2011Expert Opinion on Drug Metabolism & ToxicologyRequires access

Pharmacokinetics and metabolism update for some recent antipsychotics

Silvio Caccia

Open publisher page 38 citations

Abstract

INTRODUCTION: The search for drugs that reduce psychotic symptoms, with minimal adverse effects, has led to the development of new agents that act somewhat differently from their older antipsychotic counterparts. These agents, which include aripiprazole, lurasidone and perospirone, act by targeting both D₂ and 5-HT(1A) receptors, in addition to other characteristic receptors. AREAS COVERED: This article covers the pharmacokinetics and metabolism of aripiprazole, perospirone, lurasidone and cariprazine. The review also describes the effects of physiological and pathological variables on these drugs as well as potential drug interactions. The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents. EXPERT OPINION: Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not. We await the results of future practical effectiveness trials of these new antipsychotics and their follow-on derivatives to learn more about their benefit/risk profile compared with established antipsychotics. It is hoped that some of these newer antipsychotics will not only increase the range of pharmacotherapeutic options, but decisively improve the expectations of psychotherapy for schizophrenia.

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What this paper is about

INTRODUCTION: The search for drugs that reduce psychotic symptoms, with minimal adverse effects, has led to the development of new agents that act somewhat differently from their older antipsychotic counterparts. These agents, which include aripiprazole, lurasidone and perospirone, act by targeting both D₂ and 5-HT(1A) receptors, in addition to other characteristic receptors. AREAS COVERED: This article covers the pharmacokinetics and metabolism of aripiprazole, perospirone, lurasidone and cariprazine. The review also describes the effects of physiological and pathological variables on these drugs as well as potential drug interactions. The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents. EXPERT OPINION: Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not. We await the results of future practical effectiveness trials of these new antipsychotics and their follow-on derivatives to learn more about their benefit/risk profile compared with established antipsychotics. It is hoped that some of these newer antipsychotics will not only increase the range of pharmacotherapeutic options, but decisively improve the expectations of psychotherapy for schizophrenia.

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Available abstract

INTRODUCTION: The search for drugs that reduce psychotic symptoms, with minimal adverse effects, has led to the development of new agents that act somewhat differently from their older antipsychotic counterparts. These agents, which include aripiprazole, lurasidone and perospirone, act by targeting both D₂ and 5-HT(1A) receptors, in addition to other characteristic receptors. AREAS COVERED: This article covers the pharmacokinetics and metabolism of aripiprazole, perospirone, lurasidone and cariprazine. The review also describes the effects of physiological and pathological variables on these drugs as well as potential drug interactions. The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents. EXPERT OPINION: Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not. We await the results of future practical effectiveness trials of these new antipsychotics and their follow-on derivatives to learn more about their benefit/risk profile compared with established antipsychotics. It is hoped that some of these newer antipsychotics will not only increase the range of pharmacotherapeutic options, but decisively improve the expectations of psychotherapy for schizophrenia.

Key concepts: Lurasidone, Aripiprazole, Pharmacokinetics, Antipsychotic, Medicine, Schizophrenia (object-oriented programming), Adverse effect, Pharmacology

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