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Objective: Nonadherence is a major challenge in schizophrenia treatment. While long-acting (depot) antipsychotic medications are often recommended to address adherence problems, evidence on the comparative effectiveness of depot versus oral antipsychotics is inconsistent. We hypothesize that this inconsistency could be due to systematic differences in study design.

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The pharmacokinetics of long-acting antipsychotic medications.

Curr Clin Pharmacol

April 2015

NHS, Health Trust No. 3 Umbria, Mental Health Department, Day Hospital, Via Arcamone s.n.c. 06034 Foligno, Perugia, Italia.

The depot antipsychotics are synthesized by esterification of the active drug to a long chain fatty acid and the resultant compound is then dissolved in a vegetable oil, with the exception of some molecules of new generation characterized by microcrystalline technologies. The absorption rate constant is slower than the elimination rate constant and therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of the absorption rate, and the concentration at steady-state is a function of the elimination rate. The pharmacokinetics of depot antipsychotic medications are such that an intramuscular injection given at intervals from 1 to 4 weeks will produce adequate plasma concentrations that are sufficient to prevent relapse over the dosage interval.

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Tardive dystonia usually occurs with a delay after neuroleptic exposure in patients with major psychosis. A subgroup of patients, however, is given such medication for "mild depression" or "neurasthenia." Tardive dystonia, in general, may respond favorably to pallidal deep brain stimulation (DBS).

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Depot fluspirilene for schizophrenia.

Cochrane Database Syst Rev

January 2007

Cochrane Schizophrenia Group, Academic unit of Psychiatry and Behavioural Sciences, 15 Hyde Terrace, Leeds, UK, LS2 9LT.

Background: Antipsychotic drugs are the mainstay treatment for schizophrenia and similar psychotic disorders. Long-acting depot injections of drugs such as fluspirilene are extensively used as a means of long-term maintenance treatment.

Objectives: To review the effects of depot fluspirilene versus placebo, oral anti-psychotics and other depot antipsychotic preparations for people with schizophrenia in terms of clinical, social and economic outcomes.

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Intramuscular preparations of antipsychotics: uses and relevance in clinical practice.

Drugs

June 2003

Department of Psychiatry, Department of Clinical Sciences Luigi Sacco, University of Milan, Via G.B. Grassi 74, Milan 20157, Italy.

Intramuscular formulations of antipsychotics can be sub-divided into two groups on the basis of their pharmacokinetic features: short-acting preparations and long-acting or depot preparations. Short-acting intramuscular formulations are used to manage acute psychotic episodes. On the other hand, long-acting compounds, also called "depot", are administered as antipsychotic maintenance treatment to ensure compliance and to eliminate bioavailability problems related to absorption and first pass metabolism.

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