Related Experiment Video

Updated: Jul 17, 2026

Self-Administration of Drugs in Mouse Models of Feeding and Obesity
03:37

Self-Administration of Drugs in Mouse Models of Feeding and Obesity

Published on: June 8, 2021

Prolactin release in children treated with risperidone: impact and role of CYP2D6 metabolism

Pieter W Troost1, Bertine E Lahuis, Mirjam H Hermans

  • 1Department of Psychiatry, University Medical Center Groningen, University of Groningen, The Netherlands. p.troost@accare.nl

Journal of Clinical Psychopharmacology
|January 17, 2007
PubMed

Insights

Risperidone significantly increases prolactin levels in children with pervasive developmental disorders, with no tolerance developing over six months. CYP2D6 ultrarapid metabolism is a risk factor for higher prolactin elevation.

Area of Science:

  • Pharmacogenomics
  • Pediatric Psychiatry
  • Neuroendocrinology

Background:

  • Risperidone is frequently used in children with pervasive developmental disorders.
  • Understanding factors influencing risperidone's side effects, like prolactin elevation, is crucial for pediatric treatment.
  • The role of CYP2D6 genetic variations in this response is not well-established.

Purpose of the Study:

  • To investigate the relationship between CYP2D6 gene polymorphisms and risperidone-induced prolactin release in children.
  • To assess the changes in prolactin levels during risperidone treatment in this population.

Main Methods:

  • Twenty-five children with pervasive developmental disorders were genotyped for CYP2D6 polymorphisms.
  • Serum prolactin, risperidone, and 9-hydroxyrisperidone levels were measured at baseline, 8 weeks, and 24 weeks.
  • Adverse effects were monitored using a clinician-rated survey.

Main Results:

  • Risperidone treatment led to a significant four-fold increase in prolactin levels by week 8, which persisted at week 24.
  • Higher prolactin levels were correlated with higher risperidone dosage per kilogram, more functional CYP2D6 genes, and higher 9-hydroxyrisperidone concentrations.
  • No association was found between prolactin elevation and adverse effects, risperidone concentration, or patient age.

Conclusions:

  • Low-to-intermediate doses of risperidone cause substantial prolactin elevation in children, with no apparent tolerance development within six months.
  • CYP2D6 ultrarapid metabolism appears to be a risk factor for more pronounced prolactin increases in children treated with risperidone.
Abstract

Related Concept Videos

Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance01:23

Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance

The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
A study on guinea pigs examined the...
Pharmacokinetics in Pediatric Patients: Drug Metabolism01:24

Pharmacokinetics in Pediatric Patients: Drug Metabolism

In pediatric care, understanding the nuances of hepatic drug metabolism is crucial, as it significantly differs from that of adults. This divergence is primarily due to the developmental stage of drug-metabolizing enzymes, which affects how medications are processed in the body. In neonates, for instance, the activity of Phase I enzymes—critical for the initial breakdown of drugs—is markedly reduced, functioning at just 20–40% of the levels seen in adults. This reduction poses a challenge in...
Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption01:23

Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption

Understanding the physiological differences in the pediatric population is crucial for effective pharmacotherapy. Neonates, infants, and children exhibit significant variations in gastric pH, gastric emptying time, intestinal transit time, and biliary function. These variations profoundly affect oral drug absorption, necessitating a nuanced approach to pediatric dosing.Neonates present with a unique physiological profile, having a gastric pH greater than 4 and faster and more irregular gastric...
Antipsychotic Drugs: Typical and Atypical Agents01:21

Antipsychotic Drugs: Typical and Atypical Agents

Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
Pharmacokinetics in Pediatric Patients: Drug Distribution01:17

Pharmacokinetics in Pediatric Patients: Drug Distribution

Drug distribution in the pediatric population exhibits unique challenges and considerations due to the physiological differences between children, particularly neonates and infants, and adults. A crucial aspect of pediatric pharmacology is understanding how these differences impact the pharmacokinetics of various drugs, necessitating age-specific dosing strategies to ensure efficacy and safety.Neonates and infants have a higher total body water content, ~75%–90% of their body weight, compared...
Factors Affecting Drug Response: Overview01:21

Factors Affecting Drug Response: Overview

When it comes to infants and young children, they are typically administered smaller doses of medication in comparison to adults. This is primarily because their organ functions still need to fully develop, meaning their bodies are not as efficient at metabolizing or eliminating drugs. Additionally, their blood-brain barrier is more permeable than in adults. As a result, high concentrations of drugs can easily penetrate the central nervous system (CNS), potentially leading to neurological...