazine can be effective in treating schizophrenia and bipolar disorder. 22 12 19 14 Furthermore, there is a consistent finding that cariprazine may be less likely to cause significant weight gain and metabolic abnormalities compared to some other antipsychotics. 16 24 22 12

Differences between studies

Variations exist in the reported effectiveness and side effects of cariprazine across different research studies. 22 12 19 14

Precautions for application in real life

While cariprazine holds potential for treating schizophrenia and bipolar disorder, it is important to be aware of the potential side effects. 22 12 19 14 Before starting treatment, it is crucial to discuss the risks and management of potential side effects with your doctor to make an informed decision. 22 12 19 14

Limitations of current research

The research on cariprazine is still ongoing and more studies are needed to fully understand its long-term effects and its interactions with other medications. 22 12 19 14

Future research directions

Future research should focus on gathering more extensive data on the long-term effectiveness of cariprazine, particularly in terms of its impact on quality of life and functional outcomes. 22 12 19 14 Further investigation into its interactions with other medications is also crucial for ensuring safe and effective use. 22 12 19 14

Conclusion

Cariprazine holds potential as a promising new antipsychotic treatment for schizophrenia and bipolar disorder. 22 12 19 14 It is essential to be aware of potential side effects and to work closely with your doctor to manage your treatment effectively. 22 12 19 14

Literature analysis of 24 papers
Positive Content
22
Neutral Content
0
Negative Content
2
Article Type
0
1
2
9
19
1.

Efficacy and Safety of Cannabidiol in Epilepsy: A Systematic Review and Meta-Analysis.

Author: LattanziSimona, BrigoFrancesco, TrinkaEugen, ZaccaraGaetano, CagnettiClaudia, Del GiovaneCinzia, SilvestriniMauro

Anti-seizure properties
Abuse liability

Cannabidiol (CBD), a non-psychoactive component of Cannabis sativa, shows promise as a new therapeutic option for epilepsy. CBD exhibits anti-seizure properties through multiple mechanisms, including modulation of ionic channels and neurotransmitter transporters.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Meta-AnalysisA statistical technique that integrates the results of multiple studies to draw more general conclusions about a particular issue.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

3.

Pathophysiology and management of Akathisia 70 years after the introduction of the chlorpromazine, the first antipsychotic.

Author: ZareifopoulosN, KatsarakiM, StratosP, VilliotouV, SkaltsaM, DimitriouA, KarveliM, EfthimiouP, LagadinouM, VelissarisD

Akathisia

Akathisia, a distressing side effect of psychiatric drugs characterized by restlessness and an inability to sit still, is commonly associated with antipsychotic drugs that block dopamine D2 receptors. However, akathisia has also been reported with other drugs like SSRIs, SNRIs, stimulants, and mirtazapine.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

4.

Case Report: Functional and Symptomatic Improvement With Cariprazine in Various Psychiatric Patients: A Case Series.

Author: VannucchiTommaso, TaddeucciCostanza, TatiniLorenzo

Alleviate symptoms
Improved functioning
Well-tolerated
Sedation
Weight gain

This case series highlights the effectiveness of cariprazine, a third-generation antipsychotic, in treating various psychiatric disorders, including bipolar disorder and psychosis, while offering good tolerability and improving daily functioning in patients.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

7.

The role of kinetic context in apparent biased agonism at GPCRs.

Author: Klein HerenbrinkCarmen, SykesDavid A, DonthamsettiPrashant, CanalsMeritxell, CoudratThomas, ShonbergJeremy, ScammellsPeter J, CapuanoBen, SextonPatrick M, CharltonSteven J, JavitchJonathan A, ChristopoulosArthur, LaneJ Robert

Pathway-specific drugs

Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes. This study found that kinetic context can have a profound influence on the apparent bias of a series of agonists for the dopamine D2 receptor.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

The role of dopamine D<sub>3</sub> receptors in the mechanism of action of cariprazine.

Author: CalabreseFrancesca, TaraziFrank I, RacagniGiorgio, RivaMarco A

Schizophrenia treatment

Cariprazine is a new atypical antipsychotic drug (APD) that shows partial agonism at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors, and antagonism at the 5-HT2B receptor. It may be particularly effective for treating the negative symptoms and cognitive deficits of schizophrenia by targeting the dopamine D3 receptor. In animal models, cariprazine has been shown to improve anhedonia and cognitive deficits.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

9.

Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.

Author: ChenZhangcheng, FanLuyu, WangHuan, YuJing, LuDengyu, QiJianzhong, NieFen, LuoZhipu, LiuZhen, ChengJianjun, WangSheng

Antidepressant activity
Antipsychotic activity
Cognitive improvement
Motor side effects

This study presents crystal structures of aripiprazole and cariprazine bound to a serotonin receptor (5-HT<sub>2A</sub>R). These structures shed light on how these drugs bind to different receptors and their varying effects. The study suggests that a new drug design can achieve antipsychotic effects without side effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

Case series: Cariprazine in early-onset schizophrenia.

Author: IvanovaElena, MaslinkovaDesislava, PolnarevaNadia, MilanovaVihra

Negative symptom treatment

This article presents two cases of young patients with predominantly negative symptoms of schizophrenia who experienced improvement after switching to cariprazine from atypical antipsychotics. Cariprazine is a novel partial agonist of D3 and D2 receptors with good tolerability and efficacy in treating schizophrenic symptoms, particularly negative symptoms.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

13.

The Treatment of Adult Bipolar Disorder with Aripiprazole: A Systematic Review.

