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Bioconversion and P-gp-Mediated Transport of Depot Fluphenazine Prodrugs after Intramuscular Injection.

J Pharm Sci

July 2023

Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto, Japan; Daiichi University of Pharmacy, Fukuoka, Japan. Electronic address:

Fluphenazine (FPZ) decanoate, an ester-type prodrug formulated as a long-acting injection (LAI), is used in the treatment of schizophrenia. FPZ enanthate was also developed as an LAI formulation, but is no longer in use clinically because of the short elimination half-life of FPZ, the parent drug, after intramuscular injection. In the present study, the hydrolysis of FPZ prodrugs was evaluated in human plasma and liver to clarify the reason for this difference in elimination half-lives.

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Introduction: Many psychiatric, long-acting injectable (LAI) medications are available, and each product comes with its own unique challenges. Improper administration can lead to pain, decreased efficacy, and loss of trust in the patient-provider relationship. This study was conducted to determine if a pharmacist-led, 1-hour training was successful in increasing psychiatric LAI medication knowledge through a pretest and posttest.

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Background: Depot antipsychotics are commonly used to improve adherence and clinical outcomes such as relapse and readmission. Dosing regimens vary but are commonly two- and four-weekly. To date, the effect of administration at two-weekly or four-weekly intervals on outcome has not been examined in a meta-analysis.

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Fluphenazine decanoate (depot) and enanthate for schizophrenia.

Cochrane Database Syst Rev

February 2015

Enhance Reviews Ltd, Central Office, Cobweb Buildings, The Lane, Lyford, Wantage, UK, OX12 0EE.

Background: Intramuscular injections (depot preparations) offer an advantage over oral medication for treating schizophrenia by reducing poor compliance. The benefits gained by long-acting preparations, however, may be offset by a higher incidence of adverse effects.

Objectives: To assess the effects of fluphenazine decanoate and enanthate versus oral anti-psychotics and other depot neuroleptic preparations for individuals with schizophrenia in terms of clinical, social and economic outcomes.

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[A history of antipsychotic long-acting injections in the treatment of schizophrenia].

Encephale

February 2015

Centre hospitalier, 27, rue du 4(e)-RSM, 68250 Rouffach, France. Electronic address:

From a historical perspective, this article describes the use of antipsychotic long-acting injections (LAI) in the treatment of schizophrenia, a disorder that was defined in the final years of the 19th century. An efficient treatment for schizophrenia was discovered only in 1952 with the introduction of chlorpromazine, a phenothiazine derivative. Fairly soon, antipsychotics became available as LAI.

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