Clinical and plasma level characteristics of intramuscular and oral loxapine

@article{Simpson2004ClinicalAP,
  title={Clinical and plasma level characteristics of intramuscular and oral loxapine},
  author={George M. Simpson and Thomas B. Cooper and J. Hillary Lee and Michael A. Young},
  journal={Psychopharmacology},
  year={2004},
  volume={56},
  pages={225-232}
}
The intramuscular and oral forms of loxapine succinate were compared in their clinical, side effect, and blood level characteristics in ten hospitalized chronic schizophrenic patients. The first phase of the study determined the single dose that produced moderate sedation (i.e., the sedation threshold), and this dose was essentially the same for the two forms. Continuous administration of the two forms using the individualized sedation threshold dosage also failed to indicate any clinical or… Expand
Brain Disposition and Catalepsy After Intranasal Delivery of Loxapine: Role of Metabolism in PK/PD of Intranasal CNS Drugs
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The metabolite 7-hydroxy-loxapine, but not loxAPine, was the main contributor to the catalepsy observed after intranasal and oral loxapines treatment. Expand
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The inhalation of multiple doses of inhaled loxapine were well tolerated in study subjects and provided a safe, well‐tolerated means for rapidly and reliably achieving therapeutic plasma concentrations of loxAPine. Expand
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The inhalation of Staccato loxapine represents a safe, well‐tolerated means for rapidly achieving therapeutic plasma concentrations of loxAPine and no clinically meaningful changes were noted in hematology results, blood chemistry, vital signs, or respiratory function. Expand
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Intramuscular injection of olanzapine may provide substantial benefit in rapidly treating inpatients with acute dementia-related agitation and no significant differences among treatment groups were seen in vital signs, including orthostasis. Expand
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  • 2016
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An overview of a new inhaled formulation of the established antipsychotic loxapine, which aims to provide a more rapidly acting agent for the treatment of acute agitation without the disadvantages of intramuscular or intravenous injection, is presented. Expand
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Characterization of the circulating metabolites for a new chemical entity in humans is essential for safety assessment, an understanding of their contributions to pharmacologic activities, and theirExpand
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In vitro identification of the human cytochrome p450 enzymes involved in the oxidative metabolism of loxapine
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In vitro studies were conducted to identify the hepatic cytochrome P450 (CYP) enzymes responsible for the oxidative metabolism of loxapine to 8‐hydroxyloxabine, 7‐HydroxylOxapine, N‐desmethylloxapines (amoxapin) and loxAPine N‐oxide, and indicated that l oxapine was mainly metabolized by human liver microsomes. Expand
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