Abstract
The depot antipsychotics are synthesized by esterification of the active drug to a long chain fatty acid and theresultant compound is then dissolved in a vegetable oil, with the exception of some molecules of new generationcharacterized by microcrystalline technologies. The absorption rate constant is slower than the elimination rate constantand therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of theabsorption rate, and the concentration at steady-state is a function of the elimination rate The pharmacokinetics of depotantipsychotic medications are such that an intramuscular injection given at intervals from 1 to 4 weeks will produceadequate plasma concentrations that are sufficient to prevent relapse over the dosage interval. Such medication is useful inpatients who do not reliably take their oral medication. The pharmacokinetics and clinical actions of various depotformulations of antipsychotic drugs have been extensively studied. The clinical pharmacokinetics of the depotantipsychotics for which plasma level studies are available (i.e. fluphenazine enanthate and decanoate, haloperidoldecanoate, bromperidol decanoate, clopenthixol decanoate, flupenthixol decanoate, perphenazine onanthat, pipotiazineundecylenate, pipotiazine palmitate, fluspirilene, Long-acting injectable risperidone, olanzapine pamoate, paliperidonepalmitate, Long-acting iloperidone, Long-acting injectable aripiprazole) are reviewed. The proper study of these agentshas been handicapped until recently by the necessity of accurately measuring subnanomolar concentrations in plasma.Their kinetic properties, the relationship of plasma concentrations to clinical effects, and conversion from oral toinjectable therapy are discussed.
Keywords:Absorption, antipsychotics, kinetics, long-acting, plasma level, relapse.
Current Clinical Pharmacology
Title:The Pharmacokinetics of Long-Acting Antipsychotic Medications
Volume: 9Issue: 3
Author(s):Stefano Spanarello and Teresa La Ferla
Affiliation:
Keywords:Absorption, antipsychotics, kinetics, long-acting, plasma level, relapse.
Abstract: The depot antipsychotics are synthesized by esterification of the active drug to a long chain fatty acid and theresultant compound is then dissolved in a vegetable oil, with the exception of some molecules of new generationcharacterized by microcrystalline technologies. The absorption rate constant is slower than the elimination rate constantand therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of theabsorption rate, and the concentration at steady-state is a function of the elimination rate The pharmacokinetics of depotantipsychotic medications are such that an intramuscular injection given at intervals from 1 to 4 weeks will produceadequate plasma concentrations that are sufficient to prevent relapse over the dosage interval. Such medication is useful inpatients who do not reliably take their oral medication. The pharmacokinetics and clinical actions of various depotformulations of antipsychotic drugs have been extensively studied. The clinical pharmacokinetics of the depotantipsychotics for which plasma level studies are available (i.e. fluphenazine enanthate and decanoate, haloperidoldecanoate, bromperidol decanoate, clopenthixol decanoate, flupenthixol decanoate, perphenazine onanthat, pipotiazineundecylenate, pipotiazine palmitate, fluspirilene, Long-acting injectable risperidone, olanzapine pamoate, paliperidonepalmitate, Long-acting iloperidone, Long-acting injectable aripiprazole) are reviewed. The proper study of these agentshas been handicapped until recently by the necessity of accurately measuring subnanomolar concentrations in plasma.Their kinetic properties, the relationship of plasma concentrations to clinical effects, and conversion from oral toinjectable therapy are discussed.
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Cite this article as:
Spanarello Stefano and Ferla La Teresa, The Pharmacokinetics of Long-Acting Antipsychotic Medications, Current Clinical Pharmacology 2014; 9 (3) .https://dx.doi.org/10.2174/15748847113089990051
| DOI https://dx.doi.org/10.2174/15748847113089990051 | Print ISSN 1574-8847 |
| Publisher Name Bentham Science Publisher | Online ISSN 2212-3938 |
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