Title: An Overview on Cariprazine

Author: Rama Lakshmi Devadi

 DOI: https://dx.doi.org/10.18535/jmscr/v10i1.01

Abstract

Schizophrenia is a serious mental disorder with a long and painful course. It contributes significantly to the worldwide burden of disease caused by mental health conditions. Relapses are common in schizophrenia, and each one worsens clinical symptoms, cognitive impairment, social and vocational performance, and overall quality of life. Cariprazine is a new antipsychotic that acts as a partial D2, D3 receptor agonist with a preference for the D3 receptor over the D2 receptor, whereas many existing antipsychotics favor the D2.The dopamine D3 receptor, in particular, has been proposed as a potential target for the treatment of unipolar depression. When flexibly dosed at 3–9 mg/day for up to 48 weeks, cariprazine was typically safe and well tolerated in patients with schizophrenia. Cariprazine binds with high potency to D3 dopamine, D2 dopamine, and 5HT2B serotonin receptors, but only moderately to 5HT1A and 5HT2A serotonin receptors, a profile that differs from brexpiprazole and aripiprazole.

Keywords: schizophrenia, Cariprazine, dopamine D3 receptor, mental health disorders.

References

  1. Leggio GM, Salomone S, Bucolo C, et al. Dopamine D(3) receptor as a new pharmacological target for the treatment of depression. European journal of pharmacology. 2013 Nov 5;719(1- 3):25-33. doi: 10.1016/j.ejphar.2013.07.022. PubMed PMID: 23872400.
  2. Lacroix LP, Hows ME, Shah AJ, et al. Selective antagonism at dopamine D3 receptors enhances monoaminergic and cholinergic neurotransmission in the rat anterior cingulate cortex. Neuropsychopharmacology: official publication of the American College of Neuropsychopharmacology. 2003 May;28(5):839-49. doi: 10.1038/sj.npp.1300114. PubMed PMID: 12637956.
  3. Strakowski SM, Adler CM, Almeida J, et al. The functional neuroanatomy of bipolar disorder: a consensus model. Bipolar disorders. 2012 Jun;14(4):313-25. doi: 10.1111/j.1399- 5618.2012.01022.x. PubMed PMID: 22631617; PubMed Central PMCID: PMC3874804.
  4. Gyertyan I, Kiss B, Saghy K, et al. Cariprazine (RGH-188), a potent D3/D2 dopamine receptor partial agonist, binds to dopamine D3 receptors in vivo and shows antipsychotic-like and procognitive effects in rodents. Neurochemistry international. 2011 Nov;59(6):925-35. doi: 10.1016/j.neuint.2011.07.002. PubMed PMID: 21767587.
  5. Duric V, Banasr M, Franklin T, et al. Cariprazine Exhibits Anxiolytic and Dopamine D3 ReceptorDependent Antidepressant Effects in the Chronic Stress Model. The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsycho-pharmacologicum. 2017 Oct 1;20(10):788-796. doi: 10.1093/ijnp/pyx038. PubMed PMID: 28531264; PubMed Central PMCID: PMC5632312.
  6. Andrew J. Cutler,1 * Suresh Durgam,2 Yao Wang,3 Raffaele Migliore,2 Kaifeng Lu,2 István Laszlovszky,4 and György Németh4CNS Spectrums (2018), 23, 39–50. © Cambridge University Press 2017. This is an Open Access article, distributed under the terms of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted re-use, distribution, and reproduction in any medium, provided the original work is properly cited.
  7. Department of Clinical Research, Gedeon Richter Plc., Budapest, Hungary, 2 Department of Medical Affairs, Gedeon Richter Plc, Budapest, Hungary, 3 Department of Clinical Research and Development, Mitsubishi Tanabe Pharma Corporation, Tokyo, Japan doi:10.1017/S1092852917000220
  8. Actavis Pharma Inc. Vraylar TM (cariprazine) capsules: US prescribing information. 2017. http://www.allergan.com/. Accessed 28 Apr 2017.
  9. Periclou A, Phillips L, Bihorel S, et al. Characterization of population pharmacokinetics of cariprazine and its major metabolites [abstract no. 104]. In: 169th annual meeting of the American Psychiatric Association. 2016.
  10. Reagila SPC. Reagila [Summary of Product Characteristics]. Update 06/25/2018. https://www.ema. europa.eu/en/documents/product-information/ reagila-epar-product-information_en.pdf. Accessed 4 May 2021
  11. Keks N, Hope J, Schwartz D, et al. Comparative tolerability of dopamine D2/3 receptor partial agonists for schizophrenia. CNS Drugs. 2020;34(5): 473–507.
  12. Calabrese F, Tarazi FI, Racagni G, Riva MA. The role of dopamine D3 receptors in the mechanism of action of cariprazine. CNS Spectr. 2020;25(3): 343–51.
  13. Girgis RR, Slifstein M, D’Souza D, et al. Preferential binding to dopamine D3 over D2 receptors by cariprazine in patients with schizophrenia using PET with the D3/D2 receptor ligand [(11)C]-(?)-PHNO. Psychopharmacology. 2016;233(19–20):3503–12.
  14. Durgam S, Litman RE, Papadakis K, et al. Cariprazine in the treatment of schizophrenia: a proofof-concept trial. Int Clin Psychopharmacol. 2016;31(2):61–8.

Corresponding Author

Rama Lakshmi Devadi

Registered Pharmacist, Bridgeport, Connecticut- 06614