Literature DB >> 35233132

Cariprazine pharmacokinetics.

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Abstract

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Year:  2022        PMID: 35233132      PMCID: PMC8882455          DOI: 10.18773/austprescr.2022.005

Source DB:  PubMed          Journal:  Aust Prescr        ISSN: 0312-8008


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In the new drug comment Cariprazine hydrochloride for schizophrenia there is a possible error.1 The comment ‘when deciding which drug to prescribe for controlling acute schizophrenia, it may be a consideration that cariprazine takes five days to reach 90% of its steady-state concentration’ could be misleading. The product information states ‘Cariprazine has two pharmacologically active metabolites with similar activities as cariprazine, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR). Total cariprazine (sum of cariprazine + DCAR and DDCAR) exposure approaches 50% of steady state exposure in ~ 1 week of daily dosing while 90% of steady state is achieved in 3 weeks’. While the steady-state concentration of the parent compound may be reached in a week, that of the pharmacologically active metabolites (similar potency to parent compound) will take significantly longer. Among the papers considered by the Editorial Executive Committee when discussing the new drug comment on cariprazine1a was the Australian Public Assessment Report published by the Therapeutic Goods Administration. When assessing population pharmacokinetics, this states that the ‘Median time to achieve 90% steady state for cariprazine and the metabolite DCAR was 5 days, and 21 days for the metabolite DDCAR’. The time to steady state will indeed be longer if all three molecules are considered. From a practical perspective, it is probably cariprazine and desmethyl cariprazine that contribute to the early effects of the drug.2
  2 in total

Review 1.  Treating schizophrenia with cariprazine: from clinical research to clinical practice. Real world experiences and recommendations from an International Panel.

Authors:  Andrea Fagiolini; José Ángel Alcalá; Thomas Aubel; Wojciech Bienkiewicz; Mats Magnus Knut Bogren; Joaquim Gago; Giancarlo Cerveri; Michael Colla; Francisco Collazos Sanchez; Alessandro Cuomo; Frieling Helge; Eduardo Iacoponi; Per-Axel Karlsson; Pradeep Peddu; Mauro Pettorruso; Henrique Jorge Ramos Pereira; Johan Sahlsten Schölin; Ingo Bernd Vernaleken
Journal:  Ann Gen Psychiatry       Date:  2020-09-26       Impact factor: 3.455

Review 2.  Cariprazine hydrochloride for schizophrenia.

Authors: 
Journal:  Aust Prescr       Date:  2021-09-01
  2 in total

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