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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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Efficacy of typical and atypical antipsychotics for primary and comorbid anxiety symptoms or disorders: a review.

J Clin Psychiatry

September 2006

Department of Psychiatry, the Bipolar Disorders Research Center, University Hospitals of Cleveland/Case Western Reserve University, School of Medicine, Cleveland, Ohio, USA.

Objective: The efficacy of antipsychotics in the treatment of primary or comorbid anxiety disorders or anxiety symptoms in major depressive disorder or bipolar disorder was reviewed.

Data Sources: English-language literature cited in MEDLINE from January 1, 1968, to December 31, 2005, was searched with the keywords anxiety disorder, anxiety symptoms, generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, posttraumatic stress disorder, social phobia, bipolar disorder, major depressive disorder, Hamilton Rating Scale for Anxiety, antipsychotics, typical antipsychotics, atypical antipsychotics, fluphenazine, haloperidol, perphenazine, pimozide, thiothixene, trifluoperazine, loxapine, molindone, chlorpromazine, mesoridazine, thioridazine, fluspirilene, penfluridol, pipothiazine, flupenthixol, clozapine, olanzapine, risperidone, quetiapine, ziprasidone, aripiprazole, amisulpride, and clinical trial. Randomized, double-blind, placebo-controlled trials and open-label studies with a minimum of 20 subjects with a DSM-III/IV or ICD-10 diagnosis of anxiety disorder and studies without a DSM-III/IV or ICD-10 diagnosis of anxiety disorder but with Hamilton Rating Scale for Anxiety (HAM-A) scores as an outcome were prioritized.

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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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[Neuroleptics with prolonged action].

Neurol Neurocir Psiquiatr

November 1978

In the last twenty years, the study of long-acting neuroleptic drugs has been active and promising progress in maintenance of psychotic patients. At present, there are several long-acting derivatives of phenothiazines, e.g.

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