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Related Concept Videos

Hepatic Drug Excretion: Enterohepatic Cycling01:17

Hepatic Drug Excretion: Enterohepatic Cycling

Enterohepatic cycling involves the active secretion of drugs and their metabolites into the bile via transporters in the canalicular membrane of hepatocytes. This secretion is an integral part of the digestive process, releasing these substances into the gastrointestinal (GI) tract.
Post-release drugs and metabolites can be reabsorbed into the body from the intestine. For conjugated metabolites like glucuronides, reabsorption requires enzymatic hydrolysis by intestinal microflora. This...
Drug Elimination: Non-Renal Routes01:23

Drug Elimination: Non-Renal Routes

The liver plays a pivotal role in eliminating drugs and their metabolites, primarily through a process known as biliary excretion. This process involves the hepatocytes, the primary cells in the liver that generate bile. A range of transporters actively expels polar drugs or hydrophilic drug metabolites into the bile, which transports the drugs and metabolites into the small intestine. From here, they are eventually expelled from the body through feces. In some instances, the original drug or a...
Introduction to Metabolism01:30

Introduction to Metabolism

Metabolism encompasses all biochemical reactions in a living organism, facilitating both the breakdown and synthesis of biomolecules. These metabolic processes are categorized into catabolic and anabolic pathways, which operate in a coordinated manner to ensure energy balance and cellular function.Catabolic Pathways and Energy ReleaseCatabolic pathways involve the breakdown of complex macromolecules such as carbohydrates, lipids, and proteins into smaller structures like monosaccharides, fatty...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
Drug Biotransformation: Overview01:28

Drug Biotransformation: Overview

Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...
What is Metabolism?00:52

What is Metabolism?

Overview

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Related Experiment Video

Updated: May 27, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
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Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures

Published on: March 28, 2017

Why do metabolites circulate?

Dennis A Smith1, Deepak Dalvie

  • 1School of Biomedical Sciences, University of Liverpool, Liverpool, UK. professordennis@deltic50.freeserve.co.uk

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
|November 26, 2011
PubMed
Summary

Understanding drug metabolite circulation is key for better in vitro/in vivo correlations. This study explores why drug metabolites remain in circulation, focusing on lipid permeability and transport mechanisms.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Toxicology

Background:

  • Drug metabolism and excretion aim to eliminate drugs, yet metabolites often persist in circulation.
  • High circulating concentrations of drug metabolites necessitate understanding their disposition for accurate in vitro/in vivo correlations.

Purpose of the Study:

  • To investigate the reasons behind the abundance of drug metabolites in circulation.
  • To differentiate the roles of passive efflux and active transport in metabolite distribution.
  • To explain the high circulating concentrations of glucuronide metabolites.

Main Methods:

  • Categorizing metabolites based on lipid permeability (high vs. low).
  • Analyzing the influence of factors like MRP3 efflux, plasma protein binding, and distribution.

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Arteriovenous Metabolomics to Measure In Vivo Metabolite Exchange in Brown Adipose Tissue

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Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
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  • Proposing the use of metabolite maps for visualizing complex processes.

    • Main Results:

    • Low lipid permeability, MRP3-mediated efflux, high plasma protein binding, and restricted distribution explain high circulating glucuronide metabolite concentrations.
    • Distinguishing between highly and lowly lipid-permeable metabolites aids in dissecting transport mechanisms.

    Conclusions:

    • Understanding metabolite disposition, particularly lipid permeability and transport, is crucial for drug development.
    • Metabolite maps offer a simplified approach to visualizing complex drug metabolism and excretion pathways.