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Long-acting injectable formulations of antipsychotic drugs for the treatment of schizophrenia

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Abstract

Antipsychotic drugs have been used to treat patients with schizophrenia and other psychotic disorders. Long-acting injectable antipsychotic drugs are useful for improving medication compliance with a better therapeutic option to treat patients who lack insight or adhere poorly to oral medication. Several long-acting injectable antipsychotic drugs are clinically available. Haloperidol decanoate and fluphenazine decanoate are first-generation depot drugs, but the use of these medicines has declined since the advent of second-generation depot agents, such as long-acting risperidone, paliperidone palmitate, and olanzapine pamoate. The second-generation depot drugs are better tolerated and have fewer adverse neurological side effects. Long-acting injectable risperidone, the first depot formulation of an atypical antipsychotic drug, was prepared by encapsulating risperidone into biodegradable microspheres. Paliperidone palmitate is an aqueous suspension of nanocrystal molecules, and olanzapine pamoate is a microcrystalline salt of olanzapine and pamoic acid suspended in aqueous solution. This review summarizes the characteristics and recent research of formulations of each long-acting injectable antipsychotic drug.

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Acknowledgments

This research was financially supported by the Ministry of Knowledge Economy (MKE) and Korea Institute for Advancement in Technology (KIAT) through the Research and Development for Regional Industry. This research was also supported by the leading industry and equipments of the ChungCheong Leading Industry Office of the Korean Ministry of Knowledge.

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Correspondence to Dong Hee Na.

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Eun Ji Park and Sarmila Amatya contributed equally to this work.

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Park, E.J., Amatya, S., Kim, M.S. et al. Long-acting injectable formulations of antipsychotic drugs for the treatment of schizophrenia. Arch. Pharm. Res. 36, 651–659 (2013). https://doi.org/10.1007/s12272-013-0105-7

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