Related Experiment Video
Updated: Jun 12, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Atypical antipsychotic metabolism and excretion
J J Sheehan1, J K Sliwa, J C Amatniek
1Ortho-McNeil Janssen Scientific Affairs, Titusville, New Jersey 08560-0200, USA. jsheeha2@its.jnj.com
Background:
The metabolic/biotransformation pathways of atypical antipsychotics (aripiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, and ziprasidone) have been characterized and reviewed. However, comparisons of excretory pathways remain unexplored.
Objective:
To analyze the excretion profile of atypical antipsychotic agents and compare the overall magnitude of metabolism (changed vs. unchanged drug) and route of excretion (feces vs. urine). Secondary objectives include providing: 1) dosing information in hepatic and renal impairment, and 2) context of the specific enzymes and pathways involved in each agents' biotransformation.
Methods:
Published literature and each manufacturer's radiolabeled drug absorption, distribution, metabolism and excretion data and U.S. prescribing information were reviewed.
Results:
With the exception of paliperidone, atypical antipsychotics undergo extensive metabolism (i.e.,
Conclusions:
Understanding the differences in the elimination profiles of atypical antipsychotics agents may permit better-informed drug and dose selection in special populations such as those with comorbid conditions (e.g. hepatitis, diabetes, end-stage renal disease) or pharmacogenetic variability; or at risk for drug-drug interactions. The use of patient tailored drug and dose-selection may result in greater treatment efficacy and a reduction in adverse events.
Related Concept Videos
Pharmacokinetics in Obese Patients: Drug Metabolism and Excretion
Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance
A study on guinea pigs examined the...
Antipsychotic Drugs: Typical and Atypical Agents
Drug Elimination: Overview
Excretion refers to removing a drug from the body, either in its unchanged form or as its metabolites. Nonvolatile and polar drugs are primarily excreted through the kidneys, with other pathways including bile, sweat, saliva, and milk. Volatile drugs such as anesthetic gases are excreted via the...
Drug Excretion: Miscellaneous Routes
Drug Elimination: Non-Renal Routes
