Clinical and plasma level characteristics of intramuscular and oral loxapine

  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},
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
The metabolite 7-hydroxy-loxapine, but not loxAPine, was the main contributor to the catalepsy observed after intranasal and oral loxapines treatment. Expand
Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens
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
Pharmacokinetics of Loxapine Following Inhalation of a Thermally Generated Aerosol in Healthy Volunteers
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
Comparison of Rapidly Acting Intramuscular Olanzapine, Lorazepam, and Placebo: A Double-blind, Randomized Study in Acutely Agitated Patients with Dementia
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
Inhaled loxapine for the urgent treatment of acute agitation associated with schizophrenia or bipolar disorder
  • C. Pollack
  • Medicine
  • Current medical research and opinion
  • 2016
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
Which Metabolites Circulate ? s
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
Possible Manic Side-Effects of Loxapine
  • J. Gojer
  • Psychology, Medicine
  • Canadian journal of psychiatry. Revue canadienne de psychiatrie
  • 1992
The patient had severe reflux esophagitis and presumed peptic ulcer, which was successfully treated with ranitidine, and experienced the onset of galactorrhoea with spontaneous milk let down, followed by what proved to be 26 months of amenorrhea. Expand
Dosing antipsychotics in special populations of patients with schizophrenia: Severe psychotic agitation, first psychotic episode and elderly patients.
Antipsychotic (AP) dosing is well established in nonelderly patients with acute exacerbations of schizophrenia, but not in special populations, and in elderly patients, particularly in older people with dementia-related psychosis. Expand
In vitro identification of the human cytochrome p450 enzymes involved in the oxidative metabolism of loxapine
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
Clinical Pharmacology (Pharmacokinetics)
The present chapter describes the pharmacokinetics of antipsychotic drugs in psychiatric patients and normal human volunteers and the possible relationship between pharmacokinetic data, particularly plasma levels, and clinical effects. Expand


Clinical Pharmacokinetics of Chlordiazepoxide
Oral chlordiazepoxide is rapidly and completely absorbed, but intramuscular injection is painful and results in slow and erratic absorption, which is prolonged in the elderly, in those with cirrhosis, and in those receiving concurrent disulfiram therapy. Expand
A Double‐Blind Comparison of Loxapine Succinate and Trifluoperazine in Newly Admitted Schizophrenic Patients
Loxapine succinate was judged to be an effective treatment for newly admitted schizophrenic patients through a four-week double-blind comparison with trifluoperazine. Expand
The Brief Psychiatric Rating Scale
The Brief Psychiatric Rating Scale was developed to provide a rapid assessment technique particularly suited to the evaluation of patient change. Sixteen symptom constructs which have resulted fromExpand
A modification of an earlier rating scale for extrapyramidal system disturbance is described, and evidence for the validity and reliability of the scale is presented. The usefulness of the scale inExpand
Experimental Design: Procedures for the Behavioral Sciences
Chapter 1. Research Strategies and the Control of Nuisance Variables Chapter 2. Experimental Designs: an Overview Chapter 3. Fundamental Assumptions in Analysis of Variance Chapter 4. CompletelyExpand
Clinical pharmacokinetics of Chlordiazepoxide . In : Pharmacokinetics of psychoactive drugs : blood levels and clinical response , L . A . Gottschalk and S . Merlis , eds . New York : Spectrum
  • 1976