Author: MuneerAther

Manic episode prevention
Manic episode treatment
Mixed episode prevention
Mixed episode treatment

Aripiprazole is a novel antipsychotic that is effective in the treatment of bipolar disorder. It is well-studied and has been shown to be effective in the treatment and prophylaxis of manic and mixed episodes, but has no effectiveness in acute and recurrent bipolar depression.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

14.

Novel D<sub>2</sub>/5-HT receptor modulators related to cariprazine with potential implication to schizophrenia treatment.

Author: JuzaRadomir, VojtechovaIveta, Stefkova-MazochovaKristyna, DehaenWim, PetrasekTomas, PrchalLukas, KobrlovaTereza, JanousekJiri, VlcekPremysl, MezeiovaEva, SvozilDaniel, KarasovaJana Zdarova, PejchalJaroslav, StarkHolger, SatalaGrzegorz, BojarskiAndrzej J, KubackaMonika, MogilskiSzczepan, RandakovaAlena, MusilekKamil, SoukupOndrej, KorabecnyJan

Cognitive function
Schizophrenia treatment
Side effects

This study presents the design, synthesis, and biological evaluation of 1,4-disubstituted aromatic piperazines as potential multi-target ligands for the treatment of schizophrenia. Two compounds, 21 and 24, showed promising activity as dopamine type 2 receptor antagonists and moderate 5-HT3 receptor antagonists.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

16.

Clinical pharmacology of atypical antipsychotics: an update.

Author: MauriM C, PalettaS, MaffiniM, ColasantiA, DragognaF, Di PaceC, AltamuraA C

Antipsychotic treatment
Weight management

This review summarizes the clinical pharmacology and pharmacodynamic data related to atypical antipsychotics, including clozapine, risperidone, paliperidone, olanzapine, quetiapine, amisulpride, ziprasidone, aripiprazole, asenapine, iloperidone, lurasidone and cariprazine. It also provides a summary of their acute pharmacokinetic properties. Four new second-generation antipsychotics are available: iloperidone, asenapine, lurasidone and in the next future cariprazine. These new agents are advisable for the lower propensity to give weight gain and metabolic abnormalities compared with older second-generation antipsychotics. Lurasidone seems to be best in terms of minimizing unwanted alterations in body weight and metabolic variables. Therapeutic drug monitoring is not strictly necessary for all of the new antipsychotic drugs because there are no unequivocal data supporting a relationship between plasma drug levels and clinical outcomes or side effects. The exception can be represented by clozapine for which plasma levels of 350-420 ng/ml are reported to be associated with an increased probability of a good clinical response. Also for olanzapine an established therapeutic range (20-50 ng/ml) is proposed to yield an optimal response and minimize side effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

17.

D<sub>2</sub> Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine.

Author: ShenYudao, McCorvyJohn D, MartiniMichael L, RodriguizRamona M, PogorelovVladimir M, WardKaren M, WetselWilliam C, LiuJing, RothBryan L, JinJian

D2R activation

Compound 38 (MS1768), a potent partial agonist, was discovered as a G<sub>i/o</sub>-biased D<sub>2</sub> receptor agonist that selectively activates the G<sub>i/o</sub> pathway over β-arrestin2. In in vivo studies, compound 38 showed high D<sub>2</sub>R receptor occupancy in mice and effectively inhibited phencyclidine-induced hyperlocomotion.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

19.

Clinical potential of cariprazine in the treatment of acute mania.

Author: AltınbaşKürşat, GuloksuzSinan, OralEsat Timuçin

Bipolar disorder treatment
Schizophrenia treatment
Akathisia
Extrapyramidal symptoms

Cariprazine, a novel antipsychotic with dopamine D2 and D3 receptor antagonist-partial agonist properties, has shown effectiveness in treating schizophrenia and acute manic episodes associated with bipolar disorder. While it has a favorable side effect profile, including minimal weight gain and metabolic disturbances, it is associated with a higher incidence of akathisia and tremor.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

22.

[Cariprazine for acute and maintenance treatment of schizophrenia].

Author: SpoelstraS K, VisserL, KnegteringH

Schizophrenia treatment
Akathisia
Extrapyramidal effects

Cariprazine, a D3 receptor partial agonist, offers a unique approach to schizophrenia treatment. Its long half-life may allow for non-daily dosing. It showed effectiveness against positive and negative symptoms, with extrapyramidal symptoms being a common side effect.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : Dutch

23.

A review of the pharmacology, efficacy and tolerability of recently approved and upcoming oral antipsychotics: an evidence-based medicine approach.

Author: CitromeLeslie

Antipsychotic treatment
Akathisia
Extrapyramidal side effects
Metabolic abnormalities
QTc prolongation
Somnolence
Weight gain

Newly approved oral antipsychotics, including iloperidone, asenapine, and lurasidone, offer potential benefits over existing agents but differ in their side effect profiles. Lurasidone appears to minimize weight gain and metabolic abnormalities, while other agents have varying effects on QT interval, akathisia, and sedation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

24.

Clinical Pharmacokinetics of Atypical Antipsychotics: An Update.

Author: MauriMassimo Carlo, PalettaSilvia, Di PaceChiara, ReggioriAlessandra, CirnigliaroGiovanna, ValliIsabel, AltamuraAlfredo Carlo

Improved efficacy
Side effects

Therapeutic drug monitoring (TDM) is being explored for second-generation antipsychotics to improve efficacy and manage side effects. The review examines the clinical pharmacokinetic data for various antipsychotics, proposing optimal plasma concentration ranges for some drugs and highlighting the need for further research on others.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

